Yamanouchi Pharmaceutical Company Ltd.

Astellas Pharma Gmbh

Tatsuya Maruyama

Takayuki Suzuki

Kenichi Onda

Toshiyuki Takasu

Toshiyasu Mase

Masahiko Hayakawa

Hiromu Hara

Munetoshi Saito

Tetsuo Matsui

Takumi Takahashi

Masashi Ukai

Shuichi Sato

Kunihiro Niigata

Souichirou Kawazoe

Yuji Awamura

Kenichirou Sakamoto

Masayuki Shibasaki

Makoto Takeuchi

Hiroyuki Moritomo

Satoshi Miyamoto

Kenji Negoro

Satoshi Hayashibe

Toru Kontani

Kyoichi Maeno

Takenori Kimura

Tetsuya Kimizuka

Akiyoshi Shimaya

Reiko Koike

Osamu Noshiro

Ryosuke Nakano

Hisataka Shikama

Eiko Hirasaki

Masako Umeda

Jun Irie

(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.

Provided is a compound having excellent dipeptidyl peptidase IV-inhibiting activity, and a remedy based on the activity for insulin-dependent diabetes (type 1 diabetes), especially for non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, and obesity.

2-cyano-4-fluoropyrrolidine derivative or its salt

Amide derivatives or salts thereof

An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle.

Amide derivatives and medicinal compositions thereof

Bisoxadiazolidine derivative

This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;

Tri (lower alkoxy) benzene derivatives

Tri(lower alkoxy) benzene derivatives

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

Tri(lower alkoxy)benzene derivatives

Benzimidazolinone derivatives of the general formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch; R.sup.4 and R.sup.5, which may be the same or different, each is a lower alkyl group or R.sup.4 and R.sup.5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when ##STR2## is a piperidino or diethylamino group, at least one of R.sup.1, R.sup.2 and R.sup.3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity.

Benzimidazolinone derivatives

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Tsukuba, Japan

Tatsuya Maruyama