Protease inhibitors
US-9200006-B2 · Dec 1, 2015 · US
US10329266B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10329266-B2 |
| Application number | US-201815941947-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 30, 2018 |
| Priority date | Sep 24, 2008 |
| Publication date | Jun 25, 2019 |
| Grant date | Jun 25, 2019 |
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Compounds of the formula II: wherein R 1 and R 2 are independently H, F or CH 3 ; or R 1 forms an ethynyl bond and R 2 is H or C 3 -C 6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF 3 , OMe or halo; R 3 is C 1 -C 3 alkyl or C 3 -C 6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R 3 is C 3 -C 6 cycloalkyl it may alternatively be gem substituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A 1 is CH or N, A 2 is CR 6 R7 or NR 6 , provided at least one of A 1 and A 2 comprises N; R 6 is H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 3 alkyl-O—C 1 -C 3 alkyl, or when A 2 is C, R 6 can also be C 1 -C 4 alkoxy or F; R 7 is H, C 1 -C 4 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.
Opening claim text (preview).
The invention claimed is: 1. A compound of the formula 2. A process of preparation of the compound according to claim 1 , comprising the step of deprotecting the ketal compound of the formula with trifluoroacetic acid to obtain the ketone of claim 1 .
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