CA2465247A1 - Benzimidazoles and analogues and their use as protein kinases inhibitors - Google Patents
Benzimidazoles and analogues and their use as protein kinases inhibitors Download PDFInfo
- Publication number
- CA2465247A1 CA2465247A1 CA002465247A CA2465247A CA2465247A1 CA 2465247 A1 CA2465247 A1 CA 2465247A1 CA 002465247 A CA002465247 A CA 002465247A CA 2465247 A CA2465247 A CA 2465247A CA 2465247 A1 CA2465247 A1 CA 2465247A1
- Authority
- CA
- Canada
- Prior art keywords
- benzoimidazol
- carboxylic acid
- pyrazol
- indazol
- dimethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Abstract
The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
Claims (238)
1. A pharmaceutical composition comprising a compound of general formula (Ix) wherein X represents C-R2 and W, Y and Z, which may be identical or different, represent CH or CR3; or W represents CH, X represents N, Y represents CH or CR3, and Z represents CH
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR-I; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
AS represents H or alkyl;
R 1 represents aryl or heteroaryl, each optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NYlY2, -C(=O)OR4, -N(R6)C(°O)R4~ -N(R6)C(°O)NYlY2~ -N(R5)C(=O)OR4~ -N(R6)SO2R4~ -N(R~)SO2N1'IY2~
-NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYIY2, -OS(O)nR4, -S(O)nR4, -S(O)nNYlY2 and -S(O) nOR4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NYIY2, -C(=O)OR4, -NYlY2, -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -N(R6)C(=O)OR4, -N(R6)SOzR4, -N(R6)S02NYIY2, -OR4, _OCF2H, -OCF3, -OC(=O)R4, -OC(=O)~'1Y2~ -s(O)nR4~ -S(O)nI'n'lY2 or -S(O) nOR4; or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY 1 Y2, -C(=O)OR4, -NYIY2, -N(R6)C(=O)R4, -N(R~)C(=O)NYIY2, -N(R6)C(=O)OR4, -N(R6)SOZR4, -N(R6)S02NYIY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYIY2, -S(O)nR4, -S(O)nNYlY2 or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NY1Y2, -NY1Y2, -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -OR5, or the group -NY1Y2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate;
together with one or more pharmaceutically acceptable carriers or excipients.
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR-I; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
AS represents H or alkyl;
R 1 represents aryl or heteroaryl, each optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NYlY2, -C(=O)OR4, -N(R6)C(°O)R4~ -N(R6)C(°O)NYlY2~ -N(R5)C(=O)OR4~ -N(R6)SO2R4~ -N(R~)SO2N1'IY2~
-NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYIY2, -OS(O)nR4, -S(O)nR4, -S(O)nNYlY2 and -S(O) nOR4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NYIY2, -C(=O)OR4, -NYlY2, -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -N(R6)C(=O)OR4, -N(R6)SOzR4, -N(R6)S02NYIY2, -OR4, _OCF2H, -OCF3, -OC(=O)R4, -OC(=O)~'1Y2~ -s(O)nR4~ -S(O)nI'n'lY2 or -S(O) nOR4; or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY 1 Y2, -C(=O)OR4, -NYIY2, -N(R6)C(=O)R4, -N(R~)C(=O)NYIY2, -N(R6)C(=O)OR4, -N(R6)SOZR4, -N(R6)S02NYIY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYIY2, -S(O)nR4, -S(O)nNYlY2 or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NY1Y2, -NY1Y2, -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -OR5, or the group -NY1Y2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate;
together with one or more pharmaceutically acceptable carriers or excipients.
2. A pharmaceutical composition according to claim 1 wherein R2 and R3 form a group selected from -O-CH2-O-, -O-CH2-CH2-O-; -CH2-O-CH2-, -CH2-N(R14)-CH2-, -CH2-CH2-CH2-, -CH2-C(CH3)2-CH2-, -CH2-O-CH2-CH2-, -CH2-N(R14)-CH2-CH2-, -CHI-CHI-CHI-CHI-, -CH2-C(CH3)2-CH2-CH2-, -CH=CH-CH=CH-, -N=CH-CH=CH-, -CH=N-CH=CH-, -CH=CH-N=CH- and -CH=CH-CH=N, where R14 is H or alkyl.
3. A compound of general formula (Ix) wherein X represents C-R2 and W, Y and Z, which may be identical or different, represent CH or CR3; or W represents CH, X represents N, Y represents CH or CR3, and Z represents CH
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR3; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
AS represents H or alkyl;
R1 represents aryl or heteroaryl, each optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY 1 Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY 1 Y2, -NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYlY2, -OS(O)nR4, -S(O)nR4, -S(O)nNY1Y2 and -S(O) n OR4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)S02NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1y2, -s(O)nR4, -S(O)nNY1y2 or -S(O) nOR4, or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)nNY1Y2 or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NY1Y2, -NY1Y2 -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -OR5, or the group -NY1Y2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR3; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
AS represents H or alkyl;
R1 represents aryl or heteroaryl, each optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY 1 Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY 1 Y2, -NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYlY2, -OS(O)nR4, -S(O)nR4, -S(O)nNY1Y2 and -S(O) n OR4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)S02NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1y2, -s(O)nR4, -S(O)nNY1y2 or -S(O) nOR4, or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)nNY1Y2 or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NY1Y2, -NY1Y2 -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -OR5, or the group -NY1Y2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
4. A compound of formula (Ix) wherein X represents C-R2 and W, Y and Z, which may be identical or different, represent CH or CR3; or W represents CH, X represents N, Y represents CH or CR3, and Z represents CH
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR3; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
A5 represents H or alkyl;
R1 is a pyrazolyl moiety in which R7 is hydrogen or alkyl, and R8 and R9 are independently selected from hydrogen, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(Rf)SO2NYlY2, -NY1Y2, -OR4, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)n R4 and -S(O)2NY1Y2; or R8 and R9 together with the carbon atoms to which they are attached form (i) a 5 to 8 membered carbocyclic ring optionally substituted by one or more carbocyclic ring substituents; (ii) a phenyl ring optionally substituted by one or more aryl group substituents;
(iii) a S or 6 membered heteroaromatic ring in which one or more of the ring members is/are nitrogen, oxygen or sulfur and which is optionally substituted by one or more groups selected from haloalkyl, hydroxy, halo, cyano, nitro, R4, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)SO2R4,-NY1Y2 and -OR5;
or (iv) a 5 or 6 membered heterocyclic ring optionally substituted by alkyl or oxo, and containing a heteroatom-containing group selected from O, S, SO2, and NY5, where Y5 is hydrogen, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4 or -SO2R4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)n NY1Y2 or -S(O) nOR4; or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=0)NYlY2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)n or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NYlY2, -NY1Y2, -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -ORS, or the group -NYlY2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate;
provided that the compound is other than 2-(2H-pyrazol-3-yl)-I H-benzoimidazole; 2-(5-methyl-2H-pyrazol-3-yl)-11-1-benzoimidazole; 5-methyl-6-[2-(2H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-4,5-dlHydro-2H-pyridazin-3-one; 5-methyl-6-[2-(2H-pyrazol-3-yl)-lH-benzoimidazol-4-yl]-4,5-dlHydro-2H-pyridazin-3-one; 3,5-bis(benzimidazol-2-yl)-1H-pyrazole; 5,6-dimethyl-2-(5-methyl-1H-pyrazol-3-y1)-1H-benzoimidazole; 6-methyl-2-(5-methyl-1H-pyrazol-3-yl)-1H-benzoimidazole; 5,6-dichloro-2-(5-methyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 5-nitro-2-(5-methyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 2-(5-methyl-lH-pyrazole-3-yl)-1H-benzoimidazole-5-carboxylic acid; 2-(S-phenyl-lH-pyrazole-3-yl)-lH-benzoimidazole; 5,6-dimethyl-2-(5-phenyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 5-methyl-2-(5-phenyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 6-chloro-2-(5-methyl-1H-pyrazole-3-yl)-lH-benzoimidazole; 5-chloro-2-(5-phenyl-1H-pyrazole-3-yl)-lH-benzoimidazole;
5,6-dichloro-2-(5-phenyl-lH-pyrazole-3-yl)-1H-benzoimidazole; N-[2-(5-isoquinolin-4-yl-1H-indazol-3-yl)-3H-benzoimidazol-5-yl]-methanesulfonamide; 3-(lH-benzoimidazol-2-yl)-5-(lH-indazol-4-yl)-1H-indazole, 3-[3-(1H-benzoimidazol-2-yl)-lH-indazol-5-yl]-2-methoxyphenol; 4-[3-(lH-benzoimidazol-2-yl)-1H-indazol-5-yl]isoquinoline; 4-{3-[6-(4-methyl-piperazin-I-yl)-1H-benzoimidazol-2-yl]-1H-indazol-5-yl}-isoquinoline; 4-[3-(4-chloro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]-isoquinoline; 4-[2-(1H-indazol-3-yl)-lH-benzoimidazol-5-yl]-phenol; 3-[S-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-lI-1-indazole; 3-[5-(4-methoxy-phenyl)-lH-benzoimidazol-2-yl]-lH-indazole; 3-[5-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-1H-indazole; 3-(1H-benzoimidazol-2-yl)-5-phenyl-1H-indazole; 2-(4-bromo-1-methyl-1H-pyrazol-3-yl)-lH-benzoimidazole; 2-(5-tert-butyl-1H-pyrazol-3-yl)-1H-benzoimidazole; 3-(lH-benzoimidazol-2-yl)-6-(3-methoxy-phenyl)-1H-indazole; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid; 5-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino}-2-hydroxy-benzoic acid methyl ester; 5-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino}-furan-2-carboxylic acid methyl ester; 3-(lH-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-4-methoxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (5-hydroxy-lH-pyrazol-3-yl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (lH-pyrazol-3-yl)-amide; [3-(1H-benzoimidazol-2-yl)-lH-indazol-6-yl]-[4-(2-hydroxy-ethyl)-piperidin-1-yl]-methanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (9H-purin-6-yl)-amide; 3-(1H-benzoimidazol-2-yl)-lH-indazole-6-carboxylic acid dimethylamide; [3-(lH-benzoimidazol-2-yl)-lH-indazol-6-yl]-morpholin-4-yl-methanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyrazin-2-ylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid cyclohexylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (1H-indazol-5-yl)-amide; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-pyrrolidin-1-yl-methanone;
3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (1H-indazol-5-yl)-amide; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-[4-(furan-2-carbonyl)-piperazin-1-yl]-methanone; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-(4-methyl-piperazin-1-yl)-methanone; 1-{4-[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-piperazin-1-yl)-ethanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (6-methoxy-pyridin-3-yl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyridin-4-ylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (2-morpholin-4-yl-ethyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (2-hydroxy-ethyl)-methyl-amide; 3-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino)-butyric acid ethyl ester; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-propyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid phenylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyridin-3-ylamide; 3-(6-methoxy-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-6-pyridin-4-yl-1H-indazole; 3-(5-chloro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5-fluoro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6-tort-butyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6,7-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-difluoro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-fluoro-4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-2,3-dimethyl-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-2-methyl-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid cyclopropylamide; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-sulfonic acid amide; 4-[3-(6-dimethylamino-1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-carboxylic acid methylamide; 3-methoxy-4-{3-[6-(4-methyl-piperazin-1-yl)-1H-benzoimidazol-2-yl]-1H-indazol-6-yl)-phenol; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide; 4-[3-(1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol;
3-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-2-methoxy-phenol; 3-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3,5-dimethyl-phenol;
4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-G-yl]-3-phenoxy-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1 H-indazol-6-yl]-benzene-1,3-diol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-2-methoxy-phenol; N-{3-[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-phenyl}-benzamide; 6-[2-(1,5-dimethyl-1H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-5-methyl-4,5-dihydro-2H-pyridazin-3-one; 5-methyl-6-[2-(1-methyl-1H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-4,5-dihydro-2H-pyridazin-3-one; 8-(1,5-dimethyl-1H-pyrazol-3-yl)-7H-purine; 2-(1,5-dimethyl-1H-pyrazol-3-yl)-1H-imidazo[4,5-b]pyridine or 2-(5-methyl-1H-pyrazol-3-yl)-1H-imidazo[4,5-b]pyridine.
or CR3; or W represents N, X represents CH or CR2, Y represents CH and CR3, and Z
represents CH or CR3; or W represents N, X represents CH or CR2, Y represents N, and Z is CH or CR3; or W represents N, X represents CH or CR2, Y represents CH or CR3, and Z
represents N; or W represents N, X represents N, Y represents CH or CR3, and Z represents CH or CR3;
A5 represents H or alkyl;
R1 is a pyrazolyl moiety in which R7 is hydrogen or alkyl, and R8 and R9 are independently selected from hydrogen, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(Rf)SO2NYlY2, -NY1Y2, -OR4, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)n R4 and -S(O)2NY1Y2; or R8 and R9 together with the carbon atoms to which they are attached form (i) a 5 to 8 membered carbocyclic ring optionally substituted by one or more carbocyclic ring substituents; (ii) a phenyl ring optionally substituted by one or more aryl group substituents;
(iii) a S or 6 membered heteroaromatic ring in which one or more of the ring members is/are nitrogen, oxygen or sulfur and which is optionally substituted by one or more groups selected from haloalkyl, hydroxy, halo, cyano, nitro, R4, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)SO2R4,-NY1Y2 and -OR5;
or (iv) a 5 or 6 membered heterocyclic ring optionally substituted by alkyl or oxo, and containing a heteroatom-containing group selected from O, S, SO2, and NY5, where Y5 is hydrogen, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4 or -SO2R4;
R2 and R3 are such that:
R2 and R3, which may be identical or different, represent H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)n NY1Y2 or -S(O) nOR4; or R2 represents H, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=0)NYlY2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)n or -S(O) nOR4 and R3 represents alkyl, haloalkyl, halogen and OR6; or R2 and R3 groups on adjacent carbon atoms may form a 5- to 6-membered carbon-based ring containing one or more heteroatoms, which may be identical or different, chosen from O, N and S, and which may be optionally substituted by alkyl;
R4 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each optionally substituted with one or more substituents selected from alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, halo, hydroxy, hydroxyalkyl, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NYlY2, -NY1Y2, -OR5 or alkyl substituted by -NY3Y4;
R5 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
R6 is alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;
n is zero or an integer 1 or 2;
Y1 and Y2 are independently hydrogen, alkenyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, heterocycloalkylalkyl or alkyl optionally substituted by one or more groups selected from cyano, aryl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 and -ORS, or the group -NYlY2 may form a cyclic amine;
Y3 and Y4 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group -NY3Y4 may form a cyclic amine;
where all the alkyl, alk, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals are optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate;
provided that the compound is other than 2-(2H-pyrazol-3-yl)-I H-benzoimidazole; 2-(5-methyl-2H-pyrazol-3-yl)-11-1-benzoimidazole; 5-methyl-6-[2-(2H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-4,5-dlHydro-2H-pyridazin-3-one; 5-methyl-6-[2-(2H-pyrazol-3-yl)-lH-benzoimidazol-4-yl]-4,5-dlHydro-2H-pyridazin-3-one; 3,5-bis(benzimidazol-2-yl)-1H-pyrazole; 5,6-dimethyl-2-(5-methyl-1H-pyrazol-3-y1)-1H-benzoimidazole; 6-methyl-2-(5-methyl-1H-pyrazol-3-yl)-1H-benzoimidazole; 5,6-dichloro-2-(5-methyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 5-nitro-2-(5-methyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 2-(5-methyl-lH-pyrazole-3-yl)-1H-benzoimidazole-5-carboxylic acid; 2-(S-phenyl-lH-pyrazole-3-yl)-lH-benzoimidazole; 5,6-dimethyl-2-(5-phenyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 5-methyl-2-(5-phenyl-1H-pyrazole-3-yl)-1H-benzoimidazole; 6-chloro-2-(5-methyl-1H-pyrazole-3-yl)-lH-benzoimidazole; 5-chloro-2-(5-phenyl-1H-pyrazole-3-yl)-lH-benzoimidazole;
5,6-dichloro-2-(5-phenyl-lH-pyrazole-3-yl)-1H-benzoimidazole; N-[2-(5-isoquinolin-4-yl-1H-indazol-3-yl)-3H-benzoimidazol-5-yl]-methanesulfonamide; 3-(lH-benzoimidazol-2-yl)-5-(lH-indazol-4-yl)-1H-indazole, 3-[3-(1H-benzoimidazol-2-yl)-lH-indazol-5-yl]-2-methoxyphenol; 4-[3-(lH-benzoimidazol-2-yl)-1H-indazol-5-yl]isoquinoline; 4-{3-[6-(4-methyl-piperazin-I-yl)-1H-benzoimidazol-2-yl]-1H-indazol-5-yl}-isoquinoline; 4-[3-(4-chloro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]-isoquinoline; 4-[2-(1H-indazol-3-yl)-lH-benzoimidazol-5-yl]-phenol; 3-[S-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-lI-1-indazole; 3-[5-(4-methoxy-phenyl)-lH-benzoimidazol-2-yl]-lH-indazole; 3-[5-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-1H-indazole; 3-(1H-benzoimidazol-2-yl)-5-phenyl-1H-indazole; 2-(4-bromo-1-methyl-1H-pyrazol-3-yl)-lH-benzoimidazole; 2-(5-tert-butyl-1H-pyrazol-3-yl)-1H-benzoimidazole; 3-(lH-benzoimidazol-2-yl)-6-(3-methoxy-phenyl)-1H-indazole; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid; 5-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino}-2-hydroxy-benzoic acid methyl ester; 5-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino}-furan-2-carboxylic acid methyl ester; 3-(lH-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-4-methoxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (5-hydroxy-lH-pyrazol-3-yl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (lH-pyrazol-3-yl)-amide; [3-(1H-benzoimidazol-2-yl)-lH-indazol-6-yl]-[4-(2-hydroxy-ethyl)-piperidin-1-yl]-methanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (9H-purin-6-yl)-amide; 3-(1H-benzoimidazol-2-yl)-lH-indazole-6-carboxylic acid dimethylamide; [3-(lH-benzoimidazol-2-yl)-lH-indazol-6-yl]-morpholin-4-yl-methanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyrazin-2-ylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid cyclohexylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (1H-indazol-5-yl)-amide; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-pyrrolidin-1-yl-methanone;
3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (1H-indazol-5-yl)-amide; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-[4-(furan-2-carbonyl)-piperazin-1-yl]-methanone; [3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-(4-methyl-piperazin-1-yl)-methanone; 1-{4-[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-piperazin-1-yl)-ethanone; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (6-methoxy-pyridin-3-yl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyridin-4-ylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (2-morpholin-4-yl-ethyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (2-hydroxy-ethyl)-methyl-amide; 3-{[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-amino)-butyric acid ethyl ester; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-hydroxy-propyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid phenylamide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid pyridin-3-ylamide; 3-(6-methoxy-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-6-pyridin-4-yl-1H-indazole; 3-(5-chloro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5-fluoro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6-tort-butyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(6,7-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(5,6-difluoro-1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (3-fluoro-4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-2,3-dimethyl-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-2-methyl-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid (4-hydroxy-phenyl)-amide; 3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carboxylic acid cyclopropylamide; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-sulfonic acid amide; 4-[3-(6-dimethylamino-1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-carboxylic acid methylamide; 3-methoxy-4-{3-[6-(4-methyl-piperazin-1-yl)-1H-benzoimidazol-2-yl]-1H-indazol-6-yl)-phenol; 2-[6-(4-hydroxy-2-methoxy-phenyl)-1H-indazol-3-yl]-3H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide; 4-[3-(1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol;
3-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-2-methoxy-phenol; 3-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3,5-dimethyl-phenol;
4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-G-yl]-3-phenoxy-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1 H-indazol-6-yl]-benzene-1,3-diol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-3-methoxy-phenol; 4-[3-(1H-benzoimidazol-2-yl)-1H-indazol-6-yl]-2-methoxy-phenol; N-{3-[3-(1H-benzoimidazol-2-yl)-1H-indazole-6-carbonyl]-phenyl}-benzamide; 6-[2-(1,5-dimethyl-1H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-5-methyl-4,5-dihydro-2H-pyridazin-3-one; 5-methyl-6-[2-(1-methyl-1H-pyrazol-3-yl)-3H-benzoimidazol-5-yl]-4,5-dihydro-2H-pyridazin-3-one; 8-(1,5-dimethyl-1H-pyrazol-3-yl)-7H-purine; 2-(1,5-dimethyl-1H-pyrazol-3-yl)-1H-imidazo[4,5-b]pyridine or 2-(5-methyl-1H-pyrazol-3-yl)-1H-imidazo[4,5-b]pyridine.
5. A compound according to claim 3 wherein R1 is optionally substituted heteroaryl.
6. A compound according to claim 5 wherein R1 is optionally substituted dihydrofuropyrazolyl, imidazolyl, indazolyl, indolyl, isoxazolyl, oxodihydropyridazinyl, oxodihydropyridinopyrazolyl, oxodihydropyridinyl, oxotetrahydropyrrolopyrazolyl, pyrazolyl, thiazolyl, thienopyrazolyl, tetrahydrocyclopentapyrazolyl, tetrahydroindazolyl, tetrahydropyranopyrazolyl, tetahydropyridinopyrazolyl, tetrahydropyrrolopyrazolyl or triazolyl.
7. A compound according to claim 5 heteroaryl is optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -NYlY2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NYlY2, -S(O)nR4 and -S(O)2NY1Y2.
8. A compound according to claim 6 wherein dihydrofuropyrazolyl, imidazolyl, indazolyl, indolyl, isoxazolyl, oxodihydropyridazinyl, oxodihydropyridinopyrazolyl, oxodihydropyridinyl, oxotetrahydropyrrolopyrazolyl, pyrazolyl, thiazolyl, thienopyrazolyl, tetrahydrocyclopentapyrazolyl, tetrahydroindazolyl, tetrahydropyranopyrazolyl, tetahydropyridinopyrazolyl, tetrahydropyrrolopyrazolyl or triazolyl is optionally substituted by one or more groups selected from carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(RG)SO2R4, -N(R6)SO2R4, -NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4 and -S(O)2NY1Y2.
