Patent number: 6372739
Abstract: Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same:
wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.
Type:
Grant
Filed:
July 2, 2001
Date of Patent:
April 16, 2002
Assignee:
Signal Pharmaceuticals, Inc.
Inventors:
Bernd M. Stein, David Wesley Anderson, Leah M. Gayo-Fung, Mary Doubleday, Graziella I. Shevlin, Adam Kois, Sak Khammungkhune, Ravi Kumar Jalluri, Shripad S. Bhagwat, Jeffrey A. McKie
Patent number: 6369224
Abstract: A compound of formula
wherein
n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2;
A is N or C(R2); G is N or C(R3); D is N or C(R4);
with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;
R1 is hydrogen or C1 to C4 alkyl;
R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and R6
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
April 9, 2002
Assignee:
Astra Zeneca AB
Inventors:
Eifion Phillips, Robert Mack, John Macor, Simon Semus
Patent number: 6358949
Abstract: Disclosed are compounds of the formula:
or the pharmaceutically acceptable non-toxic salts thereof wherein:
A, B, C and D are N or CH;
X is a bond or (un)substituted CH2;
R1 is lower alkenyl or (un)substituted lower alkyl;
R3 is lower alkyl; and
R2, R4, R5, and R6 are variables defined herein;
which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
March 19, 2002
Assignee:
Neurogen Corporation
Inventors:
Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, George D. Maynard, John M. Peterson, Richard Lew, Harry L. Brielmann