- 专利标题: Isoxazole compounds as inhibitors of heat shock proteins
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申请号: US10544443申请日: 2004-02-09
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公开(公告)号: US20060241106A1公开(公告)日: 2006-10-26
- 发明人: Martin Drysdale , Brian Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen James , Kwai Cheung , Thomas Matthews
- 申请人: Martin Drysdale , Brian Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen James , Kwai Cheung , Thomas Matthews
- 优先权: GB0303105.1 20030211; GB0306560.4 20030321; GB0313751.0 20030613
- 国际申请: PCT/GB04/00506 WO 20040209
- 主分类号: A61K31/541
- IPC分类号: A61K31/541 ; A61K31/5377 ; A61K31/496 ; A61K31/454 ; A61K31/42
摘要:
Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —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; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
公开/授权文献
- US07705027B2 Isoxazole compounds as inhibitors of heat shock proteins 公开/授权日:2010-04-27
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