Invention Grant
- Patent Title: Protease inhibitors
- Patent Title (中): 蛋白酶抑制剂
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Application No.: US13831267Application Date: 2013-03-14
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Publication No.: US08735395B2Publication Date: 2014-05-27
- Inventor: Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
- Applicant: Medivir AB
- Applicant Address: SE Huddinge
- Assignee: Medivir AB
- Current Assignee: Medivir AB
- Current Assignee Address: SE Huddinge
- Agency: Gorman IP Law, APC
- Priority: GB0817424.5 20080924
- Main IPC: A61K31/496
- IPC: A61K31/496 ; A61K31/454

Abstract:
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.
Public/Granted literature
- US20130231349A1 PROTEASE INHIBITORS Public/Granted day:2013-09-05
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