AR062427A1 - HETEROARILO DERIVATIVES AS CITOCINE INHIBITORS - Google Patents

HETEROARILO DERIVATIVES AS CITOCINE INHIBITORS

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Publication number
AR062427A1
AR062427A1 ARP070103676A ARP070103676A AR062427A1 AR 062427 A1 AR062427 A1 AR 062427A1 AR P070103676 A ARP070103676 A AR P070103676A AR P070103676 A ARP070103676 A AR P070103676A AR 062427 A1 AR062427 A1 AR 062427A1
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Argentina
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alkyl
group
substituted
independently
unsubstituted
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ARP070103676A
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Spanish (es)
Inventor
Christopher J Larson
Jay Zhu
Erik Boman
Justin Emst
Montalban Antonio Garrido
Lubomir Sebo
Yazhong Pei
Jan Urban
Zhijun Wang
Christopher Lum
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Kemia Inc
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Publication of AR062427A1 publication Critical patent/AR062427A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/10—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 linked by a carbon chain containing aromatic 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/08—Bridged 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
    • C07D491/08—Bridged 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
    • C07D491/12—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 three hetero rings
    • C07D491/18—Bridged systems

Abstract

La presente proporciona compuestos de bajo peso molecular utiles como inhibidores de citocina, y composiciones del mismo. Se proporcionan además métodos para la preparacion de tales agentes y su uso en prevenir y tratar condiciones mediadas por citocinas. En particular, son utiles como agentes anti-inflamatorios, anti-dolor o anti-cáncer. Reivindicacion 6: Un compuesto de la formula 1, estereoisomeros del mismo, tautomeros del mismo, solvatos del mismo, profármacos del mismo, y sales farmacéuticamente aceptables del mismo; en donde X es CH, N, o NO; Y es CH, N, NO, con la condicion de que X y Y no sean ambos CH o NO; A es F, CI, Br, I, NR2, o un grupo alquilo C1-3 o -O(alquilo C1-3), en donde el grupo alquilo se halogena parcial o completamente de manera opcional; G es un grupo arilo o heteroarilo, en donde G se sustituye por uno o más R1, R2 o R3; Ar es un grupo arilo o heteroarilo de 6 miembros; L1 es -C(O)NH-; L2 es un enlace covalente, grupo (CR'2)s, (CR'2)nO(CR'2)t, (CR'2)nNR(CR'2)t, (CR'2)nC(NOR), (CR'2)nSO2NR(CR'2)t, (CR'2)nC(O)(CR'2)t, O(CR'2)tC(O)(CR'2)n, O(CR'2)sNR(CR'2)n, O(CR'2)nC(O)NR(CR'2)t, O(CR')sNRC(O)(CR'2)n, (CR'2)nC(O)NR(CR'2)t, (CR'2)nC(O)NRNR(CR'2)t, o (CR'2)nNRC(O)O(CR'2)t; Q es un grupo alquilo, cicloalquilo, arilo, heterociclilo, cicloalquilalquilo, aralquilo, o heterociclilalquilo sustituido o no sustituido; cada R1 es independientemente F, CI, Br, I, -NR2, -CN, o un grupo alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heterociclilo, o heterociclilalquilo sustituido o no sustituido; cada R2 es independientemente F, CI, Br, I, -CN, -NO2, un grupo alquilo o heterociclilalquilo sustituido o no sustituido, -OR', -C(O)R', -C(O)OR', -C(O)NR'2, C(NR)NR2, -C(NR)NROR, -NR'2, -(CR'2)tNRR', -NRC(O)Rö, -NR'C(O)ORö, -NR'SO2Rö, -NR'C(O)NR'2, -NR'C(S)NR'2, - S(O)mRö, o -SO2NR'2; cada R3 es independientemente un grupo alquilo, alquenilo, o alquinilo sustituido o no sustituido, o un grupo -O(alquilo C1-4), en donde el grupo alquilo C1-4 se halogena parcial o completamente de manera opcional; cada R es independientemente