Derivatives of the n–-arylsulphonylaminoacyl-p-...

Details Derivatives of the n–-arylsulphonylaminoacyl-p-... Derivatives of the n–-arylsulphonylaminoacyl-p-...

C - Chemistry, Metallurgy

07

K

530/5.06, 167/10

C07K 5/06 (2006.01) C07K 5/062 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1312703

Derivatives of the N.alpha.-arylsulphonylaminoacyl-p- amidinophenylalaninamides, their preparation process, their use as medicaments and the pharmaceutical compositions containing them. ABSTRACT The present invention is concerned with compounds with the formula : (I) Image 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, alkoxy- carbonyl 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 stereo- isomers 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.

527936

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