9. A compound according to claim 3 wherein R1 is where R7 is hydrogen or alkyl, and R8 and R9 are independently selected from hydrogen, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NYlY2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(Rf)SO2R4, -N(R6)SO2NY1Y2, -NY1Y2, -OR4, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4 and -S(O)2NY1Y2; or R8 and R9 together with the carbon atoms to which they are attached form (i) a 5 to 8 membered carbocyclic ring optionally substituted by one or more carbocyclic ring substituents; (ii) a phenyl ring optionally substituted by one or more aryl group substituents; (iii) a 5 or 6 membered heteroaromatic ring in which one or more of the ring members is/are nitrogen, oxygen or sulfur and which is optionally substituted by one or more groups selected from haloalkyl, hydroxy, halo, cyano, nitro, R4, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)SO2R4, -NY1y2 and -OR5; or (iv) a 5 or 6 membered heterocyclic ring optionally substituted by alkyl or oxo, and containing a heteroatom-containing group selected from O, S, SO2, and NY5 ,where Y5 is hydrogen, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4 or -SO2R4.
10. A compound according to any one of claims 3 to 9 wherein W is CH; X is CR2; Y is CH or CR3 ;and Z is CH or CR3
11. A compound according to any one of claims 3 to 9 wherein W is CH; when X
is N; Y is CH or CR3 ;and Z is CH or CR3.
is N; Y is CH or CR3 ;and Z is CH or CR3.
12. A compound according to any one of claims 3 to 9 wherein W is N; X is CH
or CR2; Y is CH
or CR3 ;and Z is CH or CR3.
or CR2; Y is CH
or CR3 ;and Z is CH or CR3.
13. A compound according to any one of claims 3 to 9 wherein W is N; X is CH
or CR2; Y is CH
or CR3 ; and Z is N.
or CR2; Y is CH
or CR3 ; and Z is N.
14. A compound according to claim 3 of formula (Ixa) wherein R7 is hydrogen or alkyl;
R8 and R9 are independently selected from hydrogen, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)S02R4, -NYlY2, -OR4, -OC(=O)R4, -OC(=O)NYlY2, -S(O)n R4 and -S(O)2NY1Y2; or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
R8 and R9 are independently selected from hydrogen, carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)S02R4, -NYlY2, -OR4, -OC(=O)R4, -OC(=O)NYlY2, -S(O)n R4 and -S(O)2NY1Y2; or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
15. A compound according to claim 14 wherein W is CH; X is CH, Y is CH; and Z
is CH or C-CH3.
is CH or C-CH3.
16. A compound according to claim 14 wherein W represents CH; X represents CH;
Z represents CH; and Y represents C-C1-4alkyl; C-aryl; C-CN; C-NO2; C-halo; C-haloalkyl; C-heteroaryl; C-OR4;
C-C(=O)R4; C-C=O)NY1Y2; C-C(=O)OR4; C-NHC(=O)R4; C-CH(OH)aryl; C-S(O)2NY1Y2;
or C-S(O)nR4.
Z represents CH; and Y represents C-C1-4alkyl; C-aryl; C-CN; C-NO2; C-halo; C-haloalkyl; C-heteroaryl; C-OR4;
C-C(=O)R4; C-C=O)NY1Y2; C-C(=O)OR4; C-NHC(=O)R4; C-CH(OH)aryl; C-S(O)2NY1Y2;
or C-S(O)nR4.
17. A compound according to claim 16 wherein Y represents C-C(=O)-NH-CH3, C-C(=O)-N(CH3)2, C-C(=O)-NH-CHCH3 , C-C(=O)-NH-CH(CH3)2, C-C(=O)-NH-C(CH3)2-CH2OH, C-C(=O)-NH-CH2CH2CN, C-C(=O)-NH-CH2CH2OCH3,
18. A compound according to claim 14 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F, or and Z represents CH.
19. A compound according to claim 14 wherein W represents CH; X represents CH;
Y represents C-CH3 ; and Z represents C-CH3.
Y represents C-CH3 ; and Z represents C-CH3.
20. A compound according to claim 14 wherein W represents CH; X represents CR2 ; and Y
represents CR3, where R2 and R3 form the group -CH2-O-CH2; and Z represents CH.
represents CR3, where R2 and R3 form the group -CH2-O-CH2; and Z represents CH.
21. A compound according to claim 14 wherein W represents CH; X represents CR2 ; Y
represents CR3, where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3, where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
22. A compound according to claim 14 wherein R7 represents hydrogen.
23. A compound according to claim 14 wherein R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2 or -OR5.
24. A compound according to claim 14 wherein R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2 or CH(CH3)CH2CH3;
25. A compound according to claim 14 wherein R9 represents hydrogen, C1-7alkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, where R4 is alkyl optionally substituted by aryl, cycloalkyl, heteroaryl, heterocycloalkyl, or where R4 is NY1Y2 or -OR5, or where R4 is aryl, or where R4 is cycloalkyl, or where R4 is heteroaryl, or where R4 is heterocycloalkyl; or R9 represents -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2.
26. A compound according to claim 14 wherein R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2, -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH3, -C(=O)-NH-CHCH2CH2, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH, C(=O)-NH-CH2CH2OCH3, -C(=O)-N(CH3)2, -C(=O)-N(CH2CH3)2, NH-C(=O)-CH3, -NH-C(=O)-(CH2)2CH3, -NH-C(=O)-CH(CH3)2, -NH-C(=O)-C(CH3)3, -NH-C(=O)-CH2CH(CH3)2, -NH-C(=O)-CH(CH3)CH2CH3, -NH-C(=O)-CH2C(CH3)3,
27. A compound according to claim 14 wherein W represents CH;
X represents CH;
Y represents CH;
Z represents CH or C-CH3;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2; and R9 represents hydrogen, C1-7alkyl, aryl , -C(=O)NY1Y2, -N(R6)C(=O)R4, particularly -NHC(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2.
X represents CH;
Y represents CH;
Z represents CH or C-CH3;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2; and R9 represents hydrogen, C1-7alkyl, aryl , -C(=O)NY1Y2, -N(R6)C(=O)R4, particularly -NHC(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2.
28. A compound according to claim 14 wherein W represents CH; X represents CH;
Y represents 20 CH; Z represents CH or C-CH3; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3,
Y represents 20 CH; Z represents CH or C-CH3; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3,
29. A compound according to claim 14 wherein W represents CH;
X represents CH;
Z represents CH;
Y represents C-C1-4alkyl, C-aryl, C-Cn, C-NO2, C-halo, C-heteroaryl, C-OR4, C-C(=O)R4, C-C=O) NY1Y2, C-C(-O)OR4, or C-CH(OH)aryl;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2 or -OR5; and R9 represents hydrogen, C1-7alkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)c(=O)NY1Y2.
X represents CH;
Z represents CH;
Y represents C-C1-4alkyl, C-aryl, C-Cn, C-NO2, C-halo, C-heteroaryl, C-OR4, C-C(=O)R4, C-C=O) NY1Y2, C-C(-O)OR4, or C-CH(OH)aryl;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2 or -OR5; and R9 represents hydrogen, C1-7alkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)c(=O)NY1Y2.
30. Acompound according to claim 14 wherein W represents CH; X represents CH;
Z represents
Z represents
31. A compound according to claim 14 wherein W represents CH;
X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-C1;
Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-C1, C-F, or Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2, or -OR3; and R9 represents hydrogen, C1-7lkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2
X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-C1;
Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-C1, C-F, or Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2, or -OR3; and R9 represents hydrogen, C1-7lkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2
32. A compound according to claim 14 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-C1; Y represents C-CH3, C-CH2CH3, R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3], CH2CH2CH3, -CH(CH3)2 , -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH3, -C(=O)-NH-CH2CH2CH3, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
33. A compound according to claim 14 wherein W represents CH;
X represents CH;
Y represents C-CH3;
Z represents C-CH3;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2, or -OR5; and R9 represents hydrogen, C1-7alkyl , aryl, -C(=O)NY1Y2; -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2.
X represents CH;
Y represents C-CH3;
Z represents C-CH3;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl, -SR4, -NY1Y2, or -OR5; and R9 represents hydrogen, C1-7alkyl , aryl, -C(=O)NY1Y2; -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2, or alkyl substituted by -N(R6)C(=O)NY1Y2.
34. A compound according to claim 14 wherein W represents CH; X represents CH;
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3, -S-CH2CH3 or -OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2, -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH2, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3, -S-CH2CH3 or -OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2, -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH2, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
35. A compound according to claim 14 wherein W represents CH;
X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-O-CH2-;
Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl , -SR4 , -NY1Y2 , or -OR5; and R9 represents hydrogen, C1-alkyl , aryl, -C(=O)NY1Y2 ; -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -NY1Y2 , or alkyl substituted by -N(R6)C(=O)NY1Y2
X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-O-CH2-;
Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl , -SR4 , -NY1Y2 , or -OR5; and R9 represents hydrogen, C1-alkyl , aryl, -C(=O)NY1Y2 ; -N(R6)C(=O)R4, -N(R6)C(=O)NYlY2, -NY1Y2 , or alkyl substituted by -N(R6)C(=O)NY1Y2
36. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3, OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2, -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH3, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3, OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2, -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH3, -C(=O)-NH-CH2CH(CH3)2, -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
37. A compound according to claim 14 wherein W represents CH;
X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-;
Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl , -SR4 , -NY1Y2 , or -OR5; and R9 represents hydrogen, C1-7alkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2 or alkyl substituted by -N(R6)C(=O)NY1Y2
X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-;
Z represents CH;
R7 represents hydrogen;
R8 represents hydrogen, C1-4alkyl , -SR4 , -NY1Y2 , or -OR5; and R9 represents hydrogen, C1-7alkyl, aryl, -C(=O)NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -NY1Y2 or alkyl substituted by -N(R6)C(=O)NY1Y2
38. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3 , OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2 , -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH3, -C(=O)-NH-CH2CH(CH3), -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; R8 represents hydrogen, CH3, CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, -S-CH3 , OCH2CH3; and R9 represents hydrogen, -CH3, -CH2CH2CH3, -CH(CH3)2 , -CH2-CH2-CH(CH3)2, phenyl, -C(=O)-NH-CH2CH2CH3, -C(=O)-NH-CH2CH(CH3), -C(=O)-NH-CH(CH3)2, -C(=O)-NH-C(CH3)3, -C(=O)-NH-C(CH3)2CH2OH,
39. A compound according to claim 14 wherein R8 is hydrogen or -CH3; and R9 is -CH2-CH2-CH(CH3)2,
40. A compound according to claim 14 wherein R9 represents hydrogen and R8 represents -CH(CH3)2, -S-CH3, -S-CH2CH3 or .
41. A compound according to claim 14 wherein W is CH;
X is CH;
X is CH;
42. A compound according to claiml4 wherein W is CH; X is C-CH3 or C-CH2CH3; Y
is
is
43. A compound according to claim 14 wherein W is CH; X is C-OCH3; Y is CH, C-CH3, C-CH2CH3, C-C1 or C-OCH3 ; and Z is CH.
44. A compound according to claim 14 wherein W is CH; X is C-OCH2CH3; Y is C-F; and Z is CH.
45. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 atoms form the group -CH2-CH2-CH2-; and Z
represents CH.
represents CR3 where R2 and R3 atoms form the group -CH2-CH2-CH2-; and Z
represents CH.
46. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
47. A compound according to claim 14 wherein Rg is hydrogen or -CH3. and R9 is -C(=O)-NH-CH2CH3 , 48 -C(=O)-NF1-CH2CH,CH3 , -C(=O)-NH-CH(CH3)2 , -C(=O)-NH-CH,CH(CH3)2 , -C(=O)-NH-C(CH3)3 ,
48. W is CH; X is CH; Y is
49. A compound according to claim 14 wherein W is CH; X is C-CH3 or C-CH2CH3;
Y is C-CH3 or C-CH2CH3, C-C1 or C-F; and Z is CH.
Y is C-CH3 or C-CH2CH3, C-C1 or C-F; and Z is CH.
50. A compound according to claim 14 wherein W is CH; X is C-OCH3; Y is C-CH3, C-CH2CH3, C-C1, C-F, or C-OCH3; and Z is CH.
51. A compound according to claim 14 wherein W is CH; X is C-OCH2CH3; Y is C-C1 or C-F; and Z is CH.
52. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
53. A compound according to claim 14 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
54. A compound according to claim 3 of the formula (Ixb) wherein R7 is hydrogen or alkyl;
R10 is carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4 or -S(O)2NY1Y2;
and p is zero, or an integer 1;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
R10 is carboxy, cyano, halo, haloalkyl, hydroxy, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4 or -S(O)2NY1Y2;
and p is zero, or an integer 1;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
55. A compound according to claim 54 wherein W represents CH; X represents CH; Y represents CH; and Z represents CH or C-CH3.
56. A compound according to claim 54 wherein W represents CH; X represents CH; Z represents CH; and Y represents C-C1 alkyl, C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl, C-heteroaryl, C-OR4, C-C(=O)R4 , C-C=O)NY1Y2, C-C(=O)OR4, C-NHC(=O)R4 , C-CH(OH)aryl, C-S(O)2NY1Y2, or C-S(O)n R4
57. A compound according to claim 54 wherein W represents CH; X represents CH; Z represents CH; and Y represents C-CH3, C-CH2CH3,
58. A compound according to claim 54 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCF-12CH3, C-Br or C-C1; Y represents C-CH3, C-CH2CH3,
59. A compound according to claim 54 wherein W represents CH; X represents CH;
Y represents C-CH3; and Z represents C-CH3.
Y represents C-CH3; and Z represents C-CH3.
60. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
61. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
62. A compound according to claim 54 wherein R7 represents hydrogen.
63. A compound according to claim 54 wherein p is zero or one.
64. A compound according to claim 54 wherein R10 represents cyano, halo, C1-4alkyl, -OR4, or -C(=O)NY1Y2.
65. A compound according to claim 54 wherein R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2, -C(=O)-NHCH(CH3)2, or -C(=O)-N(CH3)2.
66. A compound according to claim 54 wherein W represents CH; X represents CH;
Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; and R10 represents cyano, halo, C1-4alkyl, -OR4 or -C(=O)NY1Y2
Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; and R10 represents cyano, halo, C1-4alkyl, -OR4 or -C(=O)NY1Y2
67. A compound according to claim 54 wherein W represents CH; X represents CH;
Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; and R10 represents cyano, chloro, fluoro, methyl, -OCH3 or -OCH2CH3, -C(=O)-NH2, -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; and R10 represents cyano, chloro, fluoro, methyl, -OCH3 or -OCH2CH3, -C(=O)-NH2, -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
68. A compound according to claim 54 wherein W represents CH; X represents CH;
Z
represents CH; Y represents C-C1-4alkyl, C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl, C-OR4, C-C(=O)R4 , C-C=O)NY1Y2, -C(=O)OR4, C-NHC(=O)R4, C-S(O)2NY1Y2, or C-S(O)nR4 ;
represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4, -C(=O)NY1Y2
Z
represents CH; Y represents C-C1-4alkyl, C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl, C-OR4, C-C(=O)R4 , C-C=O)NY1Y2, -C(=O)OR4, C-NHC(=O)R4, C-S(O)2NY1Y2, or C-S(O)nR4 ;
represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4, -C(=O)NY1Y2
69. A compound according to claim 54 wherein W represents CH; X represents CH;
Z
represents CH; Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3,
Z
represents CH; Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3,
70. A compound according to claim 54 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-C1; Y represents C-CH3, C-CH2CH3, Z represents CH;
R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, OR4, or -C(=O)NY1Y2
R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, OR4, or -C(=O)NY1Y2
71. A compound according to claim 54 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-C1; Y represents C-CH3, C-CH2CH3, ; Z represents CH;
R7 represents hydrogen; p is zero or one; R10 represents cyano, halo, chloro, fluoro, methyl], -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
R7 represents hydrogen; p is zero or one; R10 represents cyano, halo, chloro, fluoro, methyl], -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
72. A compound according to claim 54 wherein W represents CH; X represents CH;
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4, or -C(=O)NY1Y2
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4, or -C(=O)NY1Y2
73. A compound according to claim 54 wherein W represents CH; X represents CH;
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
Y
represents C-CH3; Z represents C-CH3; R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
74. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4 , or -C(=O)NY1Y2
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4 , or -C(=O)NY1Y2
75. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2, -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2, -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
76. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4 , or -C(=O)NY1Y2
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; p is zero or one; and R10 represents cyano, halo, C1-4alkyl, -OR4 , or -C(=O)NY1Y2
77. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2- ; Z represents CH;
R7 represents hydrogen; p is zero or one; and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2 , -C(=O)-NHCH(CH3)2 or -C(=O)-N(CH3)2.
78. A compound according to claim 54 wherein R7 represents hydrogen and p is zero.
79. A compound according to claim 54 wherein R7 represents hydrogen; p is one;
and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2, -C(=O)-N1-1CH(CH3)2 or -C(=O)-N(CH3)2.
and R10 represents cyano, chloro, fluoro, methyl, -OCH3, -OCH2CH3, -C(=O)-NH2, -C(=O)-N1-1CH(CH3)2 or -C(=O)-N(CH3)2.
80. A compound according to claim 54 wherein W is CH; X is CH; Y is CH, C-CH2CH3,
81. A compound according to claim 54 wherein W is CH; X is C-CH3 or C-CH2CH3;
Y is C-CH3, C-CH2CH3, C-CH(CH3)2, C-Br , C-C1, C-F and Z is CH.
Y is C-CH3, C-CH2CH3, C-CH(CH3)2, C-Br , C-C1, C-F and Z is CH.
82. A compound according to claim 54 wherein W is CH; X is C-OCH3; Y is CH, C-CH3, C-CH2CH3, C-C1 or C-OCH3; and Z is CH.
83. A compound according to claim 54 wherein W is CH; X is C-OCH2CH3; Y is C-F
and Z is CH.
and Z is CH.
84. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
85. A compound according to claim 54 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
86. A compound according to claim 54 wherein R7 represents hydrogen and p is zero.
87. A compound according to claim 54 wherein R7 represents hydrogen; p is one;
and R10 represents -OCH3, -OCHZCH3 or -C(=O)-NHCH(CH3)2 attached to position 5 of the indazolyl ring.
and R10 represents -OCH3, -OCHZCH3 or -C(=O)-NHCH(CH3)2 attached to position 5 of the indazolyl ring.
88. A compound according to claim 54 wherein W is CH; X is C-CH3 or C-CH2CH3;
Y is C-CH3 or C-CH2CH3 and Z is CH.
Y is C-CH3 or C-CH2CH3 and Z is CH.
89. A compound according to claim 3 of the formula (Ixc) wherein R7 is hydrogen or alkyl;
is a C5-8cycloalkyl ring; and R12 is acyl, acylamino, alkoxy, alkoxycarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, aroyl, aroylamino, aryl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxycarbonyl, arylsulfinyl, arylsulfonyl, arylthio, carboxy or an acid bioisostere, cyano, cycloalkyl, halo, heteroaroyl, heteroaryl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, heterocycloalkyl, hydroxy, nitro, trifluoromethyl, -C(=O)NYlY2, -NY1-C(=O)alkyl, -NY1SO2alkyl, -NY1Y2, -SO2NY1Y2 or alkyl, alkenyl or alkynyl each optionally substituted with aryl, cycloalkyl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY1Y2, -NY1Y2 or-OR5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
is a C5-8cycloalkyl ring; and R12 is acyl, acylamino, alkoxy, alkoxycarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, aroyl, aroylamino, aryl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxycarbonyl, arylsulfinyl, arylsulfonyl, arylthio, carboxy or an acid bioisostere, cyano, cycloalkyl, halo, heteroaroyl, heteroaryl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, heterocycloalkyl, hydroxy, nitro, trifluoromethyl, -C(=O)NYlY2, -NY1-C(=O)alkyl, -NY1SO2alkyl, -NY1Y2, -SO2NY1Y2 or alkyl, alkenyl or alkynyl each optionally substituted with aryl, cycloalkyl, heteroaryl, hydroxy, -C(=O)OR6, -C(=O)NY1Y2, -NY1Y2 or-OR5;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
90. A compound according to claim 89 wherein W represents CH; X represents CH;
Y
represents CH; and Z represents CH or C-CH3.
Y
represents CH; and Z represents CH or C-CH3.
91. A compound according to claim 89 wherein W represents C1-1; X represents CH; Z represents CH; and Y represents C-C1-4alkyl, C-aryl, C-CN, C-NO2, C-halo; C-haloalkyl, C-heteroaryl, C-OR4, C-C(=O)R4, C-C=O)NY1Y2, C-C(=O)OR4 , C-NHC(=O)R4, C-CH(OH)aryl, C-S(O)2NY1Y2, or C-S(O)nR4 .
92. A compound according to claim 89 wherein W represents CH; X represents CH;
Z represents CH; and Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 C-CH(CH3)2, C-C(=O)-NH-CH3 , C-C(=O)-N(CH3)2,C-C(=O)-NH-CH2CH3 , C-C(=O)-NH-CH(CH3)2 , C-C(=O)-NH-C(CH3)2-CH2OH , C-C(=O)-NH-CH2CH2CN , C-C(=O)-NH-CH2CH2OCH3 , C-C(=O)OH or C-C(=O)OCH3, C-NHC(=O)CH3, C-NCH(=O)CH(CH3)2, C-SO2CH3.
