Patent number: 6713471
Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I)
or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
Type:
Grant
Filed:
June 15, 2000
Date of Patent:
March 30, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
Patent number: 6399593
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.
Type:
Grant
Filed:
April 19, 2000
Date of Patent:
June 4, 2002
Assignees:
Wyeth, Ligand Pharmaceuticals, Inc.
Inventors:
Gary S. Grubb, Puwen Zhang, Arthur A. Santilli, Andrew Fensome, Eugene A. Terefenko, Andrew Q. Viet, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
Patent number: 6380235
Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula:
wherein:
A is O, S, or NR4;
B is a bond between A and C═Q, or the moiety CR5R6;
R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut
Type:
Grant
Filed:
April 19, 2000
Date of Patent:
April 30, 2002
Assignees:
American Home Products Corporation, Ligand Pharmaceuticals, Inc.
Inventors:
Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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