Abstract: Provided is a crystalline polymorphic form A of 15?-hydroxy-osaterone acetate having an improved stability (storage stability, pulverization stability, and absorption characteristics). In a powder X-ray diffraction spectrum, characteristic diffraction peaks of the crystalline polymorphic form A of 15?-hydroxy-osaterone acetate appear at diffraction angles 2? of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorphic form A has a melting point of 280 to 283° C. and is a prism crystal.

Abstract: Provided is a crystalline polymorphic form A of 15?-hydroxy-osaterone acetate having an improved stability (storage stability, pulverization stability, and absorption characteristics). In a powder X-ray diffraction spectrum, characteristic diffraction peaks of the crystalline polymorphic form A of 15?-hydroxy-osaterone acetate appear at diffraction angles 2? of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorphic form A has a melting point of 280 to 283° C. and is a prism crystal.

Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.

Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by dissolving an isopropanol-solvated crystal of ulipristal acetate in a mixed solvent containing ethanol and water, and crystallizing an ulipristal acetate from the solution without addition of a seed crystal to the solution.

Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.

Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by dissolving an isopropanol-solvated crystal of ulipristal acetate in a mixed solvent containing ethanol and water, and crystallizing an ulipristal acetate from the solution without addition of a seed crystal to the solution.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.