AU2005295734A1 - Methods of treating vascular injuries - Google Patents

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WO 2006/044509 PCT/US2005/036770 METHODS OF TREATING VASCULAR INJURIES BACKGROUND OF THE INVENTION [001] TGF# (Transforming Growth Factor 3) is a member of a large family of dimeric polypeptide growth factors that includes, for example, activins, inhibins, bone morphogenetic proteins (BMPs), growth and differentiation factors (GDFs) and mullerian inhibiting substance (MIS). TGF# exists in three isoforms (TGF31, TGF#2, and TGF#3) and is present in most cells, along with its receptors. Each isoforn is expressed in both a tissue-specific and developmentally regulated fashion. Each TGF#l isoform is synthesized as a precursor protein that is cleaved intracellularly into a C-terminal region (latency associated peptide (LAP)) and an N-terminal region known as mature or active TGF#. LAP is typically non-covalently associated with mature TGF# prior to secretion from the cell. The LAP-TGF3 complex cannot bind to the TGFO receptors and is not biologically active. TGF3 is generally released (and activated) from the complex by a variety of mechanisms including, for example, interaction with thrombospondin- 1 or plasmin. [002] Following activation, TGF# binds at high affinity to the type II receptor (TGF#RII), a constitutively active serine/threonine kinase. The ligand-bound type II receptor phosphorylates the TGF3 type I receptor (Alk 5) in a glycine/serine rich domain, which allows the type I receptor to recruit and phosphorylate downstream signaling molecules, Smad2 or Smad3. See, e.g., Huse, M. et al., Mol. Cell. 8: 671-682 (2001). Phosphorylated Smad2 or Smad3 can then complex with Smad4, and the entire hetero-Smad complex translocates to the nucleus and regulates transcription of various TGF#-responsive genes. See, e.g., Massagu6, J. Ann. Rev. Biochem. Med. 67: 773 (1998). [003] Activins are also members of the TGF# superfamily, which are distinct from TGF# in that they are homo- or heterodimers of activin fla or fib. Activins signal in a manner similar to TGF3, that is, by binding to a constitutive serine-threonine receptor kinase, activin type II receptor (ActRIIB), and activating a type I serine-threonine receptor, Alk 4, to phosphorylate Smad2 or Smad3. The consequent formation of a hetero-Smad complex with Smad4 also results in the activin-induced regulation of gene transcription. [004] Indeed, TGF3 and related factors such as activin regulate a large array of cellular processes, e.g., cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, inflammatory cell recruitment, immunosuppression, wound healing, and extracellular matrix production. See, e.g., Massagu6, J. Ann. Rev . Cell.

WO 2006/044509 PCT/US2005/036770 Biol. 6: 594-641 (1990); Roberts, A. B. and Spom M. B. Peptide Growth Factors and Their Receptors, 95: 419-472 Berlin: Springer-Verlag (1990); Roberts, A. B. and Sporn M. B. Growth Factors 8:1-9 (1993); and Alexandrow, M. G., Moses, H. L. Cancer Res. 55: 1452 1457 (1995). Hyperactivity of TGFf signaling pathway underlies many human disorders (e.g., excess deposition of extracellular matrix, an abnormally high level of inflammatory responses, fibrotic disorders, and progressive cancers). See, e.g. Blobe G.C., Schiemann W.P., Lodish H.F. N. Eng. J Med. 342: 1350-8 (2000). Similarly, activin signaling and overexpression of activin is linked to pathological disorders that involve extracellular matrix accumulation and fibrosis (see, e.g., Matsuse, T. et al., Am. J. Respir. Cell Mol. Biol. 13: 17 24 (1995); Inoue, S. et al., Biochem. Biophys. Res. Comm. 205: 441-448 (1994); Matsuse, T. et al, Am. J Pathol. 148: 707-713 (1996); De Bleser et al., Hepatology 26: 905-912 (1997); Pawlowski, J.E., et al., J. Clin. Invest. 100: 639-648 (1997); Sugiyama, M. et al., Gastroenterology 114: 550-558 (1998); Munz, B. et al., EMBO J 18: 5205-5215 (1999)), inflammatory responses (see, e.g., Rosendahl, A. et al., Am. J Repir. Cell Mol. Biol. 25: 60 68 (2001)), cachexia or wasting (see Matzuk, M. M. et al., Proc. Nat. Acad. Sci. USA 91: 8817-8821 (1994); Coerver, K.A. et al, Mol. Endocrinol. 10: 534-543 (1996); Cipriano, S.C. et al. Endocrinology 141: 2319-27 (2000)), diseases of or pathological responses in the central nervous system (see Logan, A. et al. Eur. J. Neurosci. 11: 2367-2374 (1999); Logan, A. et al. Exp. Neurol. 159: 504-510 (1999); Masliah, E. et al., Neurochem. lit. 39: 393-400 (2001); De Groot, C. J. A. et al, J Neuropathol. Exp. Neurol. 58: 174-187 (1999), John, G. R. et al, Nat Med. 8: 1115-21 (2002)) and hypertension (see Dahly, A. J. et al., Am. J. Physiol. Regul. Integr. Comp. Physiol. 283: R757-67 (2002)). Studies have shown that TGF# and activin can act synergistically to induce extracellular matrix production (see, e.g., Sugiyama, M. et al., Gastroenterology 114: 550-558, (1998)). It is therefore desirable to develop modulators (e.g., antagonists) to members of the TGFO family to prevent and/or treat disorders involving this signaling pathway. SUMMARY OF THE INVENTION [0051 In general, the compounds of formulae I, II, III, IV, V, and VI, described herein, unexpectedly exhibit systemic bioavailability and are useful in combating restenosis (e.g., coronary restenosis, peripheral restenosis, and carotid restenosis), vascular diseases (e.g., intimal thickening, vascular remodeling, or organ transplant-related vascular disease), and hypertension (e.g., primary or secondary, systolic hypertension, pulmonary hypertension or hypertension-induced vascular remodeling) when administered to a subject (e.g., a patient). 2 WO 2006/044509 PCT/US2005/036770 [006f19'Metho.ds of inhibiting intimal thickening or vascular remodeling include administering to a subject (e.g., a human patient) in need thereof an inhibitor of TGF3 type I receptor or Alk4. Embodiments of these aspects may include one or more of the following. The inhibitor is a compound of formula I, II, III, IV, V, or VI. The inhibitor is administered locally. The inhibitor is administered via an implantable device such as a delivery pump or a stent. [007] In another aspect, the invention features an implantable device, such as a delivery pump or stent, including an inhibitor of TGFP type I receptor or Alk4. The inhibitor can be a compound of formula I, II, III, IV, V, or VI. Definitions: [008] As used herein, an "alkyl" group refers to a saturated aliphatic hydrocarbon group containing 1-8 (e.g., 1-6 or 1-4) carbon atoms. An alkyl group can be straight or branched. Examples of an alkyl group include, but are not limited to, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, n-heptyl, and 2-ethylhexyl. An alkyl group can be optionally substituted with one or more substituents such as alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroarylalkoxy, amino, nitro, carboxy, cyano, halo, hydroxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, cycloalkyl alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, heterocycloalkyl carbonylamino, heterocycloalkyl-alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, urea, thiourea, sulfamoyl, sulfamide, alkoxycarbonyl, or alkylcarbonyloxy. [0091 As used herein, an "alkenyl" group refers to an aliphatic carbon group that contains 2 8 (e.g., 2-6 or 2-4) carbon atoms and at least one double bond. Like an alkyl group, an alkenyl group can be straight or branched. Examples of-an alkenyl group include, but are not limited to, allyl, isoprenyl, 2-butenyl, and 2-hexenyl. An alkenyl group can be optionally substituted with one or more substituents such as alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroarylalkoxy, amino, nitro, carboxy, cyano, halo, hydroxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, cycloalkyl alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, heterocycloalkyl carbonylamino, heterocycloalkyl-alkylcarbonylamino, heteroarylcarbonylamino, 3 WO 2006/044509 PCT/US2005/036770 heteroaralkylcafbonylamino, urea, thiourea, sulfamoyl, sulfamide, alkoxycarbonyl, or alkylcarbonyloxy. [0101 As used herein, an "alkynyl" group refers to an aliphatic carbon group that contains 2 8 (e.g., 2-6 or 2-4) carbon atoms and has at least one triple bond. An alkynyl group can be straight or branched. Examples of an alkynyl group include, but are not limited to, propargyl and butynyl. An alkynyl group can be optionally substituted with one or more substituents such as alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroarylalkoxy, amino, nitro, carboxy, cyano, halo, hydroxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, cycloalkyl-alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, heterocycloalkyl-. carbonylamino, heterocycloalkyl-alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, urea, thiourea, sulfamoyl, sulfamide, alkoxycarbonyl, or alkylcarbonyloxy. [011] As used herein, an "amino" group refers to -NxR wherein each of Rx and R is independently hydrogen, hydroxyl, alkyl, alkoxy, cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyL, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, or heteroaralkyl. When the term "amino" is not the tenninal group (e.g., alkylcarbonylamino), it is represented by -NRX wherein Rx has the same meaning as defined above. [012] As used herein, an "aryl" group refers to phenyl, naphthyl, or a benzofused group having 2 to 3 rings. For example, a benzofused group includes phenyl fused with one or two

C

4

.

8 carbocyclic moieties, e.g., 1,2,3,4-tetrahydronaphthyl, indanyl, or fluorenyl. An aryl is optionally substituted with one or more substituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl), alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, aryl, heteroaryl, alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbamoyl. 4 WO 2006/044509 PCT/US2005/036770 [0f3] As'usedler'ein, an"'aalkyl" group refers to an alkyl group (e.g., a C 1 4 alkyl group) that is substituted with an aryl group. Both "alkyl" and "aryl" are as defined above. An example of an aralkyl group is benzyl. [0141 As used herein, a "cycloalkyl" group refers to an aliphatic carbocyclic ring of 3-10 (e.g., 4-8) carbon atoms. Examples of cycloalkyl groups include cyclopropyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl, norbornyl, cubyl, octahydro-indenyl, decahydro naphthyl, bicyclo[3.2.1]octyl, bicyclo[2.2.2]octyl, bicyclo[3.3.1]nonyl, and bicyclo[3.2.3]nonyl. A "cycloalkenyl" group, as used herein, refers to a non-aromatic carbocyclic ring of 3-10 (e.g., 4-8) carbon atoms having one or more double bond. Examples of cycloalkenyl groups include cyclopentenyl, 1,4-cyclohexa-di-enyl, cycloheptenyl, cyclooctenyl, hexahydro-indenyl, octahydro-naphthyl, bicyclo[2.2.2]octenyl, and bicyclo[3.3.1]nonenyl. A cycloalkyl or cycloalkenyl group can be optionally substituted with one or more substituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl), alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, aryl, heteroaryl, alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbamoyl. [0151 As used herein, a "heterocycloalkyl" group refers to a 3- to 10-membered (e.g., 4- to 8-membered) saturated ring structure, in which one or more of the ring atoms is a heteroatom, e.g., N, 0, or S. Examples of a heterocycloalkyl group include piperidinyl, piperazinyl, tetrahydropyranyl, tetrahydrofuryl, dioxolanyl, oxazolidinyl, isooxazolidinyl, morpholinyl, octahydro-benzofuryl, octahydro-chromenyl, octahydro-thiochromenyl, octahydro-indolyl, octahydro-pyrindinyl, decahydro-quinolinyl, octahydro-benzo[b]thiophenyl, 2-oxa bicyclo[2.2.2]octyl, 1-aza-bicyclo[2.2.2]octyl, 3-aza-bicyclo[3.2.1]octyl, and 2,6-dioxa tricyclo[3.3.1.0 3

,

7 ]nonyl. A "heterocycloalkenyl" group, as used herein, refers to a 3- to 10 membered (e.g., 4- to 8-membered) non-aromatic ring structure having one or more double bonds, and wherein one or more of the ring atoms is a heteroatom, e.g., N, 0, or S. A heterocycloalkyl or heterocycloalkenyl group can be optionally substituted with one or more 5 WO 2006/044509 PCT/US2005/036770 substifuents such as alkyl including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl), alkenyl, alkynyl, cycloalkyl, (cycloalkyL)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, aryl, heteroaryl, alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, aro yl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarboriyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylaminao, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, rnercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbamoyl. [0161 A "heteroaryl" group, as used herein, refers to a nionocyclic, bicyclic, or tricyclic ring structure having 5 to 15 ring atoms wherein one or more of the ring atoms is a heteroatom, e.g., N, 0, or S, and wherein one ore more rings of the bicyclic or tricyclic ring structure is aromatic. Some examples of heteroaryl are pyridyl, furyl, pyrrolyl, thienyl, thiazolyl, oxazolyl, imidazolyl, indolyl, tetrazolyl, benzofuryl, benzthiazolyl, xanthene, thioxanthene, phenothiazine, dihydroindole, and benzo[1,3]dioxole. A heteroaryl is optionally substituted with one or more substituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl), alkenyl, alkynyl, cyclo alkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, aryl, heteroaryl, alkoxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbamoyl. A "heteroaralkyl" group, as used herein, refers to an alkyl group (e.g., a C1- alkyl group) tliat is substituted with a heteroaryl group. Both "alkyl" and "heteroaryl" are as defined above. [0171 As used herein, "cyclic moiety" includes cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, or heteroaryl, each of which has been defined previously. [018] As used herein, an "acyl" group refers to a formyl group or alkyl-C(=0)- where "alkyl" has been defined previously. Acetyl and pivaloyl are examples of acyl groups. 6 WO 2006/044509 PCT/US2005/036770 [0f9] As'us'd herein, a "carbamoyl" group refers to a group having the structure -O-CO-NRxRy or -NRX-CO-0-Rz wherein RX and R have been defined above and Rz is alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, or heteroaralkyl. [020] As used herein, a "carboxy" group and a "sulfo" group refer to -CC>OH and -S0 3 H, respectively. [021] As used herein, an "alkoxy" group refers to an alkyl-O- group wherein "alkyl" has been defined previously. [0221 As used herein, a "sulfoxy" group refers to -O-SO-Rx or -SO-0-R c, wherein Rx has been defined above. [023] As used herein, a "halogen" or "halo" group refers to fluorine, chlorine, bromine or iodine. [024] As used herein, a "sulfamoyl" group refers to the structure -SO 2 -NRxR or -NRx

SO

2 -Rz wherein Rx, R, and Rz have been defined above. [025] As used herein, a "sulfamide" group refers to the structure -NRx-S(O) 2 -NRYRz wherein Rx, R, and Rz have been defined above. [0261 As used herein, a "urea" group refers to the structure -NRx-CO-NRYRz and a "thiourea" group refers to the structure -NRx-CS-NRYRz. RX, Ry, and Rz have been defined above. [027] As used herein, an effective amount is defined as the amount which is required to confer a therapeutic effect on the treated patient, and is typically determined based on age, surface area, weight, and condition of the patient. The interrelationship of dosages for animals and humans (based on milligrams per meter squared of body surface) is described by Freireich et al., Cancer Chemother. Rep., 50: 219 (1966). Body surface are-a may be approximately determined from height and weight of the patient. See, e.g., Scientific Tables, Geigy Pharmaceuticals, Ardsley, New York, 537 (1970). As used herein, a. "patient" refers to a mammal, including a human. [0281 An antagonist is a molecule that binds to the receptor without activating the receptor. It competes with the endogenous ligand(s) or substrate(s) for binding site(s) on the receptor 7 WO 2006/044509 PCT/US2005/036770 and, thui inhibits the ability of the receptor to transduce an intracellular signal in response to endogenous ligand binding. [0291 Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. All publications, patent applications, patents, and other references mentioned herein are incorporated by reference in their entirety. In addition, the materials, methods, and examples are illustrative only and not intended to be limiting. [030] Other features and advantages of the invention will be apparent from the following detailed description, and from the claims. BRIEF DESCRIPTION OF THE DRAWINGS [031] Figure 1 is an illustration of a delivery device. DETAILED DESCRIPTION OF THE INVENTION [0321 The inhibitors described herein are effective at treating, preventing, or reducing intimal thickening, vascular remodeling, restenosis (e.g., coronary, peripheral, carotid restenosis), vascular diseases, (e.g., organ trarisplant-related, cardiac, and renal), and hypertension (e.g., primary and secondary, systolic, pulmonary, and hypertension-induced vascular remodeling resulting in target organ damage). [033] Without wishing to be bound by any particular theory, one possible explanation for the efficacy of the compounds described herein may be their inhibitory effect on the TGFp and activin pathways. [034] The pathological activation of the TGF$ and activin pathway plays a critical role in the progression of fibrotic diseases. The critical serine-threonine kinase in the TGFp type I receptor (TGFPRI) and the activin type I receptor (Alk4) are attractive targets for blockade of the TGFb pathway for several important reasons. TGFpRI kinase activity is required for TGFp signaling as is Alk4 for activin signaling. Kinases have proven to be useful targets for development of small molecule drugs. There is a good structural understanding of the TGFpRI kinase domain allowing the use of structure-based drug discovery and design to aid in the development of inhibitors. 8 WO 2006/044509 PCT/US2005/036770 [0S5] T6Ff or activin-mediated pathological changes in vascular flow and tone are often the cause of morbidity and mortality in a number of diseases (see, e.g., Gibbons G.H. and Dzau V.J. NEng. J. Med 330:1431-1438 (1994)). Typically, the initial response of the vasculature to injury is an infiltration of adventitial inflammatory cells and induction of activated myofibroblasts or smooth muscle cells (referred to as myofibroblasts from hereon). TGFp is initially produced by infiltrating inflammatory cells and activates myofibroblasts or smooth muscle cells. These activated myofibroblasts can also secrete TGFp as well as respond to it. Within the first few days following injury, myofibroblasts secreting TGFp migrate from the various layers of the vascular wall toward-s the lumen where they undergo proliferation and extracellular matrix secretion resulting in intimal thickening. Additionally, TGFP induces activated myofibroblasts to contract which results in lumenal narrowing. These vascular remodeling processes, intimal thickening and vascular contraction, restrict blood flow to the tissues supported by the effected vasculature and result in tissue damage. Activin is also produced in response to injury and shows very similar actions in inducing activated myofibroblasts or activated smooth muscle cells intimal thickening and vascular remodeling. See, for example, Pawlowski et al., Stimulation of activin A expression in rat aortic smooth muscle cells by thrombin and angiotensin II correlates with neointimal formation in vivo, published in 1997 in J. Clin. Invest. 100:639-648; Woodruff TK, Regulation of cellular and system function by activin, published in 1998 in Biochein Pharmacol. 55:953-963; Molloy et al., Novel cardiovascular actions of the activins, published in 1999 in JEndocrinol. 161(2):179-85.; and Harada K et al., Immunoreactive activin A levels in normal subjects and patients with various diseases, published in 1996 in J Clin Endocrinol Metab. 81(6):2125-30. [036] In coronary, peripheral or carotid artery disease, balloon angioplasty or stent placement is used to increase lumen size and blood flow. However, the physical damage created by stretching the vessel wall causes injury to the vessel wall tissue. TGFp elevation following injury induces myofibroblasts in 2-5 days and frequently results in restenosis within 6 months of balloon angioplasty or within a few years of stent placement in human patients. Following balloon angioplasty, both intimal thickening and vascular remodeling due to myofibroblast contraction, cause narrowing of the lurnen and decreased blood flow. Stent placement physically prevents remodeling, but hyperplasia and extracellular matrix deposition by activated myofibroblasts proliferating at the luminal side of the stent results in 9 WO 2006/044509 PCT/US2005/036770 intimal thickening within the stented vessel resulting in the eventual impairment of blood flow. [037] The treatment of arterial stenotic diseases by surgical grafts, e.g. coronary bypass or other bypass surgery, also can elicit restenosis in the grafted vessel. In particular, vein grafts undergo intimal thickening and vascular remodeling through a similar mechanism involving TGF-induced intimal thickening and vascular remodeling. In this case, the injury is either due to the overdistention of the thin-walled vein graft placed into an arterial vascular context or due to anastamotic or ischemic injury during the transplantation of the graft. [038] The loss of patency in arteriovenous or synthetic bridge graft fistulas is another vascular remodeling response involving increased TGFp production. See, e.g., Ikegaya N. et al., J. Am. Soc. Nephrol., 11:928-35 (2000); Heine G.H. et al., Kidney Int., 64:1101-7 (2003). Loss of fistula patency causes complications for renal dialysis or other treatments requiring chronic access to the circulatory system (Ascher E., Ann. Vasc. Surg., 15:89-97 (2001)). Blockade of TGFp by TGFpRI inhibitors will be beneficial for preventing restenosis and extending arteriovenous fistula patency. [0391 Elevated TGFp is implicated in chronic allograft vasculopathy both in animals and humans. Vascular injury, intimal thickening and vascular remodeling is a characteristic pathology in chronic allograft failure. The fibrotic response in chronic allograft failure initiates in the vasculature of the donor organ. Chronic allograft vasculopathy in allografted hearts often manifests within 5 years of transplantation and is the main cause of death in long term survivors of cardiac transplant. Early detection of cardiac allograft vasculopathy measured as intimal thickening by intravascular ultrasound, as well as the elevation of pla-sma TGFp, has been suggested as a prognostic marker for late cardiac allograft failure (see, e.g., Mehra MR et al., 2004, Am. J. Transplant., 4:1184). Cardiac biopsies of grafted hearts also suggest that graft tissue expression of TGFp correlates significantly to vasculopathy and the number of rejection episodes (see, e.g., Aziz, T. et al., 2000, J. Thorac. Cardiovasc. Surg.,. 119: 700). Finally, patients with high-producing TGFP 1 genotypes are more susceptible to earlier onset cardiac-transplant coronary vasculopathy (see, e.g., Densem, CG et al., 2000, J Heart Lung Transplant, 19:551; Aziz, T. et al., 2000, J. Thorac. Cardiovasc. Surg., 119: 7 00; and Holweg, CT, 2001, Transplantation, 71:1463). [0401 Elevation of TGFp can be induced by ischemic, immune and inflammatory responses to the allograft organ. Animal models of acute and chronic renal allograft rejection identify 10 WO 2006/044509 PCT/US2005/036770 the elevation of TGFD as a significant contributor to graft failure and rejection (see, e.g., Nagano, H. et al., 1997, Transplantation, 63: 1101; Paul, LC. et al., 1996, Am. J. Kidney Dis., 28: 441; and Shihab, FS. et al., 1996, Kidney it., 50: 1904). Rodent models of chronic allograft nephropathy (CAN) show elevation of TGFp mRNA and immunostaining. In renal allografts TGF immunostaining is strongly positive in interstitial inflammatory andfibrotic cells, but also in blood vessels and glomeruli. In humans, the loss of renal function 1 year post renal allograft correlates with TGFp staining in the grafted kidney. See, e.g., Cuhaci, B. et al., 1999, Transplantation, 68: 785). Graft biopsies show also that renal dysfunction correlates with chronic vascular remodeling, i.e., vasculopathy, and the degree of TGFp expression correlates significantly with chronic vasculopathy (see, e.g., Viklicky, 0. et al., 2003, Physiol Res. 52: 353). [041] The use of immunosuppressive agents such as cyclosporine A in organ transplantation has not prevented vasculopathy and chronic allograft nephropathy suggesting non-immune mechanisms are involved in allograft failure. In fact, cyclosporinA and other immunosuppressants have been shown to induce TGFp expression and may contribute to vasculopathy (see, e.g., Moien-Afshari, F. et al., 2003, Pharmacol. Ther., 100: 141; and Jain, S. et al., 2000, Transplantation, 69: 1759). [042] TGF3 is implicated in chronic allograft rejection in both renal and lung transplants due to the clear TGFp-related fibrotic pathology of this condition as well as the ability of immune suppressants, esp cyclosporin A, to induce TGF$ (Jain, S. et al., 2000 Transplantation, 69: 1759). TGFp blockade improved renal function while decreasing collagen deposition, renal TGFP expression as well as vascular afferent arteriole remodeling in a cyclosporine A-induced renal failure model using an anti-TGFp monoclonal antibody (Islam, M. et al., 2001 Kidney Int., 59: 498; Khanna, A.K. et al., 1997 Transplantation, 67: 882). These data are strongly indicative of a causal role for TGFp in the development and progression of chonic allograft vasculopathy and chronic allograft failure. [043] Hypertension is a major cause of morbidity and mortality in the U.S. population affecting approximately 1 in 3 individuals. The effect of hypertension on target organs include increased incidence of cardiac failure, myocardial infarction, stroke, renal failure, aneurysm and microvascular hemorrhage. Hypertension-induced damage to the vasculature results in vascular remodeling and intimal thickening which are a major causative factor in many of these morbidities (Weber, W.T. 2000 Curr. Opin. Cardiol. 15:264-72). Animal 11 WO 2006/044509 PCT/US2005/036770 experiments suggest that TG'p is elevated upon induction of hypertension and anti-TGFP monoclonal antibody blockade of this pathway decreases blood pressure and renal pathology in hypertensive rats (Xu, C. et al., 2001 J. Vasc. Surg., 33:570; Dahly, A.J. et al., 2002 Am. J. Physiol. Regul. Integr. Comp. Physiol., 283:R757). In humans, plasma TGFp is elev-ated in hypertensive individuals compared to normotensive controls and plasma TGFP is also higher in hypertensive individuals with manifest target organ disease compared to hypertensive individuals without apparent target organ damage (Derhaschnig, U. et al., 2002 Am. J. Hypertens., 15:207; Suthanthiran, M. 2000 Proc. Nati. Acad. Sci. US.A., 97:3479). 'There is also evidence suggesting that high TGFp-producing genotypes of TGFp are a risk factor for development of hypertension (Lijnen, P.J. 2003 Am. J. Hypertens., 16:604; Suthanthiran, M. 2000 Proc. Nati. Acad. Sci. US.A., 97:3479). Thus the inhibition of the TGF3 pathway may provide a effective therapeutic approach for hypertension or hypertension-induced organ damage. [0441 The vascular injury response in the pulmonary vasculature results in pulmonary hypertension which can lead to overload of the right heart and cardiac failure (Runo, J.R., Loyd, J.E., 2003 Lancet 361(9368):1533-44; Sitbon, 0. et al., 2002 Prog. Cardiovasc. Dis., 45: 115-28; Jeffery, T.K., Morrell, N.W. 2002 Cardiovasc. Dis., 45:173-202). PreveMtion of pulmonary vascular remodeling by TGFpRI inhibitors can be of practical utility in diseases such as primary or secondary pulmonary hypertension (Sitbon, 0. et al., 2002, Prog. Cardiovasc. Dis., 45: 115-28; Humbert, M. et al., J Am. Coll. Cardiol., 2004 43:13S -24S). Inhibition of the progression of vascular remodeling over time will prevent the progression of pulmonary pathology in these life threatening diseases. Secondary pulmonary hypertension occurs often as a manifestation of scleroderma and is one of the primary causes of morbidity and mortality in scleroderma patients (Denton, C.P., Black, C.M. 2003, Rheum. Dis. Clin. North. Am., 29:335-49). Pulmonary hypertension is also a sequalae of miced connective tissue disease, chronic obstructive pulmonary disease (COPD) and lupus erythematosis (Fagan, K.A., Badesch, D.B., 2002, Prog. Cardiovasc. Dis., 45:225-34; and Presberg, K.W., Dincer, H.E., 2003, Curr. Opin. Pulm. Med., 9:131-8). [0451 Many of the diseases described above involving vascular remodeling are particularly severe in diabetic patients (Reginelli, J.P., Bhatt, D.L., 2002, J. Invasive Cardiol., 14- Suppl E:2E-1OE). Elevated glucose in diabetes can itself induce TGFp which leads to the increased vascular remodeling and intimal thickening response to vascular injury (Ziyadeh, FJ.., Am. Soc. Nephrol., 2004, 15 Suppl 1:S55-7). In particular, diabetic patients have significantly 12 WO 2006/044509 PCT/US2005/036770 higherrates of restenosis, vein graft stenosis, peripheral artery disease, chronic allograft nephropathy and chronic allograft vasculopathy (Reginelli, J.P., Bhatt, D.L., 2002, J Invasive Cardiol., 14 Suppl E:2E-1OE; Eisen. H., Ross, H., 2004, J. Heart Lung Transplant., 23:S207 13; Valentine, H., 2004, J. Heart Lung Transplant., 23:S187-93). Thus, blockade of TGF3 is of particular utility in diabetic patients at risk for hypertension-related organ failure, diabetic nephropathy, restenosis or vein graft stenosis in coronary or peripheral arteries, and chronic failure of allograft organ transplants (Endemann, D.H. et al., 2004, Hypertension, 43(2):399 404; Ziyadeh, F.J., Am. Soc. Nephrol., 2004 15 Suppl 1:S55-7; and Jerums, G. et al., 2003, Arch. Biochem. Biophys., 419:55-62). [046] Surprisingly, TGFpRI and Alk4 antagonists are effective at treating, preventing, or reducing intimal thickening, vascular remodeling, restenosis (e.g., coronary, peripheral, and carotid restenosis), vascular diseases, (e.g., organ transplant-related, cardiac, and renal), and hypertension (e.g., systolic, pulmonary, and hypertension-induced vascular remodeling resulting in target organ damage). Changes in vascular remodeling and intimal thickening may be qualified by measuring the intimal versus medial vascular thickness. TGFpRI and Alk 4 Inhibitors [047] The TGFf and activin inhibitory activity of compounds can be assessed by methods described below. [048] Examples of these antagonists are shown below in formulae I, II, III, IV, V, and VI. [049] In one embodiment, the antagonists have the structure shown in formula I: R"L N A1-2 R Q-1 X,.

1 -Y_--R1- 2 (I) Al-a [050] In formula I, R- can be aryl, heteroaryl, aralkyl, or heteroaralkyl. Each R, independently, can be alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, 13 WO 2006/044509 PCT/US2005/036770 alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. X,., can be cycloalkyl or heterocycloalkyl. Y, 4 can be a bond, -C(O)-, -C(O)-O-, -O-C(0)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(R'-b)-, -N(R'-b)-C(O)-, -O C(0)-N(Rl-l)-, -N(R -b)-C(O)-0-, -O-_S(0), -N(R!-b)-, -N(RW-b)-S(O)p-O-, -N(R!~")-C(O)-N(R' c)-, -N(RI-b)-S(O)p-N(R'-c)-, -C(0)-N(R'-b)-S(O),-, -S(O)p-N(R'-b)-C(0)-, -C(0)-N(RI-b ) S(O),-N(R'~ )-, -C(0)-0-S(O)p-N(R'-b)-, -N(RI-b)-S(O),-N(R'-c)-C(O)-, -N(R 1-b)-S(O),-O C(O)-, -S(0),-N(R-b)-, -N(R -)-S(O),-, -N(RI-b)-, -S(0)1-, -0-, -S-, or -(C(RI-b)(RI C))q-, wherein each of RI-b and RIc is independently hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl. p can be 1 or 2, and q can be 1-4. R - can be hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkzenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl. Each of A" and A' 2 , independently, can be 0, S, N, or NR'~b, provided that at least one of A" and A" can be N. m can be 0, 1, 2, or 3. In other words, the 2 pyridyl ring can be unsubstituted or substituted with 1 to 3 R a groups. Note that when m > 2, two adjacent Rl-a groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. That is, the 2-pyridyl ring can fuse with a cyclic moiety to form a moiety, e.g., 7H-[2]pyrindinyl, 6,7-dihydro-5H-[1]pyrindinyl, 5,6,7,8-tetrahydro quinolinyl, 5,7-dihydro-furo[3,4-b]pyridinyl, or 3,4-dihydro-1H-thiopyrano[4,3-c]pyridinyl, that can be optionally substituted with one or more substituents such as alkyl (including substituted alkyl such as carboxyalkyl, hydroxyalkyl, and haloalkyl (e.g., trifluoromethyl)), alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, alkoxy, aryl, heteroaryl, aryloxy, heteroaryloxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylthio, sulfoxy, sulfamoyl, oxo, or carbamoyl. [0511 Compounds of formula I and methods for producing the same are known in the art. For instance, WO 03/087304, which is incorpoarated in its entrity by reference, describes synthetic methods for producing inhibitors of formula I. Examples of compounds of formula I include, but are not limited to, 1) 4-(4-Benzo[1,3]dioxol-5-yl-5-(6-nethyl-pyridin-2-yl)-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 14 WO 2006/044509 PCT/US2005/036770 2) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 3) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 4) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 5) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 6) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 7) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 8) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 9) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yL)-6-methyl-pyridine; 10) 2-[5-3enzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 11) 2-[5-3enzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-pyridine; 12) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 13) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 14) 4-(4-B enzo[ 1,3 ]dioxol-5-yl-5 -pyridin-2-yl- 1 H-imidazol-2-yl) -piperidine- 1 -carboxylic acid 2-chloro-benzyl ester; 15) 4-(4-B enzo[ 1,3]dioxol-5-yl-5-pyridin-2-yl- 1 H-imidazol-2-yl) -piperidine- 1 -carboxylic acid 2,4-dichloro-benzylamide; 16) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-l-yl] ethanone; 17) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-furan-2-yl-methyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 18) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-irnidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 19) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylamine; 15 WO 2006/044509 PCT/US2005/036770 20) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-phenyl-methanesulfonamide; 21) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid methyl ester; 22) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid; 23) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -carbamic acid benzyl ester; 24) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-ethyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 25) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-pyridine; 26) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-IH-imidazol-2-yl)-piperidine-1-carboxylic acid 4-nitro-benzyl ester; 27) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4,5-dimethoxy-2-nitro-benzyl ester; 28) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 3-fluoro-benzylamide; 29) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-fluoro-benzylamide; 30) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzylamide; 31) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 32) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methyl-benzylamide; 33) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methoxy-benzylamide; 34) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzylamide; 35) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzoic acid; 36) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid amide; 37) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzonitrile; 16 WO 2006/044509 PCT/US2005/036770 38) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 39) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 40) {5-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] naphthalen-1-yl}-dimethyl- amine; 41) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methyl)-piperidin-4-yl)]-3H-imidazol-4 yl}-pyridine; 42) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 43) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 44) 1-{4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonyl]-phenyl}-ethanone; 45) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methyl-benzyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 46) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-fluoro-5-trifluoromethyl-benzyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 47) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-cyclohexylmethyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 48) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-ylmethyl] cyclopropanecarboxylic acid ethyl ester; 49) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-ylmethyl] pyrrolidine-1-carboxylic acid tert-butyl ester; 50) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 51) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 52) 2-{5-Benzo[ 1,3]dioxol-5-yl-2-[1 -(butane-i -sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 53) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 54) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 17 WO 2006/044509 PCT/US2005/036770 55) 2-{5-Benzo[ 1,3]dioxol-5-yl-2-[1 -(propane- 1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 56) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonylmethyl]-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 57) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 58) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 59) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(4-fluoro-phenylmethanesulfonyl)-piperidin-4-y1]-3H imidazol-4-yl} -pyridine; 60) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 61) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 62) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-p-tolylmethanesulfonyl-piperidin-4-yl)-3H-imidazul-4 yl]-pyridine; 63) 3-(4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 64) 3-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 65) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 66) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-31H imidazol-4-yl} -pyridine; 67) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-1-yl-ethanesulfonyl)-piperidin-4-yl] -3H imidazol-4-yl} -pyridine; 68) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazcI-4 yl]-pyridine; 69) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 70) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methanesulfonyl)-piperidin-4-yl]-3K imidazol-4-yl} -pyridine; 71) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-yl-methanesulfonyl)-piperidin-4-yl]-311 imidazol-4-yl} -pyridine; 18 WO 2006/044509 PCT/US2005/036770 72) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 73) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-y1)-1H-imidazol-2-yl] pyrrolidine-1-carboxylic acid benzyl ester; 74) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 75) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-bis-trifluoromethyl-phenylmethanesulfonyl) piperidin-4-y]-3H-imidazol-4-yl} -pyridine; 76) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 77) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 78) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 79) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-y]-3H imidazol-4-yl} -pyridine; 80) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 81) 4-[5-Benzo[1,3]dioxol-5-yl-1-methyl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 82) 4-[4-Benzo[1,3]dioxol-5-yl-1-methyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 83) {4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl}-carbamic acid benzyl ester; 84) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-phenoxy-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 85) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 86) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[ 1 -(propane- 1 -sulfonyl)-pipe-ridin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 87) 2-{5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(butane-1 -sulfonyl)-piperidin-4-yl] -3H-imidazol-4-yl} 6-methyl-pyridine; 88) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 19 WO 2006/044509 PCT/US2005/036770 89) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 90) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 91) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 92) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl } -6-methyl-pyridine; 93) 2- {5-Benzo[1,3]dioxol-5-yl-2-[ 1 -(butane-I-sulfonyl)-piperidin-3-yl]-3H-imidazol-4-yl} 6-methyl-pyridine; 94) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 95) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-1H-imidazole-4-sulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 96) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-isoxazole-4-sulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 97) 4-[5-Benzo[1,3]dioxol-5-yl-1-hydroxy-4-(6-methyl-pyridin-2-yl)-1 H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 98) Butane-i -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl}-amide; 99) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imilazol-2-yl] cyclohexyl} -C-pyridin-2-yl-methanesulfonamide; 100) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-metlciyl-pyridin-2-yl)-lH imidazol-2-yl]-cyclohexyl}-amide; 101) 1-Methyl-iH-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl}-amide; 102) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)- 1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid amide; 103) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)- 1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 104) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-bromo-pyridin-2-yl)-1H-imidazo l-2-yl]-piperidine-1 carboxylic acid benzyl ester; 105) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-3-sulfonyl)-piperidia-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 20 WO 2006/044509 PCT/US2005/036770 106) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-2-trifluoromethyl-furan-3-sulfonyl) piperidin-4-yl]-3I--imidazol-4-yl} -6-methyl-pyridine; 107) 4-[2-(1-phenylmethanesulfonyl-piperidin-4-yl)-5-(6-methyl-pyridin-2-yl)-1H-imidazol 4-yl]-pyridin-2-yl- fluoride; 108) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-trifluoromethyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 109) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-bromo-pyridin-2-yl)-1-hydroxy-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 110) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-bromo-pyridine; 111) {4-[4-Benzo[ 1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- I-yl} -methanol; 112) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 113) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-2H-imidazol-2-yl]-piperidine-1 sulfonic acid dimethylamide; 114) 1-{4-[4-Benzo [1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin l-yl}-3-phenyl-propan-1-one; 115) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 116) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carbonitrile; 117) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1 -ylamine; 118) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1 -yl}-C-phenyl-methanesulfonamide; 119) N-{4-[4-Benzo [1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -methanesulfonamide; 120) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-pyridin-2-yl-methanesulfonamide; 121) 2-{5-Benzo[1,3]dioxol-5-yl-2-[4-(1H-tetrazol-5-yl)-bicyclo[2.2.2]oct-1-yl]-3H imidazol-4-yl}-6-rnethyl-pyridine; 122) N-{4-[4-Benzo [1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1 -yl}-acetamide; 21 WO 2006/044509 PCT/US2005/036770 123) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 124) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 125) Thiophene-3-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 126) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 127) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 128) Methanesulfonic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH imidazol-2-yl]-bicyclo[2.2.2]oct- 1-ylmethyl ester; 129) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetonitrile; 130) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -acetic acid; 131) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-niethanesulfonamide; 132) 2- {5-Benzo[1,3]dioxol-5-yL-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl] -3H-imidazol-4 yl} -6-methyl-pyridine; 133) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 134) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 135) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-phenyl-methanesulfonamide; 136) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-pyridin-2-yl-methanesulfonamide; 137) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid benzylamide; 138) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (pyridin-2-ylmethyl)-amide; 139) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid 3-chloro-4-fluoro-benzylamide; 22 WO 2006/044509 PCT/US2005/036770 140) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1HE-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (furan-2-ylmethyl)-airide; 141) 2-[5-Benzo[1,3]dioxol-5-yl-2-(i-methanesulfonyl-pyrroLidin-3-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 142) 2- {5-B enzo [1,3] dioxol-5-yl-2-[ 1 -(butane-i -sulfonyl)-pyrrolidin-3-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 143) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-1H-imidazole-4-sulfonyl)-pyrrolidin-3-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 144) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-pyrrolidin-3-yl)-3H-imidazol 4-yl]-6-methyl-pyridine; 145) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-pyrrolidin-3-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 146) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl } -6-methyl-pyridine; 147) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-2-yl-ethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 148) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1-sulfonylmethyl}-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 149) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfoinyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 150) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1TI-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid methylamide; 151) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1 1-imidazol-2-yl] bicyclo[2.2.2 ] octane-1 -carboxylic acid ethylamide; 152) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1Hi-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid butylamide; 153) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1Hi-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid isopropylamide; 154) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H--imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid (3-imidazol-1-yl-propyl)-amide; 155) 2-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1-sulfonylmethyl}-phenylamine; 156) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid (1-methyl-5-methylsulfanyl-1H-[1,2,4]triazol-3-yl) amide; 23 WO 2006/044509 PCT/US2005/036770 157) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid cyclohexylamide; 158) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-pyrrolidin-1-yl-methanone; 159) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid dimethylamide; 160) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid diethylamide; 161) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid dipropylamide; 162) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (5,7-difluoro-benzothiazol-2-yl)-amide; 163) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid benzothiazol-2-ylamide; 164) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (1H-benzoimidazol-2-yl)-amide; 165) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (2-hydroxy-1-methyl-2-phenyl-ethyl)-amide; 166) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (pyridin-4-ylmethyl)-amide; 167) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(3-chloro-phenyl)-methanone; 168) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(4-fluoro-phenyl)-methanone; 169) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl}-(4-methoxy-phenyl)-methanone; 170) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-cyclopropyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid; 171) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid methoxy-amide; 172) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carb oxylic acid hydroxyamide; 173) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-carbamic acid benzyl ester; 24 WO 2006/044509 PCT/US2005/036770 174) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid hydrazide; 175) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH-imidazol-2-yl] cyclohexylmethyl} -acetamide; 176) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6--methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -methanesulfonamide; 177) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-phenyl-methanesulfonamide; 178) Butane-1-sulfonic acid {4-[4-benzo[ 1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl}-amide; 179) Propane-2-sulfonic acid {4-[4-benzo [1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl} -amide; 180) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-2-yl-methanesulfonamide; 181) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-4-yl-methanesulfonamide; 182) (4-Methoxy-benzyl)-{4-[5-(6-methyl-pyridin-2-yl)-2-(1-phenylmethanesulfonyl piperidin-4-yl)-1H-imidazol-4-yl]-pyridin-2-yl}-amine; 183) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 184) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 185) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5- [1,2,4]triazolo[ 1,5-a]pyridin-6-yl- 1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 186) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 187) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid aide; 188) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid; 189) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-rnethyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 190) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 25 WO 2006/044509 PCT/US2005/036770 191) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1 I{-imidazol-2 yl] -bicyclo [ 2 .2.