hidrogeno o un grupo alquilo C1-6 sustituido o no sustituido; cada R' es independientemente hidrogeno, o un grupo alquilo, cicloalquilo, cicloalquilalquilo, aralquilo, heterociclilo, o heterociclilalquilo sustituido o no sustituido; cada Rö es independientemente un grupo alquilo, cicloalquilo, arilo, heterociclilo, cicloalquilalquilo, aralquilo o heterociclilalquilo sustituido o no sustituido; cada m es independientemente 0, 1 o 2; n es 0, 1, o 2; s es 1, 2, o 3; y cada t es independientemente 0, 1, o 2; a condicion de que el compuesto no sea 5-(bifenil-4-il)-6-cloro-N-(6-metoxipiridin-3-il)nicotinamida.The present provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. Methods for the preparation of such agents and their use in preventing and treating cytokine mediated conditions are also provided. In particular, they are useful as anti-inflammatory, anti-pain or anti-cancer agents. Claim 6: A compound of formula 1, stereoisomers thereof, tautomers thereof, solvates thereof, prodrugs thereof, and pharmaceutically acceptable salts thereof; where X is CH, N, or NO; Y is CH, N, NO, with the proviso that X and Y are not both CH or NO; A is F, CI, Br, I, NR2, or a C1-3 alkyl group or -O (C1-3 alkyl), wherein the alkyl group is partially or completely optionally halogenated; G is an aryl or heteroaryl group, wherein G is substituted by one or more R1, R2 or R3; Ar is a 6-membered aryl or heteroaryl group; L1 is -C (O) NH-; L2 is a covalent bond, group (CR'2) s, (CR'2) nO (CR'2) t, (CR'2) nNR (CR'2) t, (CR'2) nC (NOR), (CR'2) nSO2NR (CR'2) t, (CR'2) nC (O) (CR'2) t, O (CR'2) tC (O) (CR'2) n, O (CR ' 2) sNR (CR'2) n, O (CR'2) nC (O) NR (CR'2) t, O (CR ') sNRC (O) (CR'2) n, (CR'2) nC (O) NR (CR'2) t, (CR'2) nC (O) NRNR (CR'2) t, or (CR'2) nNRC (O) O (CR'2) t; Q is an alkyl, cycloalkyl, aryl, heterocyclyl, cycloalkylalkyl, aralkyl, or substituted or unsubstituted heterocyclylalkyl group; each R1 is independently F, CI, Br, I, -NR2, -CN, or an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, or substituted or unsubstituted heterocyclyl alkyl group; each R2 is independently F, CI, Br, I, -CN, -NO2, a substituted or unsubstituted alkyl or heterocyclylalkyl group, -OR ', -C (O) R', -C (O) OR ', -C (O) NR'2, C (NR) NR2, -C (NR) NROR, -NR'2, - (CR'2) tNRR ', -NRC (O) Rö, -NR'C (O) ORö, -NR'SO2Rö, -NR'C (O) NR'2, -NR'C (S) NR'2, - S (O) mRö, or -SO2NR'2; each R3 is independently an alkyl, alkenyl, or substituted or unsubstituted alkynyl group, or a group -O (C1-4 alkyl), wherein the C1-4 alkyl group is partially or completely halogenated optionally; each R is independently hydrogen or a substituted or unsubstituted C1-6 alkyl group; each R 'is independently hydrogen, or an alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, heterocyclyl, or substituted or unsubstituted heterocyclylalkyl group; each Rö is independently a substituted or unsubstituted alkyl, cycloalkyl, aryl, heterocyclyl, cycloalkylalkyl, aralkyl or heterocyclylalkyl group; each m is independently 0, 1 or 2; n is 0, 1, or 2; s is 1, 2, or 3; and each t is independently 0, 1, or 2; provided that the compound is not 5- (biphenyl-4-yl) -6-chloro-N- (6-methoxypyridin-3-yl) nicotinamide.

ARP070103676A 2006-08-17 2007-08-17 HETEROARILO DERIVATIVES AS CITOCINE INHIBITORS AR062427A1 (en)

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US89147007P 2007-02-23 2007-02-23

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AR (1) AR062427A1 (en)
CL (1) CL2007002375A1 (en)
PE (1) PE20080906A1 (en)
TW (1) TW200815422A (en)
WO (1) WO2008021388A1 (en)

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