Somatostatin analogs

US4162248A · kind A · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Robert G. Strachan · Warrington, US
• William J. Paleveda, Jr. · Lansdale, US
• Daniel F. Veber · Ambler, US
• Frederick W. Holly · Abington, US

Key dates

• Filing date: Apr 7, 1978
• Grant date: Jul 24, 1979
• Expiry date: Apr 7, 1998

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Somatostatin analogs having the structural formula: Cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] Wherein PA1 X is ##STR1## and n=0 to 4; A is Lys, (.epsilon.-INOC) Lysine; PA1 B is Asn, Ala, .alpha.-aminobutyric acid; PA1 C is Ser, Gly; PA1 J, k, l and m are 0 to 1; with the proviso that j, k, l, and m are not all 1 and not all 0, Wherein the ring formed by the peptide backbone contains 24 to 33 atoms and the pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting release of insulin, decreasing gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.