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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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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Dibenzo chromene derivatives and their use as ERbeta selective ligands
  • Dibenzo chromene derivatives and their use as ERbeta selective ligands
  • Dibenzo chromene derivatives and their use as ERbeta selective ligands

Examples

Experimental program
Comparison scheme
Effect test

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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
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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