Renin-inhibitory oligopeptides, their preparation and use

C - Chemistry – Metallurgy – 07 – K

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530/5.02, 167/10

C07K 5/02 (2006.01) A61K 31/415 (2006.01) A61K 38/05 (2006.01) C07D 233/64 (2006.01)

Patent

CA 1338300

Compounds of formula (I): Image (I) [in which: A is a carbon-carbon bond or C1 - C3 alkylene; B is imino group or C1 - C2 alkylene; R1 is C1 - C4 alkyl, C1 - C4 alkoxy, heterocyclic or optionally substituted amino; R2 is optionally substituted phenyl or optionally substituted naphthyl; R3 is thiazolyl, isoxazolyl or imidazolyl; R4 is isopropyl or cyclohexyl; R5 and R6 are C1 - C4 alkyl, or, together with the carbon atom to which they are attached, C3 - C7 cycloalkyl; R7 is hydrogen, optionally substituted C1 - C6 alkyl group; and R8 is hydrogen or C1 - C4 alkyl] have renin-inhibitory and, hence, hypotensive activities and are of value in the diagnosis and treatment of hypertension induced by failures in the renin-angiotensin system. They may be prepared by reacting together appropriate amino acids or derivatives thereof.

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