2 ]octane- 1 -carboxylic acid amide; 192) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl] -bicyclo [2.2.2]octane- 1 -carboxylic acid hydroxyamide; 193) N-{4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-sulfamide; 194) Sulfamic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl ester; 195) {4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 196) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carbonyl} -methanesulfonamide; 197) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carbonyl} -benzenesulfonanide; 198) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxylic acid methyl ester; 199) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxylic acid; 200) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} acetamide; 201) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-bicyclo [2.2.2]octane 1-carboxylic acid methyl ester; 202) 4 -[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl] -bicyclo [2.2.2] octane 1-carboxylic acid; 203) 4 -[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid hydroxyamide; 204) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid amide; 205) N- {4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-cyclohexyl} methanesulfonamide; 206) 2,2,2-Trifluoro-N-{4-[4-(6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imicLazol-2-yl] cyclohexyl} -acetamide; 207) 4

-[

4 -(5-Fluoro-6-methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl- 1 H-imidazol 2-yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 26 WO 2006/044509 PCT/US2005/036770 2US) {4-L2-LI -(Butane-i -sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)- 1H-imidazol-4 yl]-pyridin-2-yl} -(4-methoxy-benzyl)-amine; 209) 4-[2-[ 1 -(Butane-i -sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)- IH-imidazol-4 yl]-pyridin-2-ylamine; 210) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-ethyl-pyridine; 211) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2] octane-i -carboxylic acid amide; 212) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-iH imidazol-2-yl]-bicyclo[2.2.2] octane-i -carboxylic acid hydroxyamide; 213) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; and 214) N-{ 4 -[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide. [052] In another embodiment, the antagonists have the structure shown below in formula II: YII-2 // (R11-2)n 4X 11 -1 ") IN Xu 3 N N XrI-4 [0531 In formula II, each of Xr.

1 , Xr- 2 , XI..

3 , and Xr- 4 can be independently CR-X or N, provided that only two of Xna 1 , Xr.

2 , Xr- 3 , and Xr..

4 can be N simultaneously. Each of Y 1 11 and Y- 2 can be independently CR"- or N, provided that at least one of Y 1 1

.

1 and Y 1

..

2 must be N. In other words, the ring having Yr..1 and Y 1

..

2 ring atoms can be a pyrimidinyl or pyridyl. Each R-1 can be independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, 27 WO 2006/044509 PCT/US2005/036770 heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, hetero aryloxy, heteroarylsulfanyl, or heteroaroyl. Each R"2 can be independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), N(alkyl)(cycloalkyl), -NH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosalfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylearbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaninoalkylaanino, (heteroaryl)arylsulfonylaninoalkylcarbonylaminoalkylamino, arylsulfonylaininoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl. m can be 0, 1, 2, 3, or 4, and when m 2, two adjacent RH1 groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. n can be 0, 1, 2, or 3, and when n 2, two adjacent R11- 2 groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. Each of RIIx and R""- can be independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamiao, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, 28 WO 2006/044509 PCT/US2005/036770 heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl. [054] As defined above in formula II, when m >_2, two adjacent R11 groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. That is, the 2 pyridyl ring can fuse with a 4- to 8-membered cyclic moiety to form a moiety such as 7H [1]pyrindinyl, 6,7-dihydro-5H-[1]pyrindinyl, 5,6,7,8-tetrahydro-quinolinyl, 5,7-dihydro furo[3,4-b]pyridinyl, or 3,4-dihydro-1H-thiopyrano[4,3-c]pyridinyl. The fused ring moiety can be optionally substituted with one or more substituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl; see the definitori of "alkyl" below), alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, alkoxy, aryl, heteroaryl, aryloxy, heteroaryloxy, aralkyloxy, heteroarylalkoxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, cycloalkyl-alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, heterocycloalkyl-carbonylamino, heterocycloalkyl alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbarnoyl. [0551 Similarly, when n >_2, two adjacent RI 2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety, thereby forming a ring fused with the pyridyl or pyrimidinyl group. Some examples of such a moiety are shown below: N N N N ON [0561 The 4- to 8-membered cyclic moiety formed by two adjacent Rr1 2 groups can be optionally substituted with substituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoromethyl; see the definiton of "alkyl" below), alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, alkoxy, aryl, heteroaryl, aryloxy, heteroaryloxy, aralkyloxy, heteroarylalkoxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, 29 WO 2006/044509 PCT/US2005/036770 alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, cycloalkyl-alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, heterocycloalkyl carbonylamino, heterocycloalkyl-alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylsulfanyl, sulfoxy, urea, thiourea, sulfamoyl, sulfamide, oxo, or carbamoyl. [057] Compounds of formula II and methods for producing the same are known in the art. For instance, WO 04/022054, which is incorpoarated in its entrity by reference, describes synthetic methods for producing inhibitors of formula II. Examples of compounds of formula II include, but are not limited to, 215) 4-[2-(6-Methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 216) 4-(2-pyridin-2-yl-pyrazolo[1,5-a]pyridin-3-yl)-pyrimidin-2-ylamine; 217) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 218) 2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-pyrazol [1 ,5-a]pyridine; 219) 4-[2-(6-chloro-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 220) 2-(6-methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-pyrazolo [1,5 c]pyrimidine; 221) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrazin-3-yl]-pyrimidin-2-ylamine; 222) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrimidin-3-yl]-pyrimidin-2-ylamine; 223) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; or a pharmaceutically acceptable salt or N-oxide thereof. [058] In another embodiment, the antagonists have the structure shown in formula III: YmI-2 R 111-2 / / (R-)n

-~~~~~Y-

1 (III) N N XIII- 4 [059] In formula III, each of X 1 1

-

1 , X 1 m- 2 , X 1 1 1

-

3 , and Xm-4 can be independently CRmIIx or N, provided that only two of XmII-1, XmI- 2 , Xm 1

-

3 , and Xm 1

-

4 can be N simultaneously. Each of Ym 11 1 and Ym-2 can be independently CR'-y or N, provided that at least one of Ym-1 and YI-2 30 WO 2006/044509 PCT/US2005/036770 must be N. Each of R'"' can be independently alkyl, alknyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboK-y, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocyclo alkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyL, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. Each of R 1-2 can be independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cyclocalkyl), NH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, (cycloalkyl)alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloallcyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonyl amino, heteroaralkylcarbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkyl-anaino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl. m can be 0, 1, 2, 3, or 4, and when m >2, two adjacent R" 1 u groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. n can be 0, 1, 2, or 3, and when n >2, two adjacent Rr' 2 groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. Each of Ru 11 x and R"' can be independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cyclc alkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsiilfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, 31 WO 2006/044509 PCT/US2005/036770 (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylainino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaxalkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl; or a pharmaceutically acceptable salt or N-oxide thereof. [060] Compounds of formula III and methods for producing the same are known iDL the art. For instance, WO 04/21989, which is incorpoarated in its entrity by reference, describes synthetic methods for producing inhibitors of formula III. Examples of compounds of formula III include, but are not limited to, 224) (2-Methoxy-ethyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 225) (3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylanjino} propyl)-carbamic acid tert-butyl ester; 226) (3-Imidazol-1-yl-propyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 227) (4-Methoxy-benzyl)-{4-[2-(6-niethyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 228) [2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridin 6-yl]-methanol; 229) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 230) (4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylaniino} butyl)-carbamic acid tert-butyl ester; 231) (4-Amino-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 232) (5-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylaniino} pentyl)-carbamic acid tert-butyl ester; 233) [3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-6-yl] methanol; 32 WO 2006/044509 PCT/US2005/036770 234) [3 -( 2 -amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-7-yl] methanol; 235) [3 -(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2 a]pyridin-8-yl] -(2-morpholin-4-yl--ethyl)-amine; 236) [3 -(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-8-yl]-(2-pyridin-2-yl-ethyl)-amnine; 237) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2 aljpyridin-8-yl] -(2-pyridin-3 -yl-ethyl)-amine; 238) [3-(2-methanesulfonyl-pyrimidin-4-yl) -2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-6-yl]-methaniol; 239) [3-(2-Amino-pyrimidin.-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2 a]pyridin-8-yl]-(2-pyridin-4-yl-ethyl)-amine; 240) [3 -(2-Ar-nino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-8-yl] -(3 -morpholin-4-yl-propyl)-amine; 241) [3-(4-Methyl-piperazin- 1-yl)-propyl-f {4- [2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-3-yl]-pyrimidin-2-yl} -amine; 244) [3 -(4-Methyl-piperidin- 1-yl)-propyl] - 4-[2-(6-metliyl-pyridin-2-yl)-imidazo[ 1,2 a]pyridin-3-yl]-pyrimidin-2-yl} -amine; 245) [4-(2-Pyridin-2-yl-imidazo [1 ,2-a]pyridin-3 -yl)-pyrimidin-2-yl]-pyridin-3-ylmethyl amine; 246) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3 -yl]-pyrimidin-2-yl} -((R)- 1 phenyl-ethyl)-amine; 247) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl] -pyrimidin-2-yl} -((S)- 1 phenyl-ethyl)-arnine; 248) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3 -yl]-pyrimidin-2-yl} -( H tetrazol-5-yl)-amine; 249) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-aljpyridin-3-yl]-pyrimidin-2-yl} -(2H pyrazol-3-yl)-amine; 250) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2-yl} -(2 morpholin-4-yl-ethyl)-amine; 251) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3 -yl]-pyrimidin-2-yl} -(2-pyridin 2-yl-ethyl)-arnine; 252) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2-yl} -(2-pyridin 3 -yl-ethyl)-amnine; 33 WO 2006/044509 PCT/US2005/036770 253) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 4-yl-ethyl)-amine; 254) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 morpholin-4-yl-propyl)-amine; 255) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 piperidin- 1-yl-propyl)-amine; 256) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} [1,3,4]thiadiazol-2-yl-amine; 257) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 258) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 6-carboxylic acid methyl ester; 259) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 7-carboxylic acid ethyl ester; 260) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2 a]pyrimidin-7-ylamine; 261) {7,7-Dimethyl-8-[5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-pentyl]-2-oxo-4-trifluoromethyl-7,8-dihydro-2H-1 oxa-8-aza-anthracen-5-yl}-methanesulfonic acid; 262) 2-(2,'7-Difluoro-6-hydroxy-3-oxo-9,9a-dihydro-3H-xanthen-9-yl)-3,5,6-trifluoro-4-[(4 {4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butylcarbamoyl)-methylsulfanyl]-benzoic acid; 263) -(6-lMethyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-imidazc>[1,2-a]pyridine; 264) 2-(6-Nethyl-pyridin-2-yl)-3-(2-piperidin- 1 -yl-pyrimidin-4-yl)-imidazo [1,2-a]pyridine; 265) 2-(6-Nethyl-pyridin-2-yl)-3-(2-pyrrolidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 266) 2-(6--Nethyl-pyridin-2-yl)-3-[2-(1H-tetrazol-5-yl)-pyrimidin-4-yl]-imidazo[1,2 a]pyridine; 267) 2-(6-IMethyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyridine; 268) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyrimidin-7-ylamine; 269) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-8 ylamine; 270) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonitrile; 271) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid; 34 WO 2006/044509 PCT/US2005/036770 2'/2) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylrnethyl)-amide; 273) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 274) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-dimethylamino-ethyl)-amide; 275) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-methoxy-ethyl)-amide; 276) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 277) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide; 278) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid amide; 279) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid cyclopropylamide; 280) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ethylamide; 281) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid hydroxyamide; 282) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methoxy-amide; 283) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methyl ester; 284) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid; 285) 3

-(

2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 286) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-amino-ethyl)-anride; 287) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-dimethylamino-ethyl)-amide; 288) 3-(2-Amino-pyrimidin-4-yl)-2--(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-hydroxy-ethyl)-ainide; 35 WO 2006/044509 PCT/US2005/036770 289) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-oxo-2-pyridin-3-yl-ethyl)-amide; 290) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 291) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (piperidin-3-yl-methyl)-amide; 292) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid 2,2-dimethylhydrazide; 293) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid amide; 294) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid cyclopropylamide; 295) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethyl ester; 296) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethylamide; 297) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid hydroxyamide; 298) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid methoxy-amide; 299) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 ylamine; 300) 3-(2-Azetidin-1-yl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine; 301) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-7-carboxylic acid ethyl ester; 302) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carboxylic acid methyl ester; 303) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-7-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 304) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-8-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 305) 3,3-Dimethyl-N-[2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl) imidazo[1,2-a]pyrimidin-7-yl]-butyramide; 306) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carbonitrile; 36 WO 2006/044509 PCT/US2005/036770 307) 3-(2-Methylsulfanyl-pyrimidin-4-yl)-2-pyridin-2-yl-imidazo[1,2-a]pyridine; 308) 3,6-Dichloro-N-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butyl)-2-(2,4,5,7-Tetrachloro-6-hydroxy-3-oxo-9,9a-dihydro-31 xanthen-9-yl)-terephthalamic acid; 309) 3-[2-(2-Methyl-aziridin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyridine; 310) 3-[2-(4-Methyl-piperazin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazc>[1,2 a] pyridine; 311) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-amino} -propionic acid methyl ester; 312) 3- { [3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl] -amino } -propionic acid methyl ester; 313) 3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino

}

phenol; 314) 4-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino } ethyl)-benzenesulfonamide; 315) 4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-ylamine; 316) 4-[2-(6-Chloro-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 317) 4-[2-(6-Methyl-pyridin-2-yl)-7-trifluoromethyl-imidazo[ 1,2-a]pyridin-3-yl]-pyrimi din 2-yl-amine; 318) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 319) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbonitrile; 320) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carboxylic acid amide; 321) 4-[6-Bromo-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 322) 4-[6-Chloro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 323) 4-[6-Fluoro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 324) 4-[ 6 -Methyl- 2 -(6-methyl-pyridin-2-yl)-8-(2-morpholin-4-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 325) 4

-[

6 -Methyl- 2 -(6-methyl-pyridin-2-yl)-8-(2-pyridin-2-yl-ethylamino)-imidazo[l,2-a] pyridin-3-yl]-pyrimidin-2-ol; 37 WO 2006/044509 PCT/US2005/036770 326) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-3-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrirmiidin-2-ol; 327) 4-[ 6 -Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-4-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 328) 4-[ 6 -Methyl-2-(6-methyl-pyridin-2-yl)-8-morpholin-4-yl-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ol; 329) 4 -[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-morpholin-4-yl-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamine; 330) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 331) 4 -[7-Aminoniethyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl-amine; 332) 4-[7-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 333) 4-[ 8 -Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ol; 334) 4 -[8-Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl amine; 335) 4-[8-Bromo-6 -methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-ol; 336) 4-[8-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 337) 6-Chloro-3-( 2 -methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 338) 5-Dimethylaniino-naphthalene-1-sulfonic acid (4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylanino}-butyl)-amide; 339) 6-(2,7-Difluoro-6-hydroxy-3-oxo-3H-xanthen-9-yl)-N-(4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-isophthalamic acid; 340) 6-Amino-9-[2-carboxy-5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-phenyl]-xanthen-3-ylidene-ammonium; 341) 6-Bromo-2-(6-rnethyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 342) 6-Fluoro-2-(6-methyl-pyridin-2-yl)-3-( 2 -methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 343) 7-Amino-4-methyl-3-[(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-methyl]-2-oxo-2H-chromene-6-sulfonic acid; 38 WO 2006/044509 PCT/US2005/036770 344) Cyclobutyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 345) Cyclopentyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl }-amine; 346) Cyclopropyl-{4-[2-(6-methyl-pyridin-2-yl)-iniidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl} -amine; 347) Cyclopropyl-methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 348) Dimethyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 349) Isopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 350) Methyl- {4-[2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 350a) N-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin-2 ylamino} -ethyl)-acetamide; 351) N-(4- {4- [2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3 -yl] -pyrimidin-2-ylamino } butyl)-acetamide; 352) N,N-Dimethyl-N'-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl} -ethane- 1,2-diamine; 353) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 354) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 355) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 356) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-methanesulfonamide; 357) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl]-methanesulfonamide; 358) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-2-(3-methoxy-phenyl)-acetamide; 359) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-3,3-dimethyl-butyramide; 39 WO 2006/044509 PCT/US2005/036770 360) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iinidazo[1,2-a]pyrimidin-7 yl]-3-pyridin-3-yl-propionamide; 361) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-ixnidazo[1,2-a]pyrimidin-7 yl]-acetamide; 362) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-ixnidazo[1,2-a]pyrimidin-7 yl]-nicotinamide; 363) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-2-(3-methoxy-phenyl)-acetamide; 364) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3,3-dimethyl-butyramide; 365) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 366) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 367) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 368) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-irnidazo[1,2-a]pyrimidin-7 yl]-propionamide; 369) N-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide; 370) N1-{4-[2-(6-Methyl-pyridin-2-yl)-inidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-butane 1,4-diamine; 371) N1-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} propane-1,3-diamine; 372) N-(4- {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3 -yl]-pyrimidin-2-ylamino} butyl)-(BODIPY FL) amide; and 373) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3 -yl]-pyrimidin-2-ylamino} butyl)-(Texas Red-X) aide 374) N-[3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iniridazo[1,2-a]pyrimidin-7 yl]-acetamide; and 375) N-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide. [0611 In yet another embodiment, the antagonists have the structure shown in formula IV: 40 WO 2006/044509 PCT/US2005/036770 R IV 5 R ~6 N RIV-1._RIV-2. RV -3 -R IV-4 \~ ~ N (RV-a)m or an N-oxide or a pharmaceutically acceptable salt thereof. [0621 Each RIV-a can be independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. [063] R~IV can be a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri-O-(CH 2 )r 2 -, wherein each of r1 and r2 is independently 2 or 3. [064] R- 2 can be cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, or a bond. [065] RW~ 3 can be -C(O)-, -C(O)O-, -OC(O)-, -C(O)-N(R-b)-, -N(Rv-b)-C(O)-, -O-C(O) N(R b)-, -N(Rv ~6)-C(0)-0-, -O-S(O),-N(RI ~')-, -N(R" -)- S(O)p-0-, -N(R ~h)-C(O) N(R v-)-, -N(Rv -b)-S(O)p-N(Rv ~6)-, -C(O)-N(Re-b)-S(O)p-, -S(O)p-N(R b)-C(O)-, -S(0), N(R! ~ )-, -N(Rw ~b)-S(O)p-, -N(R ~b)-, -S(O)p-, -0-, -S-, or -(C(R ~c)(RW))q-, or a bond; wherein each of RIV~b and RW-c is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; p is 1 or 2; and q is 1-4. 41 WO 2006/044509 PCT/US2005/036770 [066] Rv- 4 can be hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl. [0671 RW 5 can be hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoixy, cycloalkylsulfinyl, heterocycloalkyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryloxy, or heteroarylsulfinyl. [0681 R'v~ 6 can be (1) a 5- to 6-membered heterocyclyl containing 1-3 hetero ring atoms selected from the group consisting of-O-, -S-, -N=, and -NRwv-d-, wherein Rwv~d can be hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkyl alkyl, heteroaryl, or heteroaralkyl; said heterocyclyl being substituted with Rlv-' and optionally substituted with one to two Rwf; where Rrv~e is oxo, thioxo, alkoxy, alkylsulfinyl, -TI2, -NH(unsubstituted alkyl), or -N(unsubstitutec alkyl) 2 , and R'Vf can be alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, arnidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfiayl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, aikylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or [069] (2) a fused ring heteroaryl selected from the group consisting of: (RI)n (RI)n (R')n (Ri)n B' BX1 B' OB ~~~ and ', a ,)X X22 3 X2 I Axxj 2 0 x1 51Zatd2 Ring A can be an aromatic ring containing 0-4 hetero ring atoms, and ring B can be a 5- to 7 membered aromatic or nonaromatic ring containing 0-4 hetero ring atoms, provided that at least one of ring A and ring B contains one or more hetero ring atoms. Ring A' can be an aromatic ring containing 0-4 hetero ring atoms, and ring B' can be a 5- to 7-membered saturated or unsaturated ring containing 0-4 hetero ring atonis, provided that at least one of ring A' and ring B' contains one or more hetero ring atoms. Each hetero ring atom can be 42 WO 2006/044509 PCT/US2005/036770 0-, -S-, -N=, or -NR -. Each X 1 can be independently N or C. Each X 2 can be independently -0-, -S-, -N=, -NRI -g-, or -CHR ~- in which Rrv~ can be hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl. Each of Rr-h and R'vi can be independently alkyl, alkenyl, alkynyl-, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylarmino, arylcarbonylamino, heteroarylcarbonyl-amino, alkylsulfonylamino, arylsulfonylamiiio, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbcnyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkyl-sulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. n can be 0-2. m can be 0-3, and when m 2, two adjacent RIva groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety; [070] In compounds of formula IV, if R'v~ 6 is 2-naphthyridinyl, 4-quinolinyl, imidazo[1,2 a]pyridyl, or benzimidazolyl, then -R-1-R -2 -R v-3 -R- is not H, unsubstituted alkyl,

-CH

2 -C(O)-N(H)-alkyl, -CH 2 -C(O)-N(alkyl) 2 , or benzyl. 1071] Compounds of formula IV and methods for producing the same are known in the art. For instance, WO 04/072033, which is incorpoarated in its entrity by reference, describes synthetic methods for producing inhibitors of formula IV. Examples of compounds cf formula IV include, but are not limited to, 376) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propylamine, 377) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-acetamide, 378) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-methanesulfonamide, 379) dimethyl-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-amine, 380) 4-{3-pyridin-2-yl-1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-pyrazol-4-yl}-quinoline, 381) 4-[3-pyridin-2-yl-1-(3-pyrrolidin-1-yl-propyl)-1H-pyrazol-4-yl]-quinoline, 382) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, 383) 2,4-dimethoxy-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 384) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionic acid, 385) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indole, 386) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-pyridine, 387) N-hydroxy-3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-I-yl)-propionamide, 388) 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethylamine, 43 WO 2006/044509 PCT/US2005/036770 389) N-[2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethyl]-methanesulfonamide, 390) 2-methyl-4-methylsulfanyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 391) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-pyridine, 392) 2-[4-(2,3-dihydro-benzofuran-5-yl)- 1H-pyrazol-3-yl]-pyridine, 393) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[d]isoxazole, 394) 3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propionitrile, 395) N-{3-[4-benzo[1,3]dioxol-5-yl-3-(6-rnethyl-pyridin-2-yl)-pyrazol-1-yl]-propyl} methanesulfonamide, 396) 2-[4-(2,3-dihydro-benzo [1,4]dioxin- 6-yl)-1 H-pyrazol-3 -yl]-6-methyl-pyridine, 397) [4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-acetonitrile, 398) N- {2-[4-benzo [1,3]dioxol-5-yl-3-(6-inethyl-pyridin-2-yl)-pyrazol- 1 -yl]-ethyl} methanesulfonamide, 399) 4-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-2-methylsulfanyl-pyrimidine, 400) 4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-2H-phthalazin-1-one, 401) 1-[5-(3-pyridin-2-yl-1H-pyrazol-4-yL)-2,3-dihydro-indol-1-yl]-ethanone, 402) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[ 1,2,4]triazolo[1,5-a]pyridine, 403) 3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 404) 6-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-41H-benzo [1,4]oxazin-3-one, 405) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoxaline, 406) 3-(4-nitro-benzyl)-6-(3-pyridin-2-yl- 1H-pyrazol-4-yl)-3H-quinazolin-4-one, 407) 5-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 408) 4-methyl-7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3,4-dihydro-1H-benzo[e][1,4]diazepine 2,5-dione, 409) 2,3-dimethyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 410) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 410a) 1-methoxy-4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-isoquinoline, 411) 2-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 411 a) 4-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-2H-isoquinolin- 1-one, 412) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-trifluoromethyl-pyridine, 412a) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-vinyl-pyridine, 413) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propenyl-pyridine, 414) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-ethyl-pyridine, 415) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-y)-6-propyl-pyridine, 416) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-cyclopropyl-pyridine, 417) 1-[6-(4-benzo[ 1,3 ]dioxol-5-yl- 1 H-pyrazol-3 -yl)-pyridin-2-yl]-ethanol, 44 WO 2006/044509 PCT/US2005/036770 418) 4-methoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 419) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline, 420) 6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-quinazolin-4-ylamine, 421) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 422) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrido[1,2-a]pyrimidin-4-one, 423) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 424) 3-methyl-6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3H-quinazolin-4-one, 425) 4-(2-{2-[4-benzo[1, 3 ]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane-1-carboxylic acid, 426) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester, 427) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester, 428) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-isopropyl-pyridine, 429) 2-(4-benzo[1,3]dioxol-5-yl-5-trifluoromethyl-IH-pyrazol-3-yl)-6-bromo-pyridine, 430) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 431) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1 ,2,4]triazolo[1,5-a]pyridine, 432) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxalire, 432a) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-methyl-3H-quinazolin-4-one, 433) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-b]pyridazine, 433a) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline:, 434) 6-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-3-fluoro-2-rmethyl-pyridine, 435) 7-methoxy-3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 436) (4-morpholin-4-yl-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-amine, 437) 4-isopropoxy-6-(3 -pyridin-2-yl- 1H-pyrazol-4-yl)-quinazo line, 438) 6-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-quinolin-4-ylamine, 439) {4-[4-benzo[1, 3 ]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} carbamic acid benzyl ester, 440) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexylamine, 441) N- {4-[4-benzo[ 1, 3 ]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)- pyrazol- 1 -yl]-cyclohexyl} methanesulfonamide, 442) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-lH-pyrazol-4-yl]-quinoxaline, 443) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 444) 1-tert-butyl-3-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-urea, 445) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]thiadiazole, 45 WO 2006/044509 PCT/US2005/036770 446) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]oxadiazole, 447) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-benzooxazole, 448) 4-morpholin-4-yl-6-(3-pyridin-2-yl-1IH-pyrazol-4-yl)-quinazoline, 449) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 450) 4-(4-methoxy-phenyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 451) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-benzo[1,2,5]thiadiazole, 452) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzothiazole, 453) 3-(3-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 454) 5-methyl-thiophene-2-carboxylic acid [6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4 yl] -amide, 455) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-phenyl-benzo[c]isoxazole, 456) 3-(4-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 457) 3-(4-chloro-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 458) 3-(4-ethyl-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 459) (4-methoxy-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-methanone, 460) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3-thiophen-3-yl-benzo[c]isoxazole, 461) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid, 462) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-IH-indazole-3-carboxylic acid methylamide, 463) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid dimethylamide, 464) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid (2,2-dimethyl propyl)-amide, 465) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid phenylamide, 466) morpholin-4-yl-[5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazol-3-yl]-methanone, 467) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid benzylamide, and 468) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid cyclopentylamide. [072] In another embodiment, the antagonists have the structure shown in formula V. 46 WO 2006/044509 PCT/US2005/036770 (Rv-a)m N NM V-2 ()

-

Xv-Yv-R V-2 62 1V V V Rv-1 Av- 1 wherein R - can be heteroaryl. [073] Each Rva, independently, can be alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. [074] Xv can be cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or a bond. [075] Yv can be a bond, -CCO)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(Rv-b), -N(R )-C(O)-, -O-C(O)-N(')-, -), N(Rb)-0-, -O-N( - )-C(O)-, -O-S(0)p-N(RW-b)-, -N(R')- S(O)p-O-, -S(O)p-N(RW~6)-O-, -O-N(Re ~h)-S(O)p-, -N(RW-b)-C(O)-N(R'~c)-, -N(R.7~6)-S(O)p-N(Rv-)-, -C(O)-N(RW~h)-S(O)p-, -S(O),-N(Rk~ b)-C(O)-, -C(O)-N(Rv-b)-S(O)p-N(RW~c)-, -C(O)-0-S(O)p-N(Rv-b)-, -N(Rv-b)-S(O)p-N(Rk~ C)-C(O)-, -N(RW-)-S(O)p-O-C(O)-, -S(O))p-N(Rk-v), -N(R,- )S(O)p-, -N(RW~ ), -S(O)p-, -O-, -S-, or -(C(Rv~b)(Rv~c))q-. Each of R'b and RVc , independently, can be hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl. p can be 1 or 2, and q can be 1-4. [076] Rv- 2 can be hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, 47 WO 2006/044509 PCT/US2005/036770 (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl. [0771 Each of Av- 1 and A,~ 2 , independently, can be N or NR-b. It is to be understood that when A 1 is NRv-b, Av-2 is N, and vice versa. The variable, m, can be 0, 1, 2, or 3. In other words, the pyrimidinyl ring can be unsubstituted or substituted with 1-3 Rva gro-ups. Note that when m >_2, two adjacent Rv-a groups can optionally together to form a 4- tco 8-membered optionally substituted cyclic moiety. That is, the pyrimidinyl ring can fuse with a cyclic moiety to form a moiety, that can be optionally substituted with one or more sub stituents such as alkyl (including carboxyalkyl, hydroxyalkyl, and haloalkyl such as trifluoroniethyl), alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, alkoxy, aryl, heteroaryl, aryloxy, heteroaryloxy, aroyl, heteroaroyl, amino, nitro, carboxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylcarbonylamino, cyano, halo, hydroxy, acyl, mercapto, alkylthio, sulfoxy, sulfamoyl, oxo, or carbamoyl. Note also that if Xv is a bond, then Yv is a bond; RV-2 is hydrogen or alkyl; m is 1, 2, or 3; and at least one Rv-a is substituted at the 2-pyrimidinyl position (i.e., the position of the pyrimidinyl ring that is between the two nitrogeni ring atoms). [078] Compounds of formula V may be prepared by a number of known method, ds from commercially available or known starting materials. In one method, compounds of formula V are prepared according to Scheme described below. Specifically, in Scheme V-1a, optionally substituted 2-methylpyrimidine (II) is deprotonated by LDA before reacting with Rv --substituted carboxylic acid methoxy-methyl-amide (I) to form an Rv~ -(6 methylpyrimidinyl)-ketone (III), wherein Rv- 1 has been defined above. The metlioxy-methyl amide can be prepared by reacting a corresponding acid chloride (i.e., R - -CO-Cl) with N, 0-dimethylhydroxylamine hydrochloride. The Rv~l-(6-methylpyrimidinyl)-ketone (III) can then be treated with sodium nitrite in acetic acid to afford an a-keto-oxime (IV), -which can undergo a further reaction with an appropriate substituted (and optionally protected) aldehyde (VI) in the presence of ammonium acetate to yield a compound of formula V. 48 WO 2006/044509 PCT/US2005/036770 Scheme V-la (v '~1. LDA Rv Rv-a)

CH

3 mV- NaNO 2 2.RvY NOCH3 O N-N HOAc 0 (1) (Il) 1. NH 4 OAc /OH -O N / Rv-a H Xv-Yv-RV.

