Cysteine protease inhibitors

Details Cysteine protease inhibitors Cysteine protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 491/048 (2006.01) A61K 31/407 (2006.01) A61P 19/00 (2006.01)

Patent

CA 2610817

A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is -C1-C5 straight or branched chain, optionally fluorinated, alkyl or -CH2CR5C3-C4-Cycloalkyl; R4 is H; R5 is H, C1-C2 alkyl, C1-C2 haloalkyl, hydroxyl, OC1-C2alkyl, fluoro; R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle wherein the or each ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; Rb is haloalkyl; Rc is H or C1-C4 alkyl; and pharmaceutically acceptable salts, hydrates or N-oxides thereof have utility in the treatment of disorders characterised by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

Composé de formule (II) sachant que R1 et R2 est halo et que l'autre est H ou halo ; R3 est une chaîne -C1-C5 droite ou ramifiée, éventuellement fluorée, alkyle -CH2CR5C3-C4-cycloalkyle; R4 est H; R5 est H, C1-C2 alkyle, C1-C2 haloalkyle, hydroxyle, OC1-C2alkyle, fluoro; R6 est un carbocycle ou hétérocycle monocyclique ou bicyclique stable, éventuellement substitué, et le cycle ou chaque cycle comporte 4, 5 ou 6 atomes de cycle et entre 0 et 3 hétéroatomes pouvant être S, O et N; est haloalkyle; Rc est H ou C1-C4 alkyle; y compris les sels, hydrates ou N-oxydes pharmaceutiquement acceptables d'un tel composé. Ce type de composé est utile pour le traitement de troubles dont la médiation est assurée par une expression ou activation inadéquate de la cathepsine K, du type ostéoporose, arthrose, polyarthrite rhumatoïde ou métastase osseuse.

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