摘要:
A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc.This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.
摘要:
A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing abortion or for contraception.
摘要:
This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.
摘要翻译:本发明提供由下式表示的环氨基 - 苯基氨基磺酸酯衍生物,其中R 1和R 2各自代表氢或低级烷基; R 3和R 4中的每一个代表氢,卤素,氰基等; A代表氮或CH; B代表CH 2,SO 2,CO,任选取代的苯基等; R 5表示烷基,苯基,氨基等,或其盐,其表现出优异的类固醇硫酸酯酶抑制活性,并且可用于预防或治疗与类固醇如雌激素,雄激素相关的疾病, 喜欢。
摘要:
Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.
摘要翻译:由下式表示的氨基磺酸苯酯衍生物或其盐对类固醇硫酸酯酶具有强大的抑制作用,因此可用于预防或治疗与类固醇相关的疾病,例如乳腺癌,子宫内膜增生症,子宫内膜增生症,不育症等雌激素 ,子宫内膜异位症,子宫腺肌症,自身免疫性疾病,痴呆或阿尔茨海默病。其中R 1和R 2各自独立地表示氢原子或低级烷基; R 3表示氢原子,卤素原子,低级烷基,-OSO 2 NR 1 R 2,低级烷酰基氨基,硝基或氰基; A表示取代或未取代的苯基,式-X-NR 4 R 5的基团等。
摘要:
Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.
摘要:
A steroid compound represented by the formula ##STR1## which has an excellent aromatase-inhibiting effect and is useful for preventing or treating diseases caused by estrogens, such as breast cancer, uterine cancer and prostatomegaly. This compound has an oxygen or nitrogen atom as the heteroatom at the position A of the ring D and the 7-position (substituent R.sup.1) of the skeleton is substituted by --S--R.sup.2 (wherein R.sup.2 represents hydrogen, lower alkyl which may be substituted by hydroxy, amino or lower alkoxycarbonyl, lower alkenyl, aralkyl, aryl which may be substituted by halogen, amino, di(lower alkyl)amino, lower alkoxy or lower alkyl, acyl, or lower alkoxycarbonyl), --S(O)m--R.sub.3 (wherein R.sup.3 represents lower alkyl; and m represents 1 or 2), or aralkyl.
摘要:
A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing prostatic hypertrophy.
摘要:
This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.
摘要翻译:本发明提供由下式表示的环氨基 - 苯基氨基磺酸酯衍生物,其中R 1和R 2各自代表氢或低级烷基; R 3和R 4中的每一个代表氢,卤素,氰基等; A代表氮或CH; B代表CH 2,SO 2,CO,任选取代的苯基等; R 5表示烷基,苯基,氨基等,或其盐,其表现出优异的类固醇硫酸酯酶抑制活性,并且可用于预防或治疗与类固醇如雌激素,雄激素相关的疾病, 喜欢。
摘要:
Compounds are described having the formula ##STR1## wherein A denotes C.dbd.O, CH.sub.2, C.dbd.CH.sub.2 or C.dbd.CH-lower alkyl;B denotes O, NH or N-lower alkyl;X does not exist, or denotes C.dbd.O or CH.sub.2 ;n denotes 2 or 3 when X does not exist, or denotes 1 or 2 when X denotes C.dbd.O or CH.sub.2 ; andthe broken line between the 1- and 2-positions of the steroid skeleton means that a double bond may optionally exist there. These compounds have an aromatase inhibition action and are useful for prophylaxis or treatment of diseases caused by excess of estrogens, for example, breast cancer, uterine cancer, prostatic hypertrophy, etc.