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INHIBITEURS DE LA KINASE P38 A BASE D'HETEROCYCLES A 5 CHAINONS
专利权人:
NOVARTIS AG
发明人:
FRYSZMAN, OLGA M.,LANG, HENGYUAN,LAN, JIONG,CHANG, EDCON,FANG, YUNFENG
申请号:
CA2526455
公开号:
CA2526455C
申请日:
2004.06.24
申请国别(地区):
CA
年份:
2012
代理人:
摘要:
Provided is a compound of the formula:(see above formula)or a pharmaceutically acceptable salt, a solvate or a hydrate thereof,wherein: R1 ishydrogen, acyl or -P(O)(OH)2; R2 is hydrogen, halo, unsubstituted orsubstituted alkyl,alkylthio, alkylsulfinyl, alkylsulfonyl, unsubstituted or substituted alkoxy,unsubstitutedor substituted heterocyclyloxy, or alkylamino; G is an optionally substitutedaryl,aralkyl, cycloalkyl, heteroaryl, heteroaralkyl or a heterocyclyl ringoptionally fused to aphenyl ring, or G is OR83 or NR80R81; B is aryl; C is pyrazole or imidazole; Disheteroaryl, unsubstituted or substituted heteroaryl or -C(O)NR80R81; each R80and R81is independently hydrogen, alkyl, unsubstituted or substituted cycloalkyl,alkoxy,hydroxy, heteroaryl or unsubstituted or substituted heteroaryl, or togetherformunsubstituted or substituted alkylene or heteroalkylene; R83 is hydrogen,alkyl,cycloalkyl, heteroaryl or unsubstituted or substituted heteroaryl; R5 isselected fromthe group consisting of (a) hydrogen; (b) halo; (c) alkyl; (d) haloalkyl; (e)thioalkyl; (f)hydroxy; (g) amino; (h) alkylamino; (i) dialkylamino; (j) heteroalkyl; (k)unsubstitutedor substituted heterocycle; (l) unsubstituted or substitutedheterocyclylalkyl; (m)unsubstituted or substituted heterocyclylalkoxy; (n) alkylsulfonyl; (o)aminosulfonyl,mono-alkylaminosulfonyl or di-alkylaminosulfonyl; (p) heteroalkoxy; and (q)carboxy;and R6 is selected from the group consisting of: (a) hydrogen; (b) halo; (c)alkyl; and(d) alkoxy.A pharmaceutical composition containing the compound is also provided. Uses ofthecompound and composition are also provided, including uses for treatment,prevention, oramelioration of one or more symptoms of p38 kinase mediated diseases anddisorders,including, but not limited to, inflammatory diseases and disorders.
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