Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Kotobuki Pharmaceutical Co Ltd

Toshiyuki Takasu

Tatsuya Maruyama

Masashi Ukai

Shuichi Sato

Takayuki Suzuki

Kenichi Onda

Souichirou Kawazoe

Yuji Awamura

Kenichirou Sakamoto

Masayuki Shibasaki

Kunihiro Niigata

Satoshi Hayashibe

Eiji Kurosaki

Takenori Kimura

Hisataka Shikama

Eiko Hirasaki

Masako Umeda

Shunji Yamazaki

Noriaki Maeda

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in 'isolated rat bladder smooth muscle relaxation test', dose-dependently lowers the contraction frequency of rhythmic bladder contractions in 'rat rhythmic bladder contraction measurement test' and, moreover, prolongs the urination intervals in &#x201c;urination functions measurement test on cyclophosphamide-induced overactive bladder model rat&#x201d;. Owing to these effects, the above compound is useful as a remedy for overactive bladder.

Remedy for overactive bladder comprising acetic acid anilide derivative as the active ingredient

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in 'isolated rat bladder smooth muscle relaxation test', dose-dependently lowers the contraction frequency of rhythmic bladder contractions in 'rat rhythmic bladder contraction measurement test' and, moreover, prolongs the urination intervals in &#x201c;urination functions measurement test on cyclophosphamide-induced overactive bladder model rat&#x201d;. Owing to these effects, the above compound is useful as a remedy for ovaractive bladder.

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.

A Maillard reaction inhibitor containing, as an active ingredient, an amidinoheterocyclic derivative or its pharmaceutically acceptable salt, which is useful for the prevention and/or cure of various complications of diabetes and maturity-onset disorders. The amidinoheterocyclic derivatives are also useful as Maillard reaction inhibitors for cosmetics, external endermic medicines, foods, drinks, luxury grocery items and functional foods.

Pyrazole derivatives and compositions and methods of use as maillard

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Tsukuba, Japan

Toshiyuki Takasu