2 RV1 Rvl m (VI) (Rv-a) N (R \>-XvYVRv2 O N N 2. TiCl 3 , MeOH or N P(OMe) 3 or P(OEt) 3 N N (IV) (V) [0791 In another method, the above-described compounds of formula V can be prepared according to Scheme V-lb below. Specifically, 1,1-dimethoxy-propan-2-one can first react with dimethoxymethyl-dimethyl-amine at an elevated temperature to produce the intermediate 4-dimethylamino-1,1-dimethoxy-but-3-en-2-one, which can then react an Rva_ substituted amidine to form an R v-a-substituted pyrimidine-2-carbaldehyde (Ha). This carbaldehyde (Ila) can then react with aniline and diphenyl phosphite to form a resulting AP acetal, which can further couple with an Rv~1-substituted aldehyde to produced an (R~1 methyl)-pyrimidinyl-ketone (IIla). See, e.g., Journet et al., Tetrahedron Lett. 39:1717-1720 (1998). Treatment of the (R~-lmethyl)-pyrimidinyl-ketone (IIla) with sodium nitrite in acetic acid produces an a-keto-oxime (IVa), which can undergo a reaction with an appropriate substituted (and optionally protected) aldehyde (VI) to yield a compound of formula V as described in Scheme V-la above. 49 WO 2006/044509 PCT/US2005/036770 Scheme V-1b 0 NH 0 N 0 neat, 80 C v-a HBr/H20 -p N- , Ra kNH 2 Hr/0 0 / RV-aN 01 0 0/n 0 O ,OPh -1Rv CHO PHOPh 1. R 1 -CHO PhNH 2 NH CS 2 00 3 N N (PhO) 2 P(O)H Y 2. HCI N N RV-a RV-a Rv-a (Ila) (lila) 1. NH 4 0Ac Rv- 1 N, NaNO 2 OH H Xv-Yv-RV- 2 Rv- 1 N 0 (VI) I"Xv-Yv-RV-2 HOAc/THF/H 2 O NY -- N Nz N 2. TiC 3 , MeOH or H RV-a P(OMe) 3 or P(OEt) 3 N N Rv-a (IVa) (V) [080] In another method, the above-described compounds of formula V can be prepared according to Scheme V-ic below. Specifically, an (RV~-methyl)-pyrimidinyl-ketone (Ila) (described above) can be oxidized to form a pyrimidinyl-diketone (IVb), which can undergo reaction with an appropriate substituted (and optionally protected) aldehyde (VI) to yield a compound of formula V (V) as described above. 50 WO 2006/044509 PCT/US2005/036770 Scheme V-1c (Rv Rva NBS/DMSO. (Rv-rnv QN NV Rv- 1 00 (lila) (lVb) 1. NH 4 0Ac O H Xv-Yv-RV- 2 (v2 (Rv-a~r~ M (VI) N I - Xvs Rv-2 2. TiC1 3 , MeOH or Rv- N Yv' P(OMe) 3 or P(OEt) 3 H (V) [0811 If compound (VI) is in its protected form, appropriate deprotecting agents can be applied to the resulting compound after the coupling reaction of compound (IV) or (IVa) and compound (VI) to yield a compound of formula V (V). See, e.g., T. W. Greene, Protective Groups in Organic Synthesis, John Wiley & Sons, Inc., New York (1981), for suitable protecting groups. [0821 Alternatively, a compound of formula V can be prepa-red by reacting intermediate (IV) or (IVa) with an aldehyde (VII) to yield a further intermediate (VIII), which can then react with compound (IX) to yield a compound of formula V.. Note that moieties Y' and Y" are precursors of moiety Yv. See Scheme V-2 below. In addition, desired substitutions at Rva can be obtained by selecting, for example, the appropriate compound (IIa) intermediate. 51 WO 2006/044509 PCT/US2005/036770 Scheme V-2 N N 0 (IV) (Rv-a) m Rv-1 NOH 1.NH 4 OAc or 0 S Rv-1 N N N NOH H Xv-Y' (R (IVa) (R -a 1 (VII) r, . N Rv - 2. TiC1 3 , MeOH N N 0 or (Vill) N O~ ~RV v (lVb) (RZv-a )_ 0 R 1" R _________ (RV a N RmXv-Yv-RV-2 ~. N fl H N N (V) In some embodiments, moiety Xv in compound (VII) is a nitrogen-containing heterocycloalkyl (e.g., piperidine). The nitrogen ring atom can be protected by a nitrogen protecting group (e.g., Cbz, Boc, or FMOC) before coupling to compound (IV) or (IVa) and deprotected afterwards (see first step of Scheme 3) to yield compound (VIIIa). This compound can further react with various compounds (IX) to produce a compound of formula V. See second steps of Scheme V-3 below. It should be noted that compound (VIII) or compound (VIla) can be a compound of formula V as well. 52 WO 2006/044509 PCT/US2005/036770 Scheme V-3 NVN 0 (IV) (Rv-a Rv-1N 1. NH40Ac NOH or H 0N Cbz NHN H- R Rv-1 N N b Deprotection (using RV-a) N-L; NOH (I)N-Cbz (IVa) (Rv N agents,e.g.,H2, Pd/C mN Rv 1 [.IC3,MO H - orHBr/HOAc) O2. TiCI 3 , MeOH N N or (Vill) N 0V ([Vb) (Rv-a R RV- 2

SO

2 CI (IX) Rv-1 N 0-1 DIEA m I" N- S0 2 RV-2 N )1-3 [1H N,. N (V) RV-2OCOCI (IX) RVl N ) o-i 0 NaH CO 3 m NN W-2 Rv-1 1-3 Rv-2NCO (IX) N Rv 2 N N DIEA N N (Villa) N N (V)

R

2 v-COCI (IX) or (RV Rv- 1 N )0- 0 Rv- 2 COH (IX), DIEA or N R-2 Rv-zCOOH (IX), ) H coupling agent, e.g., N N HATU (V)

RV-

2 CHO (IX) Rv- 1 N ) 0-1 NaB(OAc) 3 H m-3 Rv-2 H N ,N (V) [083] Similarly, when moiety X in compound (VII) is a cycloalkyl (e.g., cyclopentyl, cyclohexyl, or bicyclo[2.2.2]octane), it can be further functionalized to form a compound of formula V as depicted in Schemes V-4, V-5a, V-5b, and V-5c below. 53 WO 2006/044509 PCT/US2005/036770 Scheme V-4 (IV) (Rk 1

R

1 1. NH 4 OAc NOH

R

or 9\, NHCbz Rv- RV 1 N 0-1 NHCbz hR~rl 1 0-1 H~,iN )1-N __________________ [ H Deprotection (using (IVa) NR- N NOH, (I)NN agents, e.g.,H 2 , Pd/C ' Rv 1 ' 2. TiCI 3 , MeCH (VilI) orHBrHOAc) 0 o k Rvl' N 0-1 NHS0 2

RV-

2 NN 0 Rv 2 ~RS0 2 CI OIX) (va, (Ib Ra0~,DE N )1-3 (lb N RVI H 0 N ,, N - N01 N4 R 2

RV

2 0C0CI (IX) (RvaT VJ ~ NaHCO 3 H f )l. N , , N Rv-i N (Rv-a) 2 -1 HO-j R-. N i NCO (IX) (Rva) Rv0 N H DIEA ! 13 H (Villa) N,, NM RV-2C0CI (IX) or RV N )0--iN RV-2COH (IX), DEA or (RV'a I 2 R-2COOH (IX), coupling N1 agent, e.g., HATU ri 'H, N,, N RVa2CHO (IX) (RRa VI N H NaB(OAc) 3 H 0I R V N MV 54 WO 2006/044509 PCT/US2005/036770 Scheme V-5a N N 0 (IV) (RV-ayv-1 NOH 1.NH 4 0Ac or 0 HA< COIOMe RV-' N N N NOH(R). (A) (EVa) (Rv-a) 1 N; R (VII) (RV i COOMe

RV-

1 H O 2. TiCl 3 , MeOH NN or (I b g-a R 0 ~(Rv , Rv 1 ' Deprotection COOH (using reagents, e.g., LOH) NN H (can be further modified according to Scheme 5b (IV) (Rv-a Rv-1 below) NOH 1. NH 4 0Ac or H)<-&OHN NN NOH (VII) (Rv-a RV 1 _ _) I~a (R-a OH RvRv-1 a2. TiCC 3 , MeOH O O N N or (V) (IVb) (RV2)m -- N 0V (Rv COOH NH(RV-b)SO 2 CII 2\OS NHRb N N N (V) 55 WO 2006/044509 PCT/US2005/036770 Scheme V-5b (R V COOH Rv-2 (Ry Rv-2 (1) m ,, ~ VOH m N> RV N N NN H (v) (V) (m X- COOH Rv- 2

NH

2 (

~

()N .,N HNF N HNHV N N ( R v a ) R v 1 CN (O Ov 1 . H T U N H rn G OOH R v-S 2 NH(Rb m NINHORV N N ~ EDV-2 [ N N,. N (4) N,,~N H2. reducing agents N N(e.g., BH 3 'THF)HNH v Rv-1 V R (RI COOH dihev-phosNhorvlazide N MR 1 (Rv(R NH2R IN N (Vv) (can be further modified according to Scheme 5c below) CR()RRRN (5) N N H (V) (V)

H

2 , Pd/C or (RV-a ) R NN HBr/HOAc H N ,, N (v) (can be further modified according to Scheme 5c below) 56 WO 2006/044509 PCT/US2005/036770 ( R6)a) N

BH

3 THF (Rva Rv 1 N OH R 2

SO

2 Cl (6) CO N THF -' NDIEA THE N N H (V) (v) (Rva Rv-2 N C (R v CN >_o0 NaCN (R 1 N N N 0N N H CRy-a Rv-i N iC(IvN) 4 C-

HCI/H

2 0 m N~ CRy) Rvj N ( N (R Hm N ,,, HN-N I' N -C COOH (v) N N H (V) Rv 1N R Rv-1 N Trifluoroactic (7) ( \>COOH HATU, NH 3 m j

CONH

2 anhydride N H DMF H H Pyridine, THF N N N -~N (V) (v) (R CN NaN 4 (R v N N-N N 3 N~~N H LICI /NHCI- N N NN H H (v) (V) 57 WO 2006/044509 PCT/US2005/036770 Scheme V-5c Rv- 2 S0 2 CI (IX) (Rv) Rv-1 N NHSO 2 Rv-2 DIEA m N H N N (V)

RV-

2 0COCI (IX) aRv1 N H NaHCO 3 , v N N (v) R v-1 (R v N R v 2 N C O (IX ) (R) R v -1 N O- v-2 N N H DiEA (V) N N (V) Rv-20CO (IX) or RH O Rv 2 COH (IX), DIEA or (Ra) NN RV-ACOOH (IX), coupling m~ N agent, e.g., HATU flH N N (V) RH

RV

2 CO (IX) or-a N NaB(OAc)H(IX), N(R Rv N gN (V) [084] As is well known to a skilled person in the art to which the present invention relates, desired substitutions can be placed on the pyrimidinyl ring in the last steps of the synthesis. See, e.g, Scheme V-6 below. 58 WO 2006/044509 PCT/US2005/036770 Scheme V-6 01 0 HNA N N N iN N )'N I HI H -« Iz H N H 2 0 2 , NaWO 4

H

2 0 H2N N -- Xv'Yv--R-2 Xv-Yv-R-XvYv-Rv-2 Rvi N H 2

SO

4 , MeOH Rv-1 N Reflux Rv-1 N (v) (V) (V) [085] Compounds of formula V wherein Rv~b is not hydrogen can also be prepared by known methods. For example, compounds of formula V wherein AvI is N and AV- 2 is NH (or vice versa) can be treated with R I (e.g., alkyl iodide) and CsCO 3 to produce a compound of formula V wherein Rv-b is alkyl. See, e.g., Liverton, et al., J Med. Chein., 42: 2180-2190 (1999). [0861 As will be obvious to a skilled person in the art to which the present invention relates, some starting materials and intermediates may need to be protected before undergoing synthetic steps as described above. For suitable protecting groups, see, e.g., T. W. Greene, Protective Groups in Organic Synthesis, John Wiley & Sons, Inc., New York (1981). [087] Examples of compounds of formula V include, but are not limited to, 469) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzamide; 470) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzonitrile; 471) 4-[5-(2-methanesulfonyl-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 472) 4-[5-(2-methoxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-lH-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 473) 4-[5-(2-hydroxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 474) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2] octane-i -carboxylic acid methyl ester; 475) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1 -carboxylic acid; 59 WO 2006/044509 PCT/US2005/036770 476) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -b icyclo [2.2.2] octane-1 -carboxylic acid amide; 477) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -b icyclo[2.2.2] octane-i -carboxylic acid hydroxyamide; 478) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid methoxy-amide; 479) 4-[5-(2-amino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid; 480) {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-iH-imid-azol-2 yl]-bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 481) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-inidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-acetamide; 482) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-iriidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 483) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-inaidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 484) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 485) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 486) 6-[2-tert-butyl-5-(2-cyclopropyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 487) 6-[5-(2-byclopropyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 488) {4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1 -yl} -methanol; 489) 6-[5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 490) 6-[2-tert-butyl-5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 491) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 492) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-piperidine- 1 carboxylic acid benzyl ester; 493) 6-[5-(2-cyclopropyl-pyrimidin-4-yl)-2-(1-methanesulfonyl-piperidin-4-yl)-3H-irnidazol 4-yl]-quinoxaline; 494) 4-[5-(2-methyl-pyrimidin-4-yl)-4-[1,2,4]triazolo[4,3-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 60 WO 2006/044509 PCT/US2005/036770 495) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid amide; 496) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carb oxylic acid; 497) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 498) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexanol; and 499) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol. [088] In still another embodiment, the antagonists have the structure shown in formula VI: RV1-5 Rv1-6 N'RVI-1_ RVI-2 -RVI-3_ vI-4 N __ (VI) N (RV1-a)m [089] In formula VI, each Rvi-a, independently, can be alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, -NH 2 , -NH(unsubstituted alkyl), -N(unsubstituted alkyl) 2 , nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. [0901 RvIN can be a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )rrO-(CH 2 )r2-, wherein each of rl and r2, independently, is 2 or 3. 61 WO 2006/044509 PCT/US2005/036770 [0911 RL-' can be cycloalkylene, heterocycloalkylene, cycloalkenylene, heterocycloalkenylene, arylene, heteroarylen.e, or a bond. [092] RV- 3 can be -C(O)-, -C(O)-O-, -O-C(O)-, -S(O),-O-, -O-S(O)p-, -C(O)-N(R Vb)-, -N(RvI-b)-C(O)-, -O-C(O)-N(Rv'-b)-, -N(Rv )-C(O)-O-, -C(O)-N(Rv-b)-0-, -O-N(R b)-C(O)-, -O-S(O)p-N(R v- )-, -N(Rv)- S(O)p-O-, -S(O)p-N(R )-O-, -O-N(Rvl-b)-S(O)p-, -N(Rv 1-b)-C(O)-N(R I-c)-, -N(Rv"-)-S(O)p-N(R I-c)-, -C(O)-N(Rv'-b)-S(O),-, -S(O)p-N(Rv 1-b)-C(O)-, -C(O)-N(R ~ b)-S(O),-N(R vI-c)-, -C(O)-O-S(O)p-N(Rv'-b)_ -N(RvI-b)-S(O),-N(Rv1-c)-C(0)-, -N(Rv'-b)-S(OD)p-O-C(O)-, -S(O)p-N(Rv'-b)-, -N(Rv'~6)-S(O)p-, -N(RvI~b)-, -S(O)p-, -0-, -S-, -(C(RVIb)(RvI~C))q-, or a bond. Each of RVIb and R~", independently, can be hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl. p can be 1 or 2 and q can be 1-4. [093] RvI~ 4 can be hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl. [0941 RI- 5 can be hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryloxy, arylsulfinyl, heteroaryloxy, or heteroarylsulfinyl. [0951 RV- 6 can be a 5- to 6-membered monocyclic heterocyclyl or a 8- to l1 -membered bicyclic heteroaryl, and optionally substituted with alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl. [0961 The value of m can be 0-3, and when m >_2, two adjacent Ra groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety. [0971 Compounds of formula VI are commercially available or may be prepared by a number of known methods from commercially available or known starting materials. 62 WO 2006/044509 PCT/US2005/036770 [0981 In one method, compounds of formula VI are prepared according to Scheme VI-1 shown below. Specifically, a pyrimidine of formula II, which contains a 2-(a, 13-unsaturated carbonyl) substituent can cyclize with hydrazine to form a pyrazole core ring to produce a 2 (pyrazol-3-yl)-pyrimidine intermediate (III). Note that the pyrimidine of formula II can be prepared by known methods (see, e.g., Jameson, D. and Guise, L. Tetrahedron Letters, 32(18): 1999-2002). The intermediate (III) can be further substituted at the 4-po sition of the pyrazole core ring with a good leaving group such as halo (e.g., iodo or bromo) by reacting with a halogenation reagent (e.g., bromination reagent such as Br 2 or iodination reagent such as N-iodosuccinimide) to form a 2-(4-halo-pyrazol-3-yl)-pyrimidine (IV). Note that halo is represented by moiety X in Scheme VI-1. The halo substituent forms an ideal platform for RvI~ 6 substitutions. For example, the iodo substituent can be converted into a boronic acid substituent (see compound (V) below), which can react with a Rv - 6 -halide (VI) (e.g., an aryl halide or a heteroaryl halide) via Suzuki coupling reaction to form a compound of formula VI. Other substitution reactions can also be employed to produce a wide range of compounds of formula VI (see, e.g., via a reaction between the protected iodinated compound (IVa) and phthalic anhydride to form a di-keto intermediate (VII), which can undergo a cyclization reaction with an Rg-substituted hydrazine to form a compound (VI); for reference, see J. Med. Chem., 44(16): 2511-2522 (2001). It should be noted that the pyrazole core ring should be properly protected (see, e.g., the N,N-dimethylaminosulfonyl group of compound (IVa)) to eliminate undesired side reactions. 63 WO 2006/044509 PCT/US2005/036770 Scheme VI-1 0 1. NaOH N O CH 3 MgI N

OCH

3 2. (COCIk, benzene >(Rvi-a N THF vi-a 3. CH 3

NH(OCH

3 ).HCI, "N O 0 C (R Et 3 N, CHCl 3 X 0 H 2

NNH

2 NH Halogenation NH DME1A - .- EtOH N N DMFQ(MA ri'N N N reagent N' DMF .(i N e.g., Br 2 N (RvI-a)m (Rvi-a)M (IV) Protecting group X 1. iPrMgBr, THF (HO) 2 B (e.g.,(CH 3

)

2

NSO

2 CI) N ,N-S0 2 2. (MeO) 3 B, THF N ,N S0 2 _ _ _ N \_

-

N\ Et 3 N, CHCl 3 N N(CH 3

)

2 00C - rt N N(CH 3

)

2 (RVI-a)m (RVi-a)m (IVa) (V) 0 iPrMgBr RvI- 6 -halide (VI) Pd (0) catalyst 0 THF Br N (e.g., Pd(Ph 3

P)

4 ) 00 - rt (e.g., ) aq. Na 2

CO

3 , DM E N 850C HO 0 ~6Rvi N N ,N O 2N -\ 2 N \N N(CH 3

)

2 N

N(CH

3

)

2 (Rvi-a)m (Rv-a")m V (VI) NaOMe R9HNNH2. H 2 0 MeOH EtOH 850C A 0 6 RvI - NaOMe, MeOH, 850C N ,NH Rg-NN or , N --- tetrabutylammonium fluoride, N iN -NNS2 THF, Ar (g), 600C (Rvi-a)m (VI) N N(CH 3

)

2 (Rvi-a)m (VI) [0991 Exemplary reactions for preparing a compound of Rv- 6 shown in Scheme VI-1 are shown below in Scheme VI-2. 64 WO 2006/044509 PCT/US2005/036770 Scheme VI-2 0 CH 3

NH

2 O RIC(OMe) 3 0 OH CDI N HCI / dioxane iN ) Rh NH 2 THF, 70C Rh NH NMP, 1100 Rh (VI) DMF

H

2

NOSO

3 H (2) N DMF-DMA N Pyridine, MeOH N- N 130C N0 0 C - rt - reflux Rh' N 2 100 Rh N NRh N (VI) O 0 O

K

2

CO

3 0 (3) HOH HCI HN HIO EtOH I N I . ~ ODII-IFI - I ~850C

NH

2 reflux N 2 H 0 (VI) HC(OMe) 3 , EtOH 1 (4) NH2 10 CN0 Ph 2 , 260 OC I N~sNO [0100] Alternatively, a compound of formula VI can be prepared according to Schenae VI-3 shown below. Specifically, a dirnethoxymethyl-substituted pyrimidine of formula (IIa) can be prepared by reacting dimethylformamide dimethylacetal with 1,1-dimethoxy-prop an-2-one to form 4-dimethylamino-1,1-dirnethoxy-but-3-en-2-one as an intermediate, which can further react with an R -substituted acetamidine (i.e., R -C(NH)-NH 2 ) to produce a compound of formula (Ila). See Reilly, T.A. et al., J. Heterocyclic Chem. 24(4):955 (1989). The compound of formula (Ila) can then be deprotected in an acidic medium (e.g., aq-ueous HBr) and react with aniline and diphenylphosphite to form a compound of formula ([Ib), which can then react with an Rvi-6-substituted aldehyde to form a compound of formula (I1c). Further reaction of a compound of formula (IIc) with N,N-dimethylformamide dimethylacetal (DMFDMA), followed by hydrazine hydrate, yields a compound of formula VI. 65 WO 2006/044509 PCT/US2005/036770 Scheme VI-3 0 N neat 0 Rvi-a NH7 - O HBr/H 2 0 N N" ~ 0 1. RvI- 6 CHO, Cs 2 CO30 OPh PhNH, N Rvi- N 2. HCI Rvi-a N Ph HP(O)(OPh) 2 Rvi-a N RVi- 6 NHPh (lc) (lib) 1. DMFDMA 2. NH2NH2 N ' Rvi- N N, NH RvI- 6 (VI) [0101] Another method for preparing a compound of formula VI is shown in Scheme VI-4 below. Note that in this Scheme, Ra' has the same meaning as Rv-a, which has been defined above, and X represents halo. Similar to the met11od described in Scheme VI-1, this method requires halogenation at the RVI~ 6 position as an intermediate step. See Nesi, R. et al., J. Chem. Soc., Perkin Trans I, 8:1667-1770 (1980); Nagamitsu, T. et al., J. Org. Chem., 60(25):8126-8127 (1995); and Guanti, G. and Riva, R. Tetrahedron: Asymmetry, 12(8):1185-1200 (2001) for references for synthesis shown in the first four steps. 66 WO 2006/044509 PCT/US2005/036770 Scheme VI-4 Ra

H

2 N NH RalO O NaOMe N EtOH Ra N MeOH N '- NH 2 c reflux N RT 1. NaOH 2. (COC0)2, benzene 0 3. CH 3

NH(OCH

3 ).HCI, O CH 3 MgI Ra N Et 3 N, CHC1 3 Ra THF 0 ON 0 R5 N 0 DMF N-NH Ra 8 , N a.yrzn/tH R / R 5 Ra 2.d8azine / EtOH R R Halogenation I, (e.g., Br 2 Ra' 8500C N ,Ra CH01 3 ) -N R -B(OH) 2 (Me) 2 NS02CI

SO

2 Pd(Ph 3

P)

4 N -NHR NaH N-N Na 2

CO

3 (aq) Ra N DMF Ra/ R 5 dioxane Rax N 900C -N S02 N-N NaOMe N-NH Ra N

R

5 MeOH Ra N 1/ R 5 YN,, R 6 8500C N a' R 6 [0102] A compound of formula VI can also be prepared via a phenylacetyl pyrimidine compound (IX) as shown in Scheme VI-5 below. Specifically, a pyrimidine carboxyaldehyde compound (VIII) is converted to the N,P acetal intermediate with aniline and diphenylphosphite. This acetal intermediate is then coupled to an aldehyde substituted with RvI~ 6 in basic condition (e.g., Cs 2

CO

3 ) to afford an enamine intermediate, which is hydrolyzed to a ketone intermediate (IX). For reference, see, e.g., Journet et al., Tetrahedron Letters v. 39, p. 1717-1720 (1998). Cyclizing the ketone intermediate (IX) with N,N 67 WO 2006/044509 PCT/US2005/036770 dimethylformamide dimethyl acetal and hydrazine affords the pyrazole ring of the desired compound of formula VI. The pyrazole ring of a compound of formula VI can also be formed by cyclizing the ketone intennediate (IX) with an Rv- 5 -substituted carboxylic acid hydrazide (X). For reference, see, e.g., Chemistry ofHeterocyclic compounds 35(11): 1319 1324 (2000). Scheme VI-5 (RVi-a)M (R)M 1.DMFDMA N N N 1. (PhO) 2 P(O)H, aniline NC DMF 2. RvI- 6 -CHO, base 6 2 / CHO 3. HCI (aq) RV1- 6 N R 2-2NH (Rv N (Vill) (IX) (VI) RvI--CO-NHNH 2 (X) HCI, THF A N N N, (RvI-a M NH Rvi-e RvI-5 (VI) [0103] Another method of preparing the intermediate (IX) is depicted in Scheme VI-6 below. For reference, see, e.g., WO 02/066462, WO 02/062792, and WO 02/062787. Scheme VI-6 (RVI-a)

RVI-

6

CH

3 1. KHMDS or LiHMDS, THF N N COOCH 3 N vi-6 2.(RVi-a)mN O (IX) [0104] Examplanry methods for preparing a compound of formula VI wherein -RvI-1-RvI 2

R~V

3 -R V~ 4 is not hydrogen are shown in Scheme VI-7 below. In reaction (A), a compound of formula VI wherein the 1-position of the pyrazole core ring is unsubstituted undergoes a substitution reaction with X-RVI-R VI-2-RVJ-3-RI-4 where X is a leaving group such as trifluoromethylsulfonate, tosylate, and halide, e.g., Cl, Br, or I. Alternatively, a compound of formula VI wherein the 1-position of the pyrazole core ring is unsubstituted can undergo a conjugate addition reaction as shown in reaction (B) below. As is well known to a skilled 68 WO 2006/044509 PCT/US2005/036770 person in the art to which this invention relates, the electrophile or acceptor in the addition reaction generally contains a double bond connecting to an electron-withdrawing group or a double bond conjugating to groups such as carbonyl, cyano, or ritro. Scheme VI-7 N N N N (A) // N X-RvI-1-Rvi-2-Rvi-3-Rvi-4 (Rvi-a)m NH (Rvi-a N-Rvi--RvI-RvI Rvi RvI 5 Rv 1

-

6 RvI-5 (VI) (VI) N N N N (B) -N __ _RvI-1-Rvi-2-Rvi--Rvi-4 N (RVI-a)m NH (RvI-a)m N Rvi-e Rvi-5 RvI-6 RvI- 5 Rv- 1 -RvI-2-RvI.3R-Rvi-4 (VI) (VI) The _RV-IR V- -R ~ -R -4 group can be further transformed into other functionalities as shown in Scheme VI-8 below. For example, a compound of forrnula VI wherein the -R- 1 RV- -R -~ -R 3 -4 group is cyanoalkyl can be reduced to aminoallcyl, which can be further converted to other functionalities such as heteroaralkyl, heterocycloalkylalkyl, and carboxylic acid. 69 WO 2006/044509 PCT/US2005/036770 Scheme VI-8

RVI-

5

RV

1

-

5

RVI-

5

RVI-

6 CNRINH RV'- 6 Nr , CN HN, NH

H

2 HOH x1NJ(CH 3

)

2 Raney NI ~ N Pd/C, MeOH NNEtOH Nr'~ N N N(x1 > 1) N N N N (vi-am (RI)vi-a (VI) (Rvi (R (R )M (RVI-a )M NaOH

CH

3

SO

2 CI EtOH, 105 C Et 3 N, CH 2 Cl 2

RV-

5 R-5NaN 3 , NH 4 CI Rv-HN C Rvi- DMF, 100*C N, --CH 3 R16CODH N+ -(Y 'S0 2 N N COOH Br-(CH 2

)

4 -Br N N K2CO3, THF N/-N (Vi) (RVI-a)M (Vi) (RVI-a).

RVI-

5 N-NH Rv- I 'N RVi-5

H

2 NOH HCI N N-(-') HATU, DIEA I1N' DMF, rt N/N (Rvi-a (VI) N/ gN (Rvi-a)M (VI) RVI-5 O N A OH N N X N/ ,,, N HVI (Rvi-a (Vl [01051 Substituents at the pyrimidinyl ring (i.e., Rvia) can also be converted into other functionalities. For example, a compound of formula VI wherein Re-a is bromo (which can be obtained by employing a bromo-substituted compound of formula VI (Sigma-Aldrich, St. Louis, MO)) can be converted into other functionalities such as alkyl, alkenyl, cycloalkyl and the like, by known methods. [01061 Likewise, substituents of the RI~ 6 moiety can be further converted into other functionalities as well. As will be obvious to a skilled person in the art, some starting materials and intermediates may need to be protected before undergoing synthetic steps as described above. For suitable protecting groups, see, e.g., T. W. Greene, Protective Groups in Organic Synthesis, John Wiley & Sons, Inc., New York (1981). 70 WO 2006/044509 PCT/US2005/036770 [01071 Examples of compounds of formula VI include, but are not limited to, 500) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-methyl-pyrimidine, 500a) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 501) 6-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 502) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 502a) 6-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 503) 6-[3-(2-cyclopropyl-pyrimidin-4-yl)- 1 H-pyrazol-4-yl]-quinoxaline, 504) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-trifluoromethyl-pyrimidine, 505) 7-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, and 506) 6-[3-(2-Trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoline. Routes of Administration [01081 As defined above, an effective amount is the amount which is required to confer a therapeutic effect on the treated subject, e.g. a patient. For a compound of formulae (I, II, III, IV, V, and VI), an effective amount can range from about 1 mg/kg to about 150 mg/kg (e.g., from about 1 mg/kg to about 100 mg/kg). Effective doses will also vary, as recognized by those skilled in the art, dependent on route of administration, excipient usage, and the possibility of co-usage with other therapeutic treatments including use of other therapeutic agents and/or radiation therapy. [0109] The compounds of formulae I, II, II, IV, V, and VI can be administered by any method that permits the delivery of the compounds to combat vascular injuries. For instance, the compounds of formulae I, II, III, IV, V, and VI can be admininistered via pills, tablets, capsules, aerosols, suppositories, liquid formulations for ingestion or injection or for use as eye or ear drops, dietary supplements, and topical preparations. A pharmaceutically acceptable composition includes the aqueou s solution of the compound of formula I, II, III, IV, V, or VI, in an isotonic saline, 5% glucose or another well-known pharmaceutically acceptable excipient. Solubilizing agents such as cyclodextrins, or other solubilizing agents well-known to those familiar with the art, can be utilized as pharmaceutical excipients for delivery of the therapeutic compounds. As to route of administration, the compositions can be administered orally, intranasally, transderamally, intradermally, vaginally, intraaurally, intraocularly, buccally, rectally, transmucosally, or via inhalation, or intravenous administration. The compositions may be delivered intravenously via a ballon catheter. The compositions can be administered to an animal (e.g., a mammal such as a human, non-human 71 WO 2006/044509 PCT/US2005/036770 primate, horse, dog, cow, pig, sheep, goat, cat, mouse, rat, guinea pig, rabbit, hamster, gerbil, ferret, lizard, reptile, or bird). [0110] The compounds of formulae I, II, III, IV, V, and VI also can be delivered by implantation (e.g., surgically) with an implantable device. Examples of implantable devices include, but are not limited to, stents, delivery pumps, vascular filters, and implantable control release compositions. Any implantable device can be used to deliver the compound provided that 1) the device, compound and any pharmaceutical composition including the compound are biocompatible, and 2) that the device can deliver or release an effective amount of the compound to confer a therapeutic effect on the treated patient within a short or over an extended period of time. 101111 Delivery of therapeutic agents via stents, delivery pumps (e.g., mini-osmoti c pumps), and other implantable devices is known in the art. See for example, "Recent Developments in Coated Stents" by Hofma et al., published in Current Interventional Cardiology -Reports 2001, 3:28-36, the entire contents of which, including references cited therein, are incorporated herein. Other descriptions of implantable devices, such as stents, can be found, e.g., in U.S. Patent Nos. 6,569,195 and 6,322,847; and PCT International PublicatioDn Numbers WO 04/0044405, WO 04/0018228, WO 03/0229390, WO 03/0228346, WO 03/0225450, WO 03/0216699, and WO 03/0204168, each of which is also incorporated herein by reference in its entirety. [01121 Referring to Figure 1, a delivery device, such as stent 10, includes a compound 20 of formula I, II, III, IV, V, or VI. The compound, as a therapeutic agent, may be incorporated into or onto the stent using methodologies known in the art. In some embodiments, a stent can include interlocked meshed cables. Each cable can include metal wires for structural support and polyermic wires for delivering the therapeutic agent. The polymeric wire can be dosed by immersing the polymer in a solution of the therapeutic agent. Alternatively, the therapeutic agent can be embedded in the polymeric wire during the formation of the wire from polymeric precursor solutions. In other embodiments, stents or implatable devices can be coated with polymeric coatings that include the therapeutic agent. The polymeric coating can be designed to control the release rate of the therapeutic agent. [0113] Controlled release of therapeutic agents can utilize various technologies. Devices are known having a monolithic layer or coating incorporating a heterogeneous solution and/or dispersion of an active agent in a polymeric substance (e.g., a polyester), where the diffusion 72 WO 2006/044509 PCT/US2005/036770 of the'i'gi isiaie initing aistheae't diffuses through the polymer to the polymer-fluid interface and is released into the surrounding fluid. In some devices, a soluble substance is also dissolved or dispersed in, or chemically bonded to, the polymeric material, such that additional pores or channels are left after the material dissolves. A matrix device is generally diffusion limited as well, but with the channels or other internal geometry of the device also playing a role in releasing the agent to the fluid. The channels can be pre-existing or left behind by released agent or other soluble substances. [0114] Erodible or degradable devices typically have the active agent physically inunobilized in the polymer. The active agent can be dissolved and/or dispersed throughout the polymeric material. The polymeric material is often hydrolytically degraded over time through hydrolysis of labile bonds, allowing the polymer to erode into the fluid and releasing the active agent into the fluid. Hydrophilic polymers have a generally faster rate of erosion relative to hydrophobic polymers. Hydrophobic polymers are believed to have almost purely surface diffusion of active agent, having erosion from the surface inwards. Hydrophilic polymers are believed to allow water to penetrate the surface of the polymer, allowing hydrolysis of labile bonds beneath the surface, which can lead to homogeneous or bulk erosion of polymer. [0115] The implantable device coating can include a blend of polymers each having a different release rate of the therapeutic agent. For instance, the coating can include a polylactic acid/polyethylene oxide (PLA-PEO) copolymer and a polylactic acid/polycaprolactone (PLA-PCL) copolymer. The polylactic acid/polyethylene oxide (PLA PEO) copolymer can exhibit a higher release rate of therapeutic agent relative to the polylactic acid/polycaprolactone (PLA-PCL) copolymer. The relative amounts and dosage rates of therapeutic agent delivered over time can be controlled by changing the relative amounts of the faster releasing polymers relative to the slower releasing polymers. For higher initial release rates the proportion of faster releasing polymer can be increased relative to the slower releasing polymer. If most of the dosage is desired to be released over a long time period, most of the polymer can be the slower releasing polymer. The stent can be coated by spraying the stent with a solution or dispersion of polymer, active agent, and solvent. The solvent can be evaporated, leaving a coating of polymer and active agent. The active agent can be dissolved and/or dispersed in the polymer. In some embodiments., the co polymers can be extruded over the stent body. 73 WO 2006/044509 PCT/US2005/036770 [0116] In still other embodiments, compounds of formula I can be administered in conjunction with one or more other agents that inhibit the TGF3 signaling pathway or treat the corresponding pathological disorders (e.g., fibrosis or progressive cancers) by way of a different mechanism of action. Examples of these agents include angiotensin converting enzyme inhibitors, nonsteroid, steroid anti-inflammatory agents, and chemotherapeutics or radiation, as well as agents that antagonize ligand binding or activation of the TGF3 receptors, e.g., anti-TGF3, anti-TGFf3 receptor antibodies, or antagonists of the TGFf3 type II receptors. [01171 The invention will be further described in the following examples, which do not in any way limit the scope of the invention described in the claims. Example 1: Balloon Catheter Injury of the Rat Carotid Artery [0118] The ability of compounds of formulae I, II, III, IV, V, and VI to prevent the stenotic fibrotic response was tested by administration of the test compounds (i.v., p.o., or s.c) to rats that have undergone balloon catheter injury of the carotid artery. [0119] Sprague Dawley rats (400g, 3 to 4 months old) were anesthetized by i.p. injection with 10 mg/kg xylazine (Xyla-Ject, Phoenix Pharmaceuticals) and & 0 mg/kg ketamine (Ketaset, Fort Dodge). The left carotid artery and the aorta were denuided with a 2F balloon catheter (Edwards Life Sciences) according to the procedure described in Clowes et al., Lab Invest. 49: 327-333 (1983). Test compounds of formulae I, II, III, IV, V, and VI were each administered to the treatment group (n=5-10 rats) (i.v., p.o., or s.c.; qcd, once per day, bid, tid or by continuous s.c. infusion via an Alzet mini-osmoticpump) starting the day of surgery and subsequently for 14 more days. The control group (n=5 rats) received the same volume of vehicle administered using the same regimen as the test compound-treated rats. The animals were sacrificed under anesthesia 14 days post-balloon injury. Exsanguination and then perfusion fixation was carried out under physiological pressure with 0.9% sodium chloride, injection USP (310 mOsmol/L, pH 5.6 (4.5-7.0)) and (10% neutral buffered formalin). The injured carotid artery was excised, post-fixed and embedded for histological and morphometic analysis. Sections (5 pm) were cut from the proximal, middle and distal segments of the denuded vessel and analyzed using image analysis software. The circumference of the lumen and the lengths of the internal elastic laniina (IEL) and the external elastic lamina (EEL) were determined by tracing along the luminal surface the perimeter of the neointima (IEL) and the perimeter of the tunica media (EEL), respectively. 74 WO 2006/044509 PCT/US2005/036770 The lumen (area within the lumen), medial (area between the IEL and EEL) and intimal (area between the lumen and the IEL) areas were a-lso determined using morphometric analysis. Statistical analysis used ANOVA to determirne statistically significant differences between the means of treatment groups (p s;0.05). M-ultiple comparisons between groups were then performed using the Dunnet's Multiple Conrparisons test. The Student t test was used to compare the means between 2 groups, and differences were considered significant if P ;0.05. All data are shown as mean + SEM. [01201 Statistically significant decreases were seen in intimal area, intimal/medial ratio, in injured arteries of test compound-treated rats compared to those of the vehicle-treated rats. Conversely, the lumen area, IEL and EEL lengths showed a statistically significant increase in injured arteries of test compound-treated rats compared to those of the vehicle-treated rats. These results show that inhibition of the TGF3RJ kinase prevents the stenotic response to balloon-catheter arterial injury by inhibiting the fibrotic expansion of the neointima anc1 vessel remodeling. Example 2: Cell-Free Assay for Evaluating Inhibition of Autophosphorylation of 'TGF# Type I Receptor [0121] The serine-threonine kinase activity of TGF# type I receptor was measured as tlie autophosphorylation activity of the cytoplasmic domain of the receptor containing an N terminal poly histidine, TEV cleavage site-tag, e.g., His-TGF#RI. The His-tagged receptor cytoplasmic kinase domains were purified front infected insect cell cultures using the Cribco BRL FastBac HTb baculovirus expression system. [01221 To a 96-well Nickel FlashPlate (NEN ]Life Science, Perkin Elmer) was added 20 t of 1.25 pCi "P-ATP/25 pM ATP in assay buffer (50 mM Hepes, 60 mM NaCl, 1 mM MgCl 2 , 2 mM DTT, 5 mM MnCl 2 , 2% glycerol, and 0.0 15% Brij* 35). 10 pl of each test compound of formula I prepared in 5% domethyl sulfoxide (DMSO) solution were added to the FlashPlate. The assay was then initiated with the addition of 20 ul of assay buffer containing 12.5 prnol of His-TGF#RI to each well. Plates were incubated for 30 minutes at room temperature and the reactions were then terminated by a single rinse with Tris-buffered saline (TBS). Radiation from each well of the plates was react on a TopCount (Packard). Total binding (no inhibition) was defined as counts measured in the presence of DMSO solution containing no test compound and non-specific binding was defined as counts measured in the presence of EDTA or no-kinase control. 75 WO 2006/044509 PCT/US2005/036770 [0123] AlternitiVely,"'the reaction performed using the above reagents and incubation conditions but in a microcentrifuge tube was analyzed by separation on a 4-20% SDS-PAGE gel and the incorporation of radiolabel into the 40 kDa His-TGFpRI SDS-PAGE band was quantitated on a Storm Phosphoimager (Molecular Dynamics). [0124] Compounds of formulae I, II, III, IV, V, and VI typically exhibited low IC 50 values of less than 10 AM; some exhibited IC 50 values of less than 1 pfM; and some even exhibited IC 50 values of less than 50 nM. Example 3: Cell-Free Assay for Evaluating Inhibition of Activin Type I Receptor Kinase Activity [01251 Inhibition of the Activin type I receptor (Alk 4) kinase autophosphorylation activity by compounds of formulae I, II, III, IV, V, and VI, can be determined in a similar manner to that described above in Example 2 except that a similarly His-tagged form of Alk 4 (His-Alk 4) is used in place of the His-TGFf3RI. 76 WO 2006/044509 PCT/US2005/036770 Example 4: TGF$ Type I Receptor Ligand Displacement FlashPlate Assay [0126] 50 nM of tritiated 4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline (custom-ordered froni PerkinElmer Life Science, Inc., Boston, MA) in assay buffer (50 mM Hepes, 60 mM NaCl 2 , 1 mM MgCl 2 , 5 mM MnCl 2 , 2 mM 1,4-dithiothreitol (DTT), 2% Brij* 35; pH 7.5) was premixed with a test compound of formula I, II, III, IV, V, or VI, in 1% DMSO solution in a v-bottom plate. Control wells containing either DMSO without any test compound or control compound in DMSO were used. To initiate the assay, His-TGF3 Type I receptor in the same assay buffer (Hepes, NaC1 2 , MgCl 2 , MnCl 2 , DTT, and 30% Brij* added fresh) was added to a. nickel coated FlashPlate (PE, NEN catalog number: SMP107), while the control wells contained only buffer (i.e., no His-TGF3 Type I receptor). The premixed solution of tritiated 4-(3-pyridin-2-yl-lH-pyrazol-4-yl)-quinoline and the test compound was then added to the wells. The wells were aspirated after an hour at room temperature and radioactivity in wells (emitted from the tritiated compound) was measured using TopCount (PerkinElmer Lifesciences, Inc., Boston MA). [0127] Compounds of formulae I, II, III, IV, V, and VI typically exhibited Ki values of less than 10 AM; some exhibited Ki values of less than 1 yM; and some even exhibited Ki values of less than 50 nM. Example 5: Assay for Evaluating Cellular Inhibition of TGF# Signaling and Cytotoxicity [0128] Biological activity of the compounds of formulae I, II, III, IV, V, and VI was determined by measuring their ability to inhibit TGF-induced PAI-Luciferase reporter activity in HepG2 cells. [01291 Specifically, HepG2 cells were stably transfected with the PAI-luciferase reporter grown in DMEM medium containing 10% FBS, penicillin (100 U/ml), streptomycin (100 ptg/ml), L-glutamine (2 mM), sodium pyruvate (1 mM), and non-essential amino acids (lx). The transfected cells were then plated at a concentration of 2.5 x 10 4 cells/well in 96-well plates and starved for 3-6 hours in media with 0.5% FBS at 37'C in a 5% CO 2 incubator. The cells were then stimulated with 2.5 ng/ml TGF3 ligand in the starvation media containing 1 % DMSO either in the presence or absence of a test compound of formula I, II, III, IV, V, or VI and incubated as described above for 24 hours. The media was washed out the following day and the luciferase reporter activity was detected using the LucLite Luciferase Reporter Gene 77 WO 2006/044509 PCT/US2005/036770 Assay kii (Packard, Cat. No. 6016911) as recommended. The plates were read on a Wallac Microbeta plate reader, the reading of which was used to determine the IC 50 values of the test compounds for inhibiting TGF3-induced PAI-Luciferase reporter activity in HepG2 cells. Compounds of formulae I, II, III, IV, V, and VI typically exhibited IC 50 values of less 10 uM. [01301 Cytotoxicity was determined using the same cell culture conditions as described above. Specifically, cell viability was determined after overnight incubation with the CytoLite cell viability kit (Packard, cat. no. 6016901). Compounds of formula I, II, III, IV, V, an-d VI typically exhibited LD 25 values greater than 10 yM. Example 6: Assay for Evaluating Inhibition of TGF@ Type I Receptor Kinase Activity in Cells [01311 The cellular inhibition of activin signaling activity by compounds of formula I, , III, IV, V, or VI is determined in a similar manner as described above iml Example 5, except that 100 rig/ml of activin is added to serum starved cells in place of the 2.5 ng/ml TGF#. Example 7: Assay for TGF#-Induced Collagen Expression Preparation of Immortalized Collagen Promotor-Green Fluorescent Protein Cells [0132] Fibroblasts are derived from the skin of adult transgenic mice expressing Green Fluorescent Protein (GFP) under the control of the collagen lA1 pro-inoter (see Krempen, K. et al., Gene Exp. 8: 151-163 (1999)). Cells are immortalized with a temperature sensitive large T antigen that is in an active stage at 33'C, and then expanded at 33'C before being transferred to 37'C at which temperature the large T antigen becomes inactive (see, e.g., Xu, S. et al., Exp. Cell Res., 220: 407-414 (1995)). Over the course of about 4 days and one split, the cells cease proliferating. The cells are then frozen in aliquots sufficient for a single 96 well plate. Assay of TGF#-induced Collagen-GFP Expression [0133] Cells are thawed, plated in complete DMEM (contains non-essential amino acids, 1mM sodium pyruvate and 2mM L-glutamine) with 10 % fetal calf serum, and then incubated for overnight at 37'C, 5% CO 2 . The cells are trypsinized in the following day and transferred into 96-well format with 30,000 cells per well in 50 Al complete DMEM containing 2 % fetal calf serum, but without phenol red. The cells are incubated at 37'C for 3 to 4 hours to allow them to adhere to the plate. Solutions containing a test compound of 78 WO 2006/044509 PCT/US2005/036770 formula I, II, III, IV, V, or VI are then added to wells with no TGF3 (in triplicates), as well as wells with 1 ng/ml TGF3 (in triplicates). DMSO is also added to all of the wells at a final concentration of 0.1%. GFP fluorescence emission at 530 nm following excitation at 485 nn is measured 48 hours after the addition of solutions containing a test compound on a CytoFluor microplate reader (PerSeptive Biosystems). The data are expressed as the ratio of TGFO-induced to non-induced for each test sample. OTHER EMBODIMENTS 101341 It is to be understood that while the invention has been described in conjunction with the detailed description thereof, the foregoing description is intended to illustrate and not limit the scope of the invention, which is defined by the scope of the following claims. Other aspects, advantages, and modifications are within the scope of the present invention. 79

Claims (40)

1. A method of inhibiting intimal thickening by administering to a subject in need thereof an inhibitor of TGFb type I receptor or Alk4.

