Astellas Pharma Gmbh

Yuji Awamura

Kenichi Suzuki

Takayuki Suzuki

Keizo Sugasawa

Tatsuya Maruyama

Souichirou Kawazoe

Kenichi Onda

Toshiyuki Takasu

Kenichirou Sakamoto

Takashi Sugane

Takahiko Tobe

Ryo Mizoguchi

Akio Miyafuji

Noritaka Hamada

Kuniyuki Sano

Takaaki Sakaida

Yu Iwakawa

Object Provided are &#x3b2;-form crystal, &#x3b3;-form crystal, and &#x3b1;-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance. Means for Resolution A solving means includes &#x3b2;-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150&#xb0; C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2&#x3b8;(&#xb0;), and the like.

Crystals of benzoxadiazole derivative

To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with &#x3b1;-form crystal and &#x3b2;-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The &#x3b1;-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The &#x3b2;-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the &#x3b1;-form crystal.

&#x3b1;-form or &#x3b2;-form crystal of acetanilide derivative

To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with &#x3b1;-form crystal and &#x3b2;-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The &#x3b1;-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The &#x3b2;-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the &#x3b1;-form crystal.

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Tsukuba, Japan

Yuji Awamura