Cathepsin cysteine protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/12 (2006.01) A61K 31/341 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/4433 (2006.01) A61K 31/445 (2006.01) A61K 31/506 (2006.01) A61K 31/55 (2006.01) A61P 19/08 (2006.01) C07D 207/24 (2006.01) C07D 211/74 (2006.01) C07D 213/65 (2006.01) C07D 309/30 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2552726

The present invention relates to a novel class of compounds mainly, leucinamide-amino-carboxylate derivatives of formula (I) wherein Y is CR1R2, O, S, -SO2, C=0 or NR9; Z is CR1R2, O, S, -SO2, C=O or NR9 and each G is independently a CR1CR2. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B and to pharmaceutical compositions thereof. These compounds are useful for treating and preventing cathepsin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

La présente invention concerne une nouvelle classe de composés, essentiellement des dérivés de leucinamide-amino-carboxylate représentés par la formule (I) dans laquelle Y est CR?1¿R?2¿, O, S, -SO¿2?, C=0 ou NR?9¿; Z est CR?1¿R?2¿, O, S, -SO¿2?, C=O ou NR?9¿ et chaque G est indépendamment un CR?1¿CR?2¿. Lesdits composés sont des inhibiteurs des cystéines protéases de type cathepsine, y compris, entre autres, des inhibiteurs de la cathepsine K, L, S et B. L'invention concerne également des compositions pharmaceutiques desdits composés. Ces composés sont utilisés dans le traitement et la prévention d'états dépendant de la cathepsine dans lesquels est indiquée l'inhibition de la résorption osseuse, par exemple l'ostéoporose.

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