GnRH antagonists IX

US4661472A · kind A · utility

Assignee

• Salk Institute for Biological Studies · US

Inventors

• Jean E. F. Rivier · Village of La Jolla, US
• Janos I. Varga · San Diego, US
• Arnold T. Hagler · San Diego, US
• R. Struthers · Encinitas, US
• Marilyn H. Perrin · Village of La Jolla, US
• Catherine L. Rivier · Village of La Jolla, US
• Wylie W. Vale, Jr. · Village of La Jolla, US

Key dates

• Filing date: May 9, 1985
• Grant date: Apr 28, 1987
• Expiry date: May 9, 2005

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/13
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are cyclic analogs of the decapeptide GnRH wherein there is a covalent bond between the residue in the 4-position and the residue in the 10-position. Examples of such bonds include the disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboxyl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group.