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Title:
NOVEL ESTROGEN RECEPTOR LIGANDS AND METHODS I
Document Type and Number:
WIPO Patent Application WO2002053522
Kind Code:
A3
Abstract:
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive 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 proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.

Inventors:
KOEHLER KONRAD (SE)
HENSSEN CECILIA (SE)
NILSSON MARITA (SE)
GILLNER MIKAEL (SE)
LIU YE (SE)
SANIN ANDREI (SE)
WILKENING ROBERT R (US)
RATCLIFFE RONALD W (US)
WENSBO DAVID (SE)
Application Number:
PCT/EP2001/015230
Publication Date:
January 08, 2004
Filing Date:
December 24, 2001
Export Citation:
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Assignee:
KAROBIO AB (SE)
MERCK & CO INC (US)
KOEHLER KONRAD (SE)
HENSSEN CECILIA (SE)
NILSSON MARITA (SE)
GILLNER MIKAEL (SE)
LIU YE (SE)
SANIN ANDREI (SE)
WILKENING ROBERT R (US)
RATCLIFFE RONALD W (US)
WENSBO DAVID (SE)
International Classes:
A61K31/05; A61K31/10; A61K31/122; A61K31/15; A61K31/352; A61K31/357; A61K31/385; A61P3/02; A61P3/04; A61P3/06; A61P5/30; A61P9/00; A61P9/10; A61P15/08; A61P19/00; A61P19/08; A61P19/10; A61K31/343; A61P25/28; A61P35/00; A61P37/02; A61P43/00; C07C35/37; C07C35/44; C07C39/17; C07C39/42; C07C49/727; C07C49/737; C07C49/747; C07C251/44; C07C323/17; C07D307/94; C07D311/96; C07D317/72; C07D339/06; C07D339/08; (IPC1-7): C07C49/747; C07C251/44; C07C323/17; C07C43/315; C07C39/42; C07C39/17; C07D339/06; C07D317/72; C07D339/08; C07D307/94; C07D311/96; A61K31/122; A61K31/045; A61K31/557; A61K31/385; A61K31/39; A61P19/00
Domestic Patent References:
WO1999066915A21999-12-29
WO2001082923A12001-11-08
Foreign References:
EP0606661A11994-07-20
EP0873992A11998-10-28
Other References:
JOVANOVIC-SANTA, SUZANA ET AL: "Synthesis and biological activity of new 16,17-secoestrone derivatives", COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS (2000), 65(1), 77-82, January 2000 (2000-01-01), XP002212976
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