Patent number: 6503939
Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the structure:
wherein: R1 and R2 are (i) H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and optionally substituted alkyl, O(alkyl), aryl, or heteroaryl; (ii) a ring or (iii) a double bond; R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is a benzene ring; heterocyclic ring; an indole or benzothiophene; or pharmaceutically acceptable salt. R6 and R7 are H, methyl, ethyl, propyl, butyl, iso-propyl, isobutyl, cyclohexyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl.
Type:
Grant
Filed:
October 15, 2001
Date of Patent:
January 7, 2003
Assignees:
Wyeth, Ligand Pharmaceuticals, Inc.
Inventors:
Gary S. Grubb, John W. Ullrich, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
Patent number: 6503900
Abstract: This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula:
wherein: R1 and R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, phenoyl or thiophenoyl; R3, R4, R5 and R6 are H, alkyl, cycloalkyl, alkoxy or cycloalkoxy; R7 is H or alkyl; R8 is H or alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods and pharmaceutical compositions utilizing them for the treatment or prevention of disorders such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
Type:
Grant
Filed:
November 2, 2001
Date of Patent:
January 7, 2003
Assignee:
Wyeth
Inventors:
Annmarie Louise Sabb, Gregory Scott Welmaker, Robert Lewis Vogel, Joan Eileen Sabalski