Peptide derivatives which inhibit renin and acid proteases

Details Peptide derivatives which inhibit renin and acid proteases Peptide derivatives which inhibit renin and acid proteases

C - Chemistry, Metallurgy

07

K

530/7.06

C07K 7/06 (2006.01) C07K 5/02 (2006.01) C07K 7/02 (2006.01)

Patent

CA 1286846

ABSTRACT OF THE DISCLOSURE Peptide derivatives modelled on the basis of pepstatin have the formula: (I) Image in which: - R1 represents an acyl group selected from the following groups: alkylcarbonyl, alkoxycarbonyl, arylcarbonyl, arylalkylcarbonyl and arylalkoxycarbonyl in which the alkyl group is optionally substituted by hydroxyl; - R2 represents phenyl or a lower alkyl group, which may be substituted by a phenyl, naphthyl or cyclohexyl group; - R3 represents a lower alkenyl, a phenyl, a naphthyl, a cycloalkyl containing 3 to 6 carbon atoms, a 5-membered or 6-membered monocyclic heterocyclic group which is unsubstituted or substituted by a lower alkyl or trifluoromethyl, or alternatively a lower alkyl substituted by a di(lower alkyl)amino group, by a carboxyl esterified by a lower alkyl or a benzyl, by a free carbamoyl or a carbamoyl substituted by one or two lower alkyls or by a phenyl, by a lower alkoxy or benzyloxy group, by a pyridylmethoxy group, by a (lower alkyl)sulfinyl or (lower alkyl)sulfonyl group, by a cycloalkyl containing from 3 to 6 carbon atoms or by a 5-membered or 6-membered monocyclic heterocyclic group which is unsubstituted or substituted by a lower alkyl or a trifluoromethyl, with the proviso that R3 is not the (imidazol-4-yl)methyl group; - R4 represents a hydroxyl, a lower alkoxy, a benzyloxy or a free amino group or an amino group substituted by one or 2 lower alkyls; - Z1 represents isopropyl, phenyl or cyclohexyl, respectively forming with the radical: Image the residue of the amino acid statin, namely (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid, of (3S,4S)-4-amino-3-hydroxy-5-phenylpentanoic acid (AHPPA) or of (3S,4S)-4-amino-5-cyclohexyl-3-hydroxy- pentanoic acid (ACHPA); and - X-Y is a dipeptide selected from Ala-Sta, Ala-Leu, Leu-Phe and Val-Sta; as well as any pharmaceutically acceptable salts of the said peptide derivative with mineral or organic acids or alkali metals or alkaline earth metals. These derivatives inhibit renin and acid proteases and are useful in the treatment of arterial tension.

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