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    • 9. 发明申请
    • 1,5-BENZOXATHIEPIN DERIVATIVES AND PROCESS FOR THEIR PREPARATION
    • 1,5-BENZOXATHIEPIN衍生物及其制备方法
    • WO1986002644A1
    • 1986-05-09
    • PCT/JP1984000526
    • 1984-11-01
    • TAKEDA CHEMICAL INDUSTRIES, Ltd.
    • TAKEDA CHEMICAL INDUSTRIES, Ltd.SUGIHARA, HirosadaHIRATA, Minoru
    • C07D327/02
    • C07D411/06C07D327/02C07D411/12
    • Novel 1,5-benzoxathiepin derivatives represented by formula (1) (wherein R1 and R2 each represents H, halogen, OH, lower alkyl or lower alkoxy, R3 and R4 each represents H or optionally substituted lower alkyl, cycloalkyl or aralkyl or, taken together with the adjacent nitrogen atom, R3 and R4 form a ring, X represents H, optionally substituted lower alkyl, optionally substituted aryl or optionally esterified or amidated carboxy, Y represents >C=O or >CH-OR5 (wherein R5 represents H, acyl or optionally substituted carbamoyl), m represents an integer of 0 to 2, and n represents an integer of 1 to 6) and salts thereof have a serotonin S receptor-blocking effect, a calcium-antagonistic effect, a brain blood vessel contraction-relaxing effect, a kidney circulation improving effect, a diuretic effect, and an antithrombotic effect, thus being useful as agents for prophylaxis and treatment of heart diseases, thrombosis, hypertension, and brain circulation troubles.
    • 由式(1)表示的新的1,5-苯并氧硫西因衍生物(其中R 1和R 2各自表示H,卤素,OH,低级烷基或低级烷氧基,R 3和R 4各自表示H或任选取代的低级烷基,环烷基或芳烷基, 与相邻的氮原子一起,R3和R4形成环,X表示H,任选取代的低级烷基,任选取代的芳基或任选酯化或酰胺化的羧基,Y表示> C = O或> CH-OR5(其中R5表示H, 酰基或任选取代的氨基甲酰基),m表示0〜2的整数,n表示1〜6的整数),其盐具有5-羟色胺S受体阻断作用,钙拮抗作用,脑血管收缩 - 舒缓效果,肾循环改善效果,利尿作用和抗血栓形成作用,因此可用作预防和治疗心脏病,血栓形成,高血压和脑循环障碍的药剂。