Z represents CH; and Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 C-CH(CH3)2, C-C(=O)-NH-CH3 , C-C(=O)-N(CH3)2,C-C(=O)-NH-CH2CH3 , C-C(=O)-NH-CH(CH3)2 , C-C(=O)-NH-C(CH3)2-CH2OH , C-C(=O)-NH-CH2CH2CN , C-C(=O)-NH-CH2CH2OCH3 , C-C(=O)OH or C-C(=O)OCH3, C-NHC(=O)CH3, C-NCH(=O)CH(CH3)2, C-SO2CH3.
93. A compound according to claim 89 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F, Z represents CH.
94. A compound according to claim 89 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F and Z represents CH.
95. A compound according to claim 89 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
96. A compound according to claim 89 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
97. A compound according to claim 89 wherein R7 represents hydrogen.
98. A compound according to claim 89 wherein represents a cyclopentyl, cyclohexyl or cycloheptyl ring.
99. A compound according to claim 89 wherein represents a cyclohexyl ring.
100. A compound according to claim 89 wherein q is zero.
101. A compound according to claim 89 wherein W represents CH; X represents CH; Y represents CH; Z represents CH or C-CH3; R4 represents hydrogen; and represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
102. A compound according to claim 89 wherein W represents CH; X represents CH; Z represents CH; Y represents C-C1-4alkyl , C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl , C-heteroaryl, C-OR4, C-C(=O)R4, C-C=O)NY1Y2, -C(=O)OR4, C-NHC(=O)R4, C-CH(OH)aryl, C-S(O)2NY1Y2, C-S(O)n R4, R7 represents hydrogen; represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
103. A compound according to claim 89 wherein W represents CH; X represents CH; Z represents CH; Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 C-CH(CH3)2, C~C(=O)~N(CH3)2, C~C(=O)~NH~CH2CH3, C~C(=O)~NH~CH(CH3)2, C~C(=O)~NH~C(CH3)2-CH2OH, C~C(=O)~NH~CH2CH2CN, C~C(=O)~NH~CH2CH2OCH3,
104. C-SO2CH3; R7 represents hydrogen; represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
105. A compound according to claim 89 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F, Z represents CH;
R7 represents hydrogen represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
R7 represents hydrogen represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
106. A compound according to claim 89 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
107. A compound according to claim 89 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; Z represents CH;
R7 represents hydrogen represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; Z represents CH;
R7 represents hydrogen represents a cyclopentyl, cyclohexyl or cycloheptyl ring; and q is zero.
108. A compound according to claim 89 wherein R7 represents hydrogen and q is zero.
109. A compound according to claim 89 wherein W is CH; X is C-CH3; Y is C-CH3;
and Z is CH.
and Z is CH.
110. A compound according to claim 3 of the formula (Ixd) where X1 is O, S, SO2, or NY5, where Y5 is hydrogen, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4 or Y5 is -SO2R4; r is zero or an integer one or two; R7 is hydrogen or alkyl; and R13 is alkyl or, when two R13 groups are attached to the same carbon atom, they form an oxo group; or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
111. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents CH; and Z represents CH or C-CH3.
112. A compound according to claim 110 wherein W represents CH; X represents CH; Z represents CH; and Y represents C-C1-4alkyl, C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl, C-heteroaryl, C-OR4, C-C(=O)R4 , C-C=O)NY1Y2 , C-C(=O)OR4 , C-NHC(=O)R4 , C-CH(OH)aryl, C-S(O)2NY1Y2 or C-S(O)n R4.
113. A compound according to claim 110 wherein W represents CH; X represents CH; Z
represents CH; and Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 or C-CH(CH3)2, C-CN, C-NO2, C-Br, C-Cl, or C-F, C-CF3 (viii) C-OR4 [e.g. C~OCH3, C~OCH2CH3, C~OCHF2, C~OCF3 C~C(=O)~N(CH3)2, C~C(=O)~NH~CH2CH3, C~C(=O)~NH~CH(CH3)2, C~C(=O)~NH~C(CH3)2-CH2OH, C~C(=O)~NH~CH2CH2CN, C~C(=O)~NH~CH2CH2OCH3, C-C(=O)OH or C-C(=O)OCH3, C-NHC(=O)CH3, C-NHC(=O)CH(CH3)2 or C-SO2CH3.
represents CH; and Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 or C-CH(CH3)2, C-CN, C-NO2, C-Br, C-Cl, or C-F, C-CF3 (viii) C-OR4 [e.g. C~OCH3, C~OCH2CH3, C~OCHF2, C~OCF3 C~C(=O)~N(CH3)2, C~C(=O)~NH~CH2CH3, C~C(=O)~NH~CH(CH3)2, C~C(=O)~NH~C(CH3)2-CH2OH, C~C(=O)~NH~CH2CH2CN, C~C(=O)~NH~CH2CH2OCH3, C-C(=O)OH or C-C(=O)OCH3, C-NHC(=O)CH3, C-NHC(=O)CH(CH3)2 or C-SO2CH3.
114. A compound according to claim 110 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F and Z represents CH.
115. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents C-CH3 ; and Z represents C-CH3.
116. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
117. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
118. A compound according to claim 110 wherein R7 represents hydrogen.
119. A compound according to claim 110 wherein X1 O, N-C(=O)R4, N-C(=O)NY1Y2 , N-C(=O)OR4, or N-SO2R4 ; and r is zero.
120. A compound according to claim 110 wherein X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3, N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
121. A compound according to claim 110 wherein r is zero.
122. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; X1 is O, N-C(=O)R4 , N-C(=O)NY1Y2, N-C(=O)OR4 , N-SO2R4 ; and r is zero.
123. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents CH; Z represents CH or C-CH3; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3, N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3 , N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
124. A compound according to claim 110 wherein W represents CH; X represents CH; Z represents CH; Y represents C-C1-4alkyl, C-aryl, C-CN, C-NO2, C-halo, C-haloalkyl, C-heteroaryl, C-OR, C-C(=O)R4 , C-C=O)NY1Y2 , -C(=O)OR4 , C-NHC(=O)R4 , C-S(O)2NY1Y2, C-S(O)n R4 ;
R7 represents hydrogen; X1 is O, N-C(=O)R4 , N-C(=O)NY1Y2 , N-C(=O)OR4 , or N-SO2R4 ; and r is zero.
R7 represents hydrogen; X1 is O, N-C(=O)R4 , N-C(=O)NY1Y2 , N-C(=O)OR4 , or N-SO2R4 ; and r is zero.
125. A compound according to claim 110 wherein W represents CH; X represents CH; Z represents CH; Y represents C-CH3, C-CH2CH3, C-CH2CH2CH3 , C-CH(CH3)2, C-CN, C-NO2, C-Br, C-Cl or C-F], C-CF3 C~OCH3, C~OCH2CH3, C~OCHF2, C~OCF3, C~C(=O)~NH~CH3, C~C(=O)~N(CH3)2, C~C(=O)~NH~CH2CH3, C~C(=O)~NH~CH(CH3)2, C~C(=O)~NH~C(CH3)2-CH2OH, C~C(=O)~NH~CH2CH2CN, C~C(=O)~NH~CH2CH2OCH3, C-C(=O)OH, C-C(=O)OCH3, C-NHC(=O)CH3, C-NHC(=O)CH(CH3)2 C-SO2CH3; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3, N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3 , N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3); and r is zero.
126. A compound according to claim 110 wherein W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F, Z represents CH;
R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2, N-C(=O)OR4 or N-SO2R4; and r is zero.
R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2, N-C(=O)OR4 or N-SO2R4; and r is zero.
127. W represents CH; X represents C-CH3, C-CH2CH3, C-CH(CH3)2, C-OCH3, C-OCH2CH3, C-Br or C-Cl; Y represents C-CH3, C-CH2CH3, C-OCH3, C-Br, C-Cl, C-F or Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3 or N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
128. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents C-CH3; Z represents C-CH3; R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2, N-C(=O)OR4 or N-SO2R4; and r is zero.
129. A compound according to claim 110 wherein W represents CH; X represents CH; Y represents C-CH3; Z represents C-CH3; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3 or N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
130. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2 , N-C(=O)OR4 or N-SO2R4 ; and r is zero.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2 , N-C(=O)OR4 or N-SO2R4 ; and r is zero.
131. A compound according to claim wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3 or N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3 or N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
132. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)R4, N-C(=O)NY1Y2, N-C(=O)OR4 or N-SO2R4 ; and r is zero.
133. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; Z represents CH; R7 represents hydrogen; X1 is O, N-C(=O)CH3, N-C(=O)CH2CH(CH3)2, N-C(=O)CH(CH3)2, N-C(=O)C(CH3)3 or N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2 N-C(=O)OCH3, N-C(=O)OCH2CH3, N-SO2CH3 or N-SO2CH(CH3)2; and r is zero.
134. A compound according to claim 110 wherein X1 is N-C(=O)CH(CH3)2, N-C(=O)CH2CH(CH3)2, N-C(=O)C(CH3)3 N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2, N-C(=O)OCH3 or N-C(=O)OCH2CH3; and r is zero.
135. A compound according to claim 110 wherein W is CH; X is CH; Y is CH, C-CH2CH3, C-CH2CH2CH3 C-CN, C-Br, C-CF3 C~OCH3, C~OCH2CH3, C~OCHF2, C~OCF3 C~C(=O)~NH~CH3, C~C(=O)~NH~CH2CH3, C~C(=O)-NH-CH(CH3)2, C~C(=O)~NH~C(CH3)2-CH2OH, C~C(=O)~NH~CH2CH2CN, C~C(=O)~NH~CH2CH2OCH3 C-C(=O)OCH3, C-C(=O)OH, C-SO2CH3 or and Z is CH.
136. A compound according to claim 110 wherein W is CH; X is C-CH3 or C-CH2CH3; Y is C-CH3, C-CH2CH3, C-CH(CH3)2, C-Br , C-Cl, C-F or and Z is CH.
137. A compound according to claim 110 wherein W is CH; X is C-OCH3; Y is CH, C-CH3, C-CH2CH3, C-Cl or C-OCH3; and Z is CH.
138. A compound according to claim 110 wherein W is CH; X is C-OCH2CH3; Y is C-F; and Z is CH.
139. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-CH2-CH2-; and Z represents CH.
140. A compound according to claim 110 wherein W represents CH; X represents CR2 and Y
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
represents CR3 where R2 and R3 form the group -CH2-O-CH2-; and Z represents CH.
141. A compound according to claim 110 wherein X1 is N-C(=O)N(CH3)2, N-C(=O)NCH(CH3)2, N-C(=O)N(CH2CH3)2, or and r is zero.
142. A compound according to claim 110 wherein W represents CH; X represents C-CH3; Y
represents C-CH3 or C-Cl; and Z represents CH.
represents C-CH3 or C-Cl; and Z represents CH.
143. A compound according to claim 3 which is 2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-[5-(pyridin-3-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5-fluoro-2-[5-methylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5,6-dimethyl-2-(5-phenethylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
4-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-(5-benzylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-morpholin-4-yl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-[5-(thiophen-2-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole hydrochloride;
5-methyl-2-(5-methylsulfanyl-4-propyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-(4-methoxy-benzylsulfanyl)-4-propyl-1H-pyrazol-3-yl)- 5-methyl-1H-benzoimidazole;
2-(5-benzylsulfanyl-4-isopropyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
3-(5-chloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
2-(4-amino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanone;
2-(1H-indazol-3-yl)-3H-benzoimidazol-4-ol;
2-phenyl-1H-imidazol[4,5-b]pyrazine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-3H-imidazo[4,5-c]pyridine;
2-(1H-indazole-3-yl)-3H-imidazo[4,5-b]pyridine;
2-(1H-pyrazol-3yl)-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
5,6-dimethyl-2-(4-phenyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(5,6-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-methoxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-chloro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-methyl)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(4,5-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-pyrazole-4-carboxylic acid ethyl ester;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-pyrazole-4-carboxylic acid ethyl ester;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
2-(5-methyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-ethoxy-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-methylsulfanyl-isoxazol-3-yl)-1H-benzoimidazole;
5-chloro-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dichloro-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
(benzoimidazol-2-yl)-5-methylthio-3-pyrazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-indazole;
2-(5-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl)-1H-benzoimidazole;
3-(5,6-di methyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
4-chloro-3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazol-5-ol;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
3-(5,6-dimethyl-1H-benzoimidazol-5-yl)-pyrazole-4-carboxylic acid;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-pyrazole-4-carboxylic acid;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide ;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-lH-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
5,6-dimethyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-ethyl-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-fluoro-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-5-trifluoromethoxy-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
5-chloro-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
5-methoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-ethoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrano[4,3-c]pyrazole;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
2-dimethylamino-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-urea;
3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-( 1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1 H-pyrazol-4-ylamine;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-I H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1, 1 -diethylurea;
5-methoxy-2-(4-nitro-1 H-pyrazol-3-yl)-1 H-benzoimidazole;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)=1H-pyrazol-4-yl]-amide;
3-[3-(S-fluoro-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin- 1 -yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [2-(2H-tetrazol-5-yl)-ethyl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)- 1H-pyrazol-4-ylamine;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid amide dihydrochloride;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
3-(5-nitro-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(4-methyl-piperazin-l-yl)-propyl]-amide;
N-[2-(1H-Indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide;
N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
2-(1H-indazol-3-yl)-3H-benzoimidazol-5-amine; or piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-[5-(pyridin-3-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5-fluoro-2-[5-methylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5,6-dimethyl-2-(5-phenethylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
4-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-(5-benzylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-morpholin-4-yl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-[5-(thiophen-2-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole hydrochloride;
5-methyl-2-(5-methylsulfanyl-4-propyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-(4-methoxy-benzylsulfanyl)-4-propyl-1H-pyrazol-3-yl)- 5-methyl-1H-benzoimidazole;
2-(5-benzylsulfanyl-4-isopropyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
3-(5-chloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
2-(4-amino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanone;
2-(1H-indazol-3-yl)-3H-benzoimidazol-4-ol;
2-phenyl-1H-imidazol[4,5-b]pyrazine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-3H-imidazo[4,5-c]pyridine;
2-(1H-indazole-3-yl)-3H-imidazo[4,5-b]pyridine;
2-(1H-pyrazol-3yl)-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
5,6-dimethyl-2-(4-phenyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(5,6-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-methoxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-chloro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-methyl)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(4,5-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-pyrazole-4-carboxylic acid ethyl ester;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-pyrazole-4-carboxylic acid ethyl ester;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
2-(5-methyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-ethoxy-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(5-methylsulfanyl-isoxazol-3-yl)-1H-benzoimidazole;
5-chloro-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dichloro-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
(benzoimidazol-2-yl)-5-methylthio-3-pyrazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-indazole;
2-(5-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl)-1H-benzoimidazole;
3-(5,6-di methyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
4-chloro-3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazol-5-ol;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
3-(5,6-dimethyl-1H-benzoimidazol-5-yl)-pyrazole-4-carboxylic acid;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-pyrazole-4-carboxylic acid;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide ;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-lH-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
5,6-dimethyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-ethyl-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-fluoro-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-5-trifluoromethoxy-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
5-chloro-6-methyl-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
5-methoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
5-ethoxy-2-(4-nitro-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrano[4,3-c]pyrazole;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
2-dimethylamino-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-urea;
3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-( 1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1 H-pyrazol-4-ylamine;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-I H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1, 1 -diethylurea;
5-methoxy-2-(4-nitro-1 H-pyrazol-3-yl)-1 H-benzoimidazole;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1 H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)=1H-pyrazol-4-yl]-amide;
3-[3-(S-fluoro-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin- 1 -yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [2-(2H-tetrazol-5-yl)-ethyl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)- 1H-pyrazol-4-ylamine;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid amide dihydrochloride;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
3-(5-nitro-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(4-methyl-piperazin-l-yl)-propyl]-amide;
N-[2-(1H-Indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide;
N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
2-(1H-indazol-3-yl)-3H-benzoimidazol-5-amine; or piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
144. A compound according to claim 14 which is 2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-( 1 H-indazol-3-yl)-1 H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-[5-(pyridin-3-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1 H-benzoimidazole;
S-fluoro-2-[5-methylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5,6-dimethyl-2-(5-phenethylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
4-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)- 1H-benzoimidazole;
5,6-dimethyl-2-(S-benzylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-[5-(thiophen-2-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole hydrochloride;
5-methyl-2-(5-methylsulfanyl-4-propyl-1H-pyrazol-3-yl)- 1H-benzoimidazole;
2-(5-(4-methoxy-benzylsulfanyl)-4-propyl-1H-pyrazol-3-yl)- 5-methyl-1H-benzoimidazole;
2-(5-benzylsulfanyl-4-isopropyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
3-(5-chloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
5,6-dimethyl-2-(4-phenyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5-methoxy-6-methyl-11-1-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
2-(5-ethoxy-1H-pyrazol-3-yl)-1H-benzoimidazole;
(benzoimidazol-2-yl)-S-methylthio-3-pyrazole;
2-(5-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-IH-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
2-dimethylamino-N-[3-(5,6-dimethyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1 H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-l,l-diethylurea;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-ditluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-Il-1-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l -dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
N-[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5-carboxylate;
5,6-dimethyl-2-(1H-indazol-3-yl)-1H-benzimidazole;
2-(1H-indazol-3-yl)-3H-benzimidazole-4-carboxylic acid;
2-(5-ethoxy-2H-pyrazol-3-yl)-1H-benzimidazole-4-carboxylic acid;
5,6-dimethyl-2-(5-methyl-2H-pyrazol-3-yl)-1H-benzimidazole;
5,6-dimethyl-2-(5-thiophen-2-yl-2H-pyrazol-3-yl)-1H-benzimidazole;
2-(4-bromo-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4,5-ethylenedioxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5-methoxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4-hydroxy-1H-benzimidazole 2-(5-ethyl-2H-pyrazol-3-yl)-5-bromo-1H-benzimidazole; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-( 1 H-indazol-3-yl)-1 H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-5-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
5,6-dimethyl-2-[5-(pyridin-3-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1 H-benzoimidazole;
S-fluoro-2-[5-methylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
5,6-dimethyl-2-(5-phenethylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
4-methyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)- 1H-benzoimidazole;
5,6-dimethyl-2-(S-benzylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
5,6-dimethyl-2-[5-(thiophen-2-ylmethylsulfanyl)-1H-pyrazol-3-yl]-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole hydrochloride;
5-methyl-2-(5-methylsulfanyl-4-propyl-1H-pyrazol-3-yl)- 1H-benzoimidazole;
2-(5-(4-methoxy-benzylsulfanyl)-4-propyl-1H-pyrazol-3-yl)- 5-methyl-1H-benzoimidazole;
2-(5-benzylsulfanyl-4-isopropyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methoxy-1H-benzoimidazole;
2-(5-methylsulfanyl-4-methyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
3-(5-chloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
3-(5,6-dichloro-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylamine;
5,6-dimethyl-2-(4-phenyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5-methoxy-6-methyl-11-1-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
2-(5-ethoxy-1H-pyrazol-3-yl)-1H-benzoimidazole;
(benzoimidazol-2-yl)-S-methylthio-3-pyrazole;
2-(5-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-IH-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
2-dimethylamino-N-[3-(5,6-dimethyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1 H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-l,l-diethylurea;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-ditluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-Il-1-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-l, l -dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1 H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
N-[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5-carboxylate;
5,6-dimethyl-2-(1H-indazol-3-yl)-1H-benzimidazole;
2-(1H-indazol-3-yl)-3H-benzimidazole-4-carboxylic acid;
2-(5-ethoxy-2H-pyrazol-3-yl)-1H-benzimidazole-4-carboxylic acid;
5,6-dimethyl-2-(5-methyl-2H-pyrazol-3-yl)-1H-benzimidazole;
5,6-dimethyl-2-(5-thiophen-2-yl-2H-pyrazol-3-yl)-1H-benzimidazole;
2-(4-bromo-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4,5-ethylenedioxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5-methoxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4-hydroxy-1H-benzimidazole 2-(5-ethyl-2H-pyrazol-3-yl)-5-bromo-1H-benzimidazole; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
145. A compound according to claim 14 which is 2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid benzylamine;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide, Example 3;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoi midazole;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(S-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
2-(S-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide; .
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide, (compound denoted as A17-B 106);
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamine;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-tritluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-y1]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-y1]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl- 1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-(3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-S-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea, Example 257(h);
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-111-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
l -[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide; or N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide, or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide, Example 3;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
5,6-dimethyl-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-1H-benzoimidazole;
6-chloro-2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
6-chloro-2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5-methyl-1H-benzoimidazole;
2-(5-methylsulfanyl-1H-pyrazol-3-yl)-5-trifluoromethyl-1H-benzoimidazole;
2-(5-cyclopropylmethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
2-(5-ethylsulfanyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoi midazole;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(S-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
2-(S-isopropyl-1H-pyrazol-3-yl)-5,6-dimethyl-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide; .
