Non-steroid progesterone receptor agonist and antagonist and compounds and methods

US5808139A · kind A · utility

Assignees

• Ligand Pharmaceuticals Incorporated · US
• The Regents of the University of California · US

Inventors

• I. Charles Pathirana · San Diego, US
• Christina S. Berger · San Diego, US
• Robert B. Stein · Rydal, US
• William Fenical · Del Mar, US
• Todd K. Jones · Solana Beach, US
• Lawrence G. Hamann · North Grafton, US
• Michael G. Johnson · San Diego, US
• Luc Farmer · Foxborough, US

Key dates

• Filing date: Sep 8, 1994
• Grant date: Sep 15, 1998
• Expiry date: Sep 8, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C69/96
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Non-steroidal compounds which are high affinity, high specificity ligands for progesterone receptors are disclosed. The compounds include synthetic derivatives of cyclocymopol and its diastereomers, spectroscopically and chromatographically pure (3R)-cyclocymopol monomethyl ether, which functions as a progesterone receptor antagonist, and spectroscopically and chromatographically pure (3S)-cyclocymopol monomethyl ether, which functions as a progesterone receptor agonist. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by progesterone receptors and for treating patients requiring progesterone receptor agonist or antagonist therapy.