Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-01-19
2000-06-27
Powers, Fiona T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514681, 549401, 568327, A61K 31352, A61K 31122, C07D31122, C07C 49643, C07C 49697
Patent
active
060807814
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to new tetralone or benzopyranone derivatives and a method for producing the derivatives. The new tetralone or benzopyranone derivatives of the present invention have inhibition activity of 17.beta.-hydroxysteroid dehydrogenase (abbreviated as 17.beta.-HSD, hereinafter), and these derivatives are useful for a therapeutic agent for preventing and/or treating androgen or estrogen dependent diseases, particularly, prostatic cancer, benign prostatic hyperplasia, virilism, mammary cancer, mastopathy, endometrial cancer, endometriosis, ovarian cancer and the like.
BACKGROUND ART
Lately, in our country, it causes trouble that androgen dependent diseases such as prostatic cancer and benign prostatic hyperplasia, and estrogen dependent diseases such as mammary cancer and endometriosis, are increasing in the morbidity. For example, the percentage of mortality of the prostatic cancer was 3.9 men per 100,000 of population by statistical data in 1984, and was about 1/10 of the non Caucasian men in the western country. However, it is increasing gradually by prolonging people's life due to improvement of medical treatment and western diet. In 1993, that percentage is 6.7 men per 100,000 of population and it is coming to European and U.S. levels. It is expected that the numbers of mortality based on the prostatic cancer in 2015 will be four times more of those in 1990. This is the worst increasing percentage in all cancers.
It has become clear from many views that subjective conditions and objective conditions of the androgen dependent diseases will be improved by depressing the androgen levels in blood. Therefore, treatment of these diseases have been accomplished by lowering the androgen in blood by castration, by administering an agonist of LH-RH to lower the androgen in blood to the castration level, and by administering anti-androgen agents antagonizing an androgen receptor to control the action of the androgen. In fact, the clinical effects are broadly noticed. However, since the castration causes a lowering of QOL, it is only proceeded in very limited diseases. The agonist of LH-RH has problems; side effect such as a bone pain or dysuria caused by a phenomenon peculiar to the agonist (temporary increase of the androgen), and rekindling for continuous existence of androgen originated from adrenal glands. Further, it is indicated that the effect of the anti-androgen agents is decreased by the development of variants of the androgen receptor during the medicine is administered. Therefore, "a method of complete blockage of the androgen" is prescribed for more effective endocrine treatment. The method is aimed to completely inhibit the androgen in blood by combination of several endocrine therapeutics, and more effective treatment is expected.
Testosterone exhibiting the most effective androgenic activity in C.sub.19 steroids having androgenic activity can be biosynthesized with 17.beta.-HSD from a substrate of andorostendione. By inhibiting this 17.beta.-HSD, the concentration of testosterone in blood is directly lowered, so that it is expected to effectively treat the above androgen dependent diseases. In addition, since this enzyme is also a biosynthetic enzyme of estoradiol having the highest estrogenic activity in C.sub.18 steroid having estrogenic activity, it is also expected to effectively treat the estrogen dependent diseases such as mammary cancer and endometriosis.
Steroid compounds and non-steroid compounds have been proposed as 17.beta.-HSD inhibitors. As the non-steroid compounds, for example, flavons and isoflavons, which are described in Biochemical and Biophysical Research Communications, Vol. 215, 1137-1144 (1995), and fatty acids, which are described in Journal of Steroid Biochemistry, Vol. 23, 357-363 (1985), are known. However, since the activity of these compounds is not satisfied, it is expected to obtain materials having higher activity.
DISCLOSURE OF INVENTION
Considering the above problems, the inventors of the present invention earnestly hav
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Nakakoshi Masamichi
Nakamura Junji
Nakayama Shoji
Yoshihama Makoto
Powers Fiona T.
Snow Brand Milk Products Co. Ltd.
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