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide, (compound denoted as A17-B 106);
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamine;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-phenyl-acetamide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-tritluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-y1]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-y1]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl- 1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-4-methyl-benzamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]- 2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-(3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoi midazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-( 1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-S-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-ylmethyl]-amide;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea, Example 257(h);
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-111-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
l -[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
4-methyl-piperazine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide; or N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide, or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
146. A compound according to claim 14 which is 3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-(1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea; or 3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
3-(5-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-methoxy-ethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid propylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(6-ethyl-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclopropylamide;
2-(4-isopropylcarbamoyl-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid phenylmethyl-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylmethyl-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid tert-butylamide;
2-(4-isobutyrylamino-1H-pyrazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzylamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-butyramide;
cyclopropanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
methoxyacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopentanecarboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
trimethylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
tert-butylacetic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
butanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
isoxazole-5-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
S(+)-2-methylbutanoic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethylurea;
cyclopropanecarboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-ethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isobutyramide;
cyclopropanecarboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3,5-dimethyl-isoxazole-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
furan-3-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-morpholin-4-yl-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-(1H-1,2,3,4-tetraazol-1-yl)-acetamide;
N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-isonicotinamide;
2-cyclopropyl-N-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-acetamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isopropyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-phenyl-urea;
1-benzyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
4-methylpiperazine-1-carboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-(1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
cyclopropanecarboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
tetrahydropyran-4-carboxylic acid [3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-yl]amide;
morpholine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(6-chloro-5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
morpholine-4-carboxylic acid[3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
3-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
morpholine-4-carboxylic acid [3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
morpholine-4-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-[3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
morpholine-4-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-methyl-3-[3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-methyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-ethyl-urea;
4-methyl-piperazine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-3-isobutyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea; or 3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
147. A compound according to claim 14 which is 3-(5-methoxy-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isopropylamide;
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-(1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea; or 3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazole-4-carboxylic acid cyclopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (tetrahydro-pyran-4-yl)-amide;
3-(5, 6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid isobutyl-amide;
cyclopropanecarboxylic acid[3-(5-ethoxy-6-ethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]amide;
1,1-dimethyl-3-[3-(1,5,6,7-tetrahydro-s-indacen-2-yl)-1H-pyrazol-4-yl]urea;
piperidine-4-carboxylic acid[3-(6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]amide;
3-[6-ethoxy-5-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea;
3-[3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
piperidine-1-carboxylic acid [3-(5-difluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
cyclopropanecarboxylic acid [3-(1,5,6,7-tetrahydro-1,3-diaza-s-indacen-2-yl)-1H-pyrazol-4-yl]amide;
piperidine-1-carboxylic acid [3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
piperidine-1-carboxylic acid [3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-cyclopropyl-3-[3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
piperidine-1-carboxylic acid [3-(5-fluoro-6-methyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-amide;
1-tert-butyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
1-cyclopropyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea;
3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethyl-urea;
1-cyclopropylmethyl-3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea; or 3-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-dimethyl-urea;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
148. A compound according to claim 54 which is 3-(1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanone;
2-(1H-indazol-3-yl)-3H-benzoimidazol-4-ol;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-3H-imidazo[4,5-c]pyridine;
2-(1H-indazole-3-yl)-3H-imidazo[4,5-b]pyridine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(5,6-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-methoxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-chloro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-methyl)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanone;
2-(1H-indazol-3-yl)-3H-benzoimidazol-4-ol;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-3H-imidazo[4,5-c]pyridine;
2-(1H-indazole-3-yl)-3H-imidazo[4,5-b]pyridine;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(5,6-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(2-methoxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-chloro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(4-methyl)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
149. A compound according to claim 54 which is 3-(1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzol midazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzol midazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole, (compound denoted as A60-B63), Example 235(q);
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3,4-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, ethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-((1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid amide dihydrochloride;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
3-(5-methoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzol midazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methyl-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-6-methoxy-1H-indazole;
3-(5-ethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-isopropyl-6-methyl-1H-benzol midazol-2-yl)-1H-indazole;
3-(5-bromo-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-bromo-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3-cyano)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(pyrid-3-yl)-1H-benzoimidazol-2-yl)-1H-indazole;
3-(6-methyl-5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-phenyl-1H-benzoimidazol-2-yl)-1H-indazole, (compound denoted as A60-B63), Example 235(q);
3-(5-(2-fluoro)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-(3,4-methylenedioxy)phenyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5-benzyloxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-methylenedioxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonitrile;
3-(5-methoxycarbonyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-ethoxy-1H-indazole;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carbonitrile;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4-fluoro-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-chloro-1H-indazole;
3-(5-n-propyl-1H-benzoimidazol-2-yl)-1H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-sulfonic acid benzylamide;
3-(5-methanesulfonyl-1H-benzoimidazol-2-yl)-1H-indazole;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-phenyl-methanol;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, ethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, methylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, isopropylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid, benzamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-((1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(2-oxo-pyrrolidin-1-yl)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-morpholin-4-yl-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-cyano-ethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
[2-(indazol-3-yl)-1H-benzoimidazol-5-yl]-carboxylic acid;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid amide dihydrochloride;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
150. A compound according to claim 54 which is 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-methoxy-1H-indazole;
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole; or 3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
3-(5-ethyl-6-methyl-1H-benzoimidazol-2-yl)-1H-indazole; or 3-(5,6-diethyl-1H-benzoimidazol-2-yl)-1H-indazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1H-indazole-5-carboxylic acid dimethylamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
151. A compound according to claim 89 which is 3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-indazole;
5,6-dimethyl-2-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl)-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,5,6,7,8-hexahydro-cycloheptapyrazole; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
5,6-dimethyl-2-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl)-1H-benzoimidazole;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,5,6,7,8-hexahydro-cycloheptapyrazole; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
152. A compound according to claim 89 which is 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-4,5,6,7-tetrahydro-1H-indazole; or 5,6-dimethyl-2-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl)-1H-benzoimidazole;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
153. A compound according to claim 110 which is 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3-methyl-butan-1-one;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl- 1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-(propane-2-sulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine; or 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrano[4,3-c]pyrazole; or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
cyclopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3-methyl-butan-1-one;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl- 1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-5-(propane-2-sulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine; or 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrano[4,3-c]pyrazole; or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound;
or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
154. A compound according to claim 110 which is 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxyl is acid diethylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3-methyl-butan-1-one; or 1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
cyclopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
isopropyl-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-morpholin-4-yl-methanone;
3-(5-chloro-6-methyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-[5-(2-morpholin-4-yl-ethoxy)-1H-benzoimidazol-2-yl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
3-(5-trifluoromethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxyl is acid diethylamide;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl-propan-1-one;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid methyl ester;
1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3-methyl-butan-1-one; or 1-[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2,2-dimethyl-propan-1-one; or or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
155. A compound according to claim 110 which is 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
cyclopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
prepared 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
3-(5-chloro-6-methyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide; or 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
cyclopropyl-[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-methanone;
3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid isopropylamide;
prepared 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide;
[3-(5,6-dimethyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-pyrrolidin-1-yl-methanone;
[3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-piperidin-1-yl-methanone;
3-(5-chloro-6-methyl-1 H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid diethylamide; or 3-(5,6-dimethyl-1H-benzoimidazol-2-yl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid dimethylamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
156. A compound according to claim 3 which is 2-(1H-indazol-3-yl)-1H-1-benzimidazole-5-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5- carboxylate;
5,6-dimethyl-2-(1H-indazol-3-yl)-1H-benzimidazole;
5-methoxy-2-(1H-indazol-3-yl)-1H-benzimidazole;
2-(1H-indazol-3-yl)-3H-benzimidazole-4-carboxylic acid;
5-bromo 2-(1H-indazol-3-yl)-31-I-benzimidazole;
2-(5-ethoxy-2H-pyrazol-3-yl)-1 H-benzimidazole-4-carboxylic acid;
5,6-dimethyl-2-(5-methyl-2H-pyrazol-3-yl)-1H-benzimidazole;
5,6-dimethyl-2-(5-thiophen-2-yl-2H-pyrazol-3-yl)-1H-benzimidazole;
2-(4-bromo-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4,5-ethylenedioxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5-methoxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4-hydroxy-1H-benzimidazole 2-(5-ethyl-2H-pyrazol-3-yl)-5-bromo-1H-benzimidazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-dimethylamino-benzylamide;
4-({[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-amino}-methyl)-piperidine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[1,3]dioxol-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1,3-dimethyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-methyl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-isopropoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-isopropyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,S-dimethyl-furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(3-acetylamino-phenoxy)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid ([2,2']bithiophenyl-S-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-cyano-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-chloro-benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-S-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-benzoimidazol-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-sulfamoyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-dimethylamino-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (benzo[b]thiophen-3-yhnethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenethyl-amide;
3-(6-phenyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(2,4-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-naphthalen-1-yl-1 H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-thianthren-1-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-biphenyl-4-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-p-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-m-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-o-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-trifluoromethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-trifluoromethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,4-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[1,3]dioxol-5-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-tert-butyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-hex-1-enyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4-dimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
3-[6-(3,4-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-trifluoromethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-ethanone;
3-(6-benzo[b]thiophen-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4,5-trimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{5-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-thiophen-2-yl}-ethanone;
1-{3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-ethanone;
3-[6-(4-benzyloxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(2-fluoro-biphenyl-4-yl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[b]thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
{3-[2-(2H-indazol-3-yl)-31-1-benzoimidazol-5-yl]-phenyl}-methanol;
3-[6-(4-ethylsulfanyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(2,4-difluoro-phenyl)-11-1-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-trifluoromethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-fluoro-2-methyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-{6-[2-(4-fluoro-phenyl)-vinyl]-1H-benzoimidazol-2-yl}-2H-indazole;
3-{6-[2-(4-chloro-phenyl)-vinyl]-1H-benzoimidazol-2-yl}-2H-indazole;
3-{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-propionic acid;
{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-(6-furan-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-benzyloxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-isopropyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methanesulfonyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-acetylamino-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid isopropylamide;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-morpholin-4-yl-methanone;
[2-(1H-indazol-3-yl)-1 H-benzoimidazol-5-yl]-(4-methyl-piperazin-1-yl)-methanone;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzyl-methyl-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-benzylamide;
2-(IH-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoitnidazole-S-carboxylic acid 3,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,4,5-trifluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (4'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3',5'-dichloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (4'-fluoro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-trifluoromethyl-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-pyridin-2-yl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
4-[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-piperazine-1-carboxylic acid tent-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
2-[5-(benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-phenyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-methyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,7-dimethyl-octa-2,6-dienyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-bromo-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
3-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxymethyl]-benzonitrile;
2-[5-(4-trifluoromethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,4-dichloro-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-pentafluorophenylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(4-tert-butyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-benzenesulfonylmethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
4-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxymethyl]-benzonitrile;
2-[5-(biphenyl-4-ylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2,3-dichioro-benzenesulfonic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2-[5-(2-morpholin-4-yl-ethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-piperidin-1-yl-ethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-methoxy-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-p-tolyl-ethanone;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-3,3,4,4,4-pentafluoro-butan-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-biphenyl-4-yl-ethanone;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-butan-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-dimethylamino-phenyl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(3-phenyl-isoxazol-5-yl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-N-phenyl-acetamide;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-3,3-dimethyl-butan-2-one;
1-adamantan-1-yl-2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-naphthalen-2-yl-ethanone;
4-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-benzonitrile;
6-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-3,4-dihydro-1H-quinolin-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-trifluoromethoxy-phenyl)-ethanone;
5-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-2-chloro-benzenesulfonamide;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-methoxy-phenyl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-cyclopropyl-ethanone;
isonicotinic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,2-dimethyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzyloxy-acetic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
4-methoxy-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
phenyl-acetic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,3,4,5,6-Pentafluoro-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
cyclopropanecarboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,2,3,3,4,4,4-heptafluoro-butyric acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
cyclopentanecarboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3-phenyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
biphenyl-4-carboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3,5-bis-trifluoromethyl-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
4-trifluoromethyl-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
thiophene-2-carboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5- carboxylate;
5,6-dimethyl-2-(1H-indazol-3-yl)-1H-benzimidazole;
5-methoxy-2-(1H-indazol-3-yl)-1H-benzimidazole;
2-(1H-indazol-3-yl)-3H-benzimidazole-4-carboxylic acid;
5-bromo 2-(1H-indazol-3-yl)-31-I-benzimidazole;
2-(5-ethoxy-2H-pyrazol-3-yl)-1 H-benzimidazole-4-carboxylic acid;
5,6-dimethyl-2-(5-methyl-2H-pyrazol-3-yl)-1H-benzimidazole;
5,6-dimethyl-2-(5-thiophen-2-yl-2H-pyrazol-3-yl)-1H-benzimidazole;
2-(4-bromo-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4,5-ethylenedioxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-5-methoxy-1H-benzimidazole;
2-(5-ethyl-2H-pyrazol-3-yl)-4-hydroxy-1H-benzimidazole 2-(5-ethyl-2H-pyrazol-3-yl)-5-bromo-1H-benzimidazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-dimethylamino-benzylamide;
4-({[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-amino}-methyl)-piperidine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[1,3]dioxol-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1,3-dimethyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-methyl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-isopropoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-isopropyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,S-dimethyl-furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(3-acetylamino-phenoxy)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid ([2,2']bithiophenyl-S-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-cyano-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-chloro-benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-S-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-benzoimidazol-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-sulfamoyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-dimethylamino-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (benzo[b]thiophen-3-yhnethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenethyl-amide;
3-(6-phenyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(2,4-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-naphthalen-1-yl-1 H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-thianthren-1-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-biphenyl-4-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-p-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-m-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-o-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-trifluoromethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-trifluoromethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,4-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[1,3]dioxol-5-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-tert-butyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-hex-1-enyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4-dimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
3-[6-(3,4-dichloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-trifluoromethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-ethanone;
3-(6-benzo[b]thiophen-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4,5-trimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{5-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-thiophen-2-yl}-ethanone;
1-{3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-ethanone;
3-[6-(4-benzyloxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(2-fluoro-biphenyl-4-yl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[b]thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
{3-[2-(2H-indazol-3-yl)-31-1-benzoimidazol-5-yl]-phenyl}-methanol;
3-[6-(4-ethylsulfanyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(2,4-difluoro-phenyl)-11-1-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-trifluoromethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-fluoro-2-methyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-{6-[2-(4-fluoro-phenyl)-vinyl]-1H-benzoimidazol-2-yl}-2H-indazole;
3-{6-[2-(4-chloro-phenyl)-vinyl]-1H-benzoimidazol-2-yl}-2H-indazole;
3-{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-propionic acid;
{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-(6-furan-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-benzyloxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-isopropyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methanesulfonyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-acetylamino-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid isopropylamide;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-morpholin-4-yl-methanone;
[2-(1H-indazol-3-yl)-1 H-benzoimidazol-5-yl]-(4-methyl-piperazin-1-yl)-methanone;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzyl-methyl-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-benzylamide;
2-(IH-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoitnidazole-S-carboxylic acid 3,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,4,5-trifluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (4'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3',5'-dichloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (4'-fluoro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-trifluoromethyl-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-pyridin-2-yl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
4-[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-piperazine-1-carboxylic acid tent-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
2-[5-(benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-phenyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-methyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,7-dimethyl-octa-2,6-dienyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-bromo-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
3-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxymethyl]-benzonitrile;
2-[5-(4-trifluoromethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,4-dichloro-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-pentafluorophenylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(4-tert-butyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-benzenesulfonylmethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
4-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxymethyl]-benzonitrile;
2-[5-(biphenyl-4-ylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2,3-dichioro-benzenesulfonic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2-[5-(2-morpholin-4-yl-ethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-piperidin-1-yl-ethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-methoxy-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-p-tolyl-ethanone;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-3,3,4,4,4-pentafluoro-butan-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-biphenyl-4-yl-ethanone;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-butan-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-dimethylamino-phenyl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(3-phenyl-isoxazol-5-yl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-N-phenyl-acetamide;
1-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-3,3-dimethyl-butan-2-one;
1-adamantan-1-yl-2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-naphthalen-2-yl-ethanone;
4-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-benzonitrile;
6-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-3,4-dihydro-1H-quinolin-2-one;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-trifluoromethoxy-phenyl)-ethanone;
5-{2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-acetyl}-2-chloro-benzenesulfonamide;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-(4-methoxy-phenyl)-ethanone;
2-[5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yloxy]-1-cyclopropyl-ethanone;
isonicotinic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,2-dimethyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzyloxy-acetic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
4-methoxy-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
phenyl-acetic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,3,4,5,6-Pentafluoro-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
cyclopropanecarboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
2,2,3,3,4,4,4-heptafluoro-butyric acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
cyclopentanecarboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3-phenyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
biphenyl-4-carboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3,5-bis-trifluoromethyl-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
4-trifluoromethyl-benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
thiophene-2-carboxylic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
157. A compound according to claim 14 which is 2-(5-ethyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole; or 2-(5-methyl-2H-pyrazol-3-yl)-5,6-dimethyl-1H-benzimidazole;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
158. A compound according to claim 54 which is 2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid benzylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-dimethylamino-benzylamide;
4-({[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-amino}-methyl)-piperidine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[1,3]dioxol-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1,3-dimethyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-methyl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-isopropoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-isopropyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,5-dimethyl-furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(3-acetylamino-phenoxy)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid ([2,2']bithiophenyl-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-cyano-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-benzoimidazol-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-sulfamoyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenylamide;
3-[6-(4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-m-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-o-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[1,3]dioxol-5-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-hex-1-enyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4-dimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
3-[6-(3,4,5-trimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{5-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-thiophen-2-yl}-ethanone;
{3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-[6-(2,4-difluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-fluoro-2-methyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-(6-furan-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-isopropyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-acetylamino-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid isopropylamide;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-morpholin-4-yl-methanone;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-(4-methyl-piperazin-1-yl)-methanone;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzyl-methyl-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-lH-benzoimidazole-5-carboxylic acid 3,4,5-trifluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-trifluoromethyl-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-pyridin-2-yl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
4-[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
2-[5-(benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-phenyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,7-dimethyl-octa-2,6-dienyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-bromo-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,4-dichloro-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-benzenesulfonylmethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(biphenyl-4-ylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-methoxy-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
isonicotinic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3-phenyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5-carboxylate;
5-methoxy-2-(1H-indazol-3-yl)-1H-benzimidazole; or 5-bromo 2-(1H-indazol-3-yl)-3H-benzimidazole;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-methylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-ethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-isopropylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-phenethylamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-morpholinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(N'-methylpiperazino)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-pyrrolidinoamide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(isobutyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-benzyl-N-methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-ethoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (naphthalen-1-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-dimethylamino-benzylamide;
4-({[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-amino}-methyl)-piperidine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[1,3]dioxol-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1,3-dimethyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-methyl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-trifluoromethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-phenoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-trifluoromethoxy-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-isopropoxy-propyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-pyrazol-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-isopropyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,5-dimethyl-furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(3-acetylamino-phenoxy)-propyl]-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid ([2,2']bithiophenyl-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-cyano-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (thiophen-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (1-methyl-1H-benzoimidazol-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 4-sulfamoyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3-methoxy-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid (furan-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-nitro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 3,5-dimethyl-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid phenylamide;
3-[6-(4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-chloro-4-fluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-m-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-o-tolyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-thiophen-3-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3-chloro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3-methoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(3,5-dimethyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-(6-benzo[1,3]dioxol-5-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-(6-hex-1-enyl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(3,4-dimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenol;
3-[6-(3,4,5-trimethoxy-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
1-{5-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-thiophen-2-yl}-ethanone;
{3-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-[6-(2,4-difluoro-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
3-[6-(4-fluoro-2-methyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
{4-[2-(2H-indazol-3-yl)-3H-benzoimidazol-5-yl]-phenyl}-methanol;
3-(6-furan-2-yl-1H-benzoimidazol-2-yl)-2H-indazole;
3-[6-(4-isopropyl-phenyl)-1H-benzoimidazol-2-yl]-2H-indazole;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (tetrahydro-pyran-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-acetylamino-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid methylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid isopropylamide;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-morpholin-4-yl-methanone;
[2-(1H-indazol-3-yl)-1H-benzoimidazol-5-yl]-(4-methyl-piperazin-1-yl)-methanone;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid benzyl-methyl-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3,4-difluoro-benzylamide;
2-(1H-indazol-3-yl)-lH-benzoimidazole-5-carboxylic acid 3,4,5-trifluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,6-difluoro-3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2'-chloro-biphenyl-4-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-trifluoromethyl-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (5-pyridin-2-yl-thiophen-2-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-imidazol-1-yl-propyl)-amide;
4-[2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
2-[5-(benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-phenyl-allyloxy)2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,7-dimethyl-octa-2,6-dienyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-bromo-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3,4-dichloro-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(2-benzenesulfonylmethyl-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(biphenyl-4-ylmethoxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
2-[5-(3-methoxy-benzyloxy)-2H-pyrazol-3-yl]-1H-benzoimidazole;
isonicotinic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
benzoic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
3-phenyl-propionic acid 5-(1H-benzoimidazol-2-yl)-1H-pyrazol-3-yl ester;
methyl 2-(1H-indazol-3-yl)-3H-benzimidazole-5-carboxylate;
5-methoxy-2-(1H-indazol-3-yl)-1H-benzimidazole; or 5-bromo 2-(1H-indazol-3-yl)-3H-benzimidazole;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
159. A compound according to claim 54 which is 2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(cyclohexylmethyl)amide;
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide; 2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
or 2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-indazol-3-yl)-1H-benzimidazole-5-carboxylic acid N-(2-furfuryl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-methanesulfonyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-nitro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-chloro-pyridin-3-ylmethyl)-amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,3-dihydro-benzofuran-5-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (benzo[b]thiophen-3-ylmethyl)-amide; 2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 3-chloro-benzylamide;
2-(1H-indazol-3-yl)-3H-benzoimidazole-4-carboxylic acid 2-methylsulfanyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-bromo-2-fluoro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 2,4-dichloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid 4-chloro-2-methyl-benzylamide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,6-difluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2,4-dichloro-6-fluoro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (3-fluoro-4-chloro-benzyl)amide;
2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-fluoro-4-chloro-6-methyl-benzyl)amide;
or 2-(1H-indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (6-methoxy-pyridin-3-ylmethyl)-amide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
160. A compound according to claim 3 which is 2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (2-piperidin-1-yl-ethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide;
N-[2-(1H-Indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide; or N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid (pyridin-2-ylmethyl)-amide;
2-(1H-Indazol-3-yl)-1H-benzoimidazole-5-carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide;
N-[2-(1H-Indazol-3-yl)-1H-benzoimidazol-5-yl]-isobutyramide; or N-[3-(5,6-Dimethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-2-piperidin-1-yl-acetamide;
or an N-oxide, prodrug, acid bioisostere, pharmaceutically acceptable salt or solvate of such compound; or an N-oxide, prodrug, or acid bioisostere of such salt or solvate.
