Dibenzo chromene derivatives and their use as ERbeta selective ligands
A technology of diphenyl and chromene, applied in the field of estrogen preparations, can solve problems such as differences in the surrounding environment of co-regulatory proteins
Inactive Publication Date: 2007-04-11
WYETH LLC
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Problems solved by technology
The exact reason why the same compounds have cell-specific effects has not been elucidated, but may be due to differences in receptor conformation and / or the environment surrounding coregulatory proteins
Method used
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Embodiment 33
[0079] X = 3-methoxyphenyl Example 34
Embodiment 35
[0081] X=3,4-Difluorophenyl Example 36
Embodiment 38
[0084] X=3,4-dimethylphenyl Example 39
[0085] X=4-cyanophenyl Example 40
[0086] X = 3-fluoro-4-methylphenyl Example 41
[0087] X=3,4-Dimethoxyphenyl Example 42
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Abstract
This invention provides estrogen receptor modulators of fomula (I), having the structure where R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, and R<8> are as defined in the specification.
Description
[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Application No. ______, filed February 23, 2005, which claims the benefit of U.S. Application 60 / 547,967, filed February 26, 2004, the disclosures of both applications being incorporated herein by reference in their entirety refer to. technical field [0003] The present invention relates to novel substituted 5H-dibenzo[c,g]chromene derivatives, their use as estrogen preparations and methods for their preparation. Background technique [0004] The pleiotropic effects of estrogen in mammalian tissues have been reported in the literature, and estrogen is now found to affect many organ systems [Mendelsohn and Karas, New England Journal of Medicine 340:1801-1811 (1999), Epperson et al., Psychosomatic Medicine 61: 676-697 (1999), Crandall, Journal of Womens Health & Gender Based Medicine 8: 1155-1166 (1999), Monk and Brodaty, Dementia & Geriatric Cognitive Disorders ...
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IPC IPC(8): C07D311/78C07D311/92A61K31/352A61P19/10
Inventor R·E·梅硕R·J·小艾德索
Owner WYETH LLC
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