2. The method of claim 1, wherein the inhibitor has the structure shown in formula I: RI-a) m NI adN A 1-2 b -X1-1-11--R 1-2() or an N-oxide or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, heteroaryl, aralkyl, or heteroaralkyl; each RJ.. is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; XI 1 is cycloalkyl or heterocycloalkyl; Yp 1 is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(R)-, -N(RE)-C(O)-, -O-C(0)-N(RE)-, -N(Rb)-C(O)-O-, -O-S(O),-N(RE)-, -N(RE)- S(O),-0-, -N(RE)-C(O)-N(Rc)-, -N(RE)-S(O)p-N(RW)-, -C(O)-N(e)-S(O),-, -S(0),-N(RE)-C(O)-, -C(O)-N(RE)-S(0)p-N(R4)-, -C(O)-O-S(0),-N(RE)-, -N(RE)-S(O)p-N(Rc)-C(O)-, -N()-S(O)p-0-C(0)-, -S(O),-N(Rb)-, -N(Rb)-S(O)p-, -N(Rb)-, -S(O)p-, -0-, -S-, or -C(Rb)(RC))q-, wherein each of Rb and Rc is independently hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; RI- is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, 80 WO 2006/044509 PCT/US2005/036770 hefer&6y&loakefyIl hieterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A-' and A1- 2 , independently, is 0, S, N, or NR, provided that at least one of A" and A1- 2 is N; and m is 0, 1, 2, or 3, and when m ;>2, two adjacent Rla groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

3. The method of claim 1, wherein the inhibitor has the structure shown in formula II: Y'11-2 (R 1~2 )n ' 1 XII- ; (Rr X1- 3 N N XII-4 NN or a pharmaceutically acceptable salt or N-oxide thereof, wherein each of XII-1, XrI-2, XrI-3, and XrI-4 is independently CRW or N, provided that no more than two Of XII-1, XrI-2, XII-3, and XII.4 can be N simultaneously; each of YrI-1 and YrI-2 is independently CRY or N, provided that at least one of YrI-1 and Yr--2 must be N; each Ra-1 is independently alkyl, alkenyl, alkynyl, alkoxy , halo, liydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each R1- 2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cycloalkyl), -NH(heterocycloalkyl), NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alky1, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, raercapto, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, 81 WO 2006/044509 PCT/US2005/036770 (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfariyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamirio, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m 2, two adjacent R 1 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n ;>-2, two adjacent R 2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of R and RY is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylanino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfairnide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl.

4. The method of claim 1, wherein the inhibitor has the structure shown in formula III 82 WO 2006/044509 PCT/US2005/036770 (III) 1 (R"'- ) Xm3 N N XIII- 4 or a pharmaceutically acceptable salt or N-oxide thereof, wherein each of Xmj- 1 , XmI- 2 , XmI-3, and Xm 1 - 4 is independently CRmI-x or N, provided that no more than two of X 1 - 1 , Xm- 2 , XII- 3 , and XIm. 4 can be N simultaneously; each of Y 1 1 1 and Ym 1 - 2 is independently CRm'Y or N, provided that at least one of Ym-1 and Ym 1 - 2 must be N; each Rm-1 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, anidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide:, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each Rm- 2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cyclocalkyl), -NH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NI(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, (cycloalkyl)alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, arainosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl(alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylarnino, (heterocycloalkyl)alkylcarbonylarnino, heteroarylcarbonylamino, 83 WO 2006/044509 PCT/US2005/036770 hetero-aIkylearbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m >2, two adjacent R"" groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n >2, two adjacent R1- 2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of Rm-x and R"-y is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylaxnino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanayl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl.

5. The method of claim 1, wherein the inhibitor has the structure shown in formula IV 84 WO 2006/044509 PCT/US2005/036770 R V 5 RE 6 Rv-Lg- IV-2-RIV- 3 -R IV-4 N (WV) (RIV-a)m or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each Rlva is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylaminro, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; R' 1 v is a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri-0-(CH2)r 2 -, wherein each of r1 and r2 is independently 2 or 3; Rw-2 is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, or a bond; R'v~' is -C(O)-, -C(O)O-, -OC(O)-, -C(O)-N(Rv'~)-, -N(Re-~)-C(O)-, -O-C(O)-N(Rv b)-, -N(RIV~6)-C(D)-0-, -O-S(O)p-N(Re-b)-, -N(RIV~h)- S(O)p-O-, -N(R' ~6)-C(O)-N(RN~ c)-, -N(R v-b)-S(0),-N(Re-~)-, -C(O)-N(Re-~)-S(O)p-, -S(O)p-N(Rv'-)-C(0)-, -S(0),-NGR" ~-, -N(R-b)-S(O),-, -N(Rw-b)-, -S(O)p-, -0-, -S-, or -C(Rb)(RW ~))q-, or a bond; wherein each of R - and RN- is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; R I-4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaraLkyl; RIV~ 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkyl, 85 WO 2006/044509 PCT/US2005/036770 heterocycloalkoxy, heterocycloalkylsulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryloxy, or heteroarylsulfinyl; R 6 is (1) a 5- to 6-membered heterocyclyl containing 1-3 hetero ring atoms selected from the group consisting of -O-, -S-, -N=, and -NR'v~d-, wherein R I-d is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; said heterocyclyl being substituted with Rwv-e and optionally substituted with one to two Rwvf; wherein RIv-e is oxo, thioxo, alkoxy, alkylsulfinyl, -NH 2 , -NH(unsubstituted alkyl), or -N(unsubstituted alkyl) 2 , and Rvf is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or (2) a fused ring heteroaryl selected from the group consisting of: (RI)n (RI)n (R')n (RI)n B' B B 1 B' 1 X0 X2 x2 '\ 1 x ,x 2 ,and ; wherein ring A is an aromatic ring containing 0-4 hetero ring atoms, and ring B is a 5- to 7 membered aromatic or nonaromatic ring containing 0-4 hetero ring atoms, provided that at least one of ring A and ring B contains one or more hetero ring atoms; ring A' is an aromatic ring containing 0-4 hetero ring atoms, and ring B' is a 5- to 7-membered saturated or unsaturated ring containing 0-4 hetero ring atoms, provided that at least one of ring A' and ring B' contains one or more hetero ring atoms; each hetero ring atom is -0-, -S-, -N=, or NRr~g-; each X 1 is independently N or C; each X 2 is independently -0-, -S-, -N=, -NRv~ , or -CHRV- -; wherein RW~- is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; each of RW- and R71 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, 86 WO 2006/044509 PCT/US2005/036770 cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarb onyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and n is 0-2; and m is 0-3, and when m _2, two adjacent R -a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; provided that if RWv~ 6 is 2-naphthyridinyl, 4-quinolinyl, imidazo[1,2-a]pyridyl, or benzimidazolyl, then -R -R -2 -Riv--Rv-~ is not H, unsubstituted a-1kyl, -CH 2 -C(O)-N(H)-alkyl, -CH 2 -C(O)-N(alkyl) 2 , or benzyl.

6. The method of claim 1, wherein the inhibitor has the structure shown in formula V (Rv-a)m N N ( Av-2 XvYvRV-2 RV 1 Av 1 or an N-oxide or a pharmaceutically acceptable salt thereof, wherein Rv~1 is heteroaryl; each Ra, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylanino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heteirocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroary-isulfanyl, or heteroaroyl; X, is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or a bond; Yv is a bond, -C(O)-, -C(O)-O-, -0-C(O)-, -S(O),-O-, -O-S(O),-, -C(O)-N(R)-, -N(Rb)-C(O)-, -O-C(O)-N(Rb)-, -N(R)-C(0)-0-, -C(0)-N(RE)-0-, -D-N(R)-C(O)-, -O-S(O),-N(RE)-, -N(R)- S(0),-0-, -S(0),-N(Re)-O-, -O-N(RE)-S(O)-p-, -N(Rb)-C(O)-N(Rc) -N(Rb)-S(O)p-N(R )-, -C(O)-N(RE)-S(O)p-, -S(O)p-N(RE)-C(O)-, -C(D)-N(RE)-S(O)p-N(R )-, 87 WO 2006/044509 PCT/US2005/036770 -C(b)"lb-'S'(O) -R('R)-, -N(R')-S(O),-N(Rc)-C(O)-, -N(Rk)-S(O)p-0-C(O)-, -S(O)p-N(R)-, -N(Rb)-S(O)p-, -N(R)-, -S(O)p-, -0-, -S-, or -(C(Re)(RC))q-, wherein each of Rb and R4, independently, is hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; Rv-2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenayl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A ~' and Av- 2 , independently, is N or NRe; and m is 0, 1, 2, or 3, and when m ;>2, two adjacent R v-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety, provided that if- X, is a bond, then Yv is a bond; R 2 is hydrogen or alkyl; m is 1, 2, or 3; and at least one RV-a is substituted at the 2-pyrimidinyl position. 88 WO 2006/044509 PCT/US2005/036770

7. The method of claim 1, wherein the inhibitor has the structure shown in formula VI: RvI-5 RvI-6 N'g A_ vl-2 gv1-3 gvI-4 ~ NN (VI) N (RV1-a)m or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each RVIa, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, NH 2 , -NH(unsubstituted alkyl), -N(unsubstituted alkyl) 2 , nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylanino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; R'- 1 is a bond, alkylene, alkenylene, alkynylene, or -(CH2)r1-O-(CH2)r 2 -, where each of ri and r2, independently, is 2 or 3; Rm 1 2 is cycloalkylene, heterocycloalkylene, cycloalkenylene, heterocycloalkenylene, arylene, heteroarylene, or a bond; Rev 3 is -C(O)-, -C(O)-0-, -O-C(O)-, -S(O),-O-, -O-S(O)p-, -C(O)-N(Rb), -N(RU)-C(O)-, -O-C(O)-N(R)-, -N(R)-C(O)-0-, -C(O)-N(RkE)-O-, -O-N(RE)-C(O)-, -O-S(O)p-N(R S NR -N(RE)- S(O),-0-, -S(O)p-N(Rk)-O-, -O-N(RE)-S(OD)p-, -N(RE)-C(O)-N(Re)-, -N(RE)-S(O)p-N(R")-, -C(0)-N(RE)-S(0)p-, -S(O),-N(RE)-C(O)-, -C(O)-N(RE )-S(O)p-N(Rc)-, -C(O)-O-S(O)p-N(RE)-, -N(Rb)-S(O)p-N(Rc)-C(O)-, -N(RE)-S(O)p-O-C(O)-, -S(O),-N(Rh, -N(R)-S(O)p-, -N(Rb)-, -S(O)p-, -0-, -S-, -(C(Rb)(Rc))q-, or a bond; wherein each of Rb and R is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; 89 WO 2006/044509 PCT/US2005/036770 pv 4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; Rv- 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryloxy, arylsulfinyl, heteroaryloxy, or heteroarylsulfinyl; R -6 is a 5- to 6-membered monocyclic heterocyclyl or a 8- to 11 -membered bicy-clic heteroaryl; each being optionally substituted with alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and m is 0-3, and when m ;>2, two adjacent RVI-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

8. The method of claim 1, wherein the inhibitor is 1) 4-(4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 2) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 3) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 4) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 5) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 6) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 7) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 8) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 90 WO 2006/044509 PCT/US2005/036770 9) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 10) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 11) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-pyridine; 12) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 13) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 14) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzyl ester; 15) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2,4-dichloro-b enzylamide; 16) 1-[4-(4-Benzo[ 1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-yl] ethanone; 17) 2-[5-Benzo[1,3 ]dioxol-5-yl-2-(1-furan-2-yl-methyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 18) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 19) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylamine; 20) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-phenyl-methanesulfonamide; 21) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 22) 4-[4-Benzo[1,3] dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 23) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 24) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-ethyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 25) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-pyridine; 26) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-nitro-benzyl ester; 91 WO 2006/044509 PCT/US2005/036770 27) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4,5-dimethoxy-2-nitro-benzyl ester; 28) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 3-fluoro-benzylamide; 29) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-fluoro-benzylamide; 30) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzylamide; 31) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 32) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methyl-benzylamide; 33) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methoxy-benzylamide; 34) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyriclin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzylamide; 35) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzoic acid; 36) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-lH-imidazol-2-yl)-piperidine-1-carboxylic acid amide; 37) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzonitrile; 38) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 39) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-pyridine; 40) {5-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] naphthalen-1-yl}-dimethyl-amine; 41) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methyl)-piperidin-4-yl)]-3H-imidazol-4 yl} -pyridine; 42) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 43) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 92 WO 2006/044509 PCT/US2005/036770 44) 1-{4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonyl]-phenyl} -ethanone; 45) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methyl-benzyl)-piperidin-4-yl-3H-imidazol-4-yl} pyridine; 46) 2- { 5-Benzo[1,3]dioxol-5-yl-2-[1-(3-fluoro-5-trifluoromethyl-benzyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 47) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-cyclohexylmethyl-piperidin-4-yl)-3H-imidiazol-4-yl] pyridine; 48) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-I -ylmethyl] cyclopropanecarboxylic acid ethyl ester; 49) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1 -ylmethyl] pyrrolidine- 1 -carboxylic acid tert-butyl ester; 50) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-p iperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 51) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazo l-4-yl] pyridine; 52) 2- {5-Benzo[1,3]dioxol-5-yl-2-[ 1 -(butane-1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 53) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidia-4-yl]-3H imidazol-4-yl}-pyridine; 54) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 55) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[1 -(propane- 1 -sulfonyl)-piperidin-4-yl]-3H-irmidazol-4 yl}-pyridine; 56) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine- 1 sulfonylmethyl]-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 57) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-pyridine; 58) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-pyridine; 59) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-fluoro-phenylmethanesulfonyl)-piperidini-4-yl]-3H imidazol-4-yl} -pyridine; 60) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 93 WO 2006/044509 PCT/US2005/036770 61) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 62) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-p-tolylmethanesulfonyl-piperidin-4-yl)-3H-imidaz-ol-4 yl]-pyridine; 63) 3-(4-Benzo[1,3]dioxol-5-yl-1 -hydroxy-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 64) 3-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 65) 4-[4-Benzo[1,3]dioxol-5-yl-1 -hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 66) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 67) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1-(2-naphthalen-1-yl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 68) 2-[5-Benzo[1,3]dioxol-5-yl-2-( 1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidaz;ol-4 yl]-pyridine; 69) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 70) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1-(pyridin-4-yl-methanesulfonyl)-piperidin-4-yl]-311 imidazol-4-yl} -pyridine; 71) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-yl-methanesulfonyl)-piperidin-4-yl]-3K imidazol-4-yl} -pyridine; 72) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 73) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] pyrrolidine- 1 -carboxylic acid benzyl ester; 74) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 75) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1-(3,5-bis-trifluoromethyl-phenylmethanesulfonyl) piperidin-4-yl]-3H-imidazol-4-yl}-pyridine; 76) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[ 1 -(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 77) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1 -(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 94 WO 2006/044509 PCT/US2005/036770 78) 2-{5-Benzo[1,3]dioxoil52 [ 1 (pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 79) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 80) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 81) 4-[5-Benzo[1,3]dioxol-5-yl-1-methyl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 82) 4-[4-Benzo[1,3]dioxol-5-yl-1-methyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 83) {4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -carbamic acid benzyl ester; 84) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-phenoxy-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 85) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 86) 2- {5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(propane- 1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 87) 2-{5-Benzo [1,3] dioxol-5-yl-2-[1 -(butane-i -sulfonyl)-piperidin-4-yl] -3H-imidazol-4-yl} 6-methyl-pyridine; 88) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 89) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 90) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 91) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-6-methyl-pyridine; 92) 2-f{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 93) 2- {5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(butane-i -sulfonyl)-piperidin-3-yl]-3H-imidazol-4-yl} 6-methyl-pyridine; 94) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 95 WO 2006/044509 PCT/US2005/036770 95) 2-{5-IBenzo[1,3]dioxoi-5-yl-2-[1-(1-methyl-iH-imidazole-4-sulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 96) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(5-methyl-isoxazole-4-sulfonyl)-piperidiin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 97) 4-[5-Benzo[1,3]dioxol-5-yl-1-hydroxy-4-(6-methyl-pyridin-2-yl)-1H-imid.azol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 98) Butane-1 -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-lH imidazol-2-yl]-cyclohexyl}-amide; 99) N-{4- [4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-pyridin-2-yl-methanesulfonamide; 100) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl} -amide; 101) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6 -methyl pyridin-2-yl)-1IH-imidazol-2-yl]-cyclohexyl}-amide; 102) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2. 2.2]octane-1-carboxylic acid amide; 103) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 104) 4-[4-Benzo [1,3] dioxol-5-yl-5-(6-bromo-pyridin-2-yl)- 1 H-imidazol-2-yl]-piperidine- 1 carboxylic acid benzyl ester; 105) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-3-sulfonyl)-piperidin-4-yl]-3 H-imidazol-4 yl} -6-methyl-pyridine; 106) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-2-trifluoromethyl-furan-3-sulfonyl) piperidin-4-yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 107) 4-[2-(1-phenylmethanesulfonyl-piperidin-4-yl)-5-(6-methyl-pyridin-2-yl)-1H-imidazol 4-yl]-pyridin-2-yl-fluoride; 108) 4-[4-iBenzo[1,3]dioxol-5-yl-5-(6-trifluoromethyl-pyridin-2-yl)-1H-imidazo1-2-y1] piperidine- 1 -carboxylic acid benzyl ester; 109) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-bromo-pyridin-2-yl)-1-hydroxy-1H-imiclazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 110) 2-[5-IBenzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-brono-pyridine; 111) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl} -methanol; 96 WO 2006/044509 PCT/US2005/036770 112) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid arnide; 113) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-2H-imidazol-2-yl]-piperidine-1 sulfonic acid dimethylamide; 114) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin 1 -yl}- 3 -phenyl-propan- 1-one; 115) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 116) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carbonitrile; 117) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylamine; 118) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-phenyl-methanesulfonamide; 119) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonarnide; 120) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-pyridin-2-yl-methanesulfonamide; 121) 2-{5-Benzo[1,3]dioxol-5-yl-2-[4-(1 H-tetrazol-5-yl)-bicyclo[2.2.2]oct-1-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 122) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]oct- 1-yl} -acetamide; 123) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-anide; 124) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 125) Thiophene-3-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-arnide; 126) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 127) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 128) Methanesulfonic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-ylmethyl ester; 97 WO 2006/044509 PCT/US2005/036770 129) {4-[4-BenIzof[ ,31dixo -yl.-(6-methyl-pyrilin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetonitrile; 130) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyricLin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -acetic acid; 131) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-methanesulfonamide; 132) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 133) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 134) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 135) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1H-imidazol-2-yl] bicyclo[2.2.2] oct-1 -ylmethyl} -C-phenyl-methanesul fonamide; 136) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyTidin-2-yl)-iH-imidazol-2-yl] bicyclo [2.2.2]oct- 1 -ylmethyl} -C-pyridin-2-yl-methanesulfonamide; 137) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridiri-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid benzylamide; 138) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridiri-2-yl)-1H-imidazol-2-y1] bicyclo[2.2.2] octane-1 -carboxylic acid (pyridin-2-ylrnethyl)-amide; 139) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridiri-2-yl)-iH-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid 3-chloro-4-fluoro-benzylamide; 140) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridiri-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid (furan-2-ylmethyl)-amide; 141) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulforiyl-pyrrolidin-3-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 142) 2- {5-Benzo [1,3]dioxol-5-yl-2- [1 -(butane- 1-sulfonyl)-pyrrolidin-3-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 143) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-1H-imidazole-4-sulfonyl)-pyrrolidin-3-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 144) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-pyrrolidin-3-yl)-3H-imidazol 4-yl]-6-methyl-pyridine; 145) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-pyrrolidin-3-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 98 WO 2006/044509 PCT/US2005/036770 146) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3 H imidazol-4-yl} -6-methyl-pyridine; 147) 2- {5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-2-yl-ethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 148) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1-sulfonylmethyl}-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 149) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 150) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methylamide; 151) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid ethylamide; 152) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid butylamide; 153) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid isopropylamide; 154) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid (3-imidazol-1-yl-propyl)-amide; 155) 2-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pipericine 1 -sulfonylmethyl} -phenylamine; 156) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid (1-methyl-5-methylsulfanyl-1H-[1,2,4]triazol-3-yl) amide; 157) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid cyclohexylamide; 158) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-pyrrolidin-1-yl-methanone; 159) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid dimethylamide; 160) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid diethylamide; 161) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid dipropylamide; 162) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid (5,7-difluoro-benzothiazol-2-yl)-amide; 99 WO 2006/044509 PCT/US2005/036770 163) 4-[4-Benzo[1,3] dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane- 1-carboxylic acid benzothiazol-2-ylamide; 164) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1-carboxylic acid (1H-benzoimidazol-2-yl)-amide; 165) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1-carboxylic acid (2-hydroxy-1-methyl-2-phenyl-ethyl)-amide; 166) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1-carboxylic acid (pyridin-4-ylmethyl)-amide; 167) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl}-(3-chloro-phenyl)-methanone; 168) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(4-fluoro-phenyl)-methanone; 169) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(4-methoxy-phenyl)-methanone; 170) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-cyclopropyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid; 171) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methoxy-amide; 172) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid hydroxyamide; 173) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-carbamic acid benzyl ester; 174) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid hydrazide; 175) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-acetamide; 176) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-methanesulfonamide; 177) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-phenyl-methanesulfonamide; 178) Butane-1 -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl}-amide; 179) Propane-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl}-amide; 100 WO 2006/044509 PCT/US2005/036770 180) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-nethyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-pyridin-2-yl-methanesulfonamide; 181) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-4-yl-methanesulfonamide; 182) (4-Methoxy-benzyl)-{4-[5-(6-methyl-pyridin-2-yl)-2-(1-phenylmethanesulfonyl piperidin-4-yl)-1H-imidazol-4-yl]-pyridin-2-yl}-amine; 183) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester; 184) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid; 185) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid methyl ester; 186) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2] octane-I -carboxylic acid hydroxyamide; 187) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid amide; 188) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1-carboxylic acid; 189) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 190) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-y1] bicyclo[2.2.2]octan-1-ol; 191) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 192) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid hydroxyamide; 193) N-{4-[5-Benzo[1,3]dioxol-5-yl-4-(6-metliyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-sulfamide; 194) Sulfamic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl ester; 195) {4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 196) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-i -carbonyl} -methanesulfonamide; 101 WO 2006/044509 PCT/US2005/036770 197) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidlazol-2-yl] bicyclo [2.2.2] octane-i -carbonyl} -benzenesulfonamide; 198) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 199) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxylic acid; 200) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} acetamide; 201) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid methyl ester; 202) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-bicyclo [2.2.2]octane 1-carboxylic acid; 203) 4 -[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-bicyclo [2.2.2] octane 1 -carboxylic acid hydroxyamide; 204) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-bicyclo [2.2.2]octane 1-carboxylic acid amide; 205) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yi]-cyclohexyl} methanesulfonamide; 206) 2,2,2-Trifluoro-N-{4-[4-(6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl] cyclohexyl} -acetamide; 207) 4-[4-(5-Fluoro-6-methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol 2-yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 208) {4-[2- [1 -(Butane-i -sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4 yl]-pyridin-2-yl}-(4-methoxy-benzyl)-amine; 209) 4-[2-[ 1 -(Butane-1 -sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-y1)- 1H-imidazol-4 yl]-pyridin-2-ylamine; 210) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-ethyl-pyridine; 211) 4 -[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyr-idin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid aide; 212) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl] -bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 213) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 102 WO 2006/044509 PCT/US2005/036770 214) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide. 215) 4-[2-(6-Methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 216) 4-(2-pyridin-2-yl-pyrazolo[1,5-a]pyridin-3-yl)-pyrimidin-2-ylamine; 217) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 218) 2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-pyrazolo[1,5-a]pyridine; 219) 4-[2-(6-chloro-pyridin-2-yl)-pyrazo lo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 220) 2 -( 6 -methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-pyrazolo[1,5 c]pyrimidine; 221) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrazin-3-yl]-pyrimidin-2-ylamine; 222) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrimidin-3-yl]-pyrimidin-2-ylamine; 223) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-clpyrimidin-3-yl]-pyrimidin-2-ylamine; 224) (2-Methoxy-ethyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 225) (3-{4-[2-(6-Methyl-pyridin-2-yl)-irnidazo(1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} propyl)-carbamic acid tert-butyl ester; 226) (3-Imidazol-1-yl-propyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 227) (4-Methoxy-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 228) [2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridin 6-yl]-methanol; 229) 3 -( 2 -Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 230) (4-{4-[2-(6-Methyl-pyridin-2-yl)-irmidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino } butyl)-carbamic acid tert-butyl ester; 231) (4-Amino-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 232) (5-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} pentyl)-carbamic acid tert-butyl ester; 233) [ 3 -( 2 -Amino-pyrimidin-4-yl)-2-(6-nethyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-6-yl] methanol; 234) [ 3 -( 2 -amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-7-yl] methanol; 103 WO 2006/044509 PCT/US2005/036770 235) L3 -(2-Amino-pfi midiii'--4ly1 ).-'6-iiiethyl-2-(6-methy1-pyridin-2-y1)-imidazo[ 1,2 ajpyridin-8-yl]-(2-morpholin-4-yl-ethyl)-amine; 236) [3 -(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[lI,2 ajpyridin-8-yl] -(2-pyridin-2-yl-ethyl)-amine; 237) [3 -(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2 allpyridin-8-yl]-(2-pyridin-3-yl-ethyl)-amine; 238) [3-(2-.methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-6-yl] -methanol; 239) [3 -(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-8-yl]-(2-pyridin-4-yl-ethyl)-amine; 240) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2 a]pyridin-8-yl]-(3 -morpholin-4-yl-propyl)-amine; 241) [3 -(4-Methyl-piperazin- 1-yl)-propyl]- {4-[2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-3-yl]-pyrimidin-2-yl} -amine; 244) [3 -(4-Methyl-piperidin- 1-yl)-propyll- {4-[2-(6-methyl-pyridin-2-yl)-imidazo [1,2 a]pyridin-3 -yl] -pyrimidin-2-yl} -amine; 245) [4-(2-Pyridin-2-yl-imidazo[1 ,2-alpyridin-3-yl)-pyrimidin-2-yl]-pyridin-3-ylmethyl amine; 246) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl] -pyrimidin-2-yl} -((R)- 1 phenyl-ethyl)-amnine; 247) {4- [2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyidin-3-yl]-pyrimidin-2-yl} -((S)- 1 phenyl-ethyl)-amnine; 248) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2-yl} -(1H tetrazol-5-yl)-amine; 249) {4- [2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl] -pyrimidin-2-yl} -(2H pyrazol-3 -yl)-amnine; 250) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin-2-yl} -(2 morpholin-4-yl-ethyl)-arnine; 251) {4-[2-(6-Methiyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl] -pyrimidin-2-yl} -(2-pyridin 2-yl-ethyl)-amine; 252) {4-[2-(6-Methyl-pyiidin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin-2-yl} -(2-pyridin 3 -yl-ethyl)-amine; 253) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2-yl} -(2-pyridin 4-yl-ethyl)-amine; 104 WO 2006/044509 PCT/US2005/036770 254) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2-yl} -(3 morpholin-4 -yl-propyl)-amine; 255) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo [1 ,2-alpyridin-3-yl]-pyrimidin-2-yl} -(3 piperidin- I -yl-propyl)-amine; 256) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-ajpyridin-3-yl]-pyrimidin-2-yl} [1,3 ,4]thiadiazol-2-yl-amine; 257) 2 -( 6 -Methy-pyridin-2-y)-3-(2-methylsufany-pyrimidin-4-y1>-imidazo [1 ,2-a]pyridine; 258) 2-(6-Methyl-pyridin-2-yl)-3 -(2-methylsulfanyl-pyrimidin-4-yl)-imidazo [1,2 -alpyridine 6-carboxylic, acid methyl ester; 259) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4yl)-imidazo[ 1,2 -alpyridine 7-carboxylic acid ethyl ester; 260) 2 -(6-Methyl-pyridin-2-y)-3-(2-methylsufanyl-pyrinidin-4-y1)4imidazo [1,2 a]pyrimidin-7-ylamine; 261) {7,7-Diiethyl-8-[5-(4- {4-[2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridiri-3 -yl] pyrimidin-2-ylamino }-butylcarbamoy)-pentyl]-2-oxo-4-trifluoromethyl-7,8dihydro-2H-1 oxa-8-aza-antliracen-5-yl} -methanesulfonic acid; 262) 2-(2,7-Difluoro-6-hydroxy-3-oxo-9,9a-dihydro-3H-xanthen-9-yl)-3 ,5 ,6-trifluoro-4- [(4 {4- [2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-ajpyridin-3-yl]-pyrimidin-2-ylamino} butylcarbamoyl)-methylsulfanyl] -benzoic acid; 263) .- (6-Methy1-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-y)imidazo[ 1,2-a]pyridine; 264) 2-(6-Methyl-pyridin-2-yl)-3-(2-piperidin- 1 -yl-pyrimidin-4-yl)-imidazo[ 1,2-alpyridine; 265) 2-(6-Methyl-pyridin-2-yl)-3-(2-pyrrolidin- 1-yl-pyrimidin-4-yl)-imidazo[ 1,2-a]pyridine; 266) 2-(6-Methyl-pyridin-2-yl)-3-[2-(1 H-tetrazol-5-yl)-pyrimidin-4-yl]-imidazo[ 1,2 a]pyridine; 267) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[ 1,2-a]pyridine; 268) 2-(6-Me~thyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[ 1,2-ajpyrimidin-7-ylanine; 269) 3 -(2-Amrino-pyrimidin-4-yl)-2-(6-methy-pyridin-2-yl)-imidazo[ 1,2-a]pyridii-8 ylamine; 270) 3 -(2-Amino-pyrimidin-4-yl)-2(6-methyl-pyridin2-y)-imidazo[ 1,2-a]pyridine-6 carbonitrile; 271) 3 -( 2 -Arnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridinec-6 carboxylic acid; 272) 3 -( 2 -Amiino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-y)-imidazo[ 1,2-a]pyridirie-6 carboxylic acid ([1 ,4]dioxan-2-ylmethyl)-ainiide; 105 WO 2006/044509 PCT/US2005/036770 273) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 274) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-dimethylamino-ethyl)-amide; 275) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-methoxy-ethyl)-amide; 276) 3 -( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 277) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide; 278) 3 -( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid amide; 279) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid cyclopropylamide; 280) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ethylamide; 281) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid hydroxyamide; 282) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methoxy-amide; 283) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methyl ester; 284) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid; 285) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 286) 3 -( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-amino-ethyl)-amide; 287) 3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-dimethylamino-ethyl)-amide; 288) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-hydroxy-ethyl)-anaide; 289) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-oxo-2-pyridin-3-yL-ethyl)-amide; 106 WO 2006/044509 PCT/US2005/036770 290) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iinidazo[1,2-a]pyridine-7 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 291) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid (piperidin-3-ylmethyl)-amide; 292) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid 2,2-dimethylhydrazide; 293) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inridazo[1,2-a]pyridine-7 carboxylic acid amide; 294) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid cyclopropylamide; 295) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-injidazo[1,2-a]pyridine-7 carboxylic acid ethyl ester; 296) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iiridazo[1,2-a]pyridine-7 carboxylic acid ethylamide; 297) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid hydroxyamide; 298) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid methoxy-amide; 299) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iniidazo[1,2-a]pyrimidin-7 ylamine; 300) 3-(2-Azetidin-1-yl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine; 301) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyridine-7-carboxylic acid ethyl ester; 302) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carboxylic acid methyl ester; 303) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-7-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 304) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-8-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 305) 3,3-Dimethyl-N-[2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl) imidazo[1,2-a]pyrimidin-7-yl]-butyramide; 306) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carbonitrile; 307) 3-(2-Methylsulfanyl-pyrimidin-4-yl)-2-pyridin-2-yl-imidazo[1,2-a]pyridine; 107 WO 2006/044509 PCT/US2005/036770 308) 3,6-Dichloro-N-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino} -butyl)-2-(2,4,5,7-Tetrachloro-6-hydroxy-3 -oxo-9,9a-dihydro-3 H xanthen-9-yl)-terephthalamic acid; 309) 3-[2-(2-Methyl-aziridin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo [1,2-a] pyridine; 310) 3-[2-(4-Methyl-piperazin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 311) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-amino}-propionic acid methyl ester; 312) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl] -amino } -propionic acid methyl ester; 313) 3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamiro} phenol; 314) 4-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylarmino} ethyl)-benzenesulfonamide; 315) 4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-ylamine; 316) 4-[2-(6-Chloro-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 317) 4-[2-(6-Methyl-pyridin-2-yl)-7-trifluoromethyl-imidazo[1,2-a]pyridin-3-yl)-pyrirnidin 2-yl-amine; 318) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 319) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbonitrile; 320) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carboxylic acid amide; 321) 4-[6-Bromo-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 322) 4-[6-Chloro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 323) 4-[6-Fluoro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 324) 4 -[ 6 -Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-morpholin-4-yl-ethylamino)-imidazo [1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 325) 4 -[ 6 -Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-2-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 326) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-3-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 108 WO 2006/044509 PCT/US2005/036770 327) 4 6-Metiy 1-2(6-methyl-pyridin-2-yl)-8-(2-pyridin-4-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 328) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-morpholin-4-yl-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ol; 329) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-morpholin-4-yl-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamine; 330) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 331) 4-[7-Aminomethyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl-amine; 332) 4-[7-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 333) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ol; 334) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl amine; 335) 4-[8-Bromo-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-ol; 336) 4-[8-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 337) 6-Chloro-3-(2-methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 338) 5-Dimethylamino -naphthalene- 1 -sulfonic acid (4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-amide; 339) 6-(2,7-Difluoro-6-hydroxy-3-oxo-3H-xanthen-9-yl)-N-(4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-isophthalamic acid; 340) 6-Amino-9-[2-carboxy-5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-phenyl]-xanthen-3-ylidene-ammonium; 341) 6-Bromo-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 342) 6-Fluoro-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 343) 7-Amino-4-methyl-3-[(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-methyl]-2-oxo-2H-chromene-6-sulfonic acid; 344) Cyclobutyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 109 WO 2006/044509 PCT/US2005/036770 345) Cyclopentyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimiclin-2 yl} -amine; 346) Cyclopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimicin-2 yl}-amine; 347) Cyclopropyl-methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 348) Dimethyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 349) Isopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrinidin-2-yl} amine; 350) Methyl-{4-[2-(6-methyl-pyridin-2-yl)-irnidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 350a) N-(2-{4-[2-(6-Methyl-pyridin-2-yl)-iinidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamino}-ethyl)-acetamide; 351) N-(4- {4-[2-(6-Methyl-pyridin-2-yl)-ini dazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2-ylamino} butyl)-acetamide; 352) N,N-Dimethyl-N'-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl} -ethane-1,2-diamine; 353) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 354) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 355) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 356) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridire-6 carbonyl]-methanesulfonamide; 357) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridiie-7 carbonyl]-methanesulfonamide; 358) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-2-(3-methoxy-phenyl)-acetanide; 359) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrirnidin-7 yl]-3,3-dimethyl-butyramide; 360) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-3-pyridin-3-yl-propionamide; 110 WO 2006/044509 PCT/US2005/036770 361) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-acetamide; 362) N-[3-( 2 -Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-nicotinamide; 363) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidaz;o[1,2 a]pyrimidin-7-yl]-2-(3-methoxy-phenyl)-acetamide; 364) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidaz;o [1,2-a] pyrimidin-7-yl]-3,3-dimethyl-butyramide; 365) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 366) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidaz;o[1,2-a] pyrimidin-7-yl]-nicotinamide; 367) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidaz-o[1,2-a] pyrimidin-7-yl]-propionamide; 368) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-propionamide; 369) N-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-y-I} acetamide; 370) N1- {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} -butane 1,4-diamine; 371) N1-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} propane-1,3-diamine; 372) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(BODIPY FL) amide; and 373) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(Texas Red-X) amide 374) N-[3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-acetamide; 375) N-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylJ acetamide, 376) 3-( 3 -pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propylamine, 377) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-acetamide, 378) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-methanesulfonarnide, 379) dimethyl-[3-( 3 -pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-amine, 380) 4-{3-pyridin-2-yl-1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-pyrazol-4-yl}-quinoline, 111 WO 2006/044509 PCT/US2005/036770 381) 4-[3 2 pyridin-_2ylT--(3pyrfolidiiill-yl-propyl)-1H-pyrazol-4-yl]-quinoline, 382) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, 383) 2,4-dimethoxy-5-(3-pyridin-2-yl-IH-pyrazol-4-yl)-pyrimidine, 384) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionic acid, 385) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indole, 386) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-pyridine, 387) N-hydroxy-3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionamide, 388) 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethylamine, 389) N-[2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethyl]-methanesulfonamide, 390) 2-methyl-4-methylsulfanyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 391) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-pyridine, 392) 2-[4-(2,3-dihydro-benzofuran-5-yl)-1H-pyrazol-3-yl]-pyridine, 393) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[d]isoxazole, 394) 3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propionitrile, 395) N-{3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propyl} methanesulfonamide, 396) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-6-methyl-pyridine, 397) [4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-acetonitrile, 398) N-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethyl} methanesulfonanide, 399) 4-[3-(6-methyl-pyridin-2-yl)- 1H-pyrazol-4-yl]-2-methylsulfanyl-pyrimidine, 400) 4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-2H-phthalazin-1-one, 401) 1-[5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-2,3-dihydro-indol-1-yl]-ethanone, 402) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 403) 3-methyl-6-(3-pyridin-2-yl-1 H-pyrazol-4-yl)-3H-quinazolin-4-one, 404) 6-(3-pyridin-2-yl-1H-pyrazol-4-y)-4H-benzo[1 ,4]oxazin-3-one, 405) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoxaline, 406) 3-(4-nitro-benzyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 407) 5-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 408) 4-methyl-7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3,4-dihydro-1H-benzo[e][1,4]diazepine 2,5-dione, 409) 2,3-dimethyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 410) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 410a) 1-methoxy-4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-isoquinoline, 411) 2-methyl-6-(3-pyridin-2-yl-1 H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 112 WO 2006/044509 PCT/US2005/036770 41 i"a)" 4L(3-byidin22y1:1H'yraz61-4"yl)-2H-isoquinolin- 1-one, 412) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-trifluoromethyl-pyridine, 412a) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-vinyl-pyridine, 413) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propenyl-pyridine, 414) 2-(4-benzo[1,3]dioxol-5-yl-iH-pyrazol-3-yl)-6-ethyl-pyridine, 415) 2-(4-benzo[1,3]dioxol-5-yl-iH-pyrazol-3-yl)-6-propyl-pyridine, 416) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-cyclopropyl-pyridine, 417) 1-[6-(4-benzo [1,3] dioxol-5-yl- 1 H-pyrazol-3-yl)-pyridin-2-yl]-ethanol, 418) 4-methoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 419) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline, 420) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-ylamine, 421) 6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-3H-quinazolin-4-one, 422) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrido[1,2-a]pyrimidin-4-one, 423) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 424) 3-methyl-6-[3-(6-methyl-pyridin-2-yl)-IH-pyrazol-4-yl]-3H-quinazolin-4-one, 425) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane- 1 -carboxylic acid, 426) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane-1-carboxylic acid methyl ester, 427) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl] bicyclo[2.2.2]octane-1-carboxylic acid methyl ester, 428) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-isopropyl-pyridine, 429) 2-(4-benzo[1,3]dioxol-5-yl-5-trifluoromethyl-1H-pyrazol-3-yl)-6-bromo-pyridine, 430) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 431) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 432) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 432a) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-methyl-3H-quinazolin-4-one, 433) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-b]pyridazine, 433a) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline, 434) 6-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-3-fluoro-2-methyl-pyridine, 435) 7-methoxy-3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 436) (4-morpholin-4-yl-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-amine, 437) 4-isopropoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 438) 6-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-quinolin-4-ylamine, 113 WO 2006/044509 PCT/US2005/036770 439) (4-["e6 6iz 'Jdfoix 5--3(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} carbamic acid benzyl ester, 440) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexylamine, 441) N-{4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} methanesulfonamide, 442) 6-[3 -(5-fluoro-6-methyl-pyridin-2-y1)-1H-pyrazol-4-yl]-quinoxaine, 443) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 444) 1-tert-butyl-3-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-urea, 445) 5-(3 -pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]thiadiazole, 446) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]oxadiazole, 447) 5-(3 -Pyridin-2-yl-1H-pyrazol-4-yl)-benzooxazole, 448) 4-norpholin-4-yl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 449) 6-[3 -(6-trifluoromethyl-pyridin-2-yl)- 1H-pyrazol-4-yl]-quinoxaline, 450) 4-(4-methoxy-phenyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 451) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-benzo[1,2,5]thiadiazole, 452) 6-(3 -pyridin-2-yl-1H-pyrazol-4-yl)-benzothiazole, 453) 3-(3-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 454) 5-niethyl-thiophene-2-carboxylic acid [6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4 yl]-amide, 455) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-phenyl-benzo[c]isoxazole, 456) 3-(4-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[clisoxazole, 457) 3-(4-chloro-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 458) 3-(4-ethyl-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 459) (4-nethoxy-phenyl)-[6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-quinazolin-4-y]-methanone, 460) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3-thiophen-3-yl-benzo[c]isoxazole, 461) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid, 462) 5-(3 -Pyridin-2-yl- IH-pyrazol-4-yl)- 1H-indazole-3-carboxylic acid metliylamide, 463) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid dimethylamide, 464) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid (2,2-dimethyl propyl)-amide, 465) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid phen ylamide, 466) morpholin-4-yl-[5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazol-3-yl]-rnethanone, 467) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid benzylamide, 468) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid cyclopentylamide; 114 WO 2006/044509 PCT/US2005/036770 469) 4f[4benzo[1,3)dix6lg-5(2'~inethylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzamide; 470) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-iH-imidazol-2-yl] benzonitrile; 471) 4-[5-(2-methanesulfonyl-pyrimidin-4-y)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 472) 4-[5-(2-methoxy-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 473) 4-[5-(2-hydroxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1-carboxylic acid methyl ester; 474) 4-[5-(2-cyclopropylamino-pyrimidin-4-y)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl] -bicyclo[2.2.2] octane-I -carboxylic acid methyl ester; 475) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl] -bicyclo [2.2.2]octane- 1 -carboxylic acid; 476) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1-carboxylic acid amide; 477) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid hydroxyamide; 478) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid methoxy-amide; 479) 4-[5-(2-amino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 480) {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 481) N-{4-[5-(2-cyclopropylatnino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-acetamide; 482) N-{4-[5-(2-cyclopropylarnino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl} -methanesulfonamide; 483) N- {4-[5-(2-cyclopropylatnino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -y)- 1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-2 ,2,2-trifluoro-acetamide; 484) 4-[5-quinoxalin-6-yl- 4 -(2-trifluoromethyl-pyrimidin-4-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 485) 4-[4-(2-cyclopropyl-pyrirnidin-4-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 486) 6-[2-tert-butyl-5-(2-cyclopropyl-pyrimidin-4-y1)-3H-imidazol-4-yl]-quinoxaline; 115 WO 2006/044509 PCT/US2005/036770 48') 6-[5-(2- y6l6ogryl-yimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 488) {4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-I -yl} -methanol; 489) 6-[5-(2-trifluoromethyl-pyrimidin-4-y)-3H-imidazol-4-y1]-quinoxaline; 490) 6-[2-tert-butyl-5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 491) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)-1H-inidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 492) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 493) 6-[5-(2-cyclopropyl-pyrimidin-4-yl)-2-(l-methanesulfonyl-piperidin-4-y)-3H-imidazol 4-yl]-quinoxaline; 494) 4-[5-(2-methyl-pyrimidin-4-yl)-4-[1,2,4]triazolo[4,3-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 495) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- I -carboxylic acid amide; 496) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid; 497) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid methyl ester; 498) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexanol, 499) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol, 500) 4-(4-benzo[1,3]dioxol-5-yl-lH-pyrazol-3-yl)-2-methyl-pyrimidine, 500a) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 501) 6-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 502) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 502a) 6-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1I-pyrazol-4-yl]-quinoxaline, 503) 6-[3-(2-cyclopropyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 504) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-trifluoromethyl-pyrimidine, 505) 7-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, or 506) 6-[3-(2-Trifluoromethyl-pyrimidin-4-yl)-1 H-pyrazol-4-yl]-quinoline.