161. A compound of the of formula (I) wherein X represents C-R2 and W, Y and Z, which may be identical or different, represent CH or CR3;
R1 represents aryl or heteroaryl chosen from pyrazolyl, triazolyl, imidazolyl, indolyl, indazolyl, thieno-pyrazolyl, tetrahydroindazolyl, tetrahydrocyclopentapyrazolyl, dihydrofuropyrazolyl, oxodihydropyridazinyl, tetrahydropyrrolopyrazolyl, oxotetrahydropyrrolopyrazolyl, tetrahydropyranopyrazolyl, tetrahydropyridinopyrazolyl, and oxodihydropyridinopyrazolyl radicals, all these radicals being optionally substituted with one or more radicals X1, X2 or X3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
R2 and R3 are such that:
either R2 and R3, which may be identical or different, represent H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4, or R2 represents H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 and R3 represents alkyl, haloalkyl, halogen or OR6, or R2 and R3 together form a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N and S;
R4 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from optionally substituted aryl, halogen, alkyl, hydroxyalkyl, OH, OR5, C(=O)NY3Y4, NY3Y4, alk-NY3Y4 and C(=O)OR6;
R5 represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl;
Y1 and Y2 are such that: either Y1 and Y2, which may be identical or different, represent H or optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl, or Y1 and Y2 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3 and Y4 are such that: either Y3 and Y4, which may be identical or different, represent hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl or Y3 and Y4 form, together with the nitrogen atom to which they are attached, an optionally substituted cyclic amino radical;
A5 represents H or alkyl;
R6 is chosen from the values of R5;
where all the alkyl, or alk, which represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals furthermore being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, acyl -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5, the phenyl radicals furthermore being optionally substituted with a dioxole radical;
n represents an integer from 0 to 2, provided that when R1 represents an indazolyl radical to give the compounds of formula (F) below:
with X representing H, R2 or R3 as defined above, then W of formula (F) necessarily represents H or unsubstituted alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
R1 represents aryl or heteroaryl chosen from pyrazolyl, triazolyl, imidazolyl, indolyl, indazolyl, thieno-pyrazolyl, tetrahydroindazolyl, tetrahydrocyclopentapyrazolyl, dihydrofuropyrazolyl, oxodihydropyridazinyl, tetrahydropyrrolopyrazolyl, oxotetrahydropyrrolopyrazolyl, tetrahydropyranopyrazolyl, tetrahydropyridinopyrazolyl, and oxodihydropyridinopyrazolyl radicals, all these radicals being optionally substituted with one or more radicals X1, X2 or X3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
R2 and R3 are such that:
either R2 and R3, which may be identical or different, represent H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4, or R2 represents H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 and R3 represents alkyl, haloalkyl, halogen or OR6, or R2 and R3 together form a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N and S;
R4 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from optionally substituted aryl, halogen, alkyl, hydroxyalkyl, OH, OR5, C(=O)NY3Y4, NY3Y4, alk-NY3Y4 and C(=O)OR6;
R5 represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl;
Y1 and Y2 are such that: either Y1 and Y2, which may be identical or different, represent H or optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl, or Y1 and Y2 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3 and Y4 are such that: either Y3 and Y4, which may be identical or different, represent hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl or Y3 and Y4 form, together with the nitrogen atom to which they are attached, an optionally substituted cyclic amino radical;
A5 represents H or alkyl;
R6 is chosen from the values of R5;
where all the alkyl, or alk, which represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals furthermore being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-COalk), -C(=O)OR6, acyl -C(=O)R6, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3Y4 and NY3Y4 radicals, the latter radicals containing alkyl, aryl and heteroaryl being themselves optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R5, the phenyl radicals furthermore being optionally substituted with a dioxole radical;
n represents an integer from 0 to 2, provided that when R1 represents an indazolyl radical to give the compounds of formula (F) below:
with X representing H, R2 or R3 as defined above, then W of formula (F) necessarily represents H or unsubstituted alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
162. A compound according to claim 160 of the formula (Ia) wherein Xa represents C-R2a; Wa, Ya and Za, which may be identical or different, represent CH or CR3a;
R1a represents aryl or heteroaryl chosen from pyrazolyl, triazolyl and indazolyl radicals, all these radicals being optionally substituted with one or more radicals X1a, X2a or X3a chosen from H, halogen, OH, R4a, OR4a, NY1aY2a, S(O)n R4a, -C(=O)NY1aY2a, -C(=O)OR4a, -N(R6a)C(=O)R4a, -N(R6a)SO2R4a, -N(R6a)C(=O)NY1aY2a, -N(R6a)C(=O)OR4a, -OC(=O)NY1aY2a, -OC(=O)R4a, -OS(O)n R4a and thienyl optionally substituted with an alkyl radical;
R2a and R3a are such that:
either R2a and R3a, which may be identical or different, represent H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a or -C(=O)OH, and R3a represents alkyl, halogen or OR4a, or R2a represents H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a or -C(=O)OH, and R3a represents alkyl, halogen or OR6a, or R2a and R3a together form an -O-CH2-O- or -O-CH2-CH2-O- ring, R4a represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from optionally substituted aryl, halogen, alkyl, hydroxyalkyl, OH, OR5a, C(=O)NY3aY4a, NY3aY4a, alk-NY3aY4a and C(=O)OR6a, R5a represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl, all these radicals being optionally substituted;
Y1a and Y2a are such that: either Y1a and Y2a, which may be identical or different, represent H, alkyl, alkoxyalkyl, aryloxyalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkyl, aryl or heteroaryl, all these radicals being optionally substituted, or Y1a and Y2a form, together with the nitrogen atom to which they are attached, an optionally substituted cyclic amino radical;
Y3a and Y4a are such that: either Y3a and Y4a, which may be identical or different, represent hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl, or Y3a and Y4a form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
A5 represents H or alkyl;
all the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals furthermore being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-C(O)R6a), -C(=O)OR6a, acyl -C(=O)R6a, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)2-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3aY4a and NY3aY4a radicals, the latter radicals containing alkyl, aryl and heteroaryl themselves being optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, alkoxy radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R6a, the phenyl radicals furthermore being optionally substituted with a dioxole radical;
R6a is chosen from the values of R5a, n represents an integer from 0 to 2; or or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
R1a represents aryl or heteroaryl chosen from pyrazolyl, triazolyl and indazolyl radicals, all these radicals being optionally substituted with one or more radicals X1a, X2a or X3a chosen from H, halogen, OH, R4a, OR4a, NY1aY2a, S(O)n R4a, -C(=O)NY1aY2a, -C(=O)OR4a, -N(R6a)C(=O)R4a, -N(R6a)SO2R4a, -N(R6a)C(=O)NY1aY2a, -N(R6a)C(=O)OR4a, -OC(=O)NY1aY2a, -OC(=O)R4a, -OS(O)n R4a and thienyl optionally substituted with an alkyl radical;
R2a and R3a are such that:
either R2a and R3a, which may be identical or different, represent H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a or -C(=O)OH, and R3a represents alkyl, halogen or OR4a, or R2a represents H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a or -C(=O)OH, and R3a represents alkyl, halogen or OR6a, or R2a and R3a together form an -O-CH2-O- or -O-CH2-CH2-O- ring, R4a represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from optionally substituted aryl, halogen, alkyl, hydroxyalkyl, OH, OR5a, C(=O)NY3aY4a, NY3aY4a, alk-NY3aY4a and C(=O)OR6a, R5a represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl, all these radicals being optionally substituted;
Y1a and Y2a are such that: either Y1a and Y2a, which may be identical or different, represent H, alkyl, alkoxyalkyl, aryloxyalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkyl, aryl or heteroaryl, all these radicals being optionally substituted, or Y1a and Y2a form, together with the nitrogen atom to which they are attached, an optionally substituted cyclic amino radical;
Y3a and Y4a are such that: either Y3a and Y4a, which may be identical or different, represent hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl, or Y3a and Y4a form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
A5 represents H or alkyl;
all the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl radicals present in the above radicals furthermore being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, acylamino (NH-C(O)R6a), -C(=O)OR6a, acyl -C(=O)R6a, hydroxyalkyl, carboxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)2-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, arylalkoxy, aryl, heteroaryl, aryloxy, aryloxyalkyl, -C(=O)-NY3aY4a and NY3aY4a radicals, the latter radicals containing alkyl, aryl and heteroaryl themselves being optionally substituted with one or more radicals chosen from halogen atoms and alkyl radicals, alkoxy radicals, free, salified or esterified carboxyl radicals and acylamino radicals NH-C(O)R6a, the phenyl radicals furthermore being optionally substituted with a dioxole radical;
R6a is chosen from the values of R5a, n represents an integer from 0 to 2; or or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
163. A compound of formula (I) wherein X represents C-R2; and W, Y and Z, which may be identical or different, represent CH or CR3;
R1 represents aryl or heteroaryl chosen from pyrazolyl, triazolyl, imidazolyl, indolyl, indazolyl, thieno-pyrazolyl, tetrahydroindazolyl, tetrahydrocyclopentapyrazolyl, dihydrofuropyrazolyl, oxodihydropyridazinyl, tetrahydropyrrolopyrazolyl, oxotetrahydropyrrolopyrazolyl, tetrahydropyrano-pyrazolyl, tetrahydropyridinopyrazolyl, and oxodihydro-pyridinopyrazolyl radicals, all these radicals optionally being substituted with one or more radicals X1, X2 or X3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl, R2 and R3 are such that:
either R2 and R3, which may be identical or different, represent H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)nNY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 or R2 represents H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 and R3 represents alkyl, haloalkyl, halogen and OR6 or R2 and R3 together form a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N and S;
R4 represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, hetero-arylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from aryl, OH, OR5, C(=O)NY3Y4, NY3Y4 and C(=O)OR6;
R5 represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl and heterocycloalkylalkyl;
R6 represents H and C1-C4 alkyl,;
n represents an integer from 0 to 2 Y1 and Y2 are such that: either Y1 and Y2, which may be identical or different, represent H, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, all these radicals being optionally substituted with one or more radicals chosen from hydroxyl, -C(=O)-NY3Y4, -C(=O)OR6 and NY3Y4, or Y1 and Y2 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3 and Y4 are such that: either Y3 and Y4, which may be identical or different, represent hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl or Y3 and Y4 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
A5 represents H or alkyl;
provided that when R1 represents an indazolyl radical to give the compound of formula (F) below:
with X representing H, R2 or R3 as defined above, then W of formula F
necessarily represents H or unsubstituted alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
R1 represents aryl or heteroaryl chosen from pyrazolyl, triazolyl, imidazolyl, indolyl, indazolyl, thieno-pyrazolyl, tetrahydroindazolyl, tetrahydrocyclopentapyrazolyl, dihydrofuropyrazolyl, oxodihydropyridazinyl, tetrahydropyrrolopyrazolyl, oxotetrahydropyrrolopyrazolyl, tetrahydropyrano-pyrazolyl, tetrahydropyridinopyrazolyl, and oxodihydro-pyridinopyrazolyl radicals, all these radicals optionally being substituted with one or more radicals X1, X2 or X3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl, R2 and R3 are such that:
either R2 and R3, which may be identical or different, represent H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)nNY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 or R2 represents H, R4, halogen, haloalkyl, OH, NO2, CN, OR4, COR4, S(O)n R4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -NY1Y2, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)n OR4, -S(O)n NY1Y2, -OC(=O)NY1Y2 or -OC(=O)R4 and R3 represents alkyl, haloalkyl, halogen and OR6 or R2 and R3 together form a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N and S;
R4 represents alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, hetero-arylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from aryl, OH, OR5, C(=O)NY3Y4, NY3Y4 and C(=O)OR6;
R5 represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl and heterocycloalkylalkyl;
R6 represents H and C1-C4 alkyl,;
n represents an integer from 0 to 2 Y1 and Y2 are such that: either Y1 and Y2, which may be identical or different, represent H, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, all these radicals being optionally substituted with one or more radicals chosen from hydroxyl, -C(=O)-NY3Y4, -C(=O)OR6 and NY3Y4, or Y1 and Y2 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3 and Y4 are such that: either Y3 and Y4, which may be identical or different, represent hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl or Y3 and Y4 form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
A5 represents H or alkyl;
provided that when R1 represents an indazolyl radical to give the compound of formula (F) below:
with X representing H, R2 or R3 as defined above, then W of formula F
necessarily represents H or unsubstituted alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
164. A compound according to claim 161 of the formula (Ia) wherein Xa represents C-R2a; and Wa, Ya and Za, which may be identical or different, represent CH or CR3a;
R1a represents aryl or heteroaryl chosen from pyrazolyl, triazolyl and indazolyl radicals, all these radicals being optionally substituted with one or more radicals X1a, X2a or X3a chosen from H, halogen, OH, R4a, OR4a, NY1aY2a, S(O)n R4a, -C(=O)NY1aY2a, -C(=O)OR4a, -N(R6a)C(=O)R4a, -N(R6a)SO2R4a, -N(R6a)C(=O)NY1aY2a, -N(R6a)C(=O)OR4a, -OC(=O)NY1aY2a and -OC(=O)R4a, -OS(O)n R4a and thienyl optionally substituted with an alkyl radical, R2a and R3a are such that:
either R2a and R3a, which may be identical or different, represent H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a, or -C(=O)OH, and R3a represents alkyl, halogen or OR6a, or R2a represents H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a, or -C(=O)OH, and R3a represents alkyl, halogen or OR6, or R2a and R3a together form an -O-CH2-O or -O-CH2-CH2-O- ring;
R4a represents alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from aryl, OH, OR5a, C(=O)NY3aY4a, NY3aY4a and C(=O)OR6a;
R5a represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl;
R6a represents H and C1-C4 alkyl;
n represents an integer from 0 to 2;
Y1a and Y2a are such that: either Y1a and Y2a, which may be identical or different, represent H, alkyl, cycloalkyl, aryl or heteroaryl, all these radicals being optionally substituted with one or more radicals chosen from hydroxyl, -C(=O)-NY3Y4, -C(=O)OR6 and NY3Y4, or Y1a and Y2a form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3a and Y4a are such that: either Y3a and Y4a, which may be identical or different, represent hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl, or Y3a and Y4a form, together with the nitrogen atom to which they are attached, a cyclic amino radical, A5 represents H or alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
R1a represents aryl or heteroaryl chosen from pyrazolyl, triazolyl and indazolyl radicals, all these radicals being optionally substituted with one or more radicals X1a, X2a or X3a chosen from H, halogen, OH, R4a, OR4a, NY1aY2a, S(O)n R4a, -C(=O)NY1aY2a, -C(=O)OR4a, -N(R6a)C(=O)R4a, -N(R6a)SO2R4a, -N(R6a)C(=O)NY1aY2a, -N(R6a)C(=O)OR4a, -OC(=O)NY1aY2a and -OC(=O)R4a, -OS(O)n R4a and thienyl optionally substituted with an alkyl radical, R2a and R3a are such that:
either R2a and R3a, which may be identical or different, represent H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a, or -C(=O)OH, and R3a represents alkyl, halogen or OR6a, or R2a represents H, R4a, halogen, OH, OR4a, C(=O)NY1aY2a, -C(=O)OR4a, or -C(=O)OH, and R3a represents alkyl, halogen or OR6, or R2a and R3a together form an -O-CH2-O or -O-CH2-CH2-O- ring;
R4a represents alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, heteroarylalkyl or arylalkyl, all these radicals being optionally substituted with one or more radicals chosen from aryl, OH, OR5a, C(=O)NY3aY4a, NY3aY4a and C(=O)OR6a;
R5a represents alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heteroarylalkyl or heterocycloalkylalkyl;
R6a represents H and C1-C4 alkyl;
n represents an integer from 0 to 2;
Y1a and Y2a are such that: either Y1a and Y2a, which may be identical or different, represent H, alkyl, cycloalkyl, aryl or heteroaryl, all these radicals being optionally substituted with one or more radicals chosen from hydroxyl, -C(=O)-NY3Y4, -C(=O)OR6 and NY3Y4, or Y1a and Y2a form, together with the nitrogen atom to which they are attached, a cyclic amino radical;
Y3a and Y4a are such that: either Y3a and Y4a, which may be identical or different, represent hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl, or Y3a and Y4a form, together with the nitrogen atom to which they are attached, a cyclic amino radical, A5 represents H or alkyl; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
165. A compound according to claim 161 of the formula IA
wherein A represents a saturated heterocyclic radical which is either a 5- or 6-membered monocyclic radical or a bicyclic radical that is not more than 10-membered, these members being such that at least two of them represent a nitrogen atom and the others, which may be identical or different, represent a carbon member or a hetero atom member chosen from O, N and S, this heterocycle A being optionally substituted with one or more radicals XA1, XA2 or XA3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y1, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
A1, A2, A3 and A4, which may be identical or different, are chosen from a hydrogen atom, halogen atoms and hydroxyl, alkyl, alkenyl, alkoxy, nitro, cyano, aryl, heteroaryl and aryloxy radicals, a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical, NA6A7 such that either A6 and A7, which may be identical or different, are chosen from a hydrogen atom and optionally substituted alkyl, alkoxyalkyl, phenoxyalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl and heteroarylalkyl radicals, or A6 and A7 form, together with the nitrogen atom to which they are attached, an optionally substituted 5- or 6-membered cyclic radical, it being understood that two consecutive radicals among A1, A2, A3 and A4 can form, with the benzimidazole radical to which they are attached, a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N
and S;
A5 represents a hydrogen atom or an alkyl radical;
R6b represents hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl and cycloalkylalkyl, all the alkyl, alkenyl, aryl, heteroaryl, aryloxy, cycloalkyl and heterocycloalkyl radicals present in the above radicals being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals, all the above alkyl, alkenyl, alkoxy and alkylthio radicals being linear or branched and containing not more than 4 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical;
n represents an integer from 0 to 2; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
wherein A represents a saturated heterocyclic radical which is either a 5- or 6-membered monocyclic radical or a bicyclic radical that is not more than 10-membered, these members being such that at least two of them represent a nitrogen atom and the others, which may be identical or different, represent a carbon member or a hetero atom member chosen from O, N and S, this heterocycle A being optionally substituted with one or more radicals XA1, XA2 or XA3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y1, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
A1, A2, A3 and A4, which may be identical or different, are chosen from a hydrogen atom, halogen atoms and hydroxyl, alkyl, alkenyl, alkoxy, nitro, cyano, aryl, heteroaryl and aryloxy radicals, a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical, NA6A7 such that either A6 and A7, which may be identical or different, are chosen from a hydrogen atom and optionally substituted alkyl, alkoxyalkyl, phenoxyalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl and heteroarylalkyl radicals, or A6 and A7 form, together with the nitrogen atom to which they are attached, an optionally substituted 5- or 6-membered cyclic radical, it being understood that two consecutive radicals among A1, A2, A3 and A4 can form, with the benzimidazole radical to which they are attached, a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N
and S;
A5 represents a hydrogen atom or an alkyl radical;
R6b represents hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl and cycloalkylalkyl, all the alkyl, alkenyl, aryl, heteroaryl, aryloxy, cycloalkyl and heterocycloalkyl radicals present in the above radicals being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals, all the above alkyl, alkenyl, alkoxy and alkylthio radicals being linear or branched and containing not more than 4 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical;
n represents an integer from 0 to 2; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
166. A compound according to claim 161 of the formula (IAa):
in which Aa represents a pyrazolyl, triazolyl or indazolyl radical, this heterocycle Aa being optionally substituted with one or more radicals XA1, XA2 or XA3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
A1a, A2a, A3a and A4a, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkoxy, nitro, cyano, phenyl and phenoxy radicals, and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6aA7a such that either A6a and A7a, which may be identical or different, are chosen from a hydrogen atom and alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, thienylalkyl and pyridylalkyl radicals, or A6a and A7a form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, pyrazolidinyl, pyrazolinyl, piperidyl, morpholino or piperazinyl radical optionally substituted on the second nitrogen atom with an alkyl or phenyl radical, which are themselves optionally substituted, it being understood that two consecutive radicals from among A1a, A2a, A3a and A4a may form, with the benzimidazole radical to which they are attached, an optionally substituted 5- to 6-membered carbon-based ring containing one or two oxygen atoms, A5a represents a hydrogen atom or an alkyl radical, the phenyl and phenoxy radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, free, salified or esterified carboxyl, and dioxole radicals;
all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 6 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
in which Aa represents a pyrazolyl, triazolyl or indazolyl radical, this heterocycle Aa being optionally substituted with one or more radicals XA1, XA2 or XA3 chosen from H, halogen, haloalkyl, OH, R4, NO2, CN, S(O)n R4, OR4, NY1Y2, COR4, -C(=O)NY1Y2, -C(=O)OR4, -C(=O)OH, -N(R6)C(=O)R4, -N(R6)SO2R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -S(O)nOR4, -S(O)n NY1Y2, -OC(=O)NY1Y2, -OS(O)n R4, -OC(=O)R4 and optionally substituted thienyl;
