发明申请
- 专利标题: PYRIMIDOTHIOPHENE COMPOUNDS
- 专利标题(中): 吡咯烷酮化合物
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申请号: US11632969申请日: 2005-07-18
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公开(公告)号: US20090069336A1公开(公告)日: 2009-03-12
- 发明人: Xavier Barril-Alonso , Paul Andrew Brough , Martin James Drysdale , Paul Webb
- 申请人: Xavier Barril-Alonso , Paul Andrew Brough , Martin James Drysdale , Paul Webb
- 申请人地址: GB Oxon GB Cambridge GB London GB London
- 专利权人: Brian William DYMOCK,VERNALIS (CAMBRIDGE) LIMITED.,CANCER RESEARCH TECHNOLOGY LTD.,THE INSTITUTE OF CANCER RESEARCH
- 当前专利权人: Brian William DYMOCK,VERNALIS (CAMBRIDGE) LIMITED.,CANCER RESEARCH TECHNOLOGY LTD.,THE INSTITUTE OF CANCER RESEARCH
- 当前专利权人地址: GB Oxon GB Cambridge GB London GB London
- 优先权: GB0416168.3 20040720
- 国际申请: PCT/GB2005/002816 WO 20050718
- 主分类号: A61K31/519
- IPC分类号: A61K31/519 ; C07D495/04 ; A61K31/496 ; A61P35/00 ; A61P31/12 ; A61P17/00 ; A61P3/00
摘要:
Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers: wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q (IA) wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 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 (i) hydrogen, a —CN group, a nitro group —NO2, or a —C(═NOH)(NH2) group, or (ii) an optionally substituted C1-C6alkyl, aryl, heterocyclic, aryl(C1-C6alkyl)-, or heterocyclic(C1-C6alkyl)- group, or (iii) a group of formula —C(═O)R5 wherein R5 is hydroxyl, optionally substituted C1-C6alkyl, C1-C6alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C1-C6alkyl)-, aryl(C1-C6alkoxy)-, heteroaryl(C1-C6alkyl)-, or heteroaryl(C1-C6alkoxy)-, or (iv) a group of formula —C(═O)NHR6 wherein R6 is primary, secondary, tertiary or cyclic amino, or hydroxyl, optionally substituted C1-C6alkyl, C1-C6alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C1-C6alkyl)-, aryl(C1-C6alkoxy)-, heteroaryl(C1-C6alkyl)-, or heteroaryl(C1-C6alkoxy)-.
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