Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof

Abstract

New octapeptides of the general formula (I), X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I) wherein X stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid, Y is the residue of an aliphatic amino acid, and A is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II), B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II) wherein B is a group removable by acidolysis or catalytic hydrogenation, C is a group for the temporary protection of the guanidino group on the Arg moiety, D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety, E is a group for the temporary protection of the imidazole group on the His moiety, and A, X and Y are as defined above, are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex. The new compounds according to the invention possess angiotensin-II antagonizing effects, and can be used in the therapy to diagnose or treat hypertensive states.

Dependencies are inferred from the claim text.