Piperazine derivative and its uses

Details Piperazine derivative and its uses Piperazine derivative and its uses

C - Chemistry, Metallurgy

07

D

C07D 303/48 (2006.01) A61K 31/495 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2226740

Compounds represented by general formula (I) or salts thereof and a process for producing the same wherein R1 represents carboxy or carboxamide; R2 represents hydrogen or lower alkyl, or R2 may be bonded to R3 or R4 to thereby form a ring; R3 and R4 represent each hydrogen, lower alkyl or sulfide, or R3 and R4 may be bonded to each other to thereby form a ring; R5 represents substituted phenyl or substituted sulfonyl represented by general formula (III): -SO2-R7 (wherein R7 represents aryl or amino); and n is 0 or 1. Because of having the effect of inhibiting cysteine protease, the compounds are useful as a preventive or remedy for various diseases in which cysteine protease participates, for example, ischemic diseases, inflammation, muscular dystrophy, immunologic diseases, essential hypertension, Alzheimer's disease, subarachnoidal bleeding, osteoporosis, etc.

L'invention porte sur des composés de formule générale (I) dans laquelle R?1¿ représente carboxy ou carboxamide; R?2¿ représente hydrogène ou alkyle inférieur ou R?2¿ peut être lié à R?3¿ ou R?4¿ de manière à former un cycle; R?3¿ et R?4¿ représentent chacun hydrogène, alkyle inférieur ou sulfure, ou R?3¿ et R?4¿ peuvent être liés ensemble pour former un cycle; R?5¿ représente un phényle ou un sulfonyle substitué de formule générale (III), -SO¿2?-R?7¿, (dans laquelle R?7¿ représente aryle ou amino); et n vaut 0 ou 1; ainsi qu'à des sels desdits composés et à leur procédé de production. En raison de leur capacité d'inhibition de la cystéine protéase, ces composés peuvent servir d'agent préventif ou curatif de différentes maladies dans laquelle la cystéine protéase joue un rôle, et notamment: les troubles ischémiques, les inflammations, la dystrophie musculaire, les troubles immunologiques, l'hypertension essentielle, la maladie d'Alzheimer, les saignements sub-arachnoïdiens, l'ostéoporose, etc.

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