Estrogen receptor modulators

Abstract

Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

Description

1 CROSS REFERENCE TO RELATED U.S. PATENT APPLICATIONS[0001] The present application claims priority under 35 U.S.C. .sctn. 119(e) from co-pending provisional U.S. patent application Ser. No. 60 / 095,772, which is incorporated herein by reference in its entirety and for all purposes.2 BACKGROUND OF THE INVENTION[0002] 2.1 Field of the Invention[0003] The present invention relates to compounds that have biological activity with respect to estrogen receptors and to the use of such compounds to treat diseases and disorders related to estrogen receptor activity. More particularly, the present invention provides selective estrogen receptor modulators ("SERMs"). The present invention therefore relates to the fields of medicine, medicinal chemistry, biochemistry, and endocrinology.[0004] 2.2 Background[0005] Estrogen is a hormone critical to normal human development and function. Although estrogen is the predominant "sex hormone" in women, in whom estrogen controls the development of female ...

AI Technical Summary

Benefits of technology

[0012] The present invention provides pyrazole estrogen receptor agonist and antagonist compounds in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described herein have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

Problems solved by technology

However, estrogen also has undesirable effects.

But, administration of estrogen is also associated with increased risks for breast and endometrial cancer as well as blood clots (Jordan 1998).

The increased risk of endometrial cancer can be addressed by the administration of progesterone (or its synthetic analog progestin) to re-initiate menstruation and thereby shed potentially malignant cells, but many older women find this undesirable (Jordan 1998).

Thus, for a long time the treatment options for the serious health problems caused by a failure to produce estrogen were limited and entailed severe risks.

However, no one drug candidate has emerged to fill the needs of women who require the benefits of estrogen replacement to live productive lives and / or treatments for estrogen-dependent cancers.

However, despite these recent advances no drug candidate has emerged to fill the needs of women who require the benefits of estrogen replacement to live productive lives and / or treatments for estrogen-dependent cancers.

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