Aldehyde derivatives as upsteine protease inhibitors

Details Aldehyde derivatives as upsteine protease inhibitors Aldehyde derivatives as upsteine protease inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 31/40 (2006.01) A61K 31/435 (2006.01) C07C 311/19 (2006.01) C07D 209/16 (2006.01) C07D 401/12 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2196182

The present invention relates to a compound of formula (Ia'), wherein Q' stands for one or two amino acid residual groups which may be substituted; R1 stands for a hydrogen atom or an optinally substituted hydrocarbon or heterocyclic group; R4 stands for an optionally esterified carboxy group or an acyl group; and X stands for an optionally substituted straight-chain or branched divalent hydrocarbon group having a chain length of 1 to 4 atoms as the linear moiety, or a salt thereof, which has strong cysteine protease inhibitory activities and is a useful prophylactic and therapeutic agent of various diseases, including bone diseases, caused by abnormal exasperation of cysteine protease.

Composé de la formule (Ia'). Dans cette formule, Q' représente un ou deux groupes acides aminés résiduels pouvant être substitués; R?1¿ représente un atome d'hydrogène ou un groupe hydrocarbure ou hétérocyclique facultativement substitué; R?4¿ représente un groupe carboxyle ou un groupe acyle facultativement estérifié; et X représente un groupe hydrocarbure divalent ramifié ou à chaîne linéaire facultativement substitués présentant une longueur de chaîne de 1 à 4 atomes comme fraction linéaire, ou un sel de cette substance, exerçant une puissante activité inhibitrice de la protéase de la cystéine et se révélant utile comme agent prophylactique et thérapeutique contre diverses maladies, notamment les maladies osseuses, causées par un déréglement de la protéase de la cystéine.

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