公开(公告)号：EP2509957A1

公开(公告)日：2012-10-17

申请号：EP10835594.2

申请日：2010-12-10

申请人： Medivir UK Ltd

发明人： AYESA, Susana ,  CARLQUIST, Peter ,  ERSMARK, Karolina ,  GRABOWSKA, Urszula ,  HEWITT, Ellen ,  JÖNSSON, Daniel ,  KAHNBERG, Pia ,  KLASSON, Björn ,  LIND, Peter ,  ODÉN, Lourdes ,  PARKES, Kevin ,  WIKTELIUS, Daniel

IPC分类号： C07D231/40 ,  A61K31/16 ,  A61K31/415 ,  A61K31/426 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P21/04 ,  A61P37/02 ,  A61P37/08 ,  C07C237/14 ,  C07D277/46

CPC分类号： C07K5/06078 ,  A61K38/05 ,  C07C271/22 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D231/40 ,  C07D277/46 ,  C07D405/12 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06139

摘要： Compounds of the formula (I) wherein R
1a is H; and R
1b is C
1 -C
6 alkyl, Carbocyclyl or Het; or R
1a and R
1b together define a saturated cyclic amine with 3-6 ring atoms; R
2a and R
2b are independently H, halo, C
1 -C
4 alkyl, C
1 -C
4 haloalkyl or C
1 -C
4 alkoxy, or R
2a and R
2b together with the carbon atom to which they are attached form a C
3 -C
6 cycloalkyl; R
3 is a branched C
5 -C
10 alkyl chain, C
2 -C
4 haloalkyl or -CH
2 C
3 -C
7 cycloalkyl; R
4 is C
1 -C
6 alkyl, C
1 -C
6 haloalkyl, C
1 -C
6 alkylamino or C
1 -C
6 dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.