GRF analogs

US4689318A · kind A · utility

Assignee

• Salk Institute for Biological Studies · US

Inventors

• Emil T. Kaiser · New York, US
• Gonul Velicelebi · San Diego, US

Key dates

• Filing date: Aug 29, 1985
• Grant date: Aug 25, 1987
• Expiry date: Aug 29, 2005

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Human pancreatic GRF and the hypothalamic GRFs for the human and several other mammalian species were earlier characterized and synthesized. The invention provides synthetic peptides which are potent stimulators of the release of pituitary GH in animals, including humans, and which have the formula: R.sub.1 -R.sub.2 R.sub.3 -Ala-R.sub.5 -R.sub.6 -R.sub.7 -R.sub.8 -R.sub.9 -R.sub.10 -R.sub.11 -R.sub.12 -R.sub.13 -Leu-R.sub.15 -Gln-Leu-R.sub.18 -R.sub.19 -R.sub.20 -R.sub.21 -Leu-Leu-Gln-Glu-R.sub.26 -R.sub.27 -R.sub.28 -Arg-Y wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, Leu, His or D-His, which has either a C.sup.a Me or N.sup.a Me substitution or is unsubstituted; R.sub.2 is Ala or D-Ala; R.sub.3 is Asp or D-Asp; R.sub.5 is Ile or Leu; R.sub.6 is Phe or Tyr; R.sub.7 is Ser or Thr; R.sub.8 is Ser, Asn, Thr or Gln; R.sub.9 is Ala or Ser; R.sub.10 is Tyr, Phe or Leu; R.sub.11 in Arg, Orn or Lys; R.sub.12 is Arg, Orn or Lys; R.sub.13 is Ile, Leu, Phe or Val; R.sub. 15 is Gly or Ala; R.sub.18 is Ala or Ser; R.sub.19 is Ser or Ala; R.sub.20 is Arg, Orn or Lys; R.sub.21 is Arg, Orn or Lys; R.sub.26 is Leu, Ile, Val or Phe; R.sub.27 is Nle, Nva or a natural amino acid; R.sub.28 is Ala, L…