9. The method of claim 1, wherein the inhibitor is administered locally.

10. The method of claim 1, wherein the inhibitor is administered via an implantable device. 116 WO 2006/044509 PCT/US2005/036770

11. "Tli ith6d"*finii 'O, "w"hier Ifinhe device is a delivery pump.

12. The method of claim 10, wherein the device is a stent.

13. A method of inhibiting vascular remodeling by administering to a subject in need thereof an inhibitor to TGFP type I receptor orAlk4.

14. The method of claim 13, wherein the inhibitor has the structure shown in formula I: R ~ N R'A 1 or an N-oxide or a pharmaceutically acceptable salt thereof, wherein R-' is aryl, heteroaryl, aralkyl, or heteroaralkyl; each R- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hkydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; X 1 . 1 is cycloalkyl or heterocycloalkyl; Y 1 . 1 is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O),-O-, -O-S(O)p-, -C(O)-N(R)-, -N(RE)-C(O)-, -O-C(O)-N(Rk)-, -N(Rk)-C(O)-0-, -O-S(0)p-N(RE)-, -N(e)- S(O)p-O-, -N(RE)-C(O)-N(Rc)-, -N(RE)-S(O)p-N(Rc)-, -C(O)-N(RE)-S(O)p-, -S(O),-N(R )-C(O)-, -C(O)-N(RE)-S(O)p-N(R )-, -C(0)-0-S(0)p-N(RE)-, -N(RO)-S(O),-N(RC)-C(O)-, -N(R)-S(O)p-0-C(O)-, -S(O)p-N(Rb)-, -N(Rb)-S(O)p-, -N(Rb)-, -S(O),-, -0-, -S-, or -(C(Rb)(RC))q-, wherein each of Rb and Rc is independently hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; p is 1 or 2; and q is 1-4; R1-2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloa.lkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; 117 WO 2006/044509 PCT/US2005/036770 each o A. ... AiA"- indipeidently, is 0, S, N, or NR, provided that at least one of A'' and A 2 is N; and m is 0, 1, 2, or 3, and when m >2, two adjacent R a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

15. The method of claim 13, wherein the inhibitor has the structure shown in formula II: Y11-2 // (R 1-2 )n X11--~ Yr-1) X 11 - 3 N or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each of Xui, Xr 1 .. 2 , Xr- 3 , and Xr- 4 is independently CR or N, provided that no niore than two of X 111 , iIr.2, Xr..3, and X. 4 can be N simultaneously; each of Y 111 and Yr- 2 is independently CRY or N, provided that at least one of Y]EI-I and Y 1 - 2 must be N; each R4 1 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, acmino, nitro, cyano, guaradino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each Rr-2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cycloalkyl), -NH(heterocycloalkyl), NIH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaxyl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, 118 WO 2006/044509 PCT/US2005/036770 (heterocycloIlky'l)alklsulfafiyl, ietfoarylsulfanyl, heteroarylalkylsulf-anyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, arninosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, hetero aralkylcarbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m 22, two adjacent R 1 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n 2, two adjacent R2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of Rx and RY is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl.

16. The method of claim 13, wherein the inhibitor has the structure shown in formula III 119 WO 2006/044509 PCT/US2005/036770 Y11-2 (R 11-2 )n (III) Xm1-2 N(Rn m N N Xm11- 4 or a pharmaceutically acceptable salt or N-oxide thereof, wherein each of Xm-1, X 1 1 - 2 , Xm1- 3 , and Xm..4 is independently CRIII-x or N, provided that only two of Xm 1 - 1 , Xm- 2 , Xm-3, and X 1 1 1 - 4 can be N simultaneously; each of Y 11 and Ym 1 - 2 is independently CR"3 or N, provided that at least one of Y 1 1 -1 and Y 1 1 12 must be N; each R1- 1 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfaniide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each R1- 2 is independently alkyl, alkenyl, alkynyl, acyl, halo,, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cyclocalkyl), -NLH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, (cycloalkyl)alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl(alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carboraylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, 120 WO 2006/044509 PCT/US2005/036770 hrlkoly.irbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylarninoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m 2, two adjacent R"" groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n L2, two adjacent R - groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of R "- and R"y is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, anino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylanino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylanino, heteroarylcarbonylaniino, heteroarylsulfonylamino, heteroaralkylcarbonylanaino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl; or a pharmaceutically acceptable salt or N-oxide thereof.

17. The method of claim 13, wherein the inhibitor has the structure shown in formula IV 121 WO 2006/044509 PCT/US2005/036770 RNv 5 RIv~ 6 N 'gV-1-RV-2 -R -3-RIV-4 N (IV) N (RIV-a or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each Riv-a is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; R"- 1 is a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri-O-(CH 2 )r 2 -, where each of r1 and r2 is independently 2 or 3; Rw- 2 is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, or a bond; Rv- is -C(O)-, -C(0)O-, -OC(O)-, -C(O)-N(R! ~b)-, -N(Rv-b)-C(O)-, -O-C(O)-N(Rv~ b)-, -N(Rv -b)-C(0)-0-, -O-S(O)p-N(Rv -b)-, -N(R! ~h)- S(O)p-0-, -N(R' -b)-C(O)-N(R v-)-, -N(R v-)-S(O)p-N(RW -b)-, -C(O)-N(R' ~6)-S(O),-, -S(O)p-N(Rv -b)-C(0)-, -S(0),-N(Rv-b) -N(Rwb)-S(O)p-, -N(Rv-b)-, -S(O)p-, -0-, -S-, or -(C(R! ~b)(RI~C))q-, or a bond; wherein each of Rwb and RW~ is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; RIV~ 4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; RIv-5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkyl, 122 WO 2006/044509 PCT/US2005/036770 heterdy"16alkoy,"h'hedrocycIoalkysulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryloxy, or heteroarylsulfinyl; R-6 is (1) a 5- to 6-membered heterocyclyl containing 1-3 hetero ring atoms selected from the group consisting of--O-, -S-, -N=, and -NRI-d-, wherein RI -d is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; said heterocyclyl being substituted with Re and optionally substituted with one to two Rvf; where R-~ is oxo, thioxo, alkoxy, alkylsulfinyl, -NH 2 , -NH(unsubstituted alkyl), or -N(unsubstituted alkyl)2, and Rvf is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or (2) a fused ring heteroaryl selected from the group consisting of: (R')n (RI)n(R)(Rn B' B B B' 1 Xi X' '2 X AK 1 (2 A 1 xOX X -z , and wherein ring A is an aromatic ring containing 0-4 hetero ring atoms, and ring B is a 5- to 7 membered aromatic or nonaromatic ring containing 0-4 hetero ring atorns, provided that at least one of ring A and ring B contains one or more hetero ring atoms; ring A' is an aromatic ring containing 0-4 hetero ring atoms, and ring B' is a 5- to 7-membered saturated or unsaturated ring containing 0-4 hetero ring atoms, provided that at least one of ring A' and ring B' contains one or more hetero ring atoms; each hetero ring atom is -0-, -S-, -N=, or NRMg-; each X 1 is independently N or C; each X 2 is independently -0-, -S-, -N=, -NRvg-, or -CHRIV-h-; wherein Re- is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; each of RI-h and R- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, 123 WO 2006/044509 PCT/US2005/036770 cycloilkyl,'cy61661Ey165y,"Ey616alkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; aind n is 0-2; and m is 0-3, and when m >2, two adjacent Riv-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; provided that if RW - 6 is 2-naphthyridinyl, 4-quinolinyl, imidazo[1,2-a]pyridyl, or benzimidazolyl, then -R -1-R -2-R -RI ~4 is not H, unsubstituted alkyl, -CH 2 -C(O)-N(H)-alkyl, -CH 2 -C(O)-N(alkyl)2, or benzyl.

18. The method of claim 13, wherein the inhibitor has the structure shown in forriula V (Rv-a )m N N(V AV-2 AV-' QV 1vvV Rv-1 Av or an N-oxide or a pharmaceutically acceptable salt thereof, wherein Rv- 1 is heteroaryl; each RVa, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hyciroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylanino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfarnoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; Xv is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or a bond; Y, is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O),-O-, -O-S(O)p-, -C(O)-N(R)-, -N(Rb)-C(O)-, -O-C(O)-N(RE)-, -N(R)-C(O)-0-, -C(O)-N(RE)-0-, -O-N(R)-C(>)-, -O-S(O)p-N(RE)-, -N(RE)- S(O)p-O-, -S(O)p-N(RE)-O-, -O-N(RE)-S(O)p-, -N(e)-C(O)-N(Rc)-, -N(e)-S(0)p-N(Rc)-, -C(O)-N(RE)-S(O),--, -S(O)p-N(e)-C(O)-, -C(O)-N(e)-S(O)p-N(Rc) 124 WO 2006/044509 PCT/US2005/036770 -C(O)-O-S(O)p-N(R")-, N S(O)pN(R)-C(O)-, -N(e)-S(O)p-O-C(O)-, -S(O),-N(R)-, -N(Rb)-S(O)p-, -N(Rb)-, -S(0),-, -0-, -S-, or -(C(R)(C))-, wherein each of Rb and Rc, independently, is hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; R- is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of AV1 and AV 2 , independently, is N or NRb; and m is 0, 1, 2, or 3, and when m ;>2, two adjacent Rvwa groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety, provided that if X, is a bond, then Yv is a bond; RV 2 is hydrogen or alkyl; m is 1, 2, or 3; and at least one Rva is substituted at the 2-pyrimidinyl position.

19. The method of claim 13, wherein the inhibitor has the structure shown in formula VI: RVI-5 RV 1 6 R RVIl- RVI- 2 - VI- 3 - RVI- 4 N (VI) N (RVIa)m or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each Rv-a, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, NH 2 , -NH(unsubstituted alkyl), -N(unsubstituted alkyl)2, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; 125 WO 2006/044509 PCT/US2005/036770 141 isabondalkylene, aikel'ylene, alkynylene, or -(CH 2 )ri-O-(CH 2 )r 2 -, wherein each of r1 and r2, independently, is 2 or 3; Rv1-2 is cycloalkylene, heterocycloalkylene, cycloalkenylene, heterocycloalkenylene, arylene, heteroarylene, or a bond; RVI- 3 is -C(O)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(R)-, -N(RE)-C(O)-, -O-C(O)-N(RE)-, -N(R0)-C(O)-0-, -C(O)-N(RE)-O-, -O-N(RE)-C(O)-, -O-S(O),-N(R)-, -N(R)- , -Sp , (O)-N(R)-O-, -- N(R)-S(O)p-, -N(R)-C(O)-N(Rc ( N ) -N(RE)-S(O)p-N(RW)-, -C(O)-N(RE)-S(O),-, -S(O)p-N(R)-C(O)-, -C(O)--N(RE)-S(O),-N(Rc _ -C(O)-O-S(O),-N(R)-, -N(R)-S(O)p-N(R)-C(O)-, -N(R)-S(O)p-O-C(O)-, -S(O),-N(R)-, -N(R)-S(O)p-, -N(R)-, -S(O),-, -0-, -S-, -(C(R')(R))q-, or a bond; wherein each of Rb and R is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; wherein p is 1 or 2 and q is 1-4; RVI~ 4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; R1 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryloxy, arylsulfinyl, heteroaryloxy, or heteroarylsulfinyl; R -6 is a 5- to 6-membered monocyclic heterocyclyl or an 8- to 11 -membered bicyclic heteroaryl; each being optionally substituted with alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and m is 0-3 and when m :2, two adjacent RV-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

20. The method of claim 13, wherein the inhibitor is 1) 4-(4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 126 WO 2006/044509 PCT/US2005/036770 2) 41(4 50rizo~ IMjdio'o-5-yI'5-pyrilin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 3) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-y]-pipeTidine-1 carboxylic acid benzyl ester; 4) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 5) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-y1)-6-methyl-pyridine; 6) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 7) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 8) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-inidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 9) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 10) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 yl]-6-methyl-pyridine; 11) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 yl]-pyridine; 12) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 -yl] pyridine; 13) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 -yl]- 6 methyl-pyridine; 14) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzyl ester; 15) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2,4-dichloro-benzylamide; 16) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1 -yl] ethanone; 17) 2-[5-3enzo[1,3]dioxol-5-yl-2-(1-furan-2-yl-methyl-piperidin-4-yl)-3H-imidlazol-4-yl] pyridine; 18) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 19) 4-[4-3enzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylamine; 127 WO 2006/044509 PCT/US2005/036770 20) IN- {4-[4-Be Inz1 1H-imidazol-2-yl] cyclohexyl} -C-phenyl-methanesulfonamide; 21) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 22) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 23) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] oct-I -yl} -carb amic acid benzyl ester; 24) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-ethyl-pyridin-2-yl)-1H-inidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 25) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-pyridine; 26) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-IH-imidazol-2-yl)-piperidine-1-carboxylic acid 4-nitro-benzyl ester; 27) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4,5-dimethoxy-2-nitro-benzyl ester; 28) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 3-fluoro-benzylamide; 29) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-fluoro-benzylamide; 30) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzylamide; 31) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(toluene-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 32) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methyl-benzylamide; 33) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methoxy-benzylamide; 34) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzylamide; 35) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-IH-imidazol-2-yl)-piperidine-1-sulfonyl] benzoic acid; 36) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid amide; 37) 4-[4-(4-Benzo[1,3]diorol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzonitrile; 128 WO 2006/044509 PCT/US2005/036770 38) -{3-benz[ o fol-2-yl-l2-'1 (4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 39) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 40) {5-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] naphthalen-1-yl}-dimethyl-amine; 41) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methyl)-piperidin-4-yl)]-3H-imidazol-4 yl} -pyridine; 42) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(proparie-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 43) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 44) 1-{4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonyl]-phenyl} -ethanone; 45) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methyl-benzyl)-piperidin-4-yl]-3H-inidazol-4-yl} pyridine; 46) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-fluoro-5-trifluoromethyl-benzyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 47) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-cyclohexylmethyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 48) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-IH-imidazol-2-yl)-piperidin-1-ylmethyl] cyclopropanecarboxylic acid ethyl ester; 49) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-ylmethyl] pyrrolidine-1-carboxylic acid tert-butyl ester; 50) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2,2-dirnethyl-[1,3]dioxolan-4-ylmethyl)-piperidin-4 yl] -3H-imidazol-4-yl} -pyridine; 51) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 52) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(butane-i1-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 53) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 54) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-pheryl-ethenesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 129 WO 2006/044509 PCT/US2005/036770 55) 2-15-Benzo[1,3]dioxol-5-yl-2-[ 1 -(ropane- 1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 56) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonylnethyl]-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 57) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-y} -pyridine; 58) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-pyridine; 59)2- {5 -Benzo[1,3]dioxol-5-yl-2-[1-(4-fluoro-phenylmethanesulfony)-piperidin-4-yl]-3H imidazo l-4-yl} -pyridine; 60) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-pyridine; 61) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 62) 2-[5 -Benzo[ 1,3]dioxol-5-yl-2-(1 -p-tolylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-pyridine; 63) 3-(4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 64) 3-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 65) 4-[4-Benzo[1,3]dioxol-5-yl-l-hydroxy-5-(6-methyl-pyridin-2- yl)-IH-inidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 66) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(pyridin-2-yl-methanesulfonyl)-piperidin-4-y]-3H imidazol-4-yl} -pyridine; 67) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-1-yl-ethanesuLfonyl)-piperidin-4-yl]-3H imidazo l-4-yl} -pyridine; 68) 2-[5 -Benzo[,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-pyridine; 69) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 70) 2- {5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 71) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(pyridin-3-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazo l-4-yl} -pyridine; 130 WO 2006/044509 PCT/US2005/036770 72) 2-1{5-BenzI'I'3'Jdi6iof r$'2-1 '(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 73) 3-[4-Benzo[1,3]dioxol-5-yl-l-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-y] pyrrolidine-1-carboxylic acid benzyl ester; 74) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 75) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-bis-trifluoromethyl-phenylmethanesulfonyl) piperidin-4-yl]-3H-imidazol-4-yl}-pyridine; 76) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -pyridine; 77) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 78) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 79) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 80) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 81) 4-[5-Benzo[1,3]dioxol-5-yl-1-methyl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 82) 4-[4-Benzo[1,3]dioxol-5-yl-1-methyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 83) {4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl}-carbarnic acid benzyl ester; 84) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-phenoxy-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 85) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 86) 2- {5-Benzo [1,3]dioxol-5-yl-2-[ 1 -(propane- 1 -sulfonyl)-piperidin-4-yl] -3H-imidazol-4 yl} -6-methyl-pyridine; 87) 2- {5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(butane-1 -sulfonyl)-piperidin-4-yl] -3H-imidazol-4-y} 6-methyl-pyridine; 88) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 131 WO 2006/044509 PCT/US2005/036770 89) '2 -hnzo[1,3i]dioxofjP5lI2-I'1yridin-4-ylmethanesulfonyl)-piperidin-4-yl] -3H imidazol-4-yl} -6-methyl-pyridine; 90) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 91) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 92) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-2-sulfoayl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 93) 2-{5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(butane-i -sulfonyl)-piperidin-3-yl]-3H-imidazol-4-y} 6-methyl-pyridine; 94) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 95) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-iH-imidazole-4-sulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 96) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-isoxazole-4-sulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 97) 4-[5-Benzo[1,3]dioxol-5-yl-1-hydroxy-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 98) Butane-1 -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl} -amide; 99) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl}-C-pyridin-2-yl-methanesulfonamide; 100) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl}-amide; 101) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl}-amide; 102) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid amide; 103) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 104) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-bromo-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 105) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-3-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 132 WO 2006/044509 PCT/US2005/036770 106) 2- {5-Benzo [1,3Eioxl-5-yl-2-[ I-(5-methyl-2-trifluoromethyl-furan-3-sulfonyl) piperidin-4-yl]-3H-imidazol-4-yl}-6-methyl-pyridine; 107) 4-[2-(1-phenylmethanesulfonyl-piperidin-4-yl)-5-(6-methyl-pyridin-2-yl)-1H-imidazol 4-yl]-pyridin-2-yl-fluoride; 108) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-trifluoromethyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1 -carboxylic acid benzyl ester; 109) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-bromo-pyridin-2-yl)-1-hydroxy-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 110) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-bromo-pyridine; 111) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]oct-1 -yl} -methanol; 112) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imiclazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid amide; 113) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-2H-imicLazol-2-yl]-piperidine-1 sulfonic acid dimethylamide; 114) 1- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-irnidazol-2-yl]-piperidin 1-yl} -3-phenyl-propan-1-one; 115) 2- {5-Benzo[1,3]dioxol-5-yl-2-[1 -(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 116) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imiclazol-2-yl] bicyclo [2.2.2]octane-1 -carbonitrile; 117) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylamine; 118) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-phenyl-methanesulfonamide; 119) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-lH-inidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 120) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-pyridin-2-yl-methanesulfonamide; 121) 2- {5-Benzo[1,3]dioxol-5-yl-2-[4-(1H-tetrazol-5-yl)-bicyclo[2.2 .2]oct-1-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 122) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imcnidazol-2-yl] bicyclo [2.2.2]oct- I-yl} -acetamide; 133 WO 2006/044509 PCT/US2005/036770 123) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 124) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 125) Thiophene-3-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 126) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 127) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(2-phenyl-ethanesulfonyl)-piperidin-4-yl-3H imidazol-4-yl}-6-methyl-pyridine; 128) Methanesulfonic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-ylmethyl ester; 129) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetonitrile; 130) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -acetic acid; 131) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl} -methanesulfonamide; 132) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 133) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 134) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 135) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-phenyl-methanesulfonamide; 136) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-pyridin-2-yl-methanesulfonamide; 137) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid benzylamide; 138) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (pyridin-2-ylmethyl)-amide; 139) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid 3-chloro-4-fluoro-benzylamide; 134 WO 2006/044509 PCT/US2005/036770 140) 4-[4-Eenzo [1 ,3]dioxolF5-yl-5-(6-methyl-pyridin-2-y1)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid (furan-2-yhnethyl)-amide; 141) 2-[5-Benzo[ 1,3] dioxol-5 -yl-2-(l -methanesulfonyl-pyrroidin-3-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 142) 2- {5-Benzo[1,3]dioxol-5-yl-2- [1 -(butane- 1-sulfonyl)-pyrrolidin-3-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 143) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-iH-imidazole-4-sulfonyl)-pyrrolidin-3-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 144) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylniethanesulfonyl-pyrrolidin-3-yl)-3H-imidazol 4-yl]-6-methyl-pyridine; 145) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-pyrrolidin-3-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 146) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 147) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-2-yl-ethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 148) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine I-sulfonylmethyl}-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 149) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 150) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-p yridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid methylamide; 151) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1-carboxylic acid ethylaniide; 152) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid butylaniide; 153) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid isopropylamide; 154) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-p yridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (3-imidazol-1-yl-propyl)-amide; 155) 2-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1 -sulfonylmethyl} -phenylamine; 156) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-p yridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (1 -methyl-5-methylsulfanyl-1H-[1,2,4]triazol-3-yl) amide; 135 WO 2006/044509 PCT/US2005/036770 157) 4 -"B enzo,o]dIioxoI5 y-5-(6"methyl-pyridin-2-yl)- IH-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid cyclohexylamide; 158) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1 H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-pyrrolidin-1-yl-methanone; 159) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid dimethylamide; 160) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-y1] bicyclo [2.2.2]octane- 1-carboxylic acid diethylamide; 161) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid dipropylamide; 162) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid (5,7-difluoro-benzothiazol-2-yl)-amide; 163) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid benzothiazol-2-ylamicle; 164) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid (1H-benzoimidazol-2-yl)-amide; 165) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1E-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (2-hydroxy-1-methyl-2-phenyl-ethyl)-amide; 166) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1iH-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (pyridin-4-ylmethyl)-axmide; 167) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-LH-imidazol-2-yl]-piperidin-1 yl}-(3-chloro-phenyl)-methanone; 168) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl}-(4-fluoro-phenyl)-methanone; 169) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(4-methoxy-phenyl)-methanone; 170) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-cyclopropyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 171) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1FH-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid methoxy-amide; 172) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1LH-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 173) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -carbamic acid benzyl ester; 136 WO 2006/044509 PCT/US2005/036770 174) 4-[4-Benzo[1,3] dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid hydrazide; 175) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH-imidazol-2-yl] cyclohexylmethyl} -acetamide; 176) N- { 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -methanesulfonamide; 177) N-{ 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-phenyl-methanesulfonamide; 178) Butane-1 -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH imidazol-2-yl]-cyclohexylmethyl}-amide; 179) Propane-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl} -amide; 180) N-{ 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexzylmethyl} -C-pyridin-2-yl-methanesulfonamide; 181) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-4-yl-methanesulfonamide; 182) (4-Methoxy-benzyl)-{4-[5-(6-methyl-pyridin-2-yl)-2-(1-phenylmethanesulfonyl piperidin-4-yl)-1H-imidazol-4-yl]-pyridin-2-yl}-amine; 183) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 184) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 185) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- I -carboxylic acid methyl ester; 186) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 187) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 188) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- I -carboxylic acid; 189) N- {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 190) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 137 WO 2006/044509 PCT/US2005/036770 191) 4 4 (6-dyclopropyl-pyridin-2-y1)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2] octane-i -carboxylic acid amide; 192) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol-2 yl]-bicyclo[2.2.2] octane-i -carboxylic acid hydroxyamide; 193) N-{4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-sulfamide; 194) Sulfamic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl ester; 195) {4-[4-(6-Methyl-pyridin-2-y1)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 196) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carbonyl} -methanesulfonamide; 197) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carbonyl} -benzenesulfonamide; 198) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin- 2 -yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxylic acid methyl ester; 199) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxylic acid; 200) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} acetamide; 201) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-bicyclo[2. 2 . 2 ]octane 1 -carboxylic acid methyl ester; 202) 4-[4-(6-Methyl-pyridin-2-yl)-5 -quinoxalin-6-yl- 1H-imidazol-2-yl] -bicyclo[2.2.2] octane 1-carboxylic acid; 203) 4-[4-(6-Methyl-pyridin-2-yL)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid hydroxyamide; 204) 4-[4-(6-Methyl-pyridin-2-y1)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-bicyclo(2.2.2]octane 1-carboxylic acid amide; 205) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} methanesulfonamide; 206) 2,2,2-Trifluoro-N-{4-[4-(6--methyl-pyridin-2-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl] cyclohexyl} -acetamide; 207) 4-[4-(5-Fluoro-6-methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol 2-yl] -bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 138 WO 2006/044509 PCT/US2005/036770 208) {4-[2-[ 1-(Buntane-1-siiffiil)-ipiP'&ridin-4-yL]-5-(6-methyl-pyridin-2-yl)-IH-imidazol-4 yl]-pyridin-2-yl}-(4-methoxy-benzyl)-amine; 209) 4-[2-[ 1 -(Butane-i -sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4 yl]-pyridin-2-ylamine; 210) 2-[5-Benzo[1,3]dioxol-5-yl-2-(l-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 y1]-6-ethyl-pyridine; 211) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 212) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 213) N- {4- [5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl- 1 H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -methanesulfonamide; 214) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -acetamide. 215) 4-[2-(6-Methyl-pyridin-2-yl)-pyrazolo(1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 216) 4-(2-pyridin-2-yl-pyrazolo[1,5-a]pyridin-3-yl)-pyrimidin-2-ylamine; 217) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 218) 2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-pyrazolo[1,5-a]pyridine; 219) 4-[2-(6-chloro-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 220) 2-(6-methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-pyrazolo[1,5 c]pyrimidine; 221) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrazin-3-yl]-pyrimidin-2-ylamine; 222) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrimidin-3-yl]-pyrimidin-2-ylamine; 223) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 224) (2-Methoxy-ethyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 225) (3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} propyl)-carbamic acid tert-butyl ester; 226) (3-Imidazol-1-yl-propyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 227) (4-Methoxy-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 228) [2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridin 6-yl]-methanol; 139 WO 2006/044509 PCT/US2005/036770 229) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 230) (4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-ajpyridin-3-yl]-pyrimidin-2-ylamino} butyl)-carbamic acid tert-butyl ester; 231) (4-Amino-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 232) (5-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} pentyl)-carbamic acid tert-butyl ester; 233) [3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazc>[1,2-alpyridin-6-yl] methanol; 234) [3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-y)-imidazo[1,2-a]pyridin-7-yl] methanol; 235) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-8-yl]-(2-morpholin-4-yl-ethyl)-amine; 236) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-2-yl-ethyl)-amine; 237) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-3-yl-ethyl)-amine; 238) [3-(2-methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-6-yl]-methanol; 239) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-4-yl-ethyl)-amine; 240) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2 a]pyridin-8-yl]-(3-morpholin-4-yl-propyl)-amine; 241) [3-(4-Methyl-piperazin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3-yl]-pyrimidin-2-y}-amine; 244) [3-(4-Methyl-piperidin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3-yl]-pyrimidin-2-yl}-amine; 245) [4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-yl]-pyridin-3-ylnethyl amine; 246) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrirnidin-2-yl}-((R)-1 phenyl-ethyl)-amine; 247) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrirnidin-2-yl}-((S)-1 phenyl-ethyl)-amine; 140 WO 2006/044509 PCT/US2005/036770 248) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-y]-pyrimidin-2-yl} -(1H tetrazol-5-yl)-amine; 249) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2H pyrazol-3-yl)-amine; 250) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2 morpholin-4-yl-ethyl)-amine; 251) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 2-yl-ethyl)-amine; 252) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 3-yl-ethyl)-amine; 253) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 4-yl-ethyl)-amine; 254) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 morpholin-4-yl-propyl)-amine; 255) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 piperidin-1-yl-propyl)-amine; 256) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} [1,3,4]thiadiazol-2-yl-amine; 257) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 258) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 6-carboxylic acid methyl ester; 259) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 7-carboxylic acid ethyl ester; 260) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2 a]pyrimidin-7-ylamine; 261) {7,7-Dimethyl-8-[5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-pentyl]-2-oxo-4-trifluoromethyl-7,8-dihydro-2 1 oxa-8-aza-anthracen-5-yl}-methanesulfonic acid; 262) 2-(2,7-Difluoro-6-hydroxy-3-oxo-9,9a-dihydro-3H-xanthen-9-y1)-3,5,6-trifluoro-4-[(4 {4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butylcarbamoyl)-methylsulfanyl]-benzoic acid; 263) -(6-Methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 264) 2-(6-Methyl-pyridin-2-yl)-3-(2-piperidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 265) 2-(6-Methyl-pyridin-2-yl)-3-(2-pyrrolidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 141 WO 2006/044509 PCT/US2005/036770 266); )2(6-Met hylI-p yr idin-2 -yl)-3 -[2-( 1 H-tetrazol-5-yl)-pyrimidifl- 4 -yl] -imidazo[ 1,2 a]pyridine; 267) 2-(6-Methyl--pyridin-2-yl)-3 -pyrimidin-4-y1-imidazoj1 ,2-a]pyridine; 268) 2-(6-Methy1-pyridin-2-y1)-3-pyrimidil-4-y1-imidazo[l ,2-a]pyrimidin-7-ylamifle; 269) 3-.(2-Amino-pyimidin-4-y1)-2-(6-mthy1-pyridil-2-yl)-imidazo [1,2-a]pyridin-8 ylamnine; 270) 3-(2-Amino-pyrimidin-4-y)-2-(6-methy-pyridil-2-yl)-imidazo [1,2-a]pyridine-6 carbonitrile; 271) 3-(2-Amino-pyrimidin-4-y)-2-(6-methY1-pyridil-2-y1)-imidazo[ 1,2-a~jpyridine-6 carboxylic acid; 272) 3-(2-Amino-pyrimidin-4-y)-2-(6-methy1-pyridifl-2-yl)-imidazo[ 1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 273) 3 -(2-Amino-pyrimidin-4-y1)-2-(6-methy-pyridil-2-yl)-imidazo [1 ,2-a]pyridine-6 carboxylic acid ([1 ,4]dioxan-2-ylmethyl)-amide; 274) 3 -(2-Amino-pyrimidin-4-y1)-2-(6-methy-pyridil-2-yl)-imidazo[1I,2-alpyridine-6 carboxylic acid (2-dimethylamnino-ethyl)-amide; 275) 3-(2-Amino-pyrimidin-4-y)-2-(6-methy-pyfldi-2-y1)-imidazo [1 ,2-a]pyridine-6 carboxylic acid (2-methoxy-ethyl)-amide; 276) 3 -(2-Amino-pyrimidin-4-y)-2-(6-methy1-pyfldil-2-yl)-imidazo [1 ,2-a]pyridine-6 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 277) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methy-pyridil-2-yl)imidazo[1I,2-a~jpyridine-6 carboxylic acid [3-(4-methyl-piperazin- 1-yl)-propyl] -amide; 278) 3-(2-Amino-pyrimidin-4-y)-2-(6-methy-pyrdi-2-Y1)lTidazo[ 1,2-.a]pyridine-6 carboxylic acid amide; 279) 3-(2-Amnino-pyrimidin-4-y)-2-(6-methy-pyridil-2-y1)-imidazo[ 1,2-a]pyridine-6 carboxylic acid cyclopropylamide; 280) 3-(2-Arnino-pyrimidin-4-y)-2-(6-methy1-PYrdil-2-y1)-imidazo[1I,2-alpyridine-6 carboxylic acid ethylamide; 281) 3-(2-Amino-pyrimidin-4-y1)-2-(6-methy1-pyfldifl-2-yl)-imidazo[ 1,2-aljpyridine-6 carboxylic acid hydroxyamide; 282) 3-2Aioprmdn--l--6mty yrdn2y)iio1 ,2-a]pyridine-6 carboxylic acid methoxy-amnide; 283) 3-2Aioprmdn4y)2(-mty yii--l-mdz[,2-aljpyridine-6 carboxylic acid methyl ester; 142 WO 2006/044509 PCT/US2005/036770 284) 3 2AmInIIpyriidin4yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid; 285) 3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 286) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-amino-ethyl)-amide; 287) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-dimethylanino-ethyl)-amide; 288) 3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2- alpyridine-7 carboxylic acid (2-hydroxy-ethyl)-amide; 289) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-oxo-2-pyridin-3-yl-ethyl)-amide; 290) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 291) 3-(2-Amino-pyrimidin-4-y1)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (piperidin-3-ylmethyl)-amide; 292) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid 2,2-dimethylhydrazide; 293) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid amide; 294) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid cyclopropylamide; 295) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethyl ester; 296) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethylamide; 297) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid hydroxyamide; 298) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid methoxy-amide; 299) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 ylamine; 300) 3-(2-Azetidin-1-yl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine; 301) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-iniidazo[1,2-a] pyridine-7-carboxylic acid ethyl ester; 143 WO 2006/044509 PCT/US2005/036770 302) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carboxylic acid xnethyl ester; 303) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-7-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 304) 3-(2-Methanesulfonyl-p yrimidin-4-yl)-8-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 305) 3,3-Dimethyl-N-[2-(6-rinethyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin- 4 -yl) imidazo[1,2-a]pyrimidin-7-yl]-butyramide; 306) 3-(2-Methanesulfonyl-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carbonitrile; 307) 3-(2-Methylsulfanyl-pyrimidin-4-yl)-2-pyridin-2-yl-imidazo[1,2-a]pyridine; 308) 3,6-Dichloro-N-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino } -butyl)-2-(2,4,5,7-Tetrachloro-6-hydroxy-3-oxo-9,9a-dihydro-3H xanthen-9-yl)-terephthalamic acid; 309) 3-[2-(2-Methyl-aziridin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a.] pyridine; 310) 3-[2-(4-Methyl-piperazin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 311) 3-{[3-(2-Amino-pyrimidiin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-amino}-propionic acid methyl ester; 312) 3- { [3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl]-amino} -propionic acid methyl ester; 313) 3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} phenol; 314) 4-(2- {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} ethyl)-benzenesulfonamide; 315) 4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-ylamine; 316) 4-[2-(6-Chloro-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 317) 4-[2-(6-Methyl-pyridin-2-yl)-7-trifluoromethyl-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl-amine; 318) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 319) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbonitrile; 320) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carboxylic acid amide; 144 WO 2006/044509 PCT/US2005/036770 321) 4 [6-Bromo-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 322) 4-[6-Chloro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 323) 4-[6-Fluoro-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 324) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-morpholin-4-yl-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 325) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-2-yl-ethylamino)-imidazo[l1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 326) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-3-yL-ethylamino)-imidazo[1,2-a] pyridin-3-yl]-pyrimidin-2-ol; 327) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-(2-pyridin-4-yl-ethylamino)-imidazo[l,2-a] pyridin-3-yl]-pyrimidin-2-ol; 328) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-8-morpholin-4-yl-imidazo[1,2-a]pyridin-3-yl) pyrimidin-2-ol; 329) 4-[6-Methyl-2-(6-methyl-pyridin-2-y1)-8-morpholin-4-y1-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamine; 330) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-y]-pyrimidin- 2 ylamine; 331) 4-[7-Aminomethyl-2-(6-methyl-pyridin-2-yl)-imidazo[1 ,2-a]pyridin-3-yl]-pyrimidin-2 yl-amine; 332) 4-[7-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 333) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ol; 334) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin- 2 -yl amine; 335) 4-[8-Bromo-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-ol; 336) 4-[8-Methyl-2-(6-methyl-pyridin-2-y1)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 337) 6-Chloro-3-(2-methanesulfonyl-pyrimidin-4-y1)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 338) 5-Dimethylamino-naphthalene-1-sulfonic acid (4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-anaide; 145 WO 2006/044509 PCT/US2005/036770 339) 6(2, 7Difluoro-6-hydroxy-3-oxo-3H-xanthen-9-yl)-N-(4-{4-[2-(6-rnethyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-y1aminol}-butyl)-isophthalamic acid; 340) 6-Amino-9-[2-carboxy-5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-phenyl]-xanthen- 3 -ylidene-ammonium; 341) 6-Bromo-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-y1)-imidazo[1,2-a] pyridine; 342) 6-Fluoro-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 343) 7-Amino-4-methyl-3-[(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-methy1]-2-oxo-2H-chromene-6-sidfonic acid; 344) Cyclobutyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-y]-pyrimidin-2-y1} amine; 345) Cyclopentyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl} -amine; 346) Cyclopropyl- {4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3 -yl]-pyrimidin-2 yl} -amine; 347) Cyclopropyl-methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 348) Dimethyl-{4-[2-(6-methyl-pyridin-2-y1)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 349) Isopropyl- {4-[2-(6-methyl-pyridin-2-y1)-inidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 350) Methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin- 2 -y1} amine; 350a) N-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamino}-ethyl)-acetamide; 351) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-acetamide; 352) N,N-Dimethyl-N'-{4-[2-(6-methyl-pyridin-2-y1)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl} -ethane-1,2-diamine; 353) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]- 3 -pyridin-3-yl-propionamide; 354) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 146 WO 2006/044509 PCT/US2005/036770 355) N122(6--ethyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 356) N-[3-(2-Amino-pyrimidin-4-y1)-2-(6-methyl-pyridin-2-yl)-irnidazo[1,2-a]pyridine-6 carbonyl]-methanesulfonamide; 357) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carbonyl]-methanesulfonamide; 358) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-i idazo[1,2-a]pyrimidin-7 yl]- 2 -( 3 -methoxy-phenyl)-acetamide; 359) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo(1,2-a]pyrimidin-7 yl]-3,3-dimethyl-butyramide; 360) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 y1]-3-pyridin-3-yl-propionamide; 361) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-acetamide; 362) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-nicotinamide; 363) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-y1)-imidazo[1,2-a] pyrimidin-7-yl]-2-(3-methoxy-phenyl)-acetamide; 364) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3,3-dimethyl-butyramide; 365) N-[3-(2-Methanesulfonyl-pyrimidin-4-y1)-2-(6-methyl-pyridi,-2-yl)-imidazo(1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 366) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 367) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-y1)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 368) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-propionamide; 369) N-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide; 370) Ni - {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3 -yl]-pyrimidin-2-yl} -butane 1,4-diamine; 371) Ni-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} propane-1,3-diamine; 147 WO 2006/044509 PCT/US2005/036770 372) NI-4 {4-[2-( 6-MeIthyI pyridin-2yl)-imidazo [1,2-a]pyridin-3 -yl] -pyrimidin-2-ylamino} butyl)-(BODIPY FL) aide; and 373) N-(4- {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(Texas Red-X) amide 374) N-[3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-acetamide; 375) N-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide. 376) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propylamine, 377) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-acetamide, 378) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-methanesulfonamide, 379) dimethyl-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-amine, 380) 4-{3-pyridin-2-yl-1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-pyrazol-4-yl}-quinoline, 381) 4-[3-pyridin-2-yl-1-(3-pyrrolidin-1-yl-propyl)-1H-pyrazol-4-yl]-quinoline, 382) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyridin-2-ylamile, 383) 2,4-dimethoxy-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 384) 3-(3-pyridin-2-yl-4-quinolin- 4 -yl-pyrazol-1-yl)-propionic acid, 385) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indole, 386) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-pyridine, 387) N-hydroxy-3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionamide, 388) 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethylamine, 389) N-[2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethyl]-methanesulfonamide, 390) 2-methyl-4-methylsulfanyl-6-(3-pyridin- 2 -yl-1H-pyrazol-4-yl)-pyrimidine, 391) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-pyridine, 392) 2-[4-(2,3-dihydro-benzofuran-5-yl)-1H-pyrazol-3-yl]-pyridine, 393) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[d]isoxazole, 394) 3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propionitrile, 395) N-{3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propyl} inethanesulfonamide, 396) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-6-methyl-pyridine, 397) [4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-acetonitrile, 398) N- {2-[4-benzo[ 1,3]dioxol-5-yl-3 -(6-methyl-pyridin-2-yl)-pyrazol- 1-yl] -ethyl} inethanesulfonamide, 399) 4-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-2-methylsulfanyl-pyrimidine, 400) 4-(3-pyridin-2-yl- 1H-pyrazol-4-yl)-2H-phthalazin- 1-one, 148 WO 2006/044509 PCT/US2005/036770 401) 1-[5-(3-pyridin-2-yl-1 H-pyrazol-4-yl)- 2 , 3 -dihydro-indol- 1 -yl]-ethanone, 402) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 403) 3-methyl-6-(3-pyridin-2-y1-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 404) 6-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-4H-benzo[ 1,4]oxazin-3 -one, 405) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoxaline, 406) 3-(4-nitro-benzyl)-6-(3-pyridin-2-yl-1H-pyrazo1-4-yl)-3H-quinazolin-4-one, 407) 5-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 408) 4-methyl-7-(3-pyridin-2-yl-1H-pyrazol-4-yl)- 3 ,4-dihydro-1H-benzo[e][1,4]diazepine 2,5-dione, 409) 2,3-dimethyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 410) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 410a) 1-niethoxy-4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-isoquinoline, 411) 2-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 411 a) 4-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-2H-isoquinolin- 1-one, 412) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-trifluoromethyl-pyridine, 412a) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-vinyl-pyridine, 413) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propenyl-pyridine, 414) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-ethyl-pyridine, 415) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propyl-pyridine, 416) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-cyclopropyl-pyridine, 417) 1-[6-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-pyridin-2-yl]-ethanol, 418) 4-methoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 419) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline, 420) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin- 4 -ylamine, 421) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 422) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrido[1,2-a]pyrimidin-4-one, 423) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol- 4 -yl]-[1,2,4]triazolo[1,5-a]pyridine, 424) 3-methyl-6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3H-quinazolin- 4 -one, 425) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane-1-carboxylic acid, 426) 4-(2- {2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2. 2 . 2 ] octane-1 -carboxylic acid methyl ester, 427) 4-[4--benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl] bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester, 428) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-isopropyl-pyridine, 149 WO 2006/044509 PCT/US2005/036770 429) 2-(4-benzo( 1,3]dioxol-5-yl-5-trifluoromethyl-1H-pyrazol-3 -yl)-6-bromo-pyridine, 430) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridinae, 431) 6-[3-(6-trifluoromethyl-pyridin-2-y1)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 432) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 432a) 6-[3-(6-cyclopropyl-pyridin-2-yl)-lH-pyrazol-4-yl]-3-methyl-3H-quinazolin- 4 -one, 433) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-b]pyridazine, 433a) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline, 434) 6-(4-benzo[1,3]dioxol-5-yl-lH-pyrazol-3-yl)-3-fluoro-2-methyl-pyridine, 435) 7-methoxy-3-methyl-6-( 3 -pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 436) (4-morpholin-4-yl-pheny1)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-amine, 437) 4-isopropoxy-6-( 3 -pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 438) 6-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-quinolin-4-ylamine, 439) {4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} carbamic acid benzyl ester, 440) 4-[4-benzo [1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexylamiae, 441) N-{4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexy methanesulfonarnide, 442) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 443) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 444) 1-tert-butyl-3-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-urea, 445) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]thiadiazole, 446) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]oxadiazole, 447) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-benzooxazole, 448) 4-morpholin-4-yl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 449) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 450) 4-(4-methoxy-phenyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 451) 5-[3-(6-methyl-pyridin-2-y1)-1IH-pyrazol-4-yl]-benzo[1,2,5]thiadiazole, 452) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzothiazole, 453) 3-(3-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 454) 5-methyl-thiophene-2-carboxylic acid [6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-quinazolin-4 yl]-amide, 455) 5-[3-(6-methyl-pyridin-2-yl)-IH-pyrazol- 4 -yl]-3-phenyl-benzo[c]isoxazole, 456) 3-(4-methoxy-phenyl)-5-(3-pyridin-2-yl-IH-pyrazol-4-yl)-benzo[c]isoxazole, 457) 3-(4-chloro-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 458) 3-(4-ethyl-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-y1)-benzo[c]isoxazole, 150 WO 2006/044509 PCT/US2005/036770 4595 (4-methoiy:eniyl)-[ 6-(1-gyidih-2-yl-1H-pyrazol-4-yl)-quinazolin- 4 -yl]-methanone, 460) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3-thiophen-3-yl-benzo[c]isoxazole, 461) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid, 462) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid methylamide, 463) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid dimethylamide, 464) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid (2,2-dimethyl propyl)-amide, 465) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid phenylamide, 466) morpholin-4-yl-[5-(3-pyridin-2-yl-IH-pyrazol-4-yl)-1H-indazol-3-yl]-methanone, 467) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid benzylamide, 468) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid cyclopentylamide; 469) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-IH-imidazol-2-yl] benzamide; 470) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzonitrile; 471) 4-[5-(2-methanesulfonyl-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester; 472) 4-[5-(2-methoxy-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid methyl ester; 473) 4-[5-(2-hydroxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 474) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 475) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo[2.2.2] octane-1 -carboxylic acid; 476) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid aide; 477) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 478) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo[2.2.2] octane-i -carboxylic acid methoxy-amide; 479) 4-[5-(2-amino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 480) {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 151 WO 2006/044509 PCT/US2005/036770 481) 4"4-[5-(2-cyclo0ropyino-p midin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-acetamide; 482) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 483) N- {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 484) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-l-ol; 485) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-IH-imidazol-2-yll bicyclo[2.2.2]octan-l-ol; 486) 6-[2-tert-butyl-5-(2-cyclopropyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 487) 6-[5-(2-byclopropyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 488) {4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl} -methanol; 489) 6-[5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 490) 6-[2-tert-butyl-5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 491) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 492) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 493) 6-[5-(2-cyclopropyl-pyrimidin-4-yl)-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol 4-yl]-quinoxaline; 494) 4-[5-(2-methyl-pyrimidin-4-yl)-4-[1,2,4]triazolo[4,3-a]pyridin- 6 -yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 495) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 496) 4-[4-(2-methyl-pyrimidin-4-y1)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 497) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2] octane- I -carboxylic acid methyl ester; 498) 4-[4-(2-methyl-pyrimidin- 4 -yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexanol, 499) 4-[4-(2-methyl-pyrimidin- 4 -yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo(2.2.2]octan-1-ol, 500) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-methyl-pyrimidine, 500a) 6-[3-(2-methyl-pyrimidin- 4 -yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 152 WO 2006/044509 PCT/US2005/036770 501j 6,3-(2-trifluoromethyn-pyrimidln-4-yl)-lH-pyrazol-4-yll-[1,2,4]triazolo[1,5-a]pyridine, 502) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 502a) 6-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 503) 6-[3-(2-cyclopropyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 504) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-trifluoromethyl-pyrimidine, 505) 7-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1IH-pyrazol- 4 -yl]-[1,2,4]triazolo[1,5-a]pyridine, or 506) 6-[3-(2-Trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoline.

