Cathepsin cysteine protease inhibitors

Details Cathepsin cysteine protease inhibitors Cathepsin cysteine protease inhibitors

A - Human Necessities

61

P

A61P 19/08 (2006.01) C07D 207/26 (2006.01) C07D 307/33 (2006.01)

Patent

CA 2552713

The present invention relates to a novel class of compounds mainly, substituted leucinamide-carboxylate derivatives of formula (I) wherein X is O or NR9, Y is CR1R2, -SO2, C=O or NR9; Z is CR1R2, O, S, -SO2 or NR9 and each G is independently a CR1CR2 and pharmaceutical compositions thereof. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B. These compounds are useful for treating and preventing cathpesin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

L'invention concerne une nouvelle classe de composés principalement des dérivés de leucinamide-carboxylate substituée de la formule (I), dans laquelle S représente O ou NR?9¿, Y représente CR?1¿R?2¿, -SO¿2?, C=O ou NR?9¿; Z représente CR?1¿R?2¿, O, S, -SO¿2? ou NR?9¿ et chaque G représente indépendamment un CR?1¿R?2¿ et ses compositions pharmaceutiques. Ces composés sont des inhibiteurs de cathépsine cystéine protéase, notamment des inhibiteurs des cathépsines K, L, S et B, et sont utilisés dans le traitement et la prévention d'états dépendant de la cathépsine où l'inhibition de la résorption osseuse, telle que l'ostéoporose, est indiquée.

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