公开(公告)号：EP2350089A1

公开(公告)日：2011-08-03

申请号：EP09783392.5

申请日：2009-09-24

申请人： Medivir AB

发明人： IVANOV, Vladimir ,  SAMUELSSON, Bertil ,  JOHANSSON, Per-Ola ,  KAHNBERG, Pia ,  WÄHLING, Horst

IPC分类号： C07D491/048 ,  A61K31/496 ,  A61P19/00

CPC分类号： C07D491/048

摘要： Compounds of the formula II, wherein 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 R
7 or NR
6 , provided at least one of A
1 and A
2 comprises N; n is 0 or 1 such that the ring containing A
1 and A
2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; 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.