A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/426 (2006.01) A61P 13/00 (2006.01) A61P 13/10 (2006.01) C07D 277/40 (2006.01)
Patent
CA 2503570
(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 "urination functions measurement test on cyclophosphamide-induced overactive bladder model rat". Owing to these effects, the above compound is useful as a remedy for overactive bladder.
L'invention concerne un anilide de l'acide (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phényléthyl)amino]éthyl]acétique ou son sel. Ce composé agit en tant que relaxant vésical puissant au cours du <= test de relaxation des muscles lisses de vessies isolées de rats >=, réduit, en fonction des doses administrées, la fréquence des contractions vésicales rythmiques lors du <= test de mesure des contractions vésicales rythmiques de rats >= et augmente, en outre, la durée des intervalles entre chaque miction au cours du <= test de mesure de la fonction urinaire de modèles de rats dotés d'une vessie dont l'hyperactivité est induite par du cyclophosphamide >=. Ces effets font du composé selon l'invention un remèdeapproprié pour traiter une vessie hyperactive.
Maruyama Tatsuya
Sato Shuichi
Takasu Toshiyuki
Ukai Masashi
Astellas Pharma Inc.
Dennison Associates
Yamanouchi Pharmaceutical Co. Ltd.
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