Cyclic regimens using cyclic urea and cyclic amide derivatives

US6399593B1 · kind B1 · utility

Assignees

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

Inventors

• Gary S. Grubb · Newtown Square, US
• Puwen Zhang · Audubon, US
• Arthur A. Santilli · Havertown, US
• Andrew Fensome · Wayne, US
• Eugene A. Terefenko · Quakertown, US
• Andrew Q. Viet · Schwenksville, US
• Jay E. Wrobel · Lawrenceville, 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: Apr 19, 2000
• Grant date: Jun 4, 2002
• Expiry date: Apr 19, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention concerns cyclic combination therapies using progestational agents and indoline derivatives which are progesterone receptor antagonists of the general structure: wherein: A, B and D are N or CH, though not all can be CH; R1 and R2 are H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R1 and R2 form a spirocyclic ring; RA is H or optionally substituted alkyl aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH2, alkyl, alkenyl, or CORC; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 membered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception.