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Protease inhibitors
专利权人:
Medivir AB
发明人:
Oden, Lourdes Salvadore,Nilsson, Magnus,Kahnberg, Pia,Samuelsson, Bertil,Grabowska, Urszula
申请号:
AU2009295898
公开号:
AU2009295898B2
申请日:
2009.09.24
申请国别(地区):
AU
年份:
2012
代理人:
摘要:
Compounds of the formula II: wherein R and R are independently H, F or CH; or R forms an ethynyl bond and R is H or C-C cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF, OMe or halo; R is C-C alkyl or C-Ccycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R is C-C cycloalkyl it may alternatively be gem subsituted with fluoro; R is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A is CH or N, A is CRR7 or NR, provided at least one Of A and A comprises N; R is H, C-C alkyl, C-C haloalkyl, C-C alkyl-O-C-C alkyl, or when A is C, R can also be C-C alkoxy or F; R is H, C-C 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.
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