ESTROGEN RECEPTOR Beta PARTIAL AGONIST HAVING ESTROGEN RECEPTOR Alpha INHIBITORY EFFECT, AND GYNECOLOGICAL DISEASE THERAPEUTIC AGENT USING SAME

Abstract

[Problem] To provide a therapeutic agent for estrogen-dependent gynecological diseases such as endometriosis, uterine fibroids, and uterus adenomyosis. [Solution] To use an estrogen receptor α-inhibiting β partial agonist represented by the formula (a), a pharmaceutically-acceptable salt thereof, or a hydrate of either of the afore-mentioned, as an active ingredient.

Description

FIELD OF THE INVENTION[0001]The present invention relates to an estrogen receptor β partial agonist having estrogen receptor α inhibitory effect, and a gynecological disease therapeutic agent using the same.BACKGROUND OF THE INVENTION[0002]There are diseases caused by abnormality of estrogen or progesterone as organic gynecological diseases. Examples of the diseases include endometriosis, uterine fibroids, and uterus adenomyosis.[0003]As treatment of such diseases, administration of gonadotropin agonist (GnRH agonist), as a drug therapy, is known, however, a period for drug administration is restricted because of the side effects such as bone mineral loss and ovarian dysfunction symptoms, thus no gynecological disease therapeutic agents for long-term use have existed yet, and so surgical therapy such as surgical resection is still a first choice.[0004]Therefore, for the treatment of gynecological disease, a drug effective for long-term administration to inhibit the growth of ectopic...

AI Technical Summary

Benefits of technology

[0022]According to the present invention, a drug for treating estrogen-dependent gynecologic

Problems solved by technology

As treatment of such diseases, administration of gonadotropin agonist (GnRH agonist), as a drug therapy, is known, however, a period for drug administration is restricted because of the side effects such as bone mineral loss and ovarian dysfunction symptoms, thus no gynecological disease therapeutic agents for long-term use have existed yet, and so surgical therapy such as surgical resection is still a first choice.

However, it is reported that this drug causes uterine body cancer, uterine sarcoma or endometriosis, thus it may not be used to treat estrogen-dependent diseases including endometriosis.

This drug, unlike tamoxifen, does not provide endogenous partial agonist action to

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