Synthesis and use of retinoid compounds having negative hormone

Details Synthesis and use of retinoid compounds having negative hormone Synthesis and use of retinoid compounds having negative hormone

1998-12-30

1999-12-28

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Silicon containing doai

514544, 514568, 514569, 514682, 556437, 560 51, 562462, 568468, C07C 6306, C07C 6538, C07F 704, A61K 3119

Patent

active

060082046

ABSTRACT:
Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

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