Astellas Pharma Gmbh

Masashi Ukai

Tatsuya Maruyama

Toshiyuki Takasu

Shuichi Sato

Masayuki Shibasaki

Masanori Suzuki

Akiyoshi Ohtake

(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

A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.

Pharmaceutical composition for treating overactive bladder

(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.

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Tsukuba, Japan

Masashi Ukai