Patent number: 6340676
Abstract: This invention provides compounds of Formula I having the structure
wherein
B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms;
R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2;
R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl);
W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2;
R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;
R4 is hydrogen or alkyl of 1-6 carbon atoms;
or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Type:
Grant
Filed:
April 20, 2001
Date of Patent:
January 22, 2002
Assignee:
American Home Products Corporation
Inventors:
Jay E. Wrobel, Zenan Li
Patent number: 6339098
Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure
wherein R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl. R1 and R2 may be taken together to form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)PCH2—, O(CH2)qO—, —CH2CH2OCH2CH2—, —CH2CH2NR7CH2CH2—. R1 and R2 may be taken together to form a double bond, the double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; or a double bond. R3 is hydrogen, hydroxyl, NH2, alkyl, substituted alkyl, alkenyl, alkynyl, substituted or, CORA.
Type:
Grant
Filed:
April 19, 2000
Date of Patent:
January 15, 2002
Assignees:
American Home Products Corporation, Ligand Pharmaceuticals, Inc.
Inventors:
Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi