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Amino derivs. of 1,2-benzisothiazole - beta:sympatholytics suitable for the treatment of coronary heart disease, hypertonia and cardiac arrhythmia

机译:氨基派生。 1,2-苯并噻唑-β:拟交感神经药适用于治疗冠心病,高渗和心律不齐

摘要

Novel amino-derivs. of 1,2-benzisothiazole are of formula (I). n is 2 or 3; R1 and R2 are H or opt. branched 1-5C alkyl; R3 is Ph, opt. mono-, di- or tri-substd. by halogen, alkyl, alkoxy, alkylthio, haloalkyl or haloalkoxy (these 2 gps. contg. 1-3 halogen), hydroxyalkyl or alkoxyalkyl (all alkyl gps. contg. 1-5C), 2-6C alkenyl, alkinyl or alkinyloxy, 3-8 ring C cycloalkoxy, methylene dioxy, amino, 1-5C alkylamino or di(1-5C)alkylamino. R3 may also be indanyl or tetrabydropaphthyl). The physiologically acceptable acid addn.-salts of (I) are also new. (I) are pharmaceuticals and can be used in heart and circulatory disorders. As a result of their beta-sympatholytic action, (I) are esp. suitable for the treatment of coronary heart disease, hypertonia and disturbances of cardiac rhythm. Suitable unit doese for humans are 1-100 (sp. 3-50) mg. (I) are strong beta-sympatholytics of low toxicity and have a therapeutic breadth 3-12 times greater than that of the known beta-sympatholitic propandol.
机译:新型氨基衍生物。 1,2-苯并噻唑具有式(I)。 n为2或3; R1和R2为H或opt。支链的1-5C烷基; R3是Ph(可选)。单,二或三取代。由卤素,烷基,烷氧基,烷硫基,卤代烷基或卤代烷氧基(这些2 gps。含1-3个卤素),羟烷基或烷氧基烷基(所有烷基gps。含1-5C),2-6C烯基,炔基或炔基氧基3 -8环C环烷氧基,亚甲基二氧基,氨基,1-5C烷基氨基或二(1-5C)烷基氨基。 R 3也可以是茚满基或四降萘基。 (I)的生理上可接受的酸加成盐也是新的。 (I)是药物,可用于心脏病和循环系统疾病。由于其β-交感神经作用,尤其是(I)。适用于治疗冠心病,高渗和心律失常。适用于人类的单位剂量是1-100(sp。3-50)mg。 (I)是低毒性的强β-交感神经药,其治疗范围比已知的β-交感神经药异丙酚大3-12倍。

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