21. The method of claim 13, wherein the inhibitor is administered locally.

22. The method of claim 13, wherein the inhibitor is administered via an implantable device.

23. The method of claim 22, wherein the device is a delivery pump.

24. The method of claim 22, wherein the device is a stent.

25. An implantable device comprising an inhibitor of TGFb type I receptor or Alk4.

26. The device of claim 25, wherein the inhibitor has the structure shown in formula I: RI-a IN N N A1 R X- 1 -Y 1 -R1 - 2 () or an N-oxide or a pharmaceutically acceptable salt thereof, wherein R" is aryl, heteroaryl, aralkyl, or heteroaralkyl; each R!- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; XI is cycloalkyl or heterocycloalkyl; 153 WO 2006/044509 PCT/US2005/036770 Y1is bond,-C(O)-,-C(O)-O-, -O-C(O)-, -S(0),-O-, -O-S(O),-, -C(O)-N(R)-, -N(RE)-C(O)-, -O-C(O)-N(R')-, -N(RE)-C(O)-O-, -O-S(0),-N(Rk)-, -N(R)- S(0),-O-, -N(RE)-C(O)-N(R4)-, -N(RE)-S(0),-N(R)-, -C(O)-N(RE)-S(O)p-, -S(O)p-N(RE)-C(O)-, -C(O)-N(R)-S(O),-N(R )-, -C(0)-O-S(O)p-N(RE)-, -N(RE)-S(0)p-N(Rc)-C(O)-, -N(R)-S(O),-O-C(O)-, -S(0)p-N(Rb)-, -N(Rb)-S(O)p-, -N(R)-, -S(O)p-, -0-, -S-, or -(C(Rb)(RC))q-, wherein each of Rb and R is independently hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; p is 1 or 2; and q is 1-4; R 2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A'-' and A' , independently, is 0, S, N, or NRb, provided that at least one of A 14 and A 12 is N; and m is 0, 1, 2, or 3, provided that when m 2, two adjacent R groups can optionally together to form a 4- to 8-membered optionally substituted cyclic moiety.

27. The device of claim 25, wherein the inhibitor has the structure shown in formula II: Y 1 1-2 T(R -)n 11 -' XII-1(RII-1m 1 3 1 N N XII- 4 or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each of Xr.. 1 , Xr- 2 , X 1 - 3 , and XII-4 is independently CRX or N, provided that no more than two of XI-1, Xr.. 2 , Xr- 3 , and Xu. 4 can be N simultaneously; each of Y 1 1 - 1 and Yr-2 is independently CRY or N, provided that at least one of Yu.. 1 and Yr.. 2 must be N; each R!~- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, 154 WO 2006/044509 PCT/US2005/036770 heteodcloallysIlfaii , ifI'ylrIoy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each R1 2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cycloalkyl), -NH(heterocycloalkyl), NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterc'aryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsilfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfirnyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamilo, alkoxycarbonylaminoalkylamnino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylamninoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkyl amino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m >_2, two adjacent Ri groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n >_2, two adjacent R 2 groups can optionally join tc>gether to form a 4- to 8-membered optionally substituted cyclic moiety; and each of Rx and RY is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbomyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino; cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonyla-nino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylalmino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfarnoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, 155 WO 2006/044509 PCT/US2005/036770 (cycloAikiljalkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl.

28.. The device of claim 25, wherein the inhibitor has the structure shown in formula III YmI-2 (R112)n (III) 2N (R"- ) X 1 3 - N N XmI- 4 or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each of Xm 111 , X1-2, XIm.3, and Xm 1 - 4 is independently CRm" or N, provided that only two of XII, Xm.2, Xm 3, and X 1 1 1 .. 4 can be N simultaneously; each of Ym 1 14 and Ym-2 is independently CRm'-Y or N, provided that at least one of Ym 111 and Ym 1 - 2 must be N; each Rl" is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each Rm- is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl)2, -NH(cycloalkyl), -N(alkyl)(cyclocalkyl), NH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl-heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, (cycloalkyl)alkoxy, aryloxy, arylalkoxy, 156 WO 2006/044509 PCT/US2005/036770 hetVr'oyl6akllyTbxy,(lietroCycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl(alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m ;--2, two adjacent R 1 - groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n >2, two adjacent R r-2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of Ru 11 x and R"I-Y is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl.

29. The device of claim 25, wherein the inhibitor has the structure shown in formula IV 157 WO 2006/044509 PCT/US2005/036770 Riv-5 RI -6 N'RI v-RIv 2 -RIv- 3 -RIV-4 N (IV) (RIV-a)m or an N-oxide or a pharmaceutically acceptable salt thereo, f, wherein each R- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsuilfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; R'~ 1 is a bond, alkylene, alkenylene, alkynylene, cr -(CH 2 )r1-O-(CH2)r2-, wherein each of r1 and r2 is independently 2 or 3; R -2 is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, or a bond; RW~ 3 is -C(O)-, -C(O)O-, -OC(O)-, -C(O)-N(Rw-)-, -N(R7-b)-C(O)-, -O-C(O)-N(Rv b)-, -N(R V-b)-C(0)-0-, -O-S(O)p-N(RW ~6)-, -N(Re-b)- S(O)p-O-, -N(Rv -b)-C(O)-N(R-c~-, -N(R v-)-S(O)p-N(R' ~6)-, -C(O)-N(ReV-b)-S(0)p-, -S(0)p-N(R7-)-C(O)-, -S(0),-N(R v-b)_ -N(Rwb)-S(O),-, -N(Rwv~b)-, -S(O)p-, -0-, -S-, or -(C(RI-b)(R C))q-, or a bond; wherein each of RWvb and RI'" is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; and p is 1 or 2 and q is 1-4; Rv4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralcyl, heteroaryl, or heteroaralkyl; R'~5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoxy, cycloalikylsulfinyl, heterocycloalkyl, 158 WO 2006/044509 PCT/US2005/036770 hefero"ybl6alk65EY,"heterocycloalkylsulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryloxy, or heteroarylsulfinyl; R- 6 is (1) a 5- to 6-membered heterocyclyl containing 1-3 hetero ring atorins selected from the group consisting of -O-, -S-, -N=, and -NRIVd-, wherein RWv~d is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; said heterocyclyl being substituted with Rw~* and optionally substituted with one to two R"' 4 ; wherein R'* is oxo, thioxo, alkoxy, alkylsulfinyl, -NH 2 , -NH(unsubstituted alkyl), or -N(unsubstituted alkyl)2, and R~f is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or (2) a fused ring heteroaryl selected from the group consisting of: (Ri)n (RI)n (In(R~ B' B X1 B' 2 2X X2 X 1 XX2, x 2 LIZ (2 .1 j o Iand% wherein ring A is an aromatic ring containing 0-4 hetero ring atoms and ring B is a 5- to 7 membered aromatic or nonaromatic ring containing 0-4 hetero ring atoms, provided that at least one of ring A and ring B contains one or more hetero ring atoms; ring A' is an aromatic ring containing 0-4 hetero ring atoms and ring B' is a 5- to 7-membered saturated or unsaturated ring containing 0-4 hetero ring atoms, provided that at least one of ring A' and ring B' contains one or more hetero ring atoms; each hetero ring atom is -0-, -S-, -N=, or NRe-g ; each X 1 is independently N or C; each X 2 is independently -0-, -S-, -N==, -NR-~E , or -CHRIV-h-; where Rv~8 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; each of R' ~" and R'' is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcagbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, 159 WO 2006/044509 PCT/US2005/036770 cyoailkyIf, cyai lkylexfcycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and n is 0-2; and m is 0-3, and when m ;>2, two adjacent RwVa groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; provided that if R- 6 is 2-naphthyridinyl, 4-quinolinyl, imidazo[1,2-a]pyridyl, or benzimidazolyl, then -R N-RI-2_- --RN 4 is not H, unsubstituted alkyl, -CH 2 -C(O)-N(H)-alkyL, -CH 2 -C(O)-N(alkyl)2, or benzyl.

30. The device of claim 25, wherein the inhibitor has the structure shown in formula V (Rva)m N N(V AV- 2 Xy-Yv--Rv-2 Rv 1 Av or an N-oxide or a pharmaceutically acceptable salt thereof, wherein Rv is heteroaryl; each Rva, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; X, is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or a bond; Yv is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O),-O-, -O-S(O),-, -C(O)-N(Rb)-, -N(RE)-C(O)-, -O-C(O)-N(R)-, -N(RE)-C(O)-0-, -C(O)-N(RE)-O-, -O-N(R)-C(O)-, -O-S(O),-N(R)-, -N(R)- S(O),-O-, -S(O)p-N(Re)-O-, -0-N(R)-S(O)p-, -N(R)-C(O)-N(RC)-, -N(R)-S(O)p-N(RC)-, -C(O)-N(R)-S(O)p-, -S(O)p-N(Rb)-C(O)-, -C(O)-N(Rb)-S(O)p-N(R)-, 160 WO 2006/044509 PCT/US2005/036770 -CtO"d S'(diNI1- ,'-N'(I" 1-S(tdp-N(Rc)-C(O)-, -N(RE)-S(O)p-0-C(O)-, -S(O),-N(R)-, -N(Re)-S(O),-, -N(Rb)-, -S(O),-, -0-, -S-, or -(C(R)(R))q-, wherein each of Rb and R, independently, is hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; p is 1 or 2 and q is 1-4; Rw 2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A - and AV 2 , independently, is N or NRb; and m is 0, 1, 2, or 3, and when m 2, two adjacent R V-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety, provided that if X, is a bond, then Yv is a bond; RV- 2 is hydrogen or alkyl; m is 1, 2, or 3; and at least one RVa is substituted at the 2-pyrimidinyl position.

31. The device of claim 25, wherein the inhibitor has the structure shown in formula VI: RvI-5 RI-6 N -Rvl--RvI-2 -RvI-3 -RvI 4 (VI) N N (RvI-a)m or an N-oxide or a pharmaceutically acceptable salt thereof, wherein each RVI-a, independently, is alkyl, alkenyl, alkynyl, alkoxy, ac-yl, halo, hydroxy, NH 2 , -NH(unsubstituted alkyl), -N(unsubstituted alkyl)2, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkcoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cyrcloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloallcyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylearbonyl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; 161 WO 2006/044509 PCT/US2005/036770 kv' i' ii1 ond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri -0(CH 2 )r 2 -, where each of r1 and r2, independently, is 2 or 3; Re-2 is cycloalkylene, heterocycloalkylene, cycloalkenylene, heterocycloalkerylene, arylene, heteroarylene, or a bond; RVI 3 is -C(O)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(R)-, -N(RE)-C(O)-, -O-C(O)-N(RE)-, -N(RE)-C(O)-0-, -C(O)-N(R)-O-, -O-N(R)-C(0)-, -O-S(O)p-N(R)-b -N(RE)- S(O),-0-, -S(O)p-N(Rb)-O-, -O-N(RE)-S(O)p-, -N(R)-C(O)-N(Rc) -N(RE)-S(O),-N(RW)-, -C(O)-N(RE)-S(0),-, -S(O)p-N(RE)-C(O)-, -C(O)-N(RE)-S(O),-N(Rch -C(O)-0-S(O),-N(Rb)-, -N(RE)-S(0),-N(R4)-C(O)-, -N(Rb)-S(O)p-O-C(O)-, -S(0),-N(Rkb) -N(R)-S(O),-, -N(R)-, -S(O),-, -0-, -S-, -(C(Rb)(RC))q-, or a bond; wherein each of R and Re is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; and p is 1 or 2 and q is 1-4; RV 1 - 4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkIyl; RV- 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryloxy, arylsulfinyl, heteroaryloxy, or heteroarylsulfinyl; Rv-6 is a 5- to 6-membered monocyclic heterocyclyl or a 8- to 11 -membered bicyclic heteroaryl; each being optionally substituted with alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and m is 0-3, and when m >2, two adjacent R VIa groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

