Aska Pharmaceutical Co., Ltd.

Other

Teikoku Hormone Mfg. Co., Ltd.

Takayoshi Nakagawa

Hiroyuki Hayashi

Koichi Miyazaki

Shigeki Iwashita

Makoto Okada

Naoyuki Koizumi

Shigehiro Takegawa

Tomohito Fujii

Hiroo Takahashi

Hajime Nawata

Toshihiko Yanase

Provided is a crystalline polymorphic form A of 15&#x3b2;-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&#x3b2;-hydroxy-osaterone acetate appear at diffraction angles 2&#x3b8; of 9.6&#xb0;&#xb1;0.2&#xb0;, 17.1&#xb0;&#xb1;0.2&#xb0;, and 20.2&#xb0;&#xb1;0.2&#xb0;. The crystalline polymorphic form A has a melting point of 280 to 283&#xb0; C. and is a prism crystal.

Crystalline polymorph of 15B-hydroxy-osaterone acetate

The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal.  The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.

Crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-D]pyrimidine-6-carboxylic acid

Crystal of 2-(3,4 dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothien[2,3-D]pyrimidine-6-carboxylic acid

Disclosed is a method for screening a compound having an activity that selectively modulates an androgen receptor, comprising a step of measuring the mRNA expression level of prostate-specific antigen or the production level of prostate-specific antigen in prostate cancer cells by contacting a test substance with the prostate cancer cells, and a step of measuring the mRNA expression level of uncoupling protein 1 or the production level of uncoupling protein 1 in adipocytes by contacting a test substance with the adipocytes. Additionally disclosed is a selective androgen receptor modulator, comprising as an active ingredient thereof a compound represented by any of structural formulas (I) to (III), and a composition for preventing or treating a lifestyle-related disease, comprising as an active ingredient thereof said selective androgen receptor modulator.

Prophylactic/therapeutic agents for lifestyle-related diseases

This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula 

Cyclic aminophenyl sulfamate derivative

Phenyl sulfamate derivatives

Growing community of inventors

Kawasaki, Japan

Takayoshi Nakagawa