Publication number: 20040082642
Abstract: The present invention relates to compounds of formula (I) and derivatives thereof, in which the variables are as defined in the claims, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell profileration, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.
Type:
Application
Filed:
November 14, 2003
Publication date:
April 29, 2004
Inventors:
Konrad Koehler, Mikael Gillner, Ye Liu, Aiping Cheng, James V Heck, Milton Lloyd Hammond, Ralph Troy Mosley, Mahmoud Rahimi-Ghadim
Patent number: 6649624
Abstract: A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I):
wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2;
Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl:
n represents 0 or 1;
Q represents a single bond or carbonyl;
T, U, V and W each independ
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
November 18, 2003
Assignee:
Banyu Pharmaceutical Co., Ltd.
Inventors:
Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
Patent number: 6562857
Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure
wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—;
n=1-5; p=1-4; q=1-4;
R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA;
RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R5 is hydrogen, alkyl, or substituted alkyl;
R6 is hydrogen, alkyl, substituted alkyl, or CORB,
RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino
Type:
Grant
Filed:
January 9, 2002
Date of Patent:
May 13, 2003
Assignee:
Wyeth
Inventors:
Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
© 2024 Justia