32. The device of claim 25, wherein the inhibitor is 1) 4-(4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-lH-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 162 WO 2006/044509 PCT/US2005/036770 2) f-(4hi z"o ii';' 1ol -yl-5-byridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 3) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 4) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 5) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 6) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 7) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 8) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 9) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 10) 2-[5-Benzo[1,3]dioxol-5-yl-2-(I-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 11) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-y)-3H-imidazol-4 yl]-pyridine; 12) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 13) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 14) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzyl ester; 15) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2,4-dichloro-benzylamide; 16) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-l-yl] ethanone; 17) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-furan-2-yl-methyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 18) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 19) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylamine; 163 WO 2006/044509 PCT/US2005/036770 20fl{4-[4dizL[T,3]dioxoi-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-phenyl-methanesulfonamide; 21) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 22) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 23) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]oct- 1-yl} -carbamic acid benzyl ester; 24) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-ethyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 25) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-pyridine; 26) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-nitro-benzyl ester; 27) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4,5-dimethoxy-2-nitro-benzyl ester; 28) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 3-fluoro-benzylamide; 29) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-fluoro-benzylamide; 30) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzylamide; 31) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 32) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methyl-benzylamide; 33) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methoxy-benzylamide; 34) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzylamide; 35) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzoic acid; 36) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid amide; 37) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzonitrile; 164 WO 2006/044509 PCT/US2005/036770 3 82L"{5"Betiif ','D*iox6I-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 39) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 40) {5-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] naphthalen-1-yl}-dimethyl-amine; 41) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methyl)-piperidin-4-yl)]-3H-imidazol-4 yl}-pyridine; 42) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 43) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 44) 1-{4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonyl]-phenyl}-ethanone; 45) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methyl-benzyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 46) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-fluoro-5-trifluoromethyl-benzyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 47) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-cyclohexylmethyl-piperidin-4-yl)-3H-imidazol-4-y] pyridine; 48) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-ylmethyl] cyclopropanecarboxylic acid ethyl ester; 49) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-ylmethyl] pyrrolidine-1-carboxylic acid tert-butyl ester; 50) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-piperidin-4 yl]-3H-imidazol-4-yl}-pyridine; 51) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 52) 2- {5-Benzo[1,3]dioxol-5-yl-2-[ 1 -(butane-i -sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 53) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 54) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 165 WO 2006/044509 PCT/US2005/036770 55)2 {5)-Ber'zd[1 '3dioxo1-5-yl-2-[1-(propane-1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 56) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonylmethyl]-7,7-dimethyl-bicyclo[2.2.1 ]heptan-2-one; 57) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-pyridine; 58) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 59) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-fluoro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-pyridine; 60) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-pyridine; 61) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H-imidazol 4-yl}-pyridine; 62) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-p-tolylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-pyridine; 63) 3-(4-Benzo[1,3]dioxol-5-yl-l-hydroxy-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 64) 3-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 65) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 66) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 67) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-1-yl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 68) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-pyridine; 69) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 70) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 71) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 166 WO 2006/044509 PCT/US2005/036770 72) Z{5"-Beriidf '3Jdiox1-5-yl-2- [1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 73) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] pyrrolidine-1-carboxylic acid benzyl ester; 74) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 75) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-bis-trifluoromethyl-phenylmethanesulfonyl) piperidin-4-yl]-3H-imidazol-4-yl}-pyridine; 76) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 77) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 78) 2-{5-Benzo[1,3]dioxol-5-yl-2-( 1 -(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 79) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 80) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 81) 4-[5-Benzo[1,3]dioxol-5-yl-1-methyl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 82) 4-[4-Benzo[1,3]dioxol-5-yl-1-rnethyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 83) {4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl}-carbamic acid benzyl ester; 84) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-phenoxy-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 85) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 86) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[ 1 -(propane-1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 87) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1 -(butane-i -sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} 6-methyl-pyridine; 88) 2-{5-Benzo[1,3]dioxol-5-yl-2-[ 1-(pyridin-3-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 167 WO 2006/044509 PCT/US2005/036770 895YL{5 neAM if1,jix5fl- 1j-y-[Y-(pyridin-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 90) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 91) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 92) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 93) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[ 1 -(butane-i -sulfonyQ)-piperidin-3 -yl]-3H-imidazol-4-yl} 6-methyl-pyridine; 94) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulf-onyl-piperidin-3-yl)-3H-imidazol-4 yl]-6-methyl-pyridine; 95) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-iH-imidazole-4-sulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 96) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-isoxazole-4-sulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 97) 4-[5-Benzo[1,3]dioxol-5-yl-l-hydroxy-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 98) Butane-i -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl--5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl}-amide; 99) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-pyridin-2-yl-methanesulfonamide; 100) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl}-amide; 101) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl}-amide; 102) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid amide; 103) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid methyl ester; 104) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-bromo-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 105) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-3-sulfonyl)-piperidin-4-y]-3H-imidazol-4 yl} -6-methyl-pyridine; 168 WO 2006/044509 PCT/US2005/036770 105)12-f{5B6i 6[T,3]dioxol-5-yl-2- [1-(5-methyl-2-trifluoromethyl-furan-3 -sulfonyl) piperidin-4-yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 107) 4-[2-(1-phenylmethanesulfonyl-piperidin-4-yl)-5-(6-methyl-pyridin-2-yl)-1H-imidazol 4-yl]-pyridin-2-yl-fluoride; 108) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-trifluoromethyl-pyridin-2-yl)- 1H-imidazol-2-yl] piperidine- I -carboxylic acid benzyl ester; 109) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-bromo-pyridin-2-yl)-1-hydroxy-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 110) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-bromo-pyridine; 111) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl} -methanol; 112) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid amide; 113) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-2H-imidazol-2-yl]-piperidine-1 sulfonic acid dimethylamide; 114) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-irnidazol-2-yl]-piperidin 1 -yl}-3-phenyl-propan-1-one; 115) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidiri-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 116) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carbonitrile; 117) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1 -ylamine; 118) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-phenyl-methanesulfonamide; 119) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 120) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-y)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-pyridin-2-yl-methanesulfonamide; 121) 2-{5-Benzo[1,3]dioxol-5-yl-2-[4-(1H-tetrazol-5-yl)-bicyclo[2.2-2]oct-1-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 122) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-y)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide; 169 WO 2006/044509 PCT/US2005/036770 12 Thflfn f ia {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 124) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 125) Thiophene-3-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 126) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 127) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 128) Methanesulfonic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-ylmethyl ester; 129) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetonitrile; 130) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]oct-1 -yl} -acetic acid; 131) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-methanesulfonamide; 132) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 133) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 134) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 135) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-phenyl-methanesulfonamide; 136) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylmethyl}-C-pyridin-2-yl-methanesulfonamide; 137) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid benzylamide; 138) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (pyridin-2-ylmethyl)-amide; 139) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid 3-chloro-4-fluoro-benzylamide; 170 WO 2006/044509 PCT/US2005/036770 140) [4 -Bei t,"3]dioi 1-yl-5-( 6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (furan-2-ylmethyl)-amide; 141) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-pyrrolidin-3-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 142) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1 -(butane-i -sulfonyl)-pyrrolidin-3-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 143) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-1H-imidazole-4-sulfonyl)-pyrrolidin-3-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 144) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-pyrrolidin-3-yl)-3H-imidazol 4-yl]-6-methyl-pyridine; 145) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-pyrrolidin-3-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 146) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 147) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-2-yl-ethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 148) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1-sulfonylmethyl}-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 149) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 150) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methylamide; 151) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid ethylamide; 152) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid butylamide; 153) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid isopropylamide; 154) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (3-imidazol-1-yl-propyl)-amide; 155) 2-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1 -sulfonylmethyl} -phenylamine; 156) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (1-methyl-5-methylsulfanyl-1H-[1,2,4]triazol-3-yl) amide; 171 WO 2006/044509 PCT/US2005/036770 15 7) "4L[ 1ei"5T t3]'}ioi'-5yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid cyclohexylamide; 158) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-pyrrolidin-1-yl-methanone; 159) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid dimethylamide; 160) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid diethylamide; 161) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid dipropylamide; 162) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (5,7-difluoro-benzothiazol-2-yl)-arnide; 163) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid benzothiazol-2-ylamide; 164) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (1H-benzoimidazol-2-yl)-amide; 165) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid (2-hydroxy-1-methyl-2-phenyl-etliyl)-amide; 166) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid (pyridin-4-ylmethyl)-amide; 167) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl}-(3-chloro-phenyl)-methanone; 168) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl} -(4-fluoro-phenyl)-methanone; 169) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin-1 yl}-(4-methoxy-phenyl)-methanone; 170) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-cyclopropyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 171) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid methoxy-amide; 172) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 173) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-carbamic acid benzyl ester; 172 WO 2006/044509 PCT/US2005/036770 1 4)" 4"did6[Tjdoxofi-yl -5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid hydrazide; 175) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-iH-imidazol-2-yl] cyclohexylmethyl}-acetamide; 176) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-methanesulfonamide; 177) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-phenyl-methanesulfonamide; 178) Butane-i -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl}-amide; 179) Propane-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl} -amide; 180) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-2-yl-methanesulfonamide; 181) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-pyridin-4-yl-methanesulfonamide; 182) (4-Methoxy-benzyl)-{4-[5-(6-methyl-pyridin-2-yl)-2-(1-phenylmethanesulfonyl piperidin-4-yl)-1H-imidazol-4-yl]-pyridin-2-yl}-amine; 183) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 184) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 185) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 186) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 187) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid amide; 188) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid; 189) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 190) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 173 WO 2006/044509 PCT/US2005/036770 1 r)4'-[6,- [p6 6.ynyridin-2yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo [2.2.2] octane-1 -carboxylic acid amide; 192) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 193) N-{4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-y1}-sulfamide; 194) Sulfamic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl ester; 195) {4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 196) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carbonyl} -methanesulfonamide; 197) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carbonyl} -benzenesulfonamide; 198) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-y)-4-(6-methyl-pyridin-2-yl)-IH imidazol-2-yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 199) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane-1 -carboxylic acid; 200) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} acetamide; 201) 4-[4-(6-Methyl-pyridin-2-y)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-bicyclo[2.2.2]octane 1 -carboxylic acid methyl ester; 202) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-bicyclo[2.2.2] octane 1-carboxylic acid; 203) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1H-imidazol-2-yl]-bicyclo [2.2.2] octane 1-carboxylic acid hydroxyamide; 204) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- IH-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid aide; 205) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexy} methanesulfonamide; 206) 2,2,2-Trifluoro-N-{4-[4-(6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] cyclohexyl} -acetamide; 207) 4-[4-(5-Fluoro-6-methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol 2-yl] -bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester; 174 WO 2006/044509 PCT/US2005/036770 208)'f4-"2-[(9dtfie ll-s ulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)- 1H-imidazol-4 yl]-pyridin-2-yl} -(4-methoxy-benzyl)-amine; 209) 4-[2-[ 1 -(Butane-i -sulfony1)-piperidin-4-yl]-5-(6-methyl-pyridin-2-yl)-1 H-imidazol-4 yl]-pyridin-2-ylamine; 210) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-ethyl-pyridine; 211) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl] -bicyclo[2.2.2] octane-i -carboxylic acid amide; 212) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl] -bicyclo[2.2.2] octane-i -carboxylic acid hydroxyamide; 213) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 214) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide. 215) 4-[2-(6-Methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 216) 4-(2-pyridin-2-yl-pyrazolo[1,5-a]pyridin-3-yl)-pyrimidin-2-ylamine; 217) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 218) 2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-pyrazolo[1,5-a]pyridine; 219) 4-[2-(6-chloro-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 220) 2-(6-methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-pyrazolo[1,5 c]pyrimidine; 221) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrazin-3-yl]-pyrimidin-2-ylamine; 222) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrimidin-3-yl]-pyrimidin-2-ylamine; 223) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 224) (2-Methoxy-ethyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 225) (3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} propyl)-carbamic acid tert-butyl ester; 226) (3-Imidazol-1-yl-propyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 227) (4-Methoxy-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 228) [2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridin 6-yl]-methanol; 175 WO 2006/044509 PCT/US2005/036770 229)"3 -(2-M6thanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 230) (4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-ylamino} butyl)-carbamic acid tert-butyl ester; 231) (4-Amino-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} - amine; 232) (5- {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} pentyl)-carbamic acid tert-butyl ester; 233) [3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-6-yl] methanol; 234) [3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-7-yl] methanol; 235) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-morpholin-4-yl-ethyl)-amine; 236) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-2-yl-ethyl)-amine; 237) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl-(2-pyridin-3-yl-ethyl)-amine; 238) [3-(2-methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-6-yl] -methanol; 239) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-4-yl-ethyl)-amine; 240) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(3-morpholin-4-yl-propyl)-amine; 241) [3-(4-Methyl-piperazin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3-yl]-pyrimidin-2-yl}-amine; 244) [3-(4-Methyl-piperidin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3-yl]-pyrimidin-2-yl}-amine; 245) [4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-yl]-pyridin-3-ylmethyl amine; 246) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-((R)-1 phenyl-ethyl)-arriine; 247) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-((S)-1 phenyl-ethyl)-aniine; 176 WO 2006/044509 PCT/US2005/036770 248)"{'4-[1-(M9ft-hyl-byldin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} -(1H tetrazol-5-yl)-amine; 249) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2H pyrazol-3-yl)-amine; 250) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2 morpholin-4-yl-ethyl)-amine; 251) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 2-yl-ethyl)-amine; 252) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 3-yl-ethyl)-amine; 253) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 4-yl-ethyl)-amine; 254) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 morpholin-4-yl-propyl)-amine; 255) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 piperidin-1-yl-propyl)-amine; 256) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} [1,3,4]thiadiazol-2-yl-amine; 257) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 258) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 6-carboxylic acid methyl ester; 259) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 7-carboxylic acid ethyl ester; 260) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2 a]pyrimidin-7-ylamine; 261) {7,7-Dimethyl-8-[5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-pentyl]-2-oxo-4-trifluoromethyl-7,8-dihydro-2H-1 oxa-8-aza-anthracen-5-yl}-methanesulfonic acid; 262) 2-(2,7-Difluoro-6-hydroxy-3-oxo-9,9a-dihydro-3H-xanthen-9-yl)-3,5,6-trifluoro-4-[(4 {4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butylcarbamoyl)-methylsulfanyl]-benzoic acid; 263) -(6-Methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 264) 2-(6-Methyl-pyridin-2-yl)-3-(2-piperidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 265) 2-(6-Methyl-pyridin-2-yl)-3-(2-pyrrolidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 177 WO 2006/044509 PCT/US2005/036770 266)f2-(6tl~VItfiy 4 pyidini-yi)-3-[2-( 1 H-tetrazol-5-yl)-pyrimidin-4-yl]-imidazo [1,2 a]pyridine; 267) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyridine; 268) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyrimidin-7-ylamine; 269) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-8 ylamine; 270) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonitrile; 271) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid; 272) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 273) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 274) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-dimethylamino-ethyl)-amide; 275) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-methoxy-ethyl)-amide; 276) 3-(2-Anino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 277) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide; 278) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid amide; 279) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid cyclopropylamide; 280) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ethylamide; 281) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid hydroxyamide; 282) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methoxy-amide; 283) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methyl ester; 178 WO 2006/044509 PCT/US2005/036770 284)'3-(2 Aifih6-'iryinidhi4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid; 285) 3-(2-Anino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 286) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-amino-ethyl)-amide; 287) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-dimethylamino-ethyl)-amide; 288) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-hydroxy-ethyl)-amide; 289) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-oxo-2-pyridin-3-yl-ethyl)-amide; 290) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 291) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (piperidin-3-ylnethyl)-amide; 292) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid 2,2-dimethylhydrazide; 293) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid amide; 294) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-inidazo[1,2-a]pyridine-7 carboxylic acid cyclopropylamide; 295) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethyl ester; 296) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethylamide; 297) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid hydroxyamide; 298) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid methoxy-amide; 299) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 ylamine; 300) 3-(2-Azetidin-1-yl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine; 301) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo [1,2-a] pyridine-7-carboxylic acid ethyl ester; 179 WO 2006/044509 PCT/US2005/036770 302)"3"-(2-MefliAhes iilfoy-'yfimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carboxylic acid methyl ester; 303) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-7-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[I ,2 a] pyridine; 304) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-8-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1 ,2 a] pyridine; 305) 3,3-Dimethyl-N-[2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl) imidazo[1,2-a]pyrimidin-7-yl]-butyramide; 306) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carbonitrile; 307) 3-(2-Methylsulfanyl-pyrimidin-4-yl)-2-pyridin-2-yl-imidazo[1,2-a]pyridine; 308) 3,6-Dichloro-N-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino} -butyl)-2-(2,4,5,7-Tetrachloro-6-hydroxy-3-oxo-9,9a-dihydro-3H xanthen-9-yl)-terephthalamic acid; 309) 3-[2-(2-Methyl-aziridin-1-yl)-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2- a] pyridine; 310) 3-[2-(4-Methyl-piperazin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 311) 3- { [3 -(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo [1,2-a]pyridine-6 carbonyl]-amino} -propionic acid methyl ester; 312) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl]-amino} -propionic acid methyl ester; 313) 3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} phenol; 314) 4-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}- ethyl)-benzenesulfonamide; 315) 4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-ylamine; 316) 4-[2-(6-Chloro-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 317) 4-[2-(6-Methyl-pyridin-2-yl)-7-trifluoromethyl-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl-amine; 318) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 319) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbonitrile; 320) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carboxylic acid amide; 180 WO 2006/044509 PCT/US2005/036770 32't) '4-'6!L bl bf6-2"-(6-"mdtli34yriydin-2-y1)-imidazo[l1,2-a]pyridii-3 -yl] -pyrimidin-2 ylamnine; 322) 4-[6-Chloro-2-(6-methyl-pyridin-2-yD)-imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2 ylamine; 323) 4-[6-Fluoro-2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridiri-3 -yl] -pyrimidin-2 ylamine; 324) 4-6Mty--6mty-yrdn2y)8(-opoi-4y tyann)iiao1,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 325) 4-6Mty--6mthlprdn2y 1-2prdn2y-ttyaio-mdz~,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 326) 4-6Mty--6mthlprdn2y 1-2prdn3y-tlyaio-mdz~,2-a] pyridin-3 -yl] -pyrimidin-2-ol; 327) 4-6Mty--6mty-yii--l-8(-yii- lehliio-mdz[1,2-a] pyridin-3 -yl] -pyrimidin-2-ol; 328) 4-[6-Methy1-2-(6-methy1-pyridin-2-y1)-8-morpholifl-4-yl-fltlidazo[1I,2-a]pyridin-3-yl] pyrirnidin-2-ol; 329) 4-[6-Methy1-2-(6-methy-pyridin-2-y)-8-morphoi-4-y-i21idazo [1 ,2-a]pyridin-3-yl] pyrimidin-2-ylamine; 330) 4-[6-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyridin-3-yl] -pyrimidin-2 ylamine; 331) 4-[7-Aminomethyl-2-(6-methyl-pyridil-2-y)-imidazoI[l,2-aL]pyridini-3-yl]-pyrimidin-2 yl-amine; 332) 4-[7-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo [1 ,2-a]pyriclin-3-yl] -pyrimidin-2 ylamine; 333) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-y)-inidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2-ol; 334) 4-[8-Benzyloxy-2-(6-methyl-pyridin-2-y)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2-yl amine; 335) 4-[8-Bromo-6-methyl-2-(6-methyl-pyridin-2-y)-imidazo[ 1, 2-a]pyridin-3-yl] -pyrimidin 2-ol; 336) 4-[8-Methyl-2-(6-methyl-pyridin-2-yl)-imidazo[ I,2-alpyriclin-3 -yl]-pyrimidin-2 ylamine; 337) 6-Chloro-3 -(2-methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyfldi-2-Y1)-imidazo [1,2 a] pyridine; 338) 5-Dimethylamino-naphthalene-l1-sulfonic acid (4- {4-[2-(6-rnethyl-pyridin-2-yl) imidazo [1 ,2-a]pyridin-3-yl] -pyrimidin-2-ylamino }-butyl)-amide; 181 WO 2006/044509 PCT/US2005/036770 31f9j 6-(2,7-dbjfid5r6'y6-fiG y-3-oxo-3H-xanthen-9-yl)-N-(4-{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-isophthalamic acid; 340) 6-Amino-9-[2-carboxy-5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino} -butylcarbamoyl)-phenyl]-xanthen-3-ylidene-ammonium; 341) 6-Bromo-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-irmidazo[1,2-a] pyridine; 342) 6-Fluoro-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-inidazo[1,2-a] pyridine; 343) 7-Amino-4-methyl-3-[(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-methyl]-2-oxo-2H-chromene-6-sulfonic acid; 344) Cyclobutyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrirnidin-2-yl} amine; 345) Cyclopentyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl}-amine; 346) Cyclopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 yl}-amine; 347) Cyclopropyl-methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 348) Dimethyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyriniidin-2-yl} amine; 349) Isopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyriniidin-2-yl- amine; 350) Methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 350a) N-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamino}-ethyl)-acetamide; 351) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-acetamide; 352) N,N-Dimethyl-N'-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl}-ethane-1,2-diamine; 353) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidaz [1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 354) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 182 WO 2006/044509 PCT/US2005/036770 35'5)"N-[2-(6 Metifl -pyridiii-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 356) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-methanesulfonamide; 357) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine- 7 carbonyl]-methanesulfonamide; 358) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidiri-7 yl]-2-(3-methoxy-phenyl)-acetamide; 359) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidirn-7 yl]-3,3-dimethyl-butyramide; 360) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidir-7 yl]-3-pyridin-3-yl-propionamide; 361) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidiri-7 yl]-acetamide; 362) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-nicotinamide; 363) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-2-(3-methoxy-phenyl)-acetamide; 364) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3,3-dimethyl-butyramide; 365) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 366) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 367) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-al pyrimidin-7-yl]-propionamide; 368) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin.-7 yl]-propionamide; 369) N-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide; 370) Ni - {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} -butane 1,4-diamine; 371) NI - {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin-2-yl} propane-1,3-diamine; 183 WO 2006/044509 PCT/US2005/036770 372)"N-'(4- {4[2"-(6:Mtliy1-pyndm-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(BODIPY FL) amide; and 373) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-alpyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(Texas Red-X) amide 374) N-[3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-acetamide; 375) N-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide. 376) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propylamine, 377) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-acetamide, 378) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-methanesulfonamide, 379) dimethyl-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-amine, 380) 4-{3-pyridin-2-yl-1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-pyrazol-4-yl}-quinoline, 381) 4-[3-pyridin-2-yl-1-(3-pyrrolidin-1-yl-propyl)-1H-pyrazol-4-yl]-quinoline, 382) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, 383) 2,4-dimethoxy-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 384) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionic acid, 385) 5-(3-pyridin-2-yl-IH-pyrazol- 4 -yl)-IH-indole, 386) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-pyridine, 387) N-hydroxy-3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionamide, 388) 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethylamine, 389) N-[2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethyl]-methanesulfonamide, 390) 2-methyl-4-methylsulfanyl-6-(3-pyridin- 2 -yl-1H-pyrazol-4-yl)-pyrimidine, 391) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-pyridine, 392) 2-[4-(2,3-dihydro-benzofuran-5-yl)-1H-pyrazol-3-yl]-pyridine, 393) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[d]isoxazole, 394) 3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propionitrile, 395) N-{3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propyl} methanesulfonamide, 396) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-6-methyl-pyridine, 397) [4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-acetonitrile, 398) N- {2-[4-benzo [1,3 ]dioxol-5 -yl-3 -(6-methyl-pyridin-2-yl)-pyrazol- 1-yl] -ethyl} methanesulfonamide, 399) 4-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-2-methylsulfanyl-pyrimidine, 400) 4-(3-pyridin-2-yl- 1 H-pyrazol-4-yl)-2H-phthalazin- 1-one, 184 WO 2006/044509 PCT/US2005/036770 4 1rf) f( Ad"fnT-['19Iiyi14-bpyraill'-4-yl)-2,3-dihydro-indol-1-yl]-ethanone, 402) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 403) 3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-ofne, 404) 6-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-4H-benzo[ 1,4]oxazin-3-one, 405) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoxaline, 406) 3-(4-nitro-benzyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quina-zolin-4-one, 407) 5-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 408) 4-methyl-7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3,4-dihydro-1H-benzo[e][1,4]diazepine 2,5-dione, 409) 2,3-dimethyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 410) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 410a) 1-methoxy-4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-isoquinoline, 411) 2-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 411 a) 4-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-2H-isoquinolin- 1-one, 412) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-6-trifluoromethyl-pyridine, 412a) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-vinyl-pyridine, 413) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-6-propenyl-pyridiLe, 414) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-6-ethyl-pyridine, 415) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propyl-pyridine, 416) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-cyclopropyl-pyridine, 417) 1-[6-(4-benzo[ 1,3]dioxol-5-yl- IH-pyrazol-3-yl)-pyridin-2-yl]-ethanol, 418) 4-methoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 419) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline, 420) 6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-quinazolin-4-ylamine, 421) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin- 4 -one, 422) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrido[1,2-a]pyrimidin-4-orie, 423) 6-[3-(6-cyclopropyl-pyridin-2-yl)-lH-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 424) 3-methyl-6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3H-quinazolin-4-one, 425) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane-1-carboxylic acid, 426) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester, 427) 4-[4-benzo(1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1 -yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester, 428) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-isopropyl-pyridine, 185 WO 2006/044509 PCT/US2005/036770 419)"2-(4"-bdii[T,3ldioi6l5- "ylL5-trifluoromethyl-1H-pyrazol-3-yl)-6-bromo-pyridine, 430) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine:, 431) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 432) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 432a) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-methyl-3H-quinazolin-4-one, 433) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-b]pyridazine, 433a) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline, 434) 6-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-3-fluoro-2-methyl-pyridine, 435) 7-methoxy-3 -methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 436) (4-morpholin-4-yl-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-amirme, 437) 4-isopropoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 438) 6-(3-Pyridin-2-yl-IH-pyrazol-4-yl)-quinolin-4-yamine, 439) {4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} carbamic acid benzyl ester, 440) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexylamine, 441) N-{4-[4-benzo [1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} methanesulfonamide, 442) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 443) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 444) 1-tert-butyl-3-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-urea, 445) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]tbiadiazole, 446) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]oxadiazole, 447) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-benzooxazole, 448) 4-morpholin-4-yl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 449) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 450) 4-(4-methoxy-phenyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 451) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-benzo[1,2,5]thiadiazole, 452) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzothiazole, 453) 3-(3-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 454) 5-methyl-thiophene-2-carboxylic acid [6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin.-4 yl]-amide, 455) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-phenyl-benzo[c]isoxazole, 456) 3-(4-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 457) 3-(4-chloro-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 458) 3-(4-ethyl-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 186 WO 2006/044509 PCT/US2005/036770 45 9) :4-Ath yji1)[6(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-methanone, 460) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3-thiophen-3-yl-benzo[c]isoxazole, 461) 5-(3-pyridin-2-yl-1H-pyrazol--4-yl)-1H-indazole-3-carboxylic acid, 462) 5-(3-Pyridin-2-yl- 1 H-pyrazol-4-yl)- 1 H-indazole-3-carboxylic acid methylamide, 463) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid dimethylamide, 464) 5-(3-pyridin-2-yl-1H-pyrazol-4-y1)-1H-indazole-3-carboxylic acid (2,2-dimethyl propyl)-amide, 465) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid phenylamide, 466) morpholin-4-yl-[5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazol-3-yl]-methanone, 467) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid benzylamide, 468) 5-(3-pyridin-2-yl-iH-pyrazol-4-yl)-1H-indazole-3-carboxylic acid cyclopentylamide; 469) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzamide; 470) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl] benzonitrile; 471) 4-[5-(2-methanesulfonyl-pyrirnidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid methyl ester; 472) 4-[5-(2-methoxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid methyl ester; 473) 4-[5-(2-hydroxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-y)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid methyl ester; 474) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 475) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1-carboxylic acid; 476) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 477) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo [2.2.2] octane-1 -carboxylic acid hydroxyamide; 478) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid methoxy-amide; 479) 4-[5-(2-amino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 480) {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]oct-1-yl}-carbarnic acid benzyl ester; 187 WO 2006/044509 PCT/US2005/036770 48 f) {1H[5:(22cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-acetamide; 482) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 483) N- {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)- 1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}--2,2,2-trifluoro-acetamide; 484) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin- 4 -yl)-1H-imidazol-2-ylI] bicyclo[2.2.2]octan-l-ol; 485) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 486) 6-[2-tert-butyl-5-(2-cyclopropyl-pyrimidin-4-yl)-3H-i-nidazol-4-yl]-quinoxaline; 487) 6-[5-(2-byclopropyl-pyrimidin-4-y1)-3H-imidazol-4-yl]-quinoxaline; 488) {4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct- 1-yl} -methanol; 489) 6-[5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 490) 6-[2-tert-butyl-5-(2-trifluoromethyl-pyrimidin-4-yl)-3 H-imidazol-4-yl]-quinoxaline; 491) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin- 4 -yl)-1H-imidazol-2-yl] piperidine-1 -carboxylic acid benzyl ester; 492) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 493) 6-[5-(2-cyclopropyl-pyrimidin-4-yl)- 2 -(I-methanesulfonyl-piperidin-4-yl)-3H-imidazol 4-yl]-quinoxaline; 494) 4-[5-(2-methyl-pyrimidin-4-yl)-4-[1,2,4]triazolo[4,3-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 495) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 496) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 497) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- I -carboxylic acid methyl ester; 498) 4-[4-(2-methyl-pyrimidin-4-y)-5-quinoxalin-6-yl-1KII-imidazol-2-yl]-cyclohexanol; 499) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1K-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol, 500) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-methyl-pyrimidine, 500a) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1 .2,4]triazolo[1,5-a]pyridine, 188 WO 2006/044509 PCT/US2005/036770 50 fJ M'6-(2-infn iiioetliy pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4] triazolo[1,5-a]pyridine, 502) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxaline, 502a) 6-[3-(2-trifluoromethyl-pyrimidin- 4 -yl)-1H-pyrazol-4-yl]-quino>xaline, 503) 6-[3-(2-cyclopropyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quinoxalirie, 504) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-trifluoromethyl-p yrimidine, 505) 7-[3-(2-trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, or 506) 6-[3-(2-Trifluoromethyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-quino line.

33. The device of claim 25, wherein device is a delivery pump.

34. The device of claim 25, wherein the device is a stent.

35. A method of treating or preventing restinosis, vascular disease, or hypertension by administering to a subject in need thereof a compound of the fonnula ~1, II, III, IV, V, or VI, or an N-oxide or a pharmaceutically acceptable salt thereof, wherein the compound of formula I has the structure: R" N adN A1-2 RQ X 1 .. 1 -YI_ 1 -R1- 2 () wherein R- is aryl, heteroaryl, aralkyl, or heteroaralkyl; each RIa is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; X 1 . 1 is cycloalkyl or heterocycloalkyl; Y 1 . 1 is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O) N(R)-, 189 WO 2006/044509 PCT/US2005/036770 bb ack~ok-6-CtO)-N(R)-, -N(RE)-C(O)-O-, -O-S(O),-N(RE)-, -N(RE)- S(0)p-OD-, -N(RB)-C(O)-N(Rc)-, -N(Rk)-S(O)p-N(R )-, -C(O)-N(Rk)-S(O),-, -S(O)p-N(RE)-C(O)-, -C(0)-N(RE)-S(O),-N(R )-, -C(O)-O-S(O),-N(RE)-, -N(Rb)-S(O),-N(R4)-C(O)-, -N(RE)-S(O),-0-C(O)-, -S(0),-N(Rk)-, -N(RE)-S(O)p-, -N(RE)-, -S(O)p-, -O-, -S-, c>r -(C(Rb)(RC))q-, wherein each of Rb and Rc is independently hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl, p is 1 or 2, and q is 1-4; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A - and A", independently, is 0, S, N, or NRW, provided that at lea-st one of A 1 and A 2 is N; and m is 0, 1, 2, or 3, and when m 2, two adjacent R a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; the compound of formula II has the structure: YII-2 (R 112 )n n (Rn )m X N XII-4 wherein each of XrI.., Xr-2, Xr-3, and Xr.. 4 is independently CRX or N, provided that -no more than two of X r1, X 1- 2 , X 1- 3 , and X 11- 4 can be N simultaneously; each of Yr 1 and Yr- 2 is independently CRY or N, provided that at least one of Y 1 1 -1 and Yr- 2 must be N; each R" 1 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, 190 WO 2006/044509 PCT/US2005/036770 heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each R- 2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cycloalkyl), NH(heterocycloalkyl), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, cycloalkyl-alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl)alkylearbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, alkoxycarbonylamrinoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m >_2, two adjacent R 1 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n >2, two adjacent R2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of Rx and RY is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, 191 WO 2006/044509 PCT/US2005/036770 "(liefer'o6y13flI1)dkl6arboiiylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroarallcylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, (cycloalkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl; the compound of formula III has the structure: 11--2 (R-r-2)n -YII- 1 (III) X111- N (R r X3N N 7 XII- 4 wherein each of Xm 1 - 1 , XmII- 2 , XIr-3, and X 1 11 - 4 is independently CRIIIX or N, provided that no more than two of XII-1, Xm 1 - 2 , Xm 1 - 3 , and X 1 1 1 - 4 can be N simultaneously; each of Y 11 and Ym-2 is independently CR'-y or N, provided that at least one of Y 11 and Ym 1 - 2 must be N; each Rm-1 is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsuilfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; each Rm- 2 is independently alkyl, alkenyl, alkynyl, acyl, halo, hydroxy, -NH 2 , -NH(alkyl), -N(alkyl) 2 , -NH(cycloalkyl), -N(alkyl)(cyclocalkyl), 192 WO 2006/044509 PCT/US2005/036770 'NH(hef6f6y6i6alky1), -NH(heteroaryl), -NH-alkyl-heterocycloalkyl, -NH-alkyl heteroaryl, -NH(aralkyl), cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, aroyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heteroaryl, heteroaralkyl, heteroaroyl, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkoxy, cycloalkyloxy, (cycloalkyl)alkoxy, aryloxy, arylalkoxy, heterocycloalkyloxy, (heterocycloalkyl)alkoxy, heteroaryloxy, heteroarylalkoxy, alkylsulfanyl, cycloalkylsulfanyl, (cycloalkyl)alkylsulfanyl, arylsulfanyl, aralkylsulfanyl, heterocycloalkylsulfanyl, (heterocycloalkyl)alkylsulfanyl, heteroarylsulfanyl, heteroarylalkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, aminosulfonyl, alkylcarbonylamino, cycloalkylcarbonylamino, (cycloalkyl(alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)alkylcarbonylamino, heteroarylcarbonylamino, heteroaralkylcarbonylamino, alkoxycarbonylaminoalkylamino, (heteroaryl)arylcarbonylaminoalkylamino, heteroaralkylcarbonylaminoalkylamino, (heteroaryl)arylsulfonylaminoalkylcarbonylaminoalkylamino, arylsulfonylaminoalkylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, or carbamoyl; m is 0, 1, 2, 3, or 4, and when m >2, two adjacent R"'M groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; n is 0, 1, 2, or 3, and when n ; 2, two adjacent Ru' 2 groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; and each of RI 11 x and R'Y is independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkylcarbonyl, (cycloalkyl)alkylcarbonyl, aroyl, aralkylcarbonyl, heterocycloalkylcarbonyl, (heterocycloalkyl)acyl, heteroaroyl, (heteroaryl)acyl, aminocarbonyl, alkylcarbonylamino, (amino)aminocarbonyl, alkylsulfonylaminocarbonyl, alkylsulfonylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, (cycloalkyl)alkylcarbonylamino, (cycloalkyl)alkylsulfonylamino, arylcarbonylamino, arylsulfonylamino, aralkylcarbonylamino, aralkylsulfonylamino, (heterocycloalkyl)carbonylamino, (heterocycloalkyl)sulfonylamino, (heterocycloalkyl)alkylcarbonylamino, (heterocycloalkyl)alkylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfonylamino, heteroaralkylcarbonylamino, heteroaralkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, 193 WO 2006/044509 PCT/US2005/036770 (cyllkyl)alkyl, (cycloalkyl)alkoxy, (cycloalkyl)alkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, (heterocycloalkyl)alkyl, (heterocycloalkyl)alkoxy, (heterocycloalkyl)alkylsulfanyl, aryl, aryloxy, arylsulfanyl, aralkyl, aralkyloxy, aralkylsulfanyl, arylalkenyl, arylalkynyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, heteroaralkyl, (heteroaryl)alkoxy, or (heteroaryl)alkylsulfanyl; the compound of formula IV has the structure: R IV-5 RI - 6 N'Rlv-i-RIV-2-RIV 3 -RIV-4 N (IV) \ N (RIV-a wherein each R*a is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; R~ 1 is a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri-0-(CH 2 )r 2 -, where each of r1 and r2 is independently 2 or 3; R -2 is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, or a bond; RI v 3 is -C(O)-, -C(O)O-, -OC(O)-, -C(O)-N(RIv~)-, -N(RIv-b)-C(O)-, -0 C(O)-N(R' -)-, -N(Rv~b)-C(0)-O, -O-S(O)p-N(Rv-b)-, -N(R ~b)- S(0),-O-, -N(Rv~ b)-C(O)-N(Rvc)-, -N(Rv~b)-S(O)p-N(Rv-b)-, -C(O)-N(R b)-S(O)p-, -S(O)p-N(R I~b) 194 WO 2006/044509 PCT/US2005/036770 CS -5(O) lN)(RVb)-, -N(RIVb)-S(O)p-, -N(RIwb)-, -S(O)p-, -0-, -S-, or (C(R ~5(RV C))q-, or a bond; wherein each of Rw-b and RW-c is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl; p is 1 or 2; and q is 1-4; RIV~ 4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; R"' 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryloxy, or heteroarylsulfinyl; R - is (1) a 5- to 6-membered heterocyclyl containing 1-3 hetero ring atoms selected from the group consisting of -0-, -S-, -N=, and -RNR-d-, where RIW-d is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; said heterocyclyl being substituted with RI - and optionally substituted with one to two Rv-; where Rw " is oxo, thioxo, alkoxy, alkylsulfinyl, -NH 2 , -NH(unsubstituted alkyl), or -N(unsubstituted alkyl) 2 , and R'v- is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocyclo, alkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or (2) a fused ring heteroaryl selected from the group consisting of: (Ri)n (RI)n (R)n(R% B' B B B' x2 X x2 23%x2 xQ) 1 1 ,and wherein ring A is an aromatic ring containing 0-4 hetero ring atoms, and ring B is a 5 to 7-membered aromatic or nonaromatic ring containing 0-4 hetero ring atois, provided that at least one of ring A and ring B contains one or more hetero ring 195 WO 2006/044509 PCT/US2005/036770 atoms; ring A' is an aromatic ring containing 0-4 hetero ring atoms, and ring B' is a 5 to 7-membered saturated or unsaturated ring containing 0-4 hetero ring atoms, provided that at least one of ring A' and ring B' contains one or more hetero ring atoms; each hetero ring atom is -0-, -S-, -N=, or -NR ~-; each X 1 is independently N or C; each X 2 is independently -0-, -S-, -N=, -- NR'~g-, or -CHRv h-; where REv-f is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroaralkyl; each of Rv-h and Rw1- is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and n is 0-2; and m is 0-3, and when m >2, two adjacent Rva groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety; provided that if RIV~ 6 is 2-naphthyridinyl, 4-quinolinyl, imidazo[1,2-a]pyridyl, or benzimidazolyl, then -- R 2-RV-Re~4 is not H, unsubstituted alkyl, -CH 2 -C(O)-N(H)-alkyl, -CH 2 -C(O)-N(alkyl) 2 , or benzyl; the compound of formula V has the structure (Rv-a)m N N(V Av-2 Xy--Yy--RyV-2 '-AV-' wherein Rv-I is heteroaryl; each Rv-a, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, 196 WO 2006/044509 PCT/US2005/036770 alrylcaroonylammfo, aryiwaroonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsalfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; X, is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or a bond; Y, is a bond, -C(O)-, -C(O)-O-, -O-C(O)-, -S(O),-O-, -O-S(O)p-, -C(O)-N(RS)-, -N(R)-C(O)-, -O-C(O)-N(R))-, -N(R)-C(O)-O-, -C(O)-N(R)-0-, -o N(RE)-C(O)-, -O-S(O),-N(RE)-, -N(Rk)- S(O),-O-, -S(O)p-N(RE)-0-, -O-N(RE)-S(O)p-, -N(RE)-C(O)-N(R)-, -N(R )-S(O)p-N(Rc)-, -C(O)-N(RE)-S(O)p-, -S(O),-N(RE)-C(O)-, -C(O)-N(RE)-S(O),-N(RC)-, -C(O)-O-S(O),-N(RE)-, -N(RE)-S(O)p-N(RW)-C(O)-, -N(RE)-S(O),-0-C(O)-, -S(O)p-N(RE)-, -N(RE)-S(O),-, -N(RE)-, -S(O),-, -O-, -S-, or -(C(Rb)(RC))q-, wherein each of Rb and R, independently, is hydrogen, hydroxy, alkyl, alkoxy, amino, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl, p is 1 or 2, and q is 1-4; Rv-2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, aralkyl, arylalkenyl, heterocycloalkyl, (heterocycloalkyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, heteroaryl, heteroaralkyl, or (heteroaryl)alkenyl; each of A v-1 and Av- 2 , independently, is N or NRb; and m is 0, 1, 2, or 3, and when m >_2, two adjacent R v-a groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety, provided that if X, is a bond, then Y, is a bond; Rv- 2 is hydrogen or alkyl; m is 1, 2, or 3; and at least one Rva is substituted at the 2-pyrimidinyl position; and the compound of formula VI has the structure: 197 WO 2006/044509 PCT/US2005/036770 RVI-5 RVI- 6 N' V1-RVI-2--RVI 3 _ RI-4 ~ N NN (VI) N (RVLa)m wherein each RVia, independently, is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, -NH 2 , -NH(unsubstituted alkyl), -N(unsubstituted alkyl) 2 , nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkyle arbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, heterocycloalkylcarbonyl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; RvI~I is a bond, alkylene, alkenylene, alkynylene, or -(CH 2 )ri-0-(CH 2 )r 2 -, where each of r1 and r2, independently, is 2 or 3; R1-2 is cycloalkylene, heterocycloalkylene, cycloalkenylene, heterocycloalkenylene, arylene, heteroarylene, or a bond; RVI 3 is -C(O)-, -C(0)-0-, -O-C(O)-, -S(O),-O-, -0-S(O)p-, -C(O)-N(Rb)-, -N(RU)-C(O)-, -O-C(O)-N(RE)-, -N(RW)-C(O)-O-, -C(O)-N(R)-0-, -O-N(RE)-C(O)-, -O-S(0)p-N(R0)-, -N(RE)- S(O)p-O-, -S(O),-N(RE)-O-, -O-N(RE)-S(O)p-, -N(RE)-C(0)-N(Rc)-, -N(Rk)-S(0)p-N(Rc)-, -C(O)-N(RE)-S(O)p-, -S(O),-N(Rk)-C(O)-, -C(O)-N(R)-S(O)j,-N(Rc)-, -C(0)-D)-S(O),-N(RE)-, -N(R0)-S(O),-N(R )-C(O)-, -N(Rb)-S(O),-0-C(O)-, -S(O),-N(Ra')-, -N(RE)-S(O)p-, -N(R)-, -S(O),-, -O-, -S-, -(C(Rb)(R))g-, or a bond; wherein each of Rb and R' is independently hydrogen, hydroxy, alkyl, aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaralkyl, p is 1 or 2, and q is 1-4; 198 WO 2006/044509 PCT/US2005/036770 visfydr6o e, ailkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, heterocycloalkenyl, (heterocycloalkenyl)alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; RVI- 5 is hydrogen, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryloxy, arylsulfinyl, heteroaryloxy, or heteroarylsulfinyl; Rvi-6 is a 5- to 6-membered monocyclic heterocyclyl or a 8- to 11 -membered bicyclic heteroaryl; each being optionally substituted with alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, gaanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamiino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyle arbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; and m is 0-3, and when m >_2, two adjacent R v- groups can optionally join together to form a 4- to 8-membered optionally substituted cyclic moiety.

36. The method of claim 35, wherein restenosis is coronary restenosis, peripheral restenosis, carotid restenosis.

37. The method of claim 35, wherein vascular disease is intimal thickening, vascular remodeling, or organ transplant-related vascular disease.

38. The method of claim 37, wherein the vascular disease is intimal thickening or vascular remodeling.

39. The method of claim 35, wherein hypertension is primary or secondary hypertension, systolic hypertension, pulmonary hypertension or hypertension-induced vascular remodeling.

