Phosphinic pseudo-peptide derivatives for selective...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/30 (2006.01) A61K 31/675 (2006.01) A61P 9/00 (2006.01) C07F 9/32 (2006.01) C07F 9/572 (2006.01)

Patent

CA 2473047

The invention relates to the use of phosphinic pseudo-peptide derivatives for production of a medicament for the selective inhibition of the active C-terminal site of angiotensin converting enzyme (I). Said derivatives are of formula (II), where, R<sb>1</sb> = optionally a normal protective group for amino functions in peptide chemistry or an amino acid or a peptide protected by the above type of protective group, R<sb>2</sb> and R<sb>3</sb> = a natural or synthetic amino acid side chain and R<sb>4</sb> and R<sb>5</sb> = a hydrogen atom or a counter-ion. The above finds application in the prevention and treatment of cardiovascular disease in humans.

L'invention concerne l'utilisation de dérivés de pseudo-peptides phosphiniques pour la préparation d'un médicament capable d'inhiber sélectivement le site actif C-terminal de l'enzyme de conversion de l'angiotensine I. Ces dérivés répondent ô la formule suivante : (1) dans laquelle :- R1 peut-être un groupement protecteur usuel des fonctions amines en chimie peptidique, ou un acide aminé ou un peptide protégé par ce même type de groupements protecteurs,- R2 et R3 correspondent ô une chaîne latérale d'acide aminé naturel ou non naturel, et- R4 et R5 représentent un atome d'hydrogène ou un contre- ion.Applications : prévention et traitement de pathologies cardiovasculaires chez l'homme.

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