Renin-inhibitory peptides and their use

C - Chemistry – Metallurgy – 07 – K

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530/5

C07K 5/06 (2006.01) C07F 9/30 (2006.01) C07K 5/02 (2006.01)

Patent

CA 1267498

ABSTRACT NEW RENIN-INHIBITORY PEPTIDES AND THEIR USE Compounds of formula R1CO-NH-CH(R2)-CONH-CH(R3)-X [wherein: R1 represents alkyl having an .alpha.-amino or protected .alpha.-amino substituent and an aryl, heterocyclic or heterocyclic-dithio substituent; R2 represents a variety of aliphatic and cycloaliphatic hydrocarbon groups, which may be substituted; R3 represents isobutyl, sec-butyl, benzyl or (C3-C8 cycloalkyl)methyl; and X represents a group of formula -CH(-A-R4)-Y (in which A represents a single bond or an alkylene group; R4 represents an optionally protected carboxy group, an optionally N-substituted carbamoyl group, an optionally N-substituted carbazoyl group or an acyl group; and Y represents a hydroxy group, a mercapto group or a formyl group), or a group of formula -P(O)(R5)-OH (in which R represents an alkyl group having at least one optionally protected carboxy, N-substituted carbamoyl, optionally N-substituted carbazoyl, C2-C7 aliphatic carboxylic acyl or aromatic carboxylic acyl substituent)]; and their salts are renin inhibitors, which may be used in the treatment of angiotensin-induced hypertension.

473519

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