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Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors
专利权人:
Brian William Dymock
发明人:
Brian William Dymock,Martin James Drysdale,Christofe Fromont,Allan Jordan,Xavier Barril-Alonso
申请号:
US12690983
公开号:
US08642594B2
申请日:
2010.01.21
申请国别(地区):
US
年份:
2014
代理人:
摘要:
Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical and R4 is a carboxylic ester, carboxamide or sulfonamide group.
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