发明授权
- 专利标题: Protease inhibitors
- 专利标题(中): 蛋白酶抑制剂
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申请号: US12739489申请日: 2009-09-24
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公开(公告)号: US08242119B2公开(公告)日: 2012-08-14
- 发明人: Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
- 申请人: Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
- 申请人地址: SE Huddinge
- 专利权人: Medivir AB
- 当前专利权人: Medivir AB
- 当前专利权人地址: SE Huddinge
- 代理机构: Birch, Stewart, Kolasch & Birch, LLP
- 优先权: GB0817424.5 20080924
- 国际申请: PCT/EP2009/062406 WO 20090924
- 国际公布: WO2010/034788 WO 20100401
- 主分类号: A61K31/496
- IPC分类号: A61K31/496 ; C07D491/04
摘要:
Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
公开/授权文献
- US20110039862A1 Protease Inhibitors 公开/授权日:2011-02-17
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