A1a, A2a, A3a and A4a, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkoxy, nitro, cyano, phenyl and phenoxy radicals, and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6aA7a such that either A6a and A7a, which may be identical or different, are chosen from a hydrogen atom and alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, thienylalkyl and pyridylalkyl radicals, or A6a and A7a form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, pyrazolidinyl, pyrazolinyl, piperidyl, morpholino or piperazinyl radical optionally substituted on the second nitrogen atom with an alkyl or phenyl radical, which are themselves optionally substituted, it being understood that two consecutive radicals from among A1a, A2a, A3a and A4a may form, with the benzimidazole radical to which they are attached, an optionally substituted 5- to 6-membered carbon-based ring containing one or two oxygen atoms, A5a represents a hydrogen atom or an alkyl radical, the phenyl and phenoxy radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, free, salified or esterified carboxyl, and dioxole radicals;
all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 6 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
167. A compound according to claim 161 of the formula IA
wherein A represents a saturated heterocyclic radical which is either a 5- or 6-membered monocyclic radical or a bicyclic radical that is not more than 10-membered, these members being such that at least two of them represent a nitrogen atom and the others, which may be identical or different, represent a carbon member or a hetero atom member chosen from O, N and S, this heterocycle A
optionally being substituted with one or more radicals XA1, XA2 or XA3 chosen from halogen atoms, alkyl, alkoxy or alkylthio radicals or thienyl radicals optionally substituted with an alkyl radical;
A1, A2, A3 and A4, which may be identical or different, are chosen from a hydrogen atom, halogen atoms and hydroxyl, alkyl, alkoxy, nitro, cyano, phenyl and phenoxy radicals, a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6A7 such that either A6 and A7, which may be identical or different, are chosen from a hydrogen atom and alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl and heteroarylalkyl radicals, or A6 and A7 form, together with the nitrogen atom to which they are attached, a 5- or 6-membered cyclic radical, it being understood that two consecutive radicals among A1, A2, A3 and A4 can form, with the benzimidazole radical to which they are attached, a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N
and S;
A5 represents a hydrogen atom or an alkyl radical;
all the phenyl, phenoxy, cycloalkyl and heteroarylalkyl radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, free, salified or esterified carboxyl, and dioxole radicals;
all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 6 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
wherein A represents a saturated heterocyclic radical which is either a 5- or 6-membered monocyclic radical or a bicyclic radical that is not more than 10-membered, these members being such that at least two of them represent a nitrogen atom and the others, which may be identical or different, represent a carbon member or a hetero atom member chosen from O, N and S, this heterocycle A
optionally being substituted with one or more radicals XA1, XA2 or XA3 chosen from halogen atoms, alkyl, alkoxy or alkylthio radicals or thienyl radicals optionally substituted with an alkyl radical;
A1, A2, A3 and A4, which may be identical or different, are chosen from a hydrogen atom, halogen atoms and hydroxyl, alkyl, alkoxy, nitro, cyano, phenyl and phenoxy radicals, a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6A7 such that either A6 and A7, which may be identical or different, are chosen from a hydrogen atom and alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl and heteroarylalkyl radicals, or A6 and A7 form, together with the nitrogen atom to which they are attached, a 5- or 6-membered cyclic radical, it being understood that two consecutive radicals among A1, A2, A3 and A4 can form, with the benzimidazole radical to which they are attached, a 5- to 6-membered carbon-based ring containing one or more hetero atoms, which may be identical or different, chosen from O, N
and S;
A5 represents a hydrogen atom or an alkyl radical;
all the phenyl, phenoxy, cycloalkyl and heteroarylalkyl radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, free, salified or esterified carboxyl, and dioxole radicals;
all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 6 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
168. A compound according to claim 161 of formula IAb wherein Ab represents a pyrazolyl or indazolyl radical optionally substituted with one or two radicals chosen from halogen atoms and OH, alkyl, alkynyl, -OR6b including alkoxy, -COR6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b, phenyl, phenylalkyl, CF3, OCF3, NO2, CN, NY1bY2b, -NH-C(=O)NY1bY2b, acylamino (NH-CO-R6b), S(O)n-alk, S(O)n-NY1bY2b, -C(=O)-NY1bY2b, -C(=O)OR6b, -NH-C(=O) R6b, -NH-S(O)n R6b, -NH-C(=O)OR6b, -N(R6b)C(=O)NY1bY2b, -OC(=O)NY1bY2b and thienyl radicals, all these radicals being optionally substituted, with NY1bY2b such that either Y1b and Y2b, which may be identical or different, are chosen from hydrogen and optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, phenyl, naphthyl, phenoxy, phenylalkyl, phenylalkylthio and naphthylalkyl or Y1b and Y2b form, together with the nitrogen atom to which they are attached, a piperidyl, hexahydrofuran, morpholinyl or morpholinylalkyl radical;
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, -OR6b including alkoxy, -CO-R6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benz-imidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimid-azole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5b represents a hydrogen atom;
all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals, with n representing an integer from 0 to 2, and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, pyridyl, thienyl, naphthyl, isoxazole, adamantyl, quinoline, quinolone, dihydroquinolone, -NH-phenyl, phenylalkyl or cycloalkylalkyl, all these radicals being optionally substituted with a morpholino, piperidyl or phenyl radical itself optionally substituted with one or more radicals chosen from halogen atoms and the cyano, CF3, OCF3, alkyl, phenyl-S(O)n-alk-phenyl, alkoxy, NH2, NHalk, N(alk)2, SO2NH2, SO2Nalk or SO2N(alk)2 radical, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, -OR6b including alkoxy, -CO-R6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benz-imidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimid-azole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5b represents a hydrogen atom;
all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals, with n representing an integer from 0 to 2, and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, pyridyl, thienyl, naphthyl, isoxazole, adamantyl, quinoline, quinolone, dihydroquinolone, -NH-phenyl, phenylalkyl or cycloalkylalkyl, all these radicals being optionally substituted with a morpholino, piperidyl or phenyl radical itself optionally substituted with one or more radicals chosen from halogen atoms and the cyano, CF3, OCF3, alkyl, phenyl-S(O)n-alk-phenyl, alkoxy, NH2, NHalk, N(alk)2, SO2NH2, SO2Nalk or SO2N(alk)2 radical, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
169. A compound according to claim 161 of the formula IAb wherein Ab represents a pyrazolyl or indazolyl radical optionally substituted with one or two radicals chosen from halogen atoms and OH, alkyl, alkynyl, alkoxy, phenyl, phenylalkyl, CF3, OCF3, NO2, CN, NY1bY2b, -NH-C(=O)NY1bY2b, acylamino (NH-CO-R6b), S(O)n-alk, S(O)n-NY1bY2b, -C(=O)-NY1bY2b, -C(=O)OR6b, -NH-C(=O)R6b, -NH-S(O)n R6b, -NH-C(=O)OR6b, -N(R6b)C(=O)NY1bY2b, -OC(=O)NY1bY2b and thienyl radicals which are optionally substituted, with NY1bY2b such that either Y1b and Y2b, which may be identical or different, are chosen from hydrogen and optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, phenyl, naphthyl, phenoxy, phenylalkyl, phenylalkylthio and naphthylalkyl or Y1b and Y2b form, together with the nitrogen atom to which they are attached, a piperidyl, hexahydrofuran, morpholinyl or morpholinylalkyl radical;
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, alkoxy, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benzimidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5b represents a hydrogen atom;
all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) or C(=O)-N(alk)2 radicals;
with n representing an integer from 0 to 2, and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkylalkyl, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, alkoxy, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benzimidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5b represents a hydrogen atom;
all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) or C(=O)-N(alk)2 radicals;
with n representing an integer from 0 to 2, and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkylalkyl, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
170. A compound according to claim 161 of the formula IAb wherein Ab represents a pyrazolyl radical substituted with one or two radicals such that one is chosen from hydrogen, halogen atoms and alkyl, alkynyl, -COR6b, phenyl, phenylalkyl, CF3, NO2, CN, NY1bY2b, -NH-C(=O)NY1bY2b, NH-CO-R6b, S(O)n-alk, S(O)n-NY1bY2b, -C(=O)-NY1bY2b, -C(=O)OR6b, -NH-C(=O)R6b, -NH-S(O)n R6b, -NH-C(=O)OR6b, -N(R6b)C(=O)NY1bY2b and thienyl radicals, all these radicals being optionally substituted, and the other is chosen from OH, -OR6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b and -OC(=O)NY1bY2b radicals, all these radicals being optionally substituted, with NY1bY2b such that Y1b and Y2b, which may be identical or different, are chosen from hydrogen and optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, phenyl, naphthyl, phenoxy, phenylalkyl, phenylalkylthio and naphthylalkyl or Y1b and Y2b form, together with the nitrogen atom to which they are attached, a piperidyl, hexahydrofuran, morpholinyl or morpholinylalkyl radical;
A1b, A2b, A3b and A4b, which may be identical or different, are such that two of them represent hydrogen and the other two, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, -OR6b (including alkoxy), -CO-R6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benz-imidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted;
A5b represents a hydrogen atom, all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals;
with n representing an integer from 0 to 2;
and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, pyridyl, thienyl, naphthyl, isoxazole, adamantyl, quinoline, quinolone, dihydroquinolone, -NH-phenyl, phenylalkyl and cycloalkylalkyl, all these radicals being optionally substituted with a morpholino, piperidyl or phenyl radical itself optionally substituted with one or more radicals chosen from halogen atoms and the cyano, CF3, OCF3, alkyl, phenyl-S(O)n-alk-phenyl, alkoxy, NH2, NHalk, N(alk)2, SO2NH2, SO2Nalk or SO2N(alk)2 radical, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
A1b, A2b, A3b and A4b, which may be identical or different, are such that two of them represent hydrogen and the other two, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkenyl, -OR6b (including alkoxy), -CO-R6b, -O-COR6b, -OS(O)n R6b, -O(CH2)n-CO-R6b, nitro, cyano, furyl, thienyl, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy radicals and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen and alkyl, alkoxyalkyl, phenoxyalkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, naphthylalkyl, thienylalkyl, piperidylalkyl, pyridylalkyl, benzothienylalkyl, pyrazolylalkyl, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl and benz-imidazolylalkyl radicals, all these radicals being optionally substituted, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical itself optionally substituted;
A5b represents a hydrogen atom, all the above radicals containing alkyl, alkenyl, phenyl, phenoxy, furyl, thienyl, piperidyl, pyridyl, pyrazolyl and benzimidazolyl being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, acylamino (NH-COR6b), -C(=O)OR6b, acyl -C(=O)R6b, hydroxyalkyl, carboxyalkyl, phenoxyalkyl, S(O)n-alk, S(O)n-NH2, S(O)n-NH(alk), S(O)n-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk) and C(=O)-N(alk)2 radicals;
with n representing an integer from 0 to 2;
and R6b representing hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, pyridyl, thienyl, naphthyl, isoxazole, adamantyl, quinoline, quinolone, dihydroquinolone, -NH-phenyl, phenylalkyl and cycloalkylalkyl, all these radicals being optionally substituted with a morpholino, piperidyl or phenyl radical itself optionally substituted with one or more radicals chosen from halogen atoms and the cyano, CF3, OCF3, alkyl, phenyl-S(O)n-alk-phenyl, alkoxy, NH2, NHalk, N(alk)2, SO2NH2, SO2Nalk or SO2N(alk)2 radical, all the alkyl, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 10 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
171. A compound according to claim 161 of the formula IAb wherein Ab represents a pyrazolyl or indazolyl radical optionally substituted with one or more radicals chosen from halogen atoms and alkyl, alkoxy and thienyl radicals;
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom;
halogen atom; hydroxyl, alkyl, alkenyl optionally substituted with phenyl itself optionally substituted with one or more halogen atoms, alkoxy, nitro, cyano, furyl, thienyl optionally substituted with acyl COalk, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy which are optionally substituted; and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen, alkyl, alkoxyalkyl containing not more than 6 carbon atoms, phenoxyalkyl optionally substituted with acylamino NH-C(O)alk, phenyl, optionally substituted phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl optionally substituted with one or more alkyl radicals, naphthylalkyl, thienylalkyl optionally substituted with alkyl or thienyl, piperidylalkyl optionally substituted with a carboxyl radical which is free, salified or esterified with an alkyl radical, pyridylalkyl optionally substituted with one or more radicals chosen from halogen and CF3, benzothienylalkyl, pyrazolylalkyl optionally substituted with one or more alkyl radicals, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl, and benzimidazolylalkyl optionally substituted with one or more alkyl radicals;
or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5a represents a hydrogen atom;
the phenyl, phenoxy and phenylalkyl radicals above being optionally substituted with one or more radicals chosen from halogen atoms, hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino and NH-COalk radicals, a carboxyl radical which is free, salified or esterified with an alkyl radical, and hydroxyalkyl, carboxyalkyl, phenoxyalkyl, alkylthio, SO2alk, SO2NH2, SO2-NH(alk), SO2-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk), C(=O)-N(alk)2 and C(O)CH3 radicals;
all the alkyl or alk, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 4 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom;
halogen atom; hydroxyl, alkyl, alkenyl optionally substituted with phenyl itself optionally substituted with one or more halogen atoms, alkoxy, nitro, cyano, furyl, thienyl optionally substituted with acyl COalk, benzothienyl, naphthyl, thianthrenyl, phenyl and phenoxy which are optionally substituted; and a carboxyl radical which is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from hydrogen, alkyl, alkoxyalkyl containing not more than 6 carbon atoms, phenoxyalkyl optionally substituted with acylamino NH-C(O)alk, phenyl, optionally substituted phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl optionally substituted with one or more alkyl radicals, naphthylalkyl, thienylalkyl optionally substituted with alkyl or thienyl, piperidylalkyl optionally substituted with a carboxyl radical which is free, salified or esterified with an alkyl radical, pyridylalkyl optionally substituted with one or more radicals chosen from halogen and CF3, benzothienylalkyl, pyrazolylalkyl optionally substituted with one or more alkyl radicals, dihydrobenzofuranylalkyl, hexahydropyranylalkyl, ethylenedioxyphenylalkyl, and benzimidazolylalkyl optionally substituted with one or more alkyl radicals;
or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical, the piperazinyl radical being optionally substituted on the second nitrogen atom with an alkyl radical, it being understood that two consecutive radicals among A1b, A2b, A3b and A4b can form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or an optionally substituted 4,5-methylenedioxybenzimidazole radical;
A5a represents a hydrogen atom;
the phenyl, phenoxy and phenylalkyl radicals above being optionally substituted with one or more radicals chosen from halogen atoms, hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino and NH-COalk radicals, a carboxyl radical which is free, salified or esterified with an alkyl radical, and hydroxyalkyl, carboxyalkyl, phenoxyalkyl, alkylthio, SO2alk, SO2NH2, SO2-NH(alk), SO2-N(alk)2, CF3, OCF3, NO2, CN, phenyl, itself optionally substituted with one or more halogen atoms, thienyl, phenoxy, phenylalkoxy, -C(=O)-NH2, -C(=O)-NH(alk), C(=O)-N(alk)2 and C(O)CH3 radicals;
all the alkyl or alk, alkenyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 4 carbon atoms, all the phenyl radicals of the above radicals furthermore being optionally substituted with a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
172. A compound according to any one of claims 168, 169, 170 or 171 wherein when one of A1b, A2b, A3b and A4b represents a carboxyl radical amidated with a radical NA6bA7b, then either one of A6b and A7b represents a hydrogen atom or an alkyl radical and the other of A6b and A7b is chosen from the values defined for A6b and A7b, or A6b and A7b form, together with the nitrogen atom to which they are attached, a 5- or 6-membered cyclic radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
173. A compound according to claim 161 wherein X, W, Y and Z are such that two or three of them represent CH and the others are chosen from CR2 and CR3 and, when two of them represent CH and CR2 and CR3 are adjacent to each other, can form a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
174. A compound according to claim 165 or claim 167 wherein A1, A2, A3 and A4 are such that two or three of them represent a hydrogen atom and, when two of them represent a hydrogen atom and the other two are on adjacent carbons, can form a dioxole radical; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
175. A compound according to claim 161 of the formula (IAa) wherein Aa represents a pyrazolyl, triazolyl or indazolyl radical, this heterocycle Aa being optionally substituted with one or more radicals XA1, XA2 or XA3 chosen from halogen atoms, alkyl, alkoxy, alkylthio radicals and thienyl radicals optionally substituted with an alkyl radical, A1a, A2a, A3a and A4a, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl, alkoxy, nitro, cyano, phenyl and phenoxy radicals, and a carboxyl radical which is free, salified, esteritied with an alkyl radical or amidated with a radical NA6aA7a such that either A6a and A7a, which may be identical or different, are chosen from a hydrogen atom and alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl, furylalkyl, thienylalkyl and pyridylalkyl radicals, or A6a and A7a form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, pyrazolidinyl, pyrazolinyl, piperidyl, morpholino or piperazinyl radical optionally substituted on the second nitrogen atom with an alkyl or phenyl radical, which are themselves optionally substituted, it being understood that two consecutive radicals from among A1a, A2a, A3a and A4a may form, with the benzimidazole radical to which they are attached, an optionally substituted 5- to 6-membered carbon-based ring containing one or two oxygen atoms, A5a represents a hydrogen atom or an alkyl radical, the phenyl and phenoxy radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino, free, salified or esterified carboxyl, and dioxole radicals, all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 6 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
176. A compound according to claim 161 wherein R1 represents a pyrazolyl or indazolyl radical.
177. A compound according to claim 166 or claim 175 wherein Aa represents an optionally substituted pyrazolyl or an optionally substituted indazolyl radical, A1a, A2a, A3a and A4a are chosen from the following values:
A1a represents hydrogen or carboxyl or forms a ring with the adjacent member A,a;
A4a represents hydrogen or carboxyl or forms a ring with the adjacent member A3a;
A2a represents a carboxyl radical that is free, salified, esterified with an optionally substituted alkyl radical or an amidated carboxyl;
A2a and A3a represent two optionally substituted alkyl radicals; and A5a represents hydrogen; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
A1a represents hydrogen or carboxyl or forms a ring with the adjacent member A,a;
A4a represents hydrogen or carboxyl or forms a ring with the adjacent member A3a;
A2a represents a carboxyl radical that is free, salified, esterified with an optionally substituted alkyl radical or an amidated carboxyl;
A2a and A3a represent two optionally substituted alkyl radicals; and A5a represents hydrogen; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
178. A compound according to claim 161 of the formula (IAb):
wherein Ab represents a pyrazolyl or indazolyl radical optionally substituted with one or more radicals chosen from halogen atoms and alkyl, alkoxy and thienyl radicals, A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl and alkoxy, nitro, cyano, phenyl and phenoxy radicals, and a carboxyl radical that is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl and furylalkyl radicals, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical optionally substituted on the second nitrogen atom with an alkyl radical, it being understood that two consecutive radicals from among A1b, A2b, A3b and A4b may form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or 4,5-methylenedioxybenzimidazole radical, A5b represents a hydrogen atom, the phenyl and phenoxy radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino and free, salified or esterified carboxyl radicals, all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 4 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
wherein Ab represents a pyrazolyl or indazolyl radical optionally substituted with one or more radicals chosen from halogen atoms and alkyl, alkoxy and thienyl radicals, A1b, A2b, A3b and A4b, which may be identical or different, are chosen from a hydrogen atom, halogen atoms, hydroxyl, alkyl and alkoxy, nitro, cyano, phenyl and phenoxy radicals, and a carboxyl radical that is free, salified, esterified with an alkyl radical or amidated with a radical NA6bA7b such that either A6b and A7b, which may be identical or different, are chosen from alkyl, phenyl, phenylalkyl, cycloalkylalkyl, cycloalkyl and furylalkyl radicals, or A6b and A7b form, together with the nitrogen atom to which they are attached, a pyrrolidinyl, morpholino or piperazinyl radical optionally substituted on the second nitrogen atom with an alkyl radical, it being understood that two consecutive radicals from among A1b, A2b, A3b and A4b may form, with the benzimidazole radical to which they are attached, an optionally substituted 4,5-ethylenedioxybenzimidazole radical or 4,5-methylenedioxybenzimidazole radical, A5b represents a hydrogen atom, the phenyl and phenoxy radicals above being optionally substituted with one or more radicals chosen from halogen atoms and hydroxyl, cyano, alkyl, alkoxy, amino, alkylamino, dialkylamino, phenylamino, phenylalkylamino and free, salified or esterified carboxyl radicals, all the alkyl, alkoxy and alkylthio radicals above being linear or branched and containing not more than 4 carbon atoms; or the racemic, enantiomeric or diastereoisomeric isomer form of such compound, or the addition salt with a mineral or an organic acid or with a mineral base of such compound.
179. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound according to any one of claims 3 to 178, together with one or more pharmaceutically acceptable carriers or excipients.
180. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of Syk comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
181. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of Syk comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
182. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of KDR comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
183. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of KDR comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
184. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of tie2 comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
185. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of tie2 comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
186. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of ITK comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
187. A method of treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of the catalytic activity of ITK comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
88. A method of treating inflammatory disease in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
189. A method of treating inflammatory disease in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
190. A method of treating cancer in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
191. A method of treating cancer in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
192. A method of treating Chronic Obstructive Pulmonary Disease, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
193. A method of treating Chronic Obstructive Pulmonary Disease, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
194. A method of treating asthma, allergic rhinitis, atopic dermatitis, allergic conjunctivitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, silicosis, pulmonary sarcoidosis, rheumatoid arthritis, osteoarthritis, rheumatoid spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis, acute and chronic urticaria, cutaneous and systemic anaphylaxis, endotoxemia, sepsis, septic shock, endotoxic shock, gram negative sepsis, diabetes, multiple sclerosis, systemic lupus erythromatosis, viral infections, bacterial infections, parasitic infections, graft vs. host disease, organ transplant rejection, reperfusion injury, Crohn's disease or ulcerative colitis, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
195. A method of treating asthma, allergic rhinitis, atopic dermatitis, allergic conjunctivitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, silicosis, pulmonary sarcoidosis, rheumatoid arthritis, osteoarthritis, rheumatoid spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis, acute and chronic urticaria, cutaneous and systemic anaphylaxis, endotoxemia, sepsis, septic shock, endotoxic shock, gram negative sepsis, diabetes, multiple sclerosis, systemic lupus erythromatosis, viral infections, bacterial infections, parasitic infections, graft vs. host disease, organ transplant rejection, reperfusion injury, Crohn's disease or ulcerative colitis, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
196. A method of treating cancers, atherosclerosis, degenerative muscle diseases, obesity, conjestive heart failure, Parkinson's, depression, schizophrenia, stroke, head trauma, spinal cord injury, Alzheimer's, neuropathic pain syndrome, amyotrophic lateral sclerosis, cachexia, osteoporosis or fibrotic diseases of the viscera, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
197. A method of treating cancers, atherosclerosis, degenerative muscle diseases, obesity, conjestive heart failure, Parkinson's, depression, schizophrenia, stroke, head trauma, spinal cord injury, Alzheimer's, neuropathic pain syndrome, amyotrophic lateral sclerosis, cachexia, osteoporosis or fibrotic diseases of the viscera, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
198. A method of treating asthma, atopic dermatitis, psoriasis, dematitis herpetiformis, eczema, necrotizing and cutaneous vasculitis, bullous disease, acute and chronic urticaria, allergic rhinitis or allergic conjunctivitis, arthritis, rheumatoid arthritis, rheumatoid spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis and osteoarthritis, Chronic Obstructive Pulmonary Disease, adult respiratory distress syndrome, silicosis, pulmonary sarcoidosis, acute synovitis, autoimmune diabetes, autoimmune encephalomyelitis, collitis, atherosclerosis, peripheral vascular disease, cardiovascular disease, cutaneous and systemic anaphylaxis, endotoxemia, sepsis, septic shock, endotoxic shock, gram negative sepsis, diabetes, multiple sclerosis, restenosis, myocarditis, B cell lymphomas, systemic lupus erythematosus, viral infections, bacterial infections, parasitic infections, graft v host disease and other transplant associated rejection events, reperfusion injury, Crohn's disease, ulcerative colitis, cancers, tumours, atherosclerosis, degenerative muscle diseases, obesity, conjestive heart failure, Parkinson's, depression, schizophrenia, stroke, head trauma, spinal cord injury, Alzheimer's, neuropathic pain syndrome, amyotrophic lateral sclerosis, cachexia, osteoporosis, fibrotic diseases of the viscera, or inflammatory bowel disease, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
199. A method of treating asthma, atopic dermatitis, psoriasis, dematitis herpetiformis, eczema, necrotizing and cutaneous vasculitis, bullous disease, acute and chronic urticaria, allergic rhinitis or allergic conjunctivitis, arthritis, rheumatoid arthritis, rheumatoid spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis and osteoarthritis, Chronic Obstructive Pulmonary Disease, adult respiratory distress syndrome, silicosis, pulmonary sarcoidosis, acute synovitis, autoimmune diabetes, autoimmune encephalomyelitis, collitis, atherosclerosis, peripheral vascular disease, cardiovascular disease, cutaneous and systemic anaphylaxis, endotoxemia, sepsis, septic shock, endotoxic shock, gram negative sepsis, diabetes, multiple sclerosis, restenosis, myocarditis, B cell lymphomas, systemic lupus erythematosus, viral infections, bacterial infections, parasitic infections, graft v host disease and other transplant associated rejection events, reperfusion injury, Crohn's disease, ulcerative colitis, cancers, tumours, atherosclerosis, degenerative muscle diseases, obesity, conjestive heart failure, Parkinson's, depression, schizophrenia, stroke, head trauma, spinal cord injury, Alzheimer's, neuropathic pain syndrome, amyotrophic lateral sclerosis, cachexia, osteoporosis, fibrotic diseases of the viscera, or inflammatory bowel disease, in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
200. A method of inhibiting angiogenesis in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
201. A method of inhibiting angiogenesis in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
202. A method according to claim 190 or claim 191 wherein the cancer being treated is colorectal, prostate, breast, thyroid, skin, colon or lung cancer.
203. A method of treating asthma in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
204. A method of treating asthma in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
205. A method of treating psoriasis in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
206. A method of treating psoriasis in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
207. A method of treating joint inflammation in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
208. A method of treating joint inflammation in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
209. A method of treating inflammatory bowel disease in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a compound according to any one of claims 3 to 178.
210. A method of treating inflammatory bowel disease in a patient in need thereof comprising administering to said patient a pharmaceutically effective amount of a composition according to any one of claims 1, 2 or 179.
211. A process for preparing the compound of formula (I) according to claim 161, characterized in that an acid of formula (D):~
R1'-COOH (D) in which R1' has the meaning given in Claim 161 for R1, in which the possible reactive functions are optionally protected with protecting groups, is subjected to an esterification reaction to give an acid ester of formula (II) R1'-COOalk ~(II) in which R1' has the meaning given above and alk represents an alkyl radical, is subjected to a reduction reaction to give the alcohol of formula (III):
R1'-CH2OH (III) in which R1' has the meaning given above, which is oxidized to the aldehyde of formula (IV):
R1'-CHO (IV) in which R1' has the meaning given above, and the compound of formula (D) or compound of formula (IV) as defined above is reacted with a diamine of formula (V):
in which W', X', Y' and Z' have the meanings given in Claim 161, respectively, for W, X, Y and Z, in which the possible reactive functions are optionally protected with protecting groups, to give a compound of formula (I'):
in which A5' has the meaning given in Claim 161 for A5, in which the possible reactive functions are optionally protected with protecting groups, and R1', W', X', Y' and Z' have the meanings given above, the compound of formula (I') being a compound which may be a compound of formula (I) and which, in order to obtain a compound or other compound of formula (I), may be subjected, if desired and if necessary, to one or more of the following conversion reactions, in any order:
a) an esterification reaction of an acid function, b) a saponification reaction of an ester function to an acid function, c) an oxidation reaction of an alkylthio group to the corresponding sulphoxide or sulphone, d) a reaction for conversion of a ketone function to an oxime function, e) a reaction for reduction of the free or esterified carboxyl function to an alcohol function, f) a reaction for conversion of the alkoxy function to a hydroxyl function, or alternatively of the hydroxyl function to an alkoxy function, g) a reaction for oxidation of an alcohol function to an aldehyde, acid or ketone function, h) a reaction for conversion of a nitrile radical to a tetrazolyl, i) a reaction for removal of the protecting groups that may be borne on the protected reactive functions, j) a salification reaction with a mineral or organic acid or with a base to give the corresponding salt, k) a reaction for resolution of the racemic forms into resolved products, the said compound of formula (I) thus being obtained in any possible racemic, enantiomeric or diastereoisomeric isomer form.
R1'-COOH (D) in which R1' has the meaning given in Claim 161 for R1, in which the possible reactive functions are optionally protected with protecting groups, is subjected to an esterification reaction to give an acid ester of formula (II) R1'-COOalk ~(II) in which R1' has the meaning given above and alk represents an alkyl radical, is subjected to a reduction reaction to give the alcohol of formula (III):
R1'-CH2OH (III) in which R1' has the meaning given above, which is oxidized to the aldehyde of formula (IV):
R1'-CHO (IV) in which R1' has the meaning given above, and the compound of formula (D) or compound of formula (IV) as defined above is reacted with a diamine of formula (V):
in which W', X', Y' and Z' have the meanings given in Claim 161, respectively, for W, X, Y and Z, in which the possible reactive functions are optionally protected with protecting groups, to give a compound of formula (I'):
in which A5' has the meaning given in Claim 161 for A5, in which the possible reactive functions are optionally protected with protecting groups, and R1', W', X', Y' and Z' have the meanings given above, the compound of formula (I') being a compound which may be a compound of formula (I) and which, in order to obtain a compound or other compound of formula (I), may be subjected, if desired and if necessary, to one or more of the following conversion reactions, in any order:
a) an esterification reaction of an acid function, b) a saponification reaction of an ester function to an acid function, c) an oxidation reaction of an alkylthio group to the corresponding sulphoxide or sulphone, d) a reaction for conversion of a ketone function to an oxime function, e) a reaction for reduction of the free or esterified carboxyl function to an alcohol function, f) a reaction for conversion of the alkoxy function to a hydroxyl function, or alternatively of the hydroxyl function to an alkoxy function, g) a reaction for oxidation of an alcohol function to an aldehyde, acid or ketone function, h) a reaction for conversion of a nitrile radical to a tetrazolyl, i) a reaction for removal of the protecting groups that may be borne on the protected reactive functions, j) a salification reaction with a mineral or organic acid or with a base to give the corresponding salt, k) a reaction for resolution of the racemic forms into resolved products, the said compound of formula (I) thus being obtained in any possible racemic, enantiomeric or diastereoisomeric isomer form.
212. A process for preparing the compound of formula (I) according to claim 1, corresponding to formula (IA) according to any one of claims 165, 167 or 174, characterized in that an acid of formula (D):
A'-COOH ~(D) in which A' has the meaning given in any one of claims 165, 167 or 174 for A, in which the possible reactive functions are optionally protected with protecting groups, is subjected to an esterification reaction to give an acid ester of formula (II) A'-COOalk ~(II) in which A' has the meaning given above and alk represents an alkyl radical, is subjected to a reduction reaction to give the alcohol of formula (III):
A'-CH2OH ~(III) in which A' has the meaning given above, which is oxidized to the aldehyde of formula (IV):
A'-CHO ~~(IV) in which A' has the meaning given above, and the compound of formula (D) or compound of formula (IV) as defined above are reacted with a diamine of formula (V):
in which A1', A2', A3' and A4' have the meanings given in any one of claims 165, 167 or 174, respectively, for A1, A2, A3 and A4, in which the possible reactive functions are optionally protected with protecting groups, to give a compound of formula (IA'):
in which A5' has the meaning given in any one of claims 165, 167 or 175 for A5, in which the possible reactive functions are optionally protected with protecting groups, and A1', A2', A3' and A4' have the meanings given above, the compound of formula (IA') is a compound which may be a compound of formula (IA) and which, in order to obtain a compound or another compound of formula (IA), may be subjected, if desired and if necessary, in any order, to one or more of the conversion reactions chosen from among the reactions a) to k) defined in Claim 211, the said compound of formula (IA) thus obtained being in any possible racemic, enantiomeric or diastereoisomeric isomer form.
A'-COOH ~(D) in which A' has the meaning given in any one of claims 165, 167 or 174 for A, in which the possible reactive functions are optionally protected with protecting groups, is subjected to an esterification reaction to give an acid ester of formula (II) A'-COOalk ~(II) in which A' has the meaning given above and alk represents an alkyl radical, is subjected to a reduction reaction to give the alcohol of formula (III):
A'-CH2OH ~(III) in which A' has the meaning given above, which is oxidized to the aldehyde of formula (IV):
A'-CHO ~~(IV) in which A' has the meaning given above, and the compound of formula (D) or compound of formula (IV) as defined above are reacted with a diamine of formula (V):
in which A1', A2', A3' and A4' have the meanings given in any one of claims 165, 167 or 174, respectively, for A1, A2, A3 and A4, in which the possible reactive functions are optionally protected with protecting groups, to give a compound of formula (IA'):
in which A5' has the meaning given in any one of claims 165, 167 or 175 for A5, in which the possible reactive functions are optionally protected with protecting groups, and A1', A2', A3' and A4' have the meanings given above, the compound of formula (IA') is a compound which may be a compound of formula (IA) and which, in order to obtain a compound or another compound of formula (IA), may be subjected, if desired and if necessary, in any order, to one or more of the conversion reactions chosen from among the reactions a) to k) defined in Claim 211, the said compound of formula (IA) thus obtained being in any possible racemic, enantiomeric or diastereoisomeric isomer form.
213. As medicinal compounds, the compounds of formula (I) as defined in any one of Claims 161 to 178, and also the addition salts with pharmaceutically acceptable mineral and organic acids or with pharmaceutically acceptable mineral and organic bases of the said compounds of formula (I).
214. As medicinal compounds, the compounds of formula (I) as defined in any one of Claims 156 to 159, and also the addition salts with pharmaceutically acceptable mineral and organic acids or with pharmaceutically acceptable mineral and organic bases of the said compounds of formula (I).
215. Pharmaceutical compositions containing, as active principle, at least one of the compounds of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, or a pharmaceutically acceptable salt of this product or a prodrug of this compound and a pharmaceutically acceptable support.
216. Use of the compounds of formula (1) as defined in any one of claims 156 to 159 or claims 161 to 178, or of pharmaceutically acceptable salts of these compounds, for the preparation of a medicinal product intended for inhibiting the activity of a kinase protein.
217. Use of a compound of formula (I) as defined in any one of claims 156 to l59 or claims 161 to 178, for the preparation of a medicinal product for treating or preventing a disease characterized by deregulation of the activity of a kinase protein.
218. Use according to claim 216, in which the kinase protein is a tyrosine kinase protein.
219. Use as defined in claim 216, in which the kinase protein is chosen from the following group:
FGFR1, FGFR2, FGFR3, FGFR4, FGFR5, flt-1, IGF-1R, KDR, PDGFR, tie2 and VEGFR.
FGFR1, FGFR2, FGFR3, FGFR4, FGFR5, flt-1, IGF-1R, KDR, PDGFR, tie2 and VEGFR.
220. Use as defined in claim 216, in which the kinase protein is KDR.
221. Use as defined in Claim 216, in which the kinase protein is tie2.
222. Use as defined in Claim 216, in which the kinase protein is in a cell culture.
223. Use as defined in Claim 216, in which the kinase protein is in a mammal.
224. Use of a compound of formula (1) as defined in any one of claims 156 to 159 or claims 161 to 178, for the preparation of a medicinal product for treating or preventing a disease chosen from the following group: disorders of the proliferation of blood vessels, fibrotic disorders, disorders of the proliferation of "mesangial" cells, metabolic disorders, allergies, asthma, thrombosis, diseases of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration and cancers.
225. Use of a product of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, for the preparation of a medicinal product for treating or preventing a disease chosen from the following group: disorders of the proliferation of blood vessels, fibrotic disorders, disorders of the proliferation of "mesangial" cells, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration and cancers.
226. Use of a compound of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, for the preparation of a medicinal product for preventing or treating diseases associated with an uncontrolled angiogenesis.
227. Use of a compound of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, for the preparation of a medicinal product for treating diseases in oncology.
228. Use of a compound of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, for the preparation of a medicinal product for treating cancers.
229. Use according to claim 227, for the treatment of solid tumours.
230. Use according to Claim 228 or 229, for the treatment of cancers that are resistant to cytotoxic agents.
231. Use according to claim 228 or 229, for the treatment of breast cancer, stomach cancer, cancer of the ovaries, cancer of the colon, lung cancer, brain cancer, cancer of the larynx, cancer of the lymphatic system, cancer of the genito-urinary tract including the bladder and the prostate, bone cancer and cancer of the pancreas.
232. Use according to claim 228 or 229, for the treatment of breast cancer, cancer of the colon or lung cancer.
233. Use of the compounds of formula (I) as defined in claims 156 to 159 or claims 161 to 178, for the preparation of medicinal products intended for cancer chemotherapy.
234. Use of the compounds of formula (I) as defined in claims 156 to 159 or claims 161 to 178, for the preparation of medicinal products intended for cancer chemotherapy alone or in combination.
235. Compounds of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, as kinase inhibitors.
236. Compounds of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, as KDR inhibitors.
237. Compounds of formula (I) as defined in any one of claims 156 to 159 or claims 161 to 178, as tie2 inhibitors.
238. A method according to claim 190 or claim 191 wherein the cancer being treated is breast cancer, stomach cancer, cancer of the ovaries, cancer of the colon, lung cancer, brain cancer, cancer of the larynx, cancer of the lymphatic system, cancer of the genito-urinary tract, bladder, prostate, bone cancer or cancer of the pancreas.
Applications Claiming Priority (11)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0113868A FR2831537B1 (en) | 2001-10-26 | 2001-10-26 | NOVEL BENZIMIDAZOLE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, THEIR USE AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND THE USE THEREOF |
FR01/13868 | 2001-10-26 | ||
GB0206893A GB0206893D0 (en) | 2002-03-22 | 2002-03-22 | Chemical compounds |
GB0206893.0 | 2002-03-22 | ||
GB0206895A GB0206895D0 (en) | 2002-03-22 | 2002-03-22 | Chemical compounds |
GB0206895.5 | 2002-03-22 | ||
US39506002P | 2002-07-11 | 2002-07-11 | |
US39515102P | 2002-07-11 | 2002-07-11 | |
US60/395,060 | 2002-07-11 | ||
US60/395,151 | 2002-07-11 | ||
PCT/GB2002/004763 WO2003035065A1 (en) | 2001-10-26 | 2002-10-24 | Benzimidazoles and analogues and their use as protein kinases inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2465247A1 true CA2465247A1 (en) | 2003-05-01 |
CA2465247C CA2465247C (en) | 2010-05-18 |
Family
ID=27515325
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2465247A Expired - Fee Related CA2465247C (en) | 2001-10-26 | 2002-10-24 | Benzimidazoles and analogues and their use as protein kinases inhibitors |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP1441725A1 (en) |
JP (1) | JP5039268B2 (en) |
AU (1) | AU2002334217B2 (en) |
BR (1) | BR0213562A (en) |
CA (1) | CA2465247C (en) |
IL (1) | IL161576A0 (en) |
MX (1) | MXPA04003954A (en) |
UY (1) | UY27516A1 (en) |
WO (1) | WO2003035065A1 (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104098513A (en) * | 2014-07-30 | 2014-10-15 | 天津市斯芬克司药物研发有限公司 | Indazole compound derivative and preparation method |
