发明名称 DERIVATIVES OF THE NALPHA-ARYLSULPHONYLAMINOACYL-P- AMIDINOPHENYLALANINAMIDES, THEIR PREPARATION PROCESS, THEIR USE AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
摘要 Derivatives of the N.alpha.-arylsulphonylaminoacyl-p-amidinophenylalaninamides, their preparation process, their use as medicaments and the pharmaceutical compositions containing them. The present invention is concerned with compounds with the formula : (I) in which : - R1 represents d lower alkyl, a lower hydroxy alkyl or a benzyl group, a phenyl group or d 4-hydroxy phenyl group: - R2 and R3, identical or different, each represents a lower alkyl or hydroxyalkyl, lower alkenyl, or lower alkynyl radical, or together with the nitrogen to which they are attached, they form a saturated heterocycle such as morpholino, thiomorpholino, pyrrolidino unsubstituted or substituted by an alkoxycarbonyl or carboxyl group, piperazino, 4-(lower alkyl)-piperazino, 4-(lower hydroxyalkyl)piperazino, or piperidino unsubstituted or substituted by a lower alkyl, benzyl, hydroxy, lower hydroxyalkyl, amino, lower aminoalkyl, alkoxycarbonyl or carboxyl group, - Ar represents a phenyl, an alpha-naphthyl or a possibly substituted beta-naphthyl group, or a possibly substituted heteroaryl group chosen from pyridyl, quinolinyl, and isoquinolinyl, as well as their stereoisomers and their mixtures and their salts with pharmaceutically acceptable mineral or organic acids. The invention is also concerned with a preparation process for the products with the formula (I), their use as medicaments and the intermediates for their synthesis.
申请公布号 CA1312703(C) 申请公布日期 1993.01.12
申请号 CA19870527936 申请日期 1987.01.22
申请人 SANOFI 发明人 BERNAT, ANDRE;DELEBASSEE, DENIS;FREHEL, DANIEL;MAFFRAND, JEAN-PIERRE;VALLEE, ERIC
分类号 A61K38/00;C07C311/15;C07D295/12;C07K5/06;C07K5/062;C07K5/065 主分类号 A61K38/00
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