C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/7.06
C07K 7/14 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1156222
ABSTRACT OF THE DISCLOSURE New octapeptides of the general formula (I), X-Arg-Val-Tyr-Ile-His-Pro-Y-OA 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 A is a (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)-Ila-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 pharmaoeutically acceptable complex. The new compounds according to the invention possess angiotensin-II antagonizing effects, and can be used in the therapy to diagnose for treat hypertensive states.
368682
Karpati Egon
Kisfaludy Lajos
Nyeki Olga
Szporny Laszlo
Fetherstonhaugh & Co.
Richter Gedeon Vegyeszeti Gyar Rt
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