40. The method of claim 35, wherein the compound is 1) 4-(4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl)-piperidine-1 carboxylic acid benzyl ester; 199 WO 2006/044509 PCT/US2005/036770 2) 4-(4'-enzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 3) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 4) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 5) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 6) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzyl ester; 7) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 8) 3-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl]-pyrrolidine-1 carboxylic acid benzyl ester; 9) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-6-methyl-pyridine; 10) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imid-azol-4 yl]-6-methyl-pyridine; 11) 2-[5-Benzo[1,3]dioxol-5-y-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imid-azol-4 yl]-pyridine; 12) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 13) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-methanesulfonyl-piperidin-4-yl)-3H-imidazol-4-yl]-6 methyl-pyridine; 14) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzyl ester; 15) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2,4-dichloro-benzylamide; 16) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidin-1-yl] ethanone; 17) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-furan-2-yl-methyl-piperidin-4-yl)-3H-imidazol-4-yl] pyridine; 18) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 19) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylamine; 200 WO 2006/044509 PCT/US2005/036770 20) N {4][4-Benzd{1~3}diox-'15-yl-5 (6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -C-phenyl-methanesulfonamide; 21) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-I -carboxylic acid methyl ester; 22) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid; 23) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 24) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-ethyl-pyridin-2-yl)-IH-inidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 25) 2-(5-Benzo[1,3]dioxol-5-yl-2-piperidin-4-yl-3H-imidazol-4-yl)-pyridine; 26) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-IH-imidazol-2-yl)-piperidine-1-carboxylic acid 4-nitro-benzyl ester; 27) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4,5-dimethoxy-2-nitro-benzyl ester; 28) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 3-fluoro-benzylamide; 29) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-fluoro-benzylamide; 30) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid benzylamide; 31) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} pyridine; 32) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methyl-benzylamide; 33) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 4-methoxy-benzylamide; 34) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid 2-chloro-benzylamide; 35) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzoic acid; 36) 4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxylic acid amide; 37) 4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] benzonitrile; 201 WO 2006/044509 PCT/US2005/036770 3 8)'22f {5enz 6 [ i,] dioxo3f-5-y-2- [ 1i-(4-chloro-benzenesulfonyl)-piperidin-4-yl] -3H imidazol-4-yl} -pyridine; 39) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-pip eridin-4-yl]-3H imidazol-4-yl} -pyridine; 40) {5-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-sulfonyl] naphthalen- 1-y1} -dimethyl-amine; 41) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methyl)-piperidin-4-yl)]-3H-imidazol-4 yl}-pyridine; 42) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(propane-2-sulfonyl)-piperidin-4-y1]-3H-imidazol- 4 yl}-pyridine; 43) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-methoxy-benzenesulfonyl)-piperidin- 4 -yl]-3H imidazol-4-yl} -pyridine; 44) 1-{4-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonyl]-phenyl}-ethanone; 45) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(4-methyl-benzyl)-piperidin-4-y1]-3H-imidazol-4-yl} pyridine; 46) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-fluoro-5-trifluoromethyl-benzyl)-piperidin- 4 -yl]-3H imidazol-4-yl} -pyridine; 47) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-cyclohexylmethyl-piperidin-4-yl)- 3 H-imidazol-4-yl] pyridine; 48) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-pip eridin-1-ylmethyl] cyclopropanecarboxylic acid ethyl ester; 49) 2-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-pip eridin-1-ylmethyl] pyrrolidine-1-carboxylic acid tert-butyl ester; 50) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2,2-dimethyl-[1,3]dioxolan-4-yhlnethyl)-piperidin-4 yl] -3H-imidazol-4-yl} -pyridine; 51) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 -yl] pyridine; 52) 2-{5-Benzo[ 1,3] dioxol-5-yl-2-[ 1 -(butane-1 -sulfonyl)-piperidin-4-yl] -3H-imidazol-4-yl} pyridine; 53) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro-phenylmethanesulfonyl)-piperidin-4-yl]- 3 H imidazol-4-yl} -pyridine; 54) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(2-phenyl-ethenesulfonyl)-piperidifn-4-yl]-3H-imidazol 4-yl} -pyridine; 202 WO 2006/044509 PCT/US2005/036770 55)" 2"'f5 n1 b["'f,'dinol-[I-2"[ fpropane- 1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 56) 1-[4-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1 sulfonylmethyl]-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 57) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-phenylmethanesulfonyl)-piperidin-4-yl1]-3H imidazol-4-yl} -pyridine; 58) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 59) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-fluoro-phenylnethanesulfonyl)-piperidin-4-yl)-3H imidazol-4-yl} -pyridine; 60) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 61) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H-in-iidazol 4-yl}-pyridine; 62) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-p-tolylmethanesulfonyl-piperidin-4-yl)-3H-imidaxzol-4 yl]-pyridine; 63) 3-(4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidirne-1 carboxylic acid benzyl ester; 64) 3-(4-Benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)-piperidine-1-carboxcylic acid benzyl ester; 65) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 66) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3 H imidazol-4-yl} -pyridine; 67) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-naphthalen-1-yl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 68) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl]-pyridine; 69) 3-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 70) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-4-yl-methanesulfonyl)-piperidin-4-yl]-3 H imidazol-4-yl} -pyridine; 71) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-3-yl-methanesulfonyl)-piperidin-4-yl]-3 H imidazol-4-yl} -pyridine; 203 WO 2006/044509 PCT/US2005/036770 72j12- {5-Benzol,'3] dixo f-2yl-2-[ 1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 73) 3-[4-Benzo[1,3]dioxol-5-yl-l-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] pyrrolidine-1-carboxylic acid benzyl ester; 74) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -pyridine; 75) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-bis-trifluoromethyl-phenylmethanesulfonyl) piperidin-4-yl]-3H-imidazol-4-yl}-pyridine; 76) 2-{5-Benzo[1,3]dioxol-5-yl-2-[l-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-pyridine; 77) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -pyridine; 78) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(pyridin-2-yl-methanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 79) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 80) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(biphenyl-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -pyridine; 81) 4-[5-Benzo[1,3]dioxol-5-yl-1-methyl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine-1-carboxylic acid benzyl ester; 82) 4-[4-Benzo[1,3]dioxol-5-yl-1-methyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 83) {4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl} -carbamic acid benzyl ester; 84) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-phenoxy-phenylmethanesulfonyl)-piperidin-4-y] 3H-inidazol-4-yl}-6-methyl-pyridine; 85) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-ethanesulfonyl-piperidin-4-yl)-3H-imidazol-4-y]-6 methyl-pyridine; 86) 2-{5-Benzo[ 1,3]dioxol-5-yl-2-[ 1 -(propane-1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 87) 2- {5-Benzo[ 1,3]dioxol-5-yl-2-[1 -(butane-1 -sulfonyl)-piperidin-4-yl]-3H-imidazol-4-yl} 6-methyl-pyridine; 88) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(pyridin-3-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 204 WO 2006/044509 PCT/US2005/036770 89)"2-'{5-Benzo[1,3]dioxol-5-yl-2-[ 1 -(pyridin-4-ylmethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 90) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(3,5-difluoro-phenylmethanesulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 91) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3-trifluoromethyl-phenylmethanesulfonyl)-piperidin-4 yl]-3H-imidazol-4-yl} -6-methyl-pyridine; 92) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl } -6-methyl-pyridine; 93) 2-{5-Benzo[ 1,3]dioxol-5-yl-2-[1 -(butane-1 -sulfonyl)-piperidin-3-yl] -3H-imidazol-4-yl} 6-methyl-pyridine; 94) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-3-yl)-3H-imidazol-4 yl] -6-methyl-pyridine; 95) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-IH-imidazole-4-sulfonyl)-piperidin-4-yl] 3H-imidazol-4-yl} -6-methyl-pyridine; 96) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(5-methyl-isoxazole-4-sulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 97) 4-[5-Benzo[1,3]dioxol-5-yl-1-hydroxy-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 98) Butane-1 -sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-cyclohexyl}-amide; 99) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexyl}-C-pyridin-2-yl-methanesulfonamide; 100) Thiophene-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl] -cyclohexyl} -amide; 101) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-cyclohexyl}-amide; 102) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid aide; 103) 4-[4-Benzo[1,3]dioxol-5-yl-1-hydroxy-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid methyl ester; 104) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-bromo-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 105) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(thiophene-3-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 205 WO 2006/044509 PCT/US2005/036770 106) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(5-methyl-2-trifluoromethyl-furan-3-sulfonyl) piperidin-4-yl]-3H-imidazol-4-y} -6-methyl-pyridine; 107) 4-[2-(1-phenylmethanesulfonyl-piperidin-4-yl)-5-(6-methyl-pyridin-2-yl)-iH-imidazol 4-yl]-pyridin-2-yl-fluoride; 108) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-trifluoromethyl-pyridin-2-yl)-1H-imidazol-2-yl] piperidine- 1-carboxylic acid benzyl ester; 109) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-bromo-pyridin-2-yl)-1-hydroxy-1H-imidazol-2-yl] piperidine- 1 -carboxylic acid benzyl ester; 110) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol-4 yl]-6-bromo-pyridine; 111) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl} -methanol; 112) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid amide; 113) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-2H-imidazol-2-yl]-piperidine-1 sulfonic acid dimethylamide; 114) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidin 1-yl} -3-phenyl-propan-i-one; 115) 2-{5 -Benzo[1,3]dioxol-5-yl-2-[1-(propane-2-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 116) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carbonitrile; 117) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylamine; 118) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-phenyl-methanesulfonamide; 119) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 120) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-C-pyridin-2-yl-methanesulfonamide; 121) 2-{5-Benzo[1,3]dioxol-5-yl-2-[4-(1H-tetrazol-5-yl)-bicyclo[2.2.2]oct-1-y1]-3H imidazol-4-yl} -6-methyl-pyridine; 122) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-y)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide; 206 WO 2006/044509 PCT/US2005/036770 123) Tliioblierfe-2sU1fiic-Ectd "{4'-[4=benzoL1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 124) 1-Methyl-1H-imidazole-4-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl pyridin-2-yl)-1H-imidazol-2-yl]-bicyclo[2.2.2]oct-1-yl}-amide; 125) Thiophene-3-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo [2.2.2]oct-1-yl}-amide; 126) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 127) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-phenyl-ethanesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 128) Methanesulfonic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]oct-1-ylmethyl ester; 129) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetonitrile; 130) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl }-acetic acid; 131) N-{4-[4-Benzo[1 ,3]dioxol-5-yl-5-(6-methyl-pyridin-2-y)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-ylinethy1}-methanesulfonamide; 132) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(biphenyl-4-sulfonyl)-piperidin-4-yl]-3H-imidazol-4 yl} -6-methyl-pyridine; 133) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-phenoxy-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl}-6-methyl-pyridine; 134) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(3,4-dichloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 135) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yhnethyl}-C-phenyl-methanesulfonamide; 136) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yhnethyl}-C-pyridin-2-yl-methanesulfonamide; 137) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid benzylamide; 138) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (pyridin-2-ylmethyl)-amide; 139) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid 3-chloro-4-fluoro-benzylamide; 207 WO 2006/044509 PCT/US2005/036770 140) 4-[4-Benzo[1,3Jdioxol-5-yl-5-(6-methyl-p yridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid (furan-2-ylmethyl)-amide; 141) 2-[5 -Benzo[ 1,3 ]dioxol-5 -yl-2-(1 -methanesulfonyl-pyrrolidin-3 -yl)-3H-imidazol-4-yl] -6 methyl-pyridine; 142) 2-{5-Benzo[1,3]dioxol-5-yl-2-[I-(butane-1-sulfonyl)-pyrrolidin-3-yl]-3H-imidazol-4 yl}-6-methyl-pyridine; 143) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(1-methyl-1H-imidazole-4-sulfonyl)-pyrrolidin-3-yl] 3H-imidazol-4-yl}-6-methyl-pyridine; 144) 2-[5-Benzo[1,3]dioxol-5-yl-2-(i-phenyhnethanesulfonyl-pyrrolidin-3-yl)-3H-imidazol 4-yl]-6-methyl-pyridine; 145) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-pyrrolidin-3-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 146) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(2-nitro--phenylmethanesulfonyl)-piperidin-4-yl]- 3 H imidazol-4-yl} -6-methyl-pyridine; 147) 2-{5-Benzo[1,3]dioxol-5-yl-2-[i-(2-naphthalen-2-yl-ethanesulfonyl)-piperidin-4-y] 3H-imidazol-4-yl}-6-methyl-pyridine; 148) 1-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine I-sulfonylmethyl}-7,7-dimethyl-bicyclo[2.2.1]heptan-2-one; 149) 2-{5-Benzo[1,3]dioxol-5-yl-2-[1-(4-chloro-benzenesulfonyl)-piperidin-4-yl]-3H imidazol-4-yl} -6-methyl-pyridine; 150) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid methylamide; 151) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid ethylainide; 152) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid butylanaide; 153) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid isopropylamide; 154) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid (3-imidazol-1-yl-propyl)-amide; 155) 2-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl]-piperidine 1 -sulfonylmethyl} -phenylamine; 156) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid (1-methyl-5-methylsulfanyl-1H-[1,2,4]triazol-3-yl) amide; 208 WO 2006/044509 PCT/US2005/036770 157) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1HI-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid cyclohexylamide; 158) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-pyrrolidin-1-yl-methanone; 159) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H--imidazol-2-yl] bicyclo[2.2.2] octane-1 -carboxylic acid dimethylamide; 160) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1Hi-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid diethylamide; 161) 4-[4-Benzo[ 1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1II-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid dipropylamide; 162) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1I-imidazol-2-yl] bicyclo[2.2.2] octane-i -carboxylic acid (5,7-difluoro-benzothia-zol-2-yl)-amide; 163) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1R-imidazol-2-y] bicyclo[2.2.2]octane- 1 -carboxylic acid benzothiazol-2-ylamide; 164) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1HI-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (1H-benzoimidazol-2-yl)-amide; 165) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1T-imidazol-2-yl] bicyclo[2.2.2]octane- I -carboxylic acid (2-hydroxy-1-methy1-2-phenyl-ethyl)-amide; 166) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1RL-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid (pyridin-4-ylmethyl)-arnide; 167) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-111-imidazol-2-yl]-piperidin-1 yl}-(3-chloro-phenyl)-methanone; 168) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-lIH-imidazol-2-yl]-piperidin-1 yl} -(4-fluoro-phenyl)-methanone; 169) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1IH-imidazol-2-yl]-piperidin-1 yl} -(4-methoxy-phenyl)-methanone; 170) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-cyclopropyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 171) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid methoxy-amide; 172) 4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H--imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid hydroxyamide; 173) {4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin- 2 -yl)-lI-imidazol-2-yl] cyclohexylmethyl} -carbamic acid benzyl ester; 209 WO 2006/044509 PCT/US2005/036770 174) 444-Benzo( 1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)- 1 H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid hydrazide; 175) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -acetamide; 176) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-methanesulfonamide; 177) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-phenyl-methanesulfonamide; 178) Butane-1-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-IH imidazol-2-yl]-cyclohexylmethyl}-amide; 179) Propane-2-sulfonic acid {4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridii-2-yl)-1H imidazol-2-yl]-cyclohexylmethyl}-amide; 180) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl} -C-pyridin-2-yl-methanesulfonamide; 181) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] cyclohexylmethyl}-C-pyridin-4-yl-methanesulfonamide; 182) (4-Methoxy-benzyl)-{4-[5-(6-methyl-pyridin-2-yl)-2-(1-phenylmethanesulfonyl piperidin-4-yl)-IH-imidazol-4-yl]-pyridin-2-yl}-amine; 183) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 184) 4-[5-(6-Methyl-pyridin-2-yl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-IH-imidazol-2-yl] bicyclo [2.2.2] octane-i -carboxylic acid; 185) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1 H-imidazol-2 yl]-bicyclo[2.2.2]octane- I -carboxylic acid methyl ester; 186) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid hydroxyamide; 187) 4-[4-(6-Methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid amide; 188) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid; 189) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 190) 4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 210 WO 2006/044509 PCT/US2005/036770 191) 4-[4-(6-Cyclopropyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid amide; 192) 4-[4-(6-Cyclopropyl-pyridin-2-y)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2 yl] -bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 193) N-{4-[5-Benzo[1,3]dioxol-5-yl-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] oct-i -yl}-sulfamide; 194) Sulfamic acid 4-[4-benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl ester; 195) {4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} carbamic acid benzyl ester; 196) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-1 -carbonyl} -methanesulfonamide; 197) N-{4-[4-Benzo[1,3]dioxol-5-yl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2] octane-i -carbonyl} -benzenesulfonamide; 198) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 199) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-y)-4-(6-methyl-pyridin-2-yl)-1H imidazol-2-yl]-bicyclo[2.2.2] octane-i -carboxylic acid; 200) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} acetamide; 201) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-bicyclo [2.2.2]octane 1-carboxylic acid methyl ester; 202) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl] -bicyclo [2.2.2] octane 1-carboxylic acid; 203) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl- 1 H-imidazol-2-yl] -bicyclo[2.2.2]octane 1-carboxylic acid hydroxyamide; 204) 4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-IH-imidazol-2-yl]-bicyclo[2.2.2]octane 1-carboxylic acid amide; 205) N-{4-[4-(6-Methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexyl} methanesulfonamide; 206) 2,2,2-Trifluoro-N-{4-[4-(6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] cyclohexyl}-acetamide; 207) 4-[4-(5-Fluoro-6-methyl-pyridin-2-yl)-5-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol 2-yl]-bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester; 211 WO 2006/044509 PCT/US2005/036770 208) {4-[2-[1 -(Butane-i-sulfonyl)-piperidin-4-yl]-5-(6-methyl-pyridin- 2 -yl)- 1H-imidazol-4 yl]-pyridin-2-yl}-(4-methoxy-benzyl)-amine; 209) 4-[2-[1 -(Butane-I -sulfonyl)-piperidin-4-yl] -5-(6-methyl-pyridin-2-yl)-IH-imidazol-4 yl]-pyridin-2-ylamine; 210) 2-[5-Benzo[1,3]dioxol-5-yl-2-(1-phenylmethanesulfonyl-piperidin-4-yl)-3H-imidazol- 4 y1]-6-ethyl-pyridine; 211) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-yl)-lH imidazol-2-yl] -bicyclo [2.2.2] octane-1 -carboxylic acid amide; 212) 4-[5-(3-Methyl-4-oxo-3,4-dihydro-quinazolin-6-yl)-4-(6-methyl-pyridin-2-y1)-1H imidazol-2-yl]-bicyclo[2.2.2] octane-1 -carboxylic acid hydroxyamide; 213) N-{4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 214) N- {4-[5-(6-Methyl-pyridin-2-yl)-4-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]oct-1-yl}-acetamide. 215) 4-[2-(6-Methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 216) 4-(2-pyridin-2-yl-pyrazolo[1,5-a]pyridin-3-yl)-pyrimidin-2-ylanine; 217) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyridin-3-yl]-pyrimidin-2-ylamine; 218) 2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-pyrazolo[1,5-a]pyridine; 219) 4-[2-(6-chloro-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 220) 2-(6-methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-pyrazolo[1,5 c]pyrimidine; 221) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-a]pyrazin-3-yl]-pyrimidin-2-ylamine; 222) 4-[2-(6-methyl-pyridin-2-y)-pyrazolo[1,5-a]pyrimidin-3-yl]-pyrimidin-2-ylamine; 223) 4-[2-(6-methyl-pyridin-2-yl)-pyrazolo[1,5-c]pyrimidin-3-yl]-pyrimidin-2-ylamine; 224) (2-Methoxy-ethyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 225) (3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} propyl)-carbamic acid tert-butyl ester; 226) (3-Imidazol-1-yl-propyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 227) (4-Methoxy-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 228) [2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridin 6-yl]-methanol; 212 WO 2006/044509 PCT/US2005/036770 229) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine; 230) (4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino } butyl)-carbamic acid tert-butyl ester; 231) (4-Amino-benzyl)-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl}-amine; 232) (5-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino } pentyl)-carbamic acid tert-butyl ester; 233) [3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-6-yl] methanol; 234) [3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-7-yl] methanol; 235) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-morpholin-4-yl-ethyl)-amine; 236) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-2-yl-ethyl)-amine; 237) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-3-yl-ethyl)-amine; 238) [3-(2-methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-6-yl]-methanol; 239) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(2-pyridin-4-yl-ethyl)-amine; 240) [3-(2-Amino-pyrimidin-4-yl)-6-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-8-yl]-(3-morpholin-4-yl-propyl)-amine; 241) [3-(4-Methyl-piperazin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3 -yl] -pyrimidin-2-yl} -amine; 244) [3-(4-Methyl-piperidin-1-yl)-propyl]-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridin-3-yl]-pyrimidin-2-yl} -amine; 245) [4-(2-Pyridin-2-yl-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-yl]-pyridin-3-ylmethyl amine; 246) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-((R)-1 phenyl-ethyl)-amine; 247) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-((S)-1 phenyl-ethyl)-amine; 213 WO 2006/044509 PCT/US2005/036770 248) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(1H tetrazol-5-yl)-amine; 249) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-( 2 H pyrazol-3-yl)-amine; 250) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2 morpholin-4-yl-ethyl)-amine; 251) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 2-yl-ethyl)-amine; 252) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl)-pyrimidin-2-yl}-(2-pyridin 3-yl-ethyl)-amine; 253) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(2-pyridin 4-yl-ethyl)-amine; 254) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl}-(3 morpholin-4-yl-propyl)-amine; 255) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yll-pyrimidin-2-yl}-(3 piperidin-1-yl-propyl)-amine; 256) {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} [1,3,4]thiadiazol-2-yl-amine; 257) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 258) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 6-carboxylic acid methyl ester; 259) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine 7-carboxylic acid ethyl ester; 260) 2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2 a]pyrimidin-7-ylamine; 261) {7,7-Dimethyl-8-[5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoy1)-pentyl)-2-oxo-4-trifluoromethyl-7,8-dihydro-2H-1 oxa-8-aza-anthracen-5-yl}-methanesulfonic acid; 262) 2-(2,7-Difluoro-6-hydroxy-3-oxo-9,9a-dihydro-3H-xanthen-9-yl)-3,5,6-trifluoro-4-[(4 {4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butylcarbamoyl)-methylsulfanyl]-benzoic acid; 263) -(6-Methyl-pyridin-2-yl)-3-(2-morpholin-4-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 264) 2-(6-Methyl-pyridin-2-yl)-3-(2-piperidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 265) 2-(6-Methyl-pyridin-2-yl)-3-(2-pyrrolidin-1-yl-pyrimidin-4-yl)-imidazo[1,2-a]pyridine; 214 WO 2006/044509 PCT/US2005/036770 266) 2-(6-Methyl-pyridin-2-yl)-3-[2-(1H-tetrazol-5-yl)-pyrimidin-4-yl]-imidazo[1,2 a]pyridine; 267) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyridine; 268) 2-(6-Methyl-pyridin-2-yl)-3-pyrimidin-4-yl-imidazo[1,2-a]pyrimidin-7-ylamine; 269) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-8 ylamine; 270) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonitrile; 271) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid; 272) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 273) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 274) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-dimethylamino-ethyl)-amide; 275) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-methoxy-ethyl)-amide; 276) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 277) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide; 278) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid amide; 279) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid cyclopropylamide; 280) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-alpyridine-6 carboxylic acid ethylamide; 281) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid hydroxyamide; 282) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methoxy-amide; 283) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carboxylic acid methyl ester; 215 WO 2006/044509 PCT/US2005/036770 284) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid; 285) 3-(2-Amino-pyrimidin-4-y1)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridime-7 carboxylic acid ([1,4]dioxan-2-ylmethyl)-amide; 286) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-amino-ethyl)-amide; 287) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-dimethylamino-ethyl)-amide; 288) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-hydroxy-ethyl)-amide; 289) 3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-oxo-2-pyridin-3-yl-ethyl)-amide; 290) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid (2-thiophen-2-yl-ethyl)-amide; 291) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-alpyridine-7 carboxylic acid (piperidin-3-ylmethyl)-amide; 292) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid 2,2-dimethylhydrazide; 293) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid amide; 294) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid cyclopropylamide; 295) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethyl ester; 296) 3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid ethylamide; 297) 3-(2-Amino-pyrimidin-4-y)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid hydroxyamide; 298) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carboxylic acid methoxy-amide; 299) 3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyriinidin-7 ylamine; 300) 3-(2-Azetidin-1-yl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo(1,2-a]pyridine; 301) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1 ,2-a] pyridine-7-carboxylic acid ethyl ester; 216 WO 2006/044509 PCT/US2005/036770 302) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carboxylic acid methyl ester; 303) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-7-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 304) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-8-methyl-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a] pyridine; 305) 3,3-Dimethyl-N-[2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl) imidazo[1,2-a]pyrimidin-7-yl]-butyramide; 306) 3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2 a]pyridine-6-carbonitrile; 307) 3-(2-Methylsulfanyl-pyrimidin-4-yl)-2-pyridin-2-yl-imidazo[1,2-a]pyridine; 308) 3,6-Dichloro-N-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butyl)-2-(2,4,5,7-Tetrachloro-6-hydroxy-3-oxo-9,9a-dihydro-3H xanthen-9-yl)-terephthalamic acid; 309) 3-[2-(2-Methyl-aziridin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyridine; 310) 3-[2-(4-Methyl-piperazin-1-yl)-pyrimidin-4-yl]-2-(6-methyl-pyridin-2-yl)-imic-azo[1,2 a] pyridine; 311) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-6 carbonyl]-amino}-propionic acid methyl ester; 312) 3-{[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridine-7 carbonyl] -amino } -propionic acid methyl ester; 313) 3-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylaniino} phenol; 314) 4-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} ethyl)-benzenesulfonaniide; 315) 4-(2-Pyridin-2-yl-i-inidazo[1,2-alpyridin-3-yl)-pyrimidin-2-ylamine; 316) 4-[2-(6-Chloro-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 317) 4-[2-(6-Methyl-pyridin-2-yl)-7-trifluoromethyl-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl-amine; 318) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamine; 319) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbonitrile; 320) 4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidine-2-carbox ylic acid amide; 217 WO 2006/044509 PCT/US2005/036770 321)4 6-[. B romo .2-(6- methyl1.pyri .din .- 2-yI)-imidazo [1 ,2-a]pyridin-3 -yl] -pyrimidin-2 ylamine; 322) 4-[6-Choro-2-(6-methy1-pyridin-2-y)-imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2 ylamine; 323) 4-[6-Fluoro-2-(6-methyl-pyfldiin-2-y)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 324) 4-6Mty--6mty-yii--l--(-opoi- lehlmn)iiao1,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 325) 4-6Mty--6mthlprdi- 1-g(-yii--letyaio-mdz~,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 326) 4-[6-Methy1-2-(6-methy1-pyridtin-2-y1)-8-(2-pyridifl 3 -yl-ethylamino)-imidazo[ 1,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 327) 4-6Mtyl2(-ety yiin-2-yl)-8-(2-pyridin-4-y-ethylamilo)-imidazo [1,2-a] pyridin-3 -yl]-pyrimidin-2-ol; 328) 4-6Mty--6mtylprdn2y) mrpoi--liio1 ,2-alpyridin-3-yl] pyrimidin-2-ol; 329) 4-6Mty--6mtylprc[n2y)8mopoi- liio1 ,2-a]pyridin-3-yl] pyrimidin-2-ylamine; 330) 4-[6-Methyl-2-(6-methyl-pyridil-2-y1)-imidazo [1 ,2-a]pyridin-3-yl]-pyrimidin-2 ylamine; 331) 4-[7-Aminomethyl-2-(6-methy-pyrdil-2-y1)-imidazo[1I,2-allpyridin-3 -yl]-pyrimidin-2 yl-amnine; 332) 4-[7-Methyl-2-(6-methyl-pyridin-2-y)-imidazo[ 1,2-a]pyridin-3-yl] -pyrimidin-2 ylamine; 333) 4-[8-Benzyloxy-2-(6-methyl-p yridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidil-2-ol; 334) 4-[8-Benzyloxy-2-(6-methyl-pyridil-2-Y1)-imidazo[ 1,2-a]pyridin-3-yl] -pyrimidin-2-yl amine; 335) 4-[8-Bromo-6-methy1-2-(6-me-thy-pyridil-2-y1)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin 2-ol; 336) 4-[g-Methyl-2-(6-methyl-pyridil-2-Y1)-imildazo[ 1,2-a]pyridin-3 -yl]-pyrimidin-2 ylamine; 337) 6-hoo3(-ehnsloy-yiii-4y 2(-ehlprdn2y)iiao1,2 a] pyridine; 338) 5-Dimethylamino-naphthalefle-l1-sulfonic acid (4- {4-[2-(6-methyl-pyridin-2-yl) imidazo[ 1,2-a]pyridin-3 -yl] -pyrimidin-2-ylamnino }-butyl)-amide; 218 WO 2006/044509 PCT/US2005/036770 339) 6-(2,7-Difluoro-6-hydroxy-3-oxo-3H-xanthen-9-yl)-N-( 4 -{4-[2-(6-methyl-pyridin-2-yl) imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino}-butyl)-isophthalamic acid; 340) 6-Amino-9-[2-carboxy-5-(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino } -butylcarbamoyl)-phenyl]-xanthen-3 -ylidene-ammonium; 341) 6-Bromo-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfai1yl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 342) 6-Fluoro-2-(6-methyl-pyridin-2-yl)-3-(2-methylsulfnyl-pyrimidin-4-yl)-imidazo[1,2-a] pyridine; 343) 7-Amino-4-methyl-3-[(4-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl] pyrimidin-2-ylamino}-butylcarbamoyl)-methyl]-2-oxo-2H-chromene- 6 -sulfonic acid; 344) Cyclobutyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine; 345) Cyclopentyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1 ,2-a]pyridin-3-yl]-pyrimidin-2 yl}-amine; 346) Cyclopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridin-3-yl]-pyrimidin-2 yl}-amine; 347) Cyclopropyl-methyl-{4-[2-(6-methyl-pyridin-2-yl)-irnidazo[1,2-a]pyridin-3-yl] pyrimidin-2-yl} -amine; 348) Dimethyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine, 349) Isopropyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[i,2,-a]pyridin-3-yl]-pyrimidin-2-yl} amine, 350) Methyl-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} amine, 350a) N-(2-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2 ylamino} -ethyl)-acetamide; 351) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-acetamide; 352) N,N-Dimethyl-N'-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin 2-yl} -ethane-1,2-diamine; 353) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 354) N-[2-(6-Methyl-pyridin-2-yl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-imidazo(1,2-a] pyrimidin-7-yl]-nicotinamide; 219 WO 2006/044509 PCT/US2005/036770 355) N-[2-(6-Methyl-pyridin-2-y)-3-(2-methylsulfanyl-pyrimidin-4-yl)-irnidazo[1,2-a] pyrimidin-7-yl]-propionamide; 356) N-[3-(2-Anino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridine-6 carbonyl]-methanesulfonamide; 357) N-[3-(2-Awnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyridine-7 carbonyl]-methanesulfonamide; 358) N-[3-(2-Amnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-2-(3-methoxy-phenyl)-acetamide; 359) N-[3-(2-Amnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyrimidin-7 yl]-3,3-dimethyl-butyramide; 360) N-[3-(2-Arnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyrimidin-7 yl]-3-pyridin-3-yl-propionamide; 361) N-[3-(2-Anino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo( 1,2-a]pyrimidin-7 yl]-acetamide; 362) N-[3-(2-Arnino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[ 1,2-a]pyrimidin-7 yl]-nicotinamide; 363) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrinidin-7-yl]-2-(3-methoxy-phenyl)-acetamide; 364) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3,3-dimethyl-butyramide; 365) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-3-pyridin-3-yl-propionamide; 366) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-nicotinamide; 367) N-[3-(2-Methanesulfonyl-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a] pyrimidin-7-yl]-propionamide; 368) N-[3-(2-Amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidin-7 yl]-propionamide; 369) N-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrinaidin-2-yl} acetamide; 370) Ni - {4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyriinidin-2-yl} -butane 1,4-diamine; 371) N1-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrinidin-2-yl} propane-1,3-diarnine; 220 WO 2006/044509 PCT/US2005/036770 372) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(BODIPY FL) amide; and 373) N-(4-{4-[2-(6-Methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-ylamino} butyl)-(Texas Red-X) amide 374) N-[3-(2-amino-pyrimidin-4-yl)-2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidiri-7 yl]-acetamide; 375) N-{4-[2-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyridin-3-yl]-pyrimidin-2-yl} acetamide. 376) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propylamine, 377) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-acetamide, 378) N-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl]-methanesulfonamide, 379) dimethyl-[3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propyl)-amine, 380) 4-{3-pyridin-2-yl-1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-pyrazol-4-yl}-quinoline, 381) 4-[3-pyridin-2-yl-1-(3-pyrrolidin-1-yl-propyl)-1H-pyrazol-4-yl]-quinoline, 382) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, 383) 2,4-dimethoxy-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrimidine, 384) 3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionic acid, 385) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-IH-indole, 386) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-1H-pyrazol-3-yl]-pyridine, 387) N-hydroxy-3-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-propionamide, 388) 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-I-yl)-ethylamine, 389) N-[2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-ethyl]-methanesulfonamide, 390) 2-methyl-4-methylsulfanyl-6-(3-pyridin- 2 -yl-1H-pyrazol-4-yl)-pyrimidine, 391) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-pyridine, 392) 2-[4-(2,3-dihydro-benzofuran-5-yl)-1H-pyrazol-3-yl]-pyridine, 393) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[d]isoxazole, 394) 3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propionitrile, 395) N-{3-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-propyl} methanesulfonamide, 396) 2-[4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-IH-pyrazol-3-yl]-6-methyl-pyridine, 397) [4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-acetonitrile, 398) N-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethyl} methanesulfonamide, 399) 4-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-2-methylsulfanyl-pyrimidine, 400) 4-(3-pyridin-2-yl-1H-pyrazol-4-yl)-2H-phthalazin- 1-one, 221 WO 2006/044509 PCT/US2005/036770 401) f""[5-(-' yfii-2 yl-T IbyrizoE4-yl)-2,3-dihydro-indol-1-yl]-ethanone, 402) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 403) 3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 404) 6-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-4H-benzo [1,4] oxazin-3-one, 405) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoxaline, 406) 3-(4-nitro-benzyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-y)-3H-quinazolin-4-one, 407) 5-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 408) 4-methyl-7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3,4-dihydro-1H-benzo[e][1,4]diazepine 2,5-dione, 409) 2,3-dimethyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin- 4 -one, 410) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-y1]-[1,2,4]triazolo[1,5-a]pyridine, 410a) 1-methoxy-4-(3-pyridin-2-yl-IH-pyrazol-4-yl)-isoquinoline, 411) 2-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 411 a) 4-(3 -pyridin-2-yl- 1 H-pyrazol-4-yl)-2H-isoquinolin- 1-one, 412) 2-(4-benzo[1,3]dioxol-5-yl-IH-pyrazol-3-yl)-6-trifluoromethyl-pyridine, 412a) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-vinyl-pyridine, 413) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propenyl-pyridine, 414) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-ethyl-pyridine, 415) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-propyl-pyridine, 416) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-cyclopropyl-pyridine, 417) 1-[6-(4-benzo[ 1,3] dioxol-5-yl- 1H-pyrazol-3-yl)-pyridin-2-yl]-ethanol, 418) 4-methoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 419) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinoline, 420) 6-(3-pyridin-2-yl-IH-pyrazol-4-yl)-quinazolin-4-ylamine, 421) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin- 4 -one, 422) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-pyrido[1,2-a]pyrimidin-4-one, 423) 6-[3-(6-cyclopropyl-pyridin-2-yl)-IH-pyrazol-4-y-[1,2,4]triazolo[1,5-a]pyridine, 424) 3-methyl-6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3H-quinazolin-4-one, 425) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo[2.2.2]octane- I -carboxylic acid, 426) 4-(2-{2-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-ethoxy} ethoxy)-bicyclo [2.2.2]octane- 1 -carboxylic acid niethyl ester, 427) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl] bicyclo [2.2.2]octane- 1 -carboxylic acid methyl ester, 428) 2-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-6-isopropyl-pyridine, 222 WO 2006/044509 PCT/US2005/036770 429) 2-(4-benzo[1,3]dioxol-5-yl-5-trifluoromethyl-1H-pyrazol-3-yl)-6-bromo-pyridine, 430) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 431) 6-[3-(6-trifluoromethyl-pyridin-2-y)-1H-pyrazol- 4 -yl]-[1,2,4]triazolo[1,5-a]pyridine, 432) 6-[3-(6-methyl-pyridin-2-yl)-IH-pyrazol-4-yl]-quinoxaline, 432a) 6-[3-(6-cyclopropyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-methyl-3H-quinazolin-4-one, 433) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-b]pyridazine, 433a) 6-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline, 434) 6-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-3-fluoro-2-methyl-pyridine, 435) 7-methoxy-3-methyl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3H-quinazolin-4-one, 436) (4-morpholin-4-yl-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin-4-yl]-amine, 437) 4-isopropoxy-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 438) 6-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-quinolin-4-ylamine, 439) {4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-1-yl]-cyclohexyl} carbamic acid benzyl ester, 440) 4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-pyrazol-I-yl]-cyclohexylamine, 441) N-{4-[4-benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-y)-pyrazol-1-yl]-cyclohexyl} methanesulfonamide, 442) 6-[3-(5-fluoro-6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 443) 7-(3-pyridin-2-yl-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridine, 444) 1-tert-butyl-3-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin- 4 -yl]-urea, 445) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]thiadiazole, 446) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[1,2,5]oxadiazole, 447) 5-(3-Pyridin-2-yl-1H-pyrazol-4-y)-benzooxazole, 448) 4-morpholin-4-yl-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 449) 6-[3-(6-trifluoromethyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoxaline, 450) 4-(4-methoxy-phenyl)-6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazoline, 451) 5-[3-(6-methyl-pyridin-2-y1)-IH-pyrazol-4-yl]-benzo[1,2,5]thiadiazole, 452) 6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzothiazole, 453) 3-(3-methoxy-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 454) 5-methyl-thiophene-2-carboxylic acid [6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quinazolin- 4 yl]-amide, 455) 5-[3-(6-methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-3-phenyl-benzo[c]isoxazole, 456) 3-(4-methoxy-pheny)-5-(3-pyridin- 2 -yl-IH-pyrazol-4-yl)-benzo[c]isoxazole, 457) 3-(4-chloro-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 458) 3-(4-ethyl-phenyl)-5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-benzo[c]isoxazole, 223 WO 2006/044509 PCT/US2005/036770 459) (4-methoxy-phenyl)-[6-(3-pyridin-2-yl-1H-pyrazol-4-yl)-quirnazolin-4-yl]-methanone, 460) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-3-thiophen-3-yl-benzo[c]isoxazole, 461) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid, 462) 5-(3-Pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid methylamide, 463) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid dimethylamide, 464) 5-(3-pyridin-2-yl-1H-pyrazol-4-y)-1H-indazole-3-carboxylic. acid (2,2-dimethyl propyl)-amide, 465) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid phenylamide, 466) morpholin-4-yl-[5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazo1-3-yl]-methanone, 467) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid benzylamide, 468) 5-(3-pyridin-2-yl-1H-pyrazol-4-yl)-1H-indazole-3-carboxylic acid cyclopentylamide, 469) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-1H-imidazol-2-yl) benzamide; 470) 4-[4-benzo[1,3]dioxol-5-yl-5-(2-methylsulfanyl-pyrimidin-4-yl)-lH-imidazol-2-yl] benzonitrile; 471) 4-[5-(2-methanesulfonyl-pyrimidin-4-yl)-4-(6-methyl-pyridii- 2 -yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 472) 4-[5-(2-methoxy-pyrinidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1 H-imidazol-2-yl] bicyclo [2.2.2] octane-1 -carboxylic acid methyl ester; 473) 4-[5-(2-hydroxy-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1IH-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 474) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2] octane-1 -carboxylic acid methyl ester; 475) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane- 1 -carboxylic acid; 476) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid amide; 477) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl] -bicyclo[2.2.2]octane- 1 -carboxylic acid hydroxyamide; 478) 4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]octane-1-carboxylic acid methoxy-amide; 479) 4-[5-(2-amino-pyrimidin-4-yl)-4-(6-methyl-pyridin-2-yl)-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1-carboxylic acid; 480) {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyridin- 2 -yl)-1H-imidazol-2 yl]-bicyclo[2.2.2]oct-1-yl}-carbamic acid benzyl ester; 224 WO 2006/044509 PCT/US2005/036770 481) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyfidin- 2 -yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-acetamide; 482) N-{4-[5-(2-cyclopropylamino-pyrimidin-4-y1)-4-(6-methyl-pyfidin- 2 -yl)-1H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-methanesulfonamide; 483) N- {4-[5-(2-cyclopropylamino-pyrimidin-4-yl)-4-(6-methyl-pyfidin- 2 -yl)- 1 H-imidazol 2-yl]-bicyclo[2.2.2]oct-1-yl}-2,2,2-trifluoro-acetamide; 484) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin-4-yl)- 1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 485) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-irnidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 486) 6-[2-tert-butyl-5-(2-cyclopropyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 487) 6-[5-(2-byclopropyl-pyrimidin-4-y1)-3H-imidazol-4-y1]-quinoxaline; 488) {4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-iinidazol-2-yl] bicyclo[2.2.2]oct-1-yl} -methanol; 489) 6-[5-(2-trifluoromethyl-pyrimidin-4-y1)-3H-imidazol-4-y1]-quinoxaline; 490) 6-[2-tert-butyl-5-(2-trifluoromethyl-pyrimidin-4-yl)-3H-imidazol-4-yl]-quinoxaline; 491) 4-[5-quinoxalin-6-yl-4-(2-trifluoromethyl-pyrimidin- 4 -yl)-1H-imidazol-2-yl] piperidine-1 -carboxylic acid benzyl ester; 492) 4-[4-(2-cyclopropyl-pyrimidin-4-yl)-5-quinoxalin- 6 -yl-1H-imidazol-2-yl]-piperidine-1 carboxylic acid benzyl ester; 493) 6-[5-(2-cyclopropyl-pyrimidin-4-yl)- 2 -(1-methanesulfonyl-piperidin-4-y)-3H-imidazol 4-yl]-quinoxaline; 494) 4-[5-(2-methyl-pyrimidin-4-yl)-4-[1,2,4]triazolo[4,3-a]pyridin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol; 495) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid amide; 496) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-IH-imidazol-2-yl] bicyclo[2.2.2]octane-1 -carboxylic acid; 497) 4-[4-(2-methyl-pyrimidin-4-yl)-5-[1,2,4]triazolo[1,5-a]pyridine-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octane- 1 -carboxylic acid methyl ester; 498) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]-cyclohexanol; and 499) 4-[4-(2-methyl-pyrimidin-4-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl] bicyclo[2.2.2]octan-1-ol, 500) 4-(4-benzo[1,3]dioxol-5-yl-1H-pyrazol-3-yl)-2-methyl-pyriniidine, 500a) 6-[3-(2-methyl-pyrimidin-4-yl)-1H-pyrazol-4-yl]-[1,2,4]triazolo[1,5-a]pyridine, 225 WO 2006/044509 PCT/US2005/036770 501) 6- 3 Z( ' 1ti66ii 6th3-pynmidini-4-y1)- 1H-.pyrazol-4-ylP[ 1 ,2,4]triazc:lo[ 1,5-a]pyridine, 502) 6-[3-(2-methyl-pyrimidin-4-yl)- 1H-pyrazol-4-yl] -quinoxaline, 5 02a) 6-[3 -(2-trifluoromethyl-pyrimidin-4-yl)- 1H-pyrazol-4-yl] -quinoxaliale, 503) 6-[3-(2-cyclopropyl-pyrimidin-4-yl)- 1H-pyrazol-4-yl] -quinoxaline, 504) 4-(4-benzo[ 1,3]dioxol-5-yl-l1H-pyrazol-3-yl)-2-trifluoromethyl-pyriniidine, 505) 7-[3-(2-trifluoromethyl-pyrimidin-4-yl)- IH-pyrazol-4-yl] 41 ,2,4]triazc~1o[ 1,5-a]pyridine, or 506) 6-[3-(2-Trifluoromethyl-pyrimidin-4-yl)- 1H-pyrazol-4-yl]-quinoline. 226