Peptides useful for inhibition of renin

US4709010A · kind A · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Gunter Holzemann · Seeheim-Jugenheim, DE
• Peter Raddatz · Darmstadt, DE
• Alfred Jonczyk · Darmstadt, DE
• Claus J. Schmitges · Groß-Umstadt, DE

Key dates

• Filing date: Oct 18, 1985
• Grant date: Nov 24, 1987
• Expiry date: Oct 18, 2005

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S530/86
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

New peptides of the formula I EQU X--Z--NH--CHR--CHOH--CH.sub.2 --CO--NH--CHR.sup.1 --CH.sub.2 --NH--CHY--C.sub.n H.sub.2n --R.sup.2 I in which PA1 X is H, R.sup.3 --O--CH.sub.2 --CO--, R.sup.3 --O--CO--, R.sup.3 --CH.sub.2 --O--CO-- or R.sup.3 --C.sub.m H.sub.2m --CO--, PA1 Z is 1 to 4 aminoacid residues which are bonded together in the manner of peptides and are selected from the group comprising Abu, Ala, Arg, Asn, Dab, Gln, Gly, His, Ile, Leu, Lys, Met, NLeu, Orn, Phe, Pro, Trp, Tyr and Val, PA1 is A, Ar-alkyl (in which the group -alkyl contains 1-4 C atoms) or cycloalkyl-alkyl having 4-11 C atoms, PA1 R.sup.1 is H or A, PA1 Y is H, A, --C.sub.p H.sub.2p --OR.sup.4, --C.sub.p H.sub.2p --NHR.sup.4, --COOR.sup.4, --CONHR.sup.4 or --CONA.sub.2, PA1 R.sup.2 is A, cycloalkyl having 3-7 C atoms, Ar, pyridyl, indolyl, imidazolyl, piperidyl, N-benzylpiperidyl or piperazinyl, PA1 R.sup.3 is A, cycloalkyl having 3-7 C atoms or Ar, PA1 R.sup.4 is H, A or cycloalkyl having 3-7 C atoms, PA1 A is alkyl having 1-6 C atoms, PA1 Ar is phenyl which is unsubstituted or substituted once or several times by A, AO, F, Cl, Br, I, CF.sub.3 and/or NH.sub.2, or is unsubstituted naphthyl, and PA1 m, n an…