The Salk Institute for Biological Studies

University of California

Ligand Pharmaceuticals, Inc.

Robert B Stein

Christina S Berger

Ronald Mark Evans

Richard Alan Heyman

Todd Kevin Jones

Lawrence G Hamann

Luc J Farmer

William H Fenical

Michael G Johnson

I Charles Pathirana

In accordance with the present invention, there is provided a method for the treatment of subjects afflicted with steroid or steroid-like hormone-responsive disease states. The invention method comprises administering to the subject an effective amount of a ligand which selectively interacts with the receptor subtype associated with the steroid or steroid-like hormone-responsive disease state, wherein said ligand interacts with said receptor subtype to a significantly greater extent than with other subtypes of the same receptor class.

Use of selective ligands for treatment of disease states responsive to

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.

Non-steroid progesterone receptor agonist and antagonist and compounds

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San Diego, CA, United States of America

Robert B Stein