Combination regimens using progesterone receptor modulators

US6759408B2 · kind B2 · utility

Assignees

• Wyeth, LLC · US
• Ligand Pharmaceuticals Incorporated · US

Inventors

• Gary S. Grubb · Newtown Square, US
• Puwen Zhang · Audubon, US
• Eugene A. Terefenko · Quakertown, US
• Andrew Fensome · Wayne, US
• Jay E. Wrobel · Lawrenceville, US
• Horace Fletcher, III · Pottstown, US
• James P. Edwards · San Diego, US
• Todd K. Jones · Solana Beach, US
• Christopher M. Tegley · Thousand Oaks, US
• Lin Zhi · San Diego, US

Key dates

• Filing date: May 9, 2002
• Grant date: Jul 6, 2004
• Expiry date: May 9, 2022

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/56
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.