Combination regimens using 3,3-substituted indoline derivatives

US6329416A · kind A · utility

Assignees

• Amerimas Home Products, Inc. · US
• Ligand Pharmaceuticals Incorporated · US

Inventors

• Gary S. Grubb · Newtown Square, US
• John W. Ullrich · Schwenksville, US
• Andrew Fensome · Wayne, 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: Dec 11, 2001
• Expiry date: Apr 19, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P15/18
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the general structure: ##STR1## wherein: R.sub.1, and R.sub.2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R.sub.1 and R.sub.2 are joined to FORM a ring comprising --CH.sub.2 (CH.sub.2).sub.n CH.sub.2 -- where n=0-5; --CH.sub.2 CH.sub.2 CMe.sub.2 CH.sub.2 CH.sub.2 --; --O(CH.sub.2).sub.m CH.sub.2 -- where m=1-4; O(CH.sub.2).sub.p O-- where p=1-4; --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 --; --CH.sub.2 CH.sub.2 N(H or alkyl)CH.sub.2 CH.sub.2 --; PA1 or R.sub.1, and R.sub.2 together comprise a double bond to CMe.sub.2 ; C(cycloalkyl), O, or C(cycloether); PA1 R.sub.3 is H, OH, NH.sub.2, COR.sup.A ; or optionally substituted alkenyl or alkynyl groups; PA2 R.sup.A =H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; PA1 R.sub.4 =H, halo, CN, NH.sub.2, or optionally substituted alkyl, alkoxy, or aminoalkyl; PA1 R.sub.5 is selected from optionally substituted benzen…