BENZOTHIAZOLESULFONAMIDE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
申请人:Asahi Kasei Kogyo Kabushiki Kaisha
公开号:EP0638564A1
公开(公告)日:1995-02-15
A benzothiazolesulfonamide derivative represented by general formula (1) and having the activity of inhibiting protein phosphorylases such as protein kinase C and myosin light-chain kinase, a pharmaceutically acceptable acid-addition salt thereof, a process for producing the same, a medicinal composition containing the same, and a drug containing the same as the active ingredient for treating or preventing asthma on the basis of the protein phosphorylase inhibitor activity. In formula (1) A represents lower alkylene; R¹ represents hydrogen or lower alkyl; R² and R³ represent each independently hydrogen or lower alkyl, or they are combined together to represent lower alkylene; and R⁴ represents hydrogen, lower alkyl, amidino or phenyl-lower alkyl, wherein the phenyl group is mono- or disubstituted by lower alkyl, lower alkoxy, halogen or methylenedioxy.
一种由通式(1)表示并具有抑制蛋白磷酸酶如蛋白激酶C和肌球蛋白轻链激酶活性的苯并噻唑磺酰胺衍生物、其药学上可接受的酸加成盐、生产该衍生物的工艺、含有该衍生物的药物组合物、以及含有该衍生物作为活性成分的药物,用于基于蛋白磷酸酶抑制活性治疗或预防哮喘。在式(1)中,A代表低级亚烷基;R¹代表氢或低级亚烷基;R²和R³各自独立地代表氢或低级亚烷基,或者它们组合在一起代表低级亚烷基;R⁴代表氢、低级亚烷基、脒基或苯基-低级亚烷基,其中苯基被低级亚烷基、低级亚烷氧基、卤素或亚甲基二氧基单取代或二取代。