Patent ID: 6136842
Filing Date: 2000-10-24
Classification: A61P,C07C,C07D

Abstract:
A method of treatment of pathologies requiring an inhibition of the endothelin-converting enzyme in warm-blooded animals comprising administering to warm-blooded animals in need thereof of an inhibition effective amount of said enzyme of a compound, of formula (I): ##STR18## in which: n represents the integer 0 or 1,R.sub.1 represents an phenyl or biphenyl radical optionally substituted by one or more radicals chosen from halogen atoms or the following radicals: optionally protected hydroxyl, linear or branched alkoxy containing up to 4 carbon atoms, phenoxy, cyano, free, salified, esterified or amidified carboxy, benzyloxy and the dioxol radical,R.sub.2 represents a hydrogen atom or a methyl radical substituted by a phenyl, phenylthio or indolyl radical and optionally by a second phenyl radical, these phenyl, phenylthio and indolyl radicals being optionally substituted by one or more radicals chosen from halogen atoms or the following radicals: optionally protected hydroxyl, linear or branched alkoxy containing up to 4 carbon atoms, cyano, free, salified, esterified or amidified carboxy, benzyloxy, thienyl, naphthyl and phenyl, these three last radicals being themselves optionally substituted by one or more radicals chosen from halogen atoms or the following radicals: optionally protected hydroxyl, linear or branched alkoxy containing up to 4 carbon atoms, cyano and free, salified, esterified or amidified carboxy,A represents the free, salified, esterified or amidified carboxy radical, the free or salified tetrazolyl radical, or an alkyl radical, containing up to 10 carbon atoms and substituted by a radical chosen from the following radicals: free, salified, esterified or amidified carboxy, the optionally protected hydroxyl, alkoxy containing up to 4 carbon atoms, phenoxy, phenyl, naphthyl, thienyl, indolyl and pyridyl, these radicals being optionally substituted by one or more radicals chosen from halogen atoms, or the following radicals: optionally protected hydroxyl, linear or branched alkoxy containing up to 4 carbon atoms, cyano and free, salified, esterified or amidified carboxy,1 and 2 indicating, if appropriate, the asymmetric centres of the products of formula (I),said products of formula (I) being in all possible racemic, enantiomeric and diastereoisomeric isomer forms, as well as the addition salts with mineral and organic acids or with the mineral and organic bases of said products of formula (I), with the exception of thiorphan.