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PYRAZOLOPYRIDINE KINASE INHIBITORS
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
JIMENEZ, JUAN-MIGUEL,SETTIMO, LUCA,FRAYSSE, DAMIEN,BRENCHLEY, GUY,BOYALL, DEAN
申请号:
NZ59078409
公开号:
NZ590784A
申请日:
2009.07.22
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 6-(1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-amine derivatives as represented by the general formula (I), or pharmaceutically acceptable salts thereof, wherein: R1 and R2 are each independently H, halogen, -OR, -N(R)2, -C(O)OR, -C(O)N(R)2, -NRC(O)R, -NRC(O)OR, -CN, -NO2, aliphatic optionally and independently substituted with one or more Ja, or cycloaliphatic optionally and independently substituted with one or more Jb Q is N, O or S ring B is a 6-membered monocyclic heteroaromatic ring optionally fused to an aromatic or non-aromatic ring and ring B is optionally substituted with one Y and independently further optionally and independently substituted with one or more Jc R3 is absent, H, or alkyl optionally and independently substituted with one or more Ja R4 is aliphatic, wherein up to three methylene units of R4 are optionally and independently replaced by G, or R4 is optionally and independently substituted with one ring C and independently further optionally and independently substituted with one or more Ja or R4 is ring C and wherein the remaining substituents are as defined herein. Representative compounds include N-((4-aminocyclohexyl)methyl)-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-amine, N1-(6-(1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-yl)-2-methylpropane-1,2-diamine and N-((4-aminocyciohexyl)methyl)-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)-5-(trifluoromethyl)pyridin-2-amine. Further disclosed is a composition comprising a compound or a pharmaceutically acceptable salt thereof as defined above, and a pharmaceutically acceptable carrier, adjuvant, or vehicle for treating or preventing a protein kinase-mediated condition such as asthma, psoriasis, arthritis, rheumatoid arthritis, joint inflammation, multiple sclerosis, diabetes, inflammatory bowel disease, transplant rejection, T-cell leukaemias, lymphomas, and lupus.
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