WO2023234970A1 (en) * | 2022-06-01 | 2023-12-07 | KUDA Therapeutics, Inc. | Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of hif-1/2a pathway inhibition, and induction of ferroptosis |
Families Citing this family (156)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MXPA04007697A (en) * | 2002-02-06 | 2004-11-10 | Vertex Pharma | Heteroaryl compounds useful as inhibitors of gsk-3. |
DE10227668A1 (en) * | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Medicines for the treatment of systemic inflammatory response syndrome |
CA2494421A1 (en) | 2002-08-06 | 2004-02-12 | Astrazeneca Ab | Condensed pyridines and pyrimidines with tie2 (tek) activity |
US7309701B2 (en) | 2002-11-19 | 2007-12-18 | Sanofi-Aventis Deutschland Gmbh | Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them |
US7462613B2 (en) | 2002-11-19 | 2008-12-09 | Sanofi-Aventis Deutschland Gmbh | Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them |
JP2004189738A (en) * | 2002-11-29 | 2004-07-08 | Nippon Nohyaku Co Ltd | Substituted anilide derivative, its intermediate, agricultural horticultural chemical and usage of the same |
GB0315657D0 (en) * | 2003-07-03 | 2003-08-13 | Astex Technology Ltd | Pharmaceutical compounds |
TWI372050B (en) * | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
KR101190964B1 (en) * | 2003-07-03 | 2012-10-12 | 아스텍스 테라퓨틱스 리미티드 | Benzimidazole derivatives and their use as protein kinases inhibitors |
AR045037A1 (en) * | 2003-07-10 | 2005-10-12 | Aventis Pharma Sa | TETRAHIDRO-1H-PIRAZOLO [3,4-C] SUBSTITUTED PYRIDINS, COMPOSITIONS THAT CONTAIN THEM AND ITS USE. |
RS51846B (en) * | 2003-09-08 | 2012-02-29 | Aventis Pharmaceuticals Inc. | Thienopyrazoles |
ES2319539T3 (en) * | 2003-09-17 | 2009-05-08 | Janssen Pharmaceutica Nv | HETEROCICLICAL COMPOUNDS CONDENSED AS SEROTONINE RECEPTOR MODULATORS. |
EP1694671A2 (en) | 2003-12-04 | 2006-08-30 | Vertex Pharmaceuticals Incorporated | Quinoxalines useful as inhibitors of protein kinases |
WO2005065686A1 (en) * | 2004-01-07 | 2005-07-21 | Adipogen Pharmaceuticals Pty Limited | Differentiation modulating agents and uses therefor |
WO2005079791A1 (en) * | 2004-02-12 | 2005-09-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders |
ITTO20040125A1 (en) * | 2004-03-01 | 2004-06-01 | Rotta Research Lab | NEW HETEROCYCLIC AMIDINS INHIBITIVE THE PRODUCTION OF NITROGEN OXIDE (NO) FOR ANTI-INFLAMMATORY AND ANALGESIC ACTIVITY |
DE102004010207A1 (en) | 2004-03-02 | 2005-09-15 | Aventis Pharma S.A. | New 4-benzimidazolyl-3(2H)-pyridazinone derivatives are kinase inhibitors, especially useful for treatment of cancer |
DE102004010194A1 (en) * | 2004-03-02 | 2005-10-13 | Aventis Pharma Deutschland Gmbh | 4-Benzimidazol-2-yl-pyridazin-3-one derivatives, their preparation and use in medicaments |
GT200500208A (en) * | 2004-08-03 | 2006-03-02 | USEFUL INDAZOLS TO TREAT CARDIOVASCULAR DISEASES | |
EP1797072A4 (en) | 2004-09-17 | 2009-09-09 | Exelixis Inc | Pyrazole kinase modulators and methods of use |
JP2008513508A (en) | 2004-09-21 | 2008-05-01 | シンタ ファーマシューティカルズ コーポレーション | Compounds used for inflammation and immunity related applications |
US7285569B2 (en) | 2004-09-24 | 2007-10-23 | Hoff Hoffmann-La Roche Inc. | Tricycles, their manufacture and use as pharmaceutical agents |
DE602005026037D1 (en) * | 2004-10-27 | 2011-03-03 | Janssen Pharmaceutica Nv | TETRAHYDRO PYRIDINYL PYRAZOLE CANNABINOID MODULATORS |
CN101830899A (en) * | 2004-12-23 | 2010-09-15 | 霍夫曼-拉罗奇有限公司 | Heterocyclic carbamate derivatives, their manufacture and use as pharmaceutical agents |
US7618964B2 (en) | 2004-12-23 | 2009-11-17 | Hoffmann-La Roche Inc. | Benzamide derivatives, their manufacture and use as pharmaceutical agents |
US20100160324A1 (en) * | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
EP1833819A1 (en) * | 2004-12-30 | 2007-09-19 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases |
JPWO2006080450A1 (en) * | 2005-01-27 | 2008-06-19 | 協和醗酵工業株式会社 | IGF-1R inhibitor |
CN101160312A (en) * | 2005-04-14 | 2008-04-09 | 霍夫曼-拉罗奇有限公司 | Tricyclic azole derivatives, their manufacture and use as pharmaceutical agents |
MX2007012477A (en) | 2005-04-14 | 2007-11-08 | Hoffmann La Roche | Aminopyrazole derivatives, their manufacture and use as pharmaceutical agents. |
EP1891048A1 (en) * | 2005-06-11 | 2008-02-27 | Vernalis (R&D) Limited | Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders |
WO2007001939A1 (en) * | 2005-06-27 | 2007-01-04 | Janssen Pharmaceutica N.V. | Tetrahydro-pyranopyrazole compounds displaying cannabinoid modulating activities |
TW200720255A (en) | 2005-07-13 | 2007-06-01 | Taiho Pharmaceutical Co Ltd | Benzoimidazole compound capable of inhibiting prostaglandin d synthetase |
CA2614156A1 (en) * | 2005-07-29 | 2007-02-15 | F. Hoffmann-La Roche Ag | Azabenzimidazole derivatives, their manufacture and use as anti-cancer agents |
JP2009503001A (en) * | 2005-08-01 | 2009-01-29 | エフ.ホフマン−ラ ロシュ アーゲー | Heterocyclic benzylamino derivatives, their production and use as pharmaceuticals |
JP2009519279A (en) * | 2005-12-15 | 2009-05-14 | エフ.ホフマン−ラ ロシュ アーゲー | Three-membered lactam derivatives, methods for their production and use as pharmaceutical agents |
JP5474354B2 (en) * | 2005-12-30 | 2014-04-16 | アステックス、セラピューティックス、リミテッド | Pharmaceutical compounds |
EP1984370A4 (en) * | 2006-01-23 | 2010-03-31 | Crystalgenomics Inc | Imidazopyridine derivatives inhibiting protein kinase activity, method for the preparation thereof and pharmaceutical composition containing same |
CN101466374B (en) * | 2006-04-14 | 2012-03-21 | 雅培制药有限公司 | Process for the preparation of indazolyl ureas that inhibit vanilloid subtype 1(VR1) receptors |
EP2049119A2 (en) * | 2006-06-29 | 2009-04-22 | Astex Therapeutics Limited | Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea |
DE102006030479A1 (en) | 2006-07-01 | 2008-03-20 | Merck Patent Gmbh | indazole |
FR2903406B1 (en) * | 2006-07-04 | 2012-08-10 | Aventis Pharma Sa | PYRAZOLYLBENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF |
CL2007002617A1 (en) | 2006-09-11 | 2008-05-16 | Sanofi Aventis | COMPOUNDS DERIVED FROM PIRROLO [2,3-B] PIRAZIN-6-ILO; PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUNDS; AND ITS USE TO TREAT INFLAMMATION OF THE ARTICULATIONS, Rheumatoid Arthritis, TUMORS, LYMPHOMA OF THE CELLS OF THE MANTO. |
MX2009004140A (en) | 2006-10-21 | 2009-07-10 | Abbott Gmbh & Co Kg | Heterocyclic compounds and their use as glycogen synthase kinase 3 inhibitors. |
DE102006060598A1 (en) * | 2006-12-21 | 2008-06-26 | Merck Patent Gmbh | New tetrahydrobenzoisoxazole compounds are mitotic motor protein Eg5 modulators useful to treat and prevent cancer, and to treat e.g. monocyte leukemia, glioblastoma, colon carcinoma, myelotic leukemia and lymphatic leukemia |
BRPI0817527A2 (en) | 2007-10-01 | 2017-05-02 | Isis Pharmaceuticals Inc | antisense modulation of human fibroblast growth factor receptor expression 4 |
GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
EP2294065B1 (en) | 2008-01-22 | 2014-03-19 | Vernalis (R&D) Ltd. | Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity |
GB0803018D0 (en) * | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
WO2009138799A1 (en) * | 2008-05-14 | 2009-11-19 | Astex Therapeutics Limited | Therapeutic uses of 1-cycl0pr0pyl-3 - [3- ( 5 -morpholin- 4 -ylmethyl- 1h-benz0imidaz0l- 2 -yl) -lh-pyrazol-4-yl] -urea |
CA2724430A1 (en) * | 2008-05-19 | 2009-11-26 | Schering Corporation | Heterocyclic compounds as factor ixa inhibitors |
BRPI0914006A2 (en) | 2008-07-03 | 2015-10-27 | Sirtris Pharmaceuticals Inc | benzimidazoles and related analogues as sirtuin modulators |
GB0821913D0 (en) | 2008-12-02 | 2009-01-07 | Price & Co | Antibacterial compounds |
TW201034675A (en) | 2008-12-18 | 2010-10-01 | Sanofi Aventis | Method for treating macular degeneration |
CN101619058A (en) * | 2009-01-08 | 2010-01-06 | 上海交通大学 | Benzimidazole-4-acid amide type derivant |
BR112012000254A2 (en) | 2009-07-08 | 2016-02-16 | Dermira Canada Inc | tofa analogues useful in treating dermatological disorders or conditions. |
KR101529767B1 (en) | 2009-08-07 | 2015-06-17 | 추가이 세이야쿠 가부시키가이샤 | Aminopyrazole derivative |
ES2835553T3 (en) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Indazole Inhibitors of the Wnt Signaling Pathway and Their Therapeutic Uses |
BR112012002942A2 (en) * | 2009-08-10 | 2015-10-13 | Epitherix Llc | indazoles as inhibitors of the wnt / b-catenin signaling pathway and their therapeutic uses. |
US8299070B2 (en) * | 2009-11-25 | 2012-10-30 | Japan Tobacco Inc. | Indole compounds and pharmaceutical use thereof |
NZ731621A (en) | 2009-12-04 | 2019-01-25 | Sunovion Pharmaceuticals Inc | Multicyclic compounds and methods of use thereof |
CA2986631C (en) | 2009-12-21 | 2020-06-02 | Samumed, Llc | 1h-pyrazolo[3,4-.beta.]pyridines and thereapeutic uses thereof |
CA2801274C (en) | 2010-06-01 | 2021-06-15 | Summit Corporation Plc | Compounds for the treatment of clostridium difficile-associated disease |
GB2482501A (en) * | 2010-08-04 | 2012-02-08 | Summit Corp Plc | Novel compounds for use in the treatment of Clostridium Difficile and associated diseases |
WO2012020725A1 (en) * | 2010-08-10 | 2012-02-16 | 塩野義製薬株式会社 | Heterocyclic derivative having npy y5 receptor antagonism |
CN102372674A (en) * | 2010-08-17 | 2012-03-14 | 上海药明康德新药开发有限公司 | Synthesis method for pharmaceutical intermediate 3-formyl-4-halogeno pyrazole |
EP2615916B1 (en) * | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel erk inhibitors |
JP5998142B2 (en) | 2010-09-27 | 2016-09-28 | アボット ゲーエムベーハー ウント カンパニー カーゲー | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
WO2012135799A1 (en) | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted 3-(1h-benzo{d}imidazol-2-yl)-1h-indazole-analogs as inhibitors of the pdk1 kinase |
EP2721156B1 (en) | 2011-06-16 | 2016-12-21 | Ionis Pharmaceuticals, Inc. | Antisense modulation of fibroblast growth factor receptor 4 expression |
DE102011111400A1 (en) | 2011-08-23 | 2013-02-28 | Merck Patent Gmbh | Bicyclic heteroaromatic compounds |
MX341504B (en) | 2011-09-14 | 2016-08-19 | Samumed Llc | Indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors. |
US9351973B2 (en) | 2011-09-22 | 2016-05-31 | Merck Sharp & Dohme Corp. | Pyrazolopyridyl compounds as aldosterone synthase inhibitors |
RU2641693C2 (en) | 2011-11-09 | 2018-01-22 | Кансер Ресёрч Текнолоджи Лимитед | 5-(pyridine-2-ylamino)-pyrasin-2-carbonitrile compounds and their therapeutic application |
PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
BR112014024284B1 (en) | 2012-05-04 | 2021-08-31 | Samumed, Llc | 1H-PIRAZOLO[3,4-B]PYRIDINES COMPOUNDS, PHARMACEUTICAL COMPOSITION INCLUDING SUCH COMPOUNDS AND THERAPEUTIC USES THEREOF |
MX358819B (en) | 2012-05-15 | 2018-09-05 | Cancer Research Tech Ltd | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridy l]amino]pyrazine-2-carbonitrile and therapeutic uses thereof. |
US9120792B2 (en) * | 2012-05-31 | 2015-09-01 | Sumitomo Chemical Company, Limited | Fused heterocyclic compound |
UA119315C2 (en) | 2012-07-03 | 2019-06-10 | Гіліад Фармассет Елелсі | Inhibitors of hepatitis c virus |
JP2015535227A (en) * | 2012-10-26 | 2015-12-10 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 3,4-disubstituted 1H-pyrazole and 4,5-disubstituted thiazole inhibitors of SYK |
MX370487B (en) | 2013-01-08 | 2019-12-16 | Samumed Llc | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof. |
GB201302927D0 (en) * | 2013-02-20 | 2013-04-03 | Cancer Therapeutics Crc Pty Ltd | Compounds |
EP2970205B1 (en) | 2013-03-14 | 2019-05-08 | Tolero Pharmaceuticals, Inc. | Jak2 and alk2 inhibitors and methods for their use |
US9394285B2 (en) | 2013-03-15 | 2016-07-19 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
ES2735355T3 (en) | 2013-03-15 | 2019-12-18 | Gilead Sciences Inc | Hepatitis C virus macrocyclic and bicyclic inhibitors |
CN104447701B (en) * | 2013-09-17 | 2019-03-22 | 广东东阳光药业有限公司 | Pyrazole derivatives and application thereof |
EP3581179A1 (en) | 2013-12-27 | 2019-12-18 | Chugai Seiyaku Kabushiki Kaisha | Fgfr gatekeeper mutant gene and drug targeting same |
US10005792B2 (en) | 2014-09-03 | 2018-06-26 | Ctxt Pty. Ltd. | Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors |
GB201415573D0 (en) | 2014-09-03 | 2014-10-15 | Cancer Therapeutics Crc Pty Ltd | Compounds |
US10494376B2 (en) | 2014-09-03 | 2019-12-03 | Ctxt Pty. Ltd. | Tetrahydroisoquinoline derived PRMT5-inhibitors |
WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
US9550779B2 (en) * | 2014-12-30 | 2017-01-24 | Novira Therapeutics, Inc. | Derivatives and methods of treating hepatitis B infections |
US9586949B2 (en) | 2015-02-09 | 2017-03-07 | Incyte Corporation | Aza-heteroaryl compounds as PI3K-gamma inhibitors |
AU2016264958B2 (en) * | 2015-05-21 | 2020-10-29 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as PAD4 inhibitors |
US10479780B2 (en) | 2015-06-17 | 2019-11-19 | Chugai Seiyaku Kabushiki Kaisha | Aminopyrazole derivatives |
WO2016202758A1 (en) * | 2015-06-18 | 2016-12-22 | Bayer Pharma Aktiengesellschaft | Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds |
WO2017023996A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
WO2017024026A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
WO2017024010A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
WO2017024021A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
WO2017023989A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
WO2017024015A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
US10604512B2 (en) | 2015-08-03 | 2020-03-31 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof |
WO2017023972A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
WO2017023975A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
WO2017023987A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
US10206908B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
WO2017024003A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
US10285982B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
WO2017024025A1 (en) | 2015-08-03 | 2017-02-09 | Sunil Kumar Kc | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
WO2017023988A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
MA43169B1 (en) | 2015-11-06 | 2022-05-31 | Incyte Corp | Heterocyclic compounds as pi3k-gamma inhibitors |
AU2016348639B2 (en) | 2015-11-06 | 2022-09-08 | Samumed, Llc | Treatment of osteoarthritis |
AR107030A1 (en) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | AZA-BENCIMIDAZOL INHIBITORS OF PAD4 |
TW201734003A (en) | 2016-01-05 | 2017-10-01 | 英塞特公司 | Pyridine and pyridimine compounds as PI3K-gamma inhibitors |
GB201604030D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604027D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604020D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604031D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604022D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
GB201604029D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
MD3464285T2 (en) | 2016-06-01 | 2023-01-31 | Biosplice Therapeutics Inc | Process for preparing N-(5-(3-(7-(3-fluorophenyl)-3H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide |
US10138248B2 (en) | 2016-06-24 | 2018-11-27 | Incyte Corporation | Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors |
JP7187437B2 (en) | 2016-07-29 | 2022-12-12 | サノビオン ファーマシューティカルズ インク | Compounds and compositions and uses thereof |
MA45795A (en) | 2016-07-29 | 2019-06-05 | Sunovion Pharmaceuticals Inc | COMPOUNDS AND COMPOSITIONS, AND ASSOCIATED USES |
KR102593742B1 (en) | 2016-10-21 | 2023-10-24 | 사뮤메드, 엘엘씨 | Methods of using indazole-3-carboxamide and their use as WNT/B-catenin signaling pathway inhibitors |
KR102558716B1 (en) | 2016-11-07 | 2023-07-21 | 사뮤메드, 엘엘씨 | Single-dose, ready-to-use injectable formulation |
CA3055292A1 (en) | 2016-12-29 | 2018-07-05 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
WO2018125799A2 (en) | 2016-12-29 | 2018-07-05 | Viamet Pharmaceuticals (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
JP7146782B2 (en) | 2017-02-16 | 2022-10-04 | サノビオン ファーマシューティカルズ インク | Methods of treating schizophrenia |
MX2020000523A (en) | 2017-08-02 | 2020-08-20 | Sunovion Pharmaceuticals Inc | Isochroman compounds and uses thereof. |
WO2019079469A1 (en) | 2017-10-18 | 2019-04-25 | Incyte Corporation | Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors |
CA3091292A1 (en) | 2018-02-16 | 2019-08-22 | Sunovion Pharmaceuticals Inc. | Salts, crystal forms, and production methods thereof |
CN108546266B (en) * | 2018-07-25 | 2020-09-22 | 上海毕得医药科技有限公司 | Synthesis method of 1,4,6, 7-tetrahydropyrane [4,3-C ] pyrazole-3-carboxylic acid |
MX2021000977A (en) | 2018-07-26 | 2021-04-12 | Sumitomo Pharma Oncology Inc | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same. |
DK3847175T3 (en) | 2018-09-05 | 2024-03-18 | Incyte Corp | CRYSTALLINE FORMS OF A PHOSPHOINOSITIDE 3-KINASE (PI3K) INHIBITOR |
CA3125350A1 (en) | 2018-12-31 | 2020-07-09 | Biomea Fusion, Llc | Irreversible inhibitors of menin-mll interaction |
CA3125353A1 (en) | 2018-12-31 | 2020-07-09 | Biomea Fusion, Llc | Inhibitors of menin-mll interaction |
WO2020150552A2 (en) * | 2019-01-17 | 2020-07-23 | Samumed, Llc | Methods of treating cartilage disorders through inhibition of clk and dyrk |
KR20210139376A (en) | 2019-03-14 | 2021-11-22 | 선오비온 파마슈티컬스 인코포레이티드 | Salts of isochromanyl compounds, and crystalline forms thereof, methods of preparation, therapeutic uses and pharmaceutical compositions |
WO2021060307A1 (en) * | 2019-09-25 | 2021-04-01 | 富士フイルム株式会社 | Imidazopyridine compound or salt thereof, and pharmaceutical composition |
JP2023507138A (en) * | 2019-12-20 | 2023-02-21 | ファイザー・インク | benzimidazole derivative |
US11738002B2 (en) | 2020-04-14 | 2023-08-29 | Sunovion Pharmaceuticals Inc. | Methods of treating neurological and psychiatric disorders |
CN112239452B (en) * | 2020-10-14 | 2022-05-10 | 武汉尚赛光电科技有限公司 | Electron transport type heteroanthracene derivative and organic electroluminescent device thereof |
CN114478511B (en) * | 2022-02-24 | 2023-06-20 | 中国药科大学 | Benzoxazole compound and preparation method, pharmaceutical composition and application thereof |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2130029A1 (en) * | 1971-06-18 | 1972-12-21 | Bayer Ag | Anthelmintic 2-pyrazolyl-benzimidazoles prodn - from 2-hydroxy -benzimidazoles and pyrazoles with phosphorus halides |
DE2130030A1 (en) * | 1971-06-18 | 1972-12-21 | Bayer Ag | Fungicidal and bactericidal agents |
BE793501A (en) * | 1971-12-31 | 1973-06-29 | Ciba Geigy | HETEROCYCLIC COMPOUNDS AND PHYTOPHARMACEUTICAL PRODUCTS WHICH CONTAIN IT |
WO1996014843A2 (en) * | 1994-11-10 | 1996-05-23 | Cor Therapeutics, Inc. | Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases |
JP4357004B2 (en) * | 1997-04-11 | 2009-11-04 | あすか製薬株式会社 | Pyrazole derivative and COX inhibitor containing the same |
CN1168727C (en) * | 1999-06-23 | 2004-09-29 | 阿文蒂斯药物德国有限公司 | Substituted benzimidazole |
PE20010306A1 (en) * | 1999-07-02 | 2001-03-29 | Agouron Pharma | INDAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM USEFUL FOR THE INHIBITION OF PROTEIN KINASE |
YU54202A (en) * | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Indazole compounds,pharmaceutical compositions,and methods for mediating or inhibiting cell proliferation |
US7064215B2 (en) * | 2001-07-03 | 2006-06-20 | Chiron Corporation | Indazole benzimidazole compounds |
-
2002
- 2002-10-24 MX MXPA04003954A patent/MXPA04003954A/en active IP Right Grant
- 2002-10-24 AU AU2002334217A patent/AU2002334217B2/en not_active Ceased
- 2002-10-24 EP EP02801954A patent/EP1441725A1/en not_active Withdrawn
- 2002-10-24 WO PCT/GB2002/004763 patent/WO2003035065A1/en active Application Filing
- 2002-10-24 BR BR0213562-0A patent/BR0213562A/en not_active Application Discontinuation
- 2002-10-24 IL IL16157602A patent/IL161576A0/en unknown
- 2002-10-24 JP JP2003537632A patent/JP5039268B2/en not_active Expired - Fee Related
- 2002-10-24 CA CA2465247A patent/CA2465247C/en not_active Expired - Fee Related
- 2002-10-25 UY UY27516A patent/UY27516A1/en unknown
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104098513A (en) * | 2014-07-30 | 2014-10-15 | 天津市斯芬克司药物研发有限公司 | Indazole compound derivative and preparation method |
CN104098513B (en) * | 2014-07-30 | 2016-08-24 | 天津市斯芬克司药物研发有限公司 | A kind of indazole compound derivative and preparation method thereof |
WO2023234970A1 (en) * | 2022-06-01 | 2023-12-07 | KUDA Therapeutics, Inc. | Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of hif-1/2a pathway inhibition, and induction of ferroptosis |
Also Published As
Publication number | Publication date |
---|---|
BR0213562A (en) | 2004-08-31 |
EP1441725A1 (en) | 2004-08-04 |
WO2003035065A1 (en) | 2003-05-01 |
MXPA04003954A (en) | 2004-11-29 |
JP5039268B2 (en) | 2012-10-03 |
AU2002334217B2 (en) | 2008-07-03 |
IL161576A0 (en) | 2004-09-27 |
CA2465247C (en) | 2010-05-18 |
JP2005509633A (en) | 2005-04-14 |
UY27516A1 (en) | 2003-04-30 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CA2465247A1 (en) | Benzimidazoles and analogues and their use as protein kinases inhibitors | |
US6897208B2 (en) | Benzimidazoles | |
AU2002334217A1 (en) | Benzimidazoles and analogues and their use as protein kinases inhibitors | |
AU2004253338B2 (en) | Benzimidazole derivatives and their use as protein kinases inhibitors | |
AU782878B2 (en) | Pyrazole compositions useful as inhibitors of erk | |
CA2775475C (en) | Pyridinylimidazolone derivatives for the inhibition of pi3 kinases | |
JP5702855B2 (en) | Nitrogen heterocyclic compounds useful as PDE10 inhibitors | |
US7173040B2 (en) | Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives | |
JP2018522046A5 (en) | ||
WO2017059191A1 (en) | Heteroaryl derivatives as sepiapterin reductase inhibitors | |
EP1979343A2 (en) | Bicyclic heteroaryl compounds as pde10 inhibitors | |
PT1841757E (en) | Heteroaromatic quinoline compounds and their use as pde10 inhibitors | |
US7129356B2 (en) | Farnesyl transferase inhibiting 4-substituted quinoline and quinazoline derivatives | |
AU2008262291A1 (en) | Substituted pyrazole compounds | |
CA2486187A1 (en) | Kinase inhibitors | |
AU2009321601A1 (en) | Pyridazinone derivatives | |
CN101072757A (en) | Benzamide derivatives that act upon the glucokinase enzyme | |
ES2550201T3 (en) | PDE10 modulators | |
US5008268A (en) | 2-aminopyrimidinone derivatives | |
US4957916A (en) | Antipsychotic 3-piperazinylbenzazole derivatives | |
KR20180091770A (en) | Novel hetero-ring compound, its preparation method, and pharmaceutical composition comprising the same | |
AU2014283879A1 (en) | Benzimidazole-2-piperazine heterocyclic compound, pharmaceutical composition thereof, preparation method and use thereof | |
WO2012176123A1 (en) | 3 - imidazolyl- indoles for the treatment of proliferative diseases | |
EP0353821B1 (en) | Antipsychotic 3-piperazinyl-benzazole derivatives | |
US5015740A (en) | Antipsychotic 3-piperazinylbenzazole derivatives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request | ||
MKLA | Lapsed |
Effective date: 20141024 |