发明申请
US20100010037A1 1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS
审中-公开
1H-PYRROLO [2,3-B]吡啶衍生物作为HSP90抑制剂有用
- 专利标题: 1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS
- 专利标题(中): 1H-PYRROLO [2,3-B]吡啶衍生物作为HSP90抑制剂有用
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申请号: US12438809申请日: 2007-08-17
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公开(公告)号: US20100010037A1公开(公告)日: 2010-01-14
- 发明人: Paul Brough , Martin Drysdale
- 申请人: Paul Brough , Martin Drysdale
- 申请人地址: GB Winnersh
- 专利权人: VERNALIS (R&D) LTD.
- 当前专利权人: VERNALIS (R&D) LTD.
- 当前专利权人地址: GB Winnersh
- 优先权: GB0617161.5 20060831
- 国际申请: PCT/GB2007/003133 WO 20070817
- 主分类号: A61K31/437
- IPC分类号: A61K31/437 ; C07D471/02 ; A61P35/04
摘要:
Compounds of formula (I) have HSP90 inhibitory activity: ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): —X-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, —O—, —S—, —S(O)—, —SO2—, or —NH—, Z is —O—, —S—, —(C═O)—, —(C═S)—, —S(O)—, —SO2—, —NRA—, or, in either orientation —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH2OH, —C(═O)NH2, —C(═O)H, —C(═O)CH3, or —NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (—CN), C1-C3alkyl optionally substituted with one or more fluorine substituents, C1-C3alkoxy optionally substituted with one or more fluorine substituents, —CH═CH2, —C≡CH, cyclopropyl and —NH2, or R3 and R4 together represent methylenedioxy (—OCH2O—) or ethylenedioxy (—OCH2CH2O—) in either of which one or more hydrogens are optionally replaced by fluorine; S1 is as defined in the description.