Cyclothiocarbamate derivatives as progesterone receptor modulators

US7081457B2 · kind B2 · utility

Assignees

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

Inventors

• Puwen Zhang · Audubon, US
• Andrew Fensome · Wayne, US
• Eugene A. Terefenko · Quakertown, US
• Lin Zhi · San Diego, US
• Todd K. Jones · Solana Beach, US
• James P. Edwards · San Diego, US
• Christopher M. Tegley · Thousand Oaks, US
• Jay E. Wrobel · Lawrenceville, US
• Mark A. Collins · Norristown, US

Key dates

• Filing date: May 6, 2002
• Grant date: Jul 25, 2006
• Expiry date: Dec 24, 2023

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure:wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.