Cysteine protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

IPC codes

C07D 295/20 (2006.01) A61K 31/145 (2006.01) A61K 31/16 (2006.01) A61K 31/341 (2006.01) A61K 31/343 (2006.01) A61K 31/415 (2006.01) A61K 31/4965 (2006.01) A61K 31/5375 (2006.01) A61P 11/00 (2006.01) A61P 17/06 (2006.01) A61P 37/00 (2006.01) C07C 215/20 (2006.01) C07C 235/74 (2006.01) C07C 311/21 (2006.01) C07D 213/71 (2006.01) C07D 215/20 (2006.01) C07D 231/12 (2006.01) C07D 231/40 (2006.01) C07D 233/64 (2006.01) C07D 239/80 (2006.01) C07D 241/12 (2006.01) C07D 275/00 (2006.01) C07D 275/03 (2006.01) C07D 307

Type

Patent

Patent number

CA 2744888

Description

Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2A and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3- C6cycloalkyl; R is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain

L'invention porte sur des composés de la formule I, dans laquelle R1a représente H ; et R1b représente alkyle en C1-C6, carbocyclyle ou Het ; ou R1a et R1b définissent ensemble une amine cyclique saturée avec 3-6 atomes de cycle ; R2a et R2b représentent H, halo, alkyle en C1-C4, haloalkyle en C1-C4, alcoxy en C1-C4 ; ou R2a et R2b conjointement avec l'atome de carbone auquel ils sont attachés forment un cycloalkyle en C3-C6 ; R représente une chaîne alkyle en C5-C10 ramifiée, haloalkyle en C2-C4 ou cycloalkyl en C3-C7-méthyle, R4 représente Het, carbocyclyle, facultativement substitué comme défini dans la description, et sur leurs sels pharmaceutiques, hydrates et N-oxydes. Ces composés et leurs sels, hydrates et N-oxydes sont des inhibiteurs de la cathepsine S et ont une utilité dans le traitement du psoriasis, de troubles auto-immuns et autres troubles tels que l'asthme, l'artériosclérose, la maladie pulmonaire obstructive chronique (COPD) et la douleur chronique.

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