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    • 38. 发明申请
    • 1,5-BENZOXATHIEPINE DERIVATIVES AND THEIR PREPARATION
    • 1,5-苯并吡喃衍生物及其制备
    • WO1985004658A1
    • 1985-10-24
    • PCT/JP1984000168
    • 1984-04-04
    • TAKEDA CHEMICAL INDUSTRIES, LTD.
    • TAKEDA CHEMICAL INDUSTRIES, LTD.SUGIHARA, HirosadaHIRATA, Minoru
    • C07D327/02
    • C07D411/06C07D327/02C07D411/12
    • Novel 1,5-benzoxathiepine derivatives represented by formula (I), wherein R1 and R2 each represents hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy, R3 and R4 each represents hydrogen, lower alkyl or optionally substituted cycloalkyl or aralkyl or, when taken together, R3 and R4 form a ring together with the adjacent nitrogen atom, X represents hydrogen, optionally substituted lower alkyl, optionally substituted aryl, or optionally esterified or amidated carboxyl, Y represents > C=O or > CH-OR5 (wherein R5 represents hydrogen, acyl, or optionally substituted amido), m represents an integer of 0 to 2, and n represents and integer of 1 to 6, and salts thereof show the effect of blocking serotonin S receptor, calcium-competitive effect, diuretic effect, and anti-thrombotic effect, and are useful for prophylaxis and treatment of ischemic heart disease, thrombosis, and hypertension.
    • 由式(I)表示的新的1,5-苯并氧硫杂环庚酮衍生物,其中R 1和R 2各自表示氢,卤素,羟基,低级烷基或低级烷氧基,R 3和R 4各自表示氢,低级烷基或任选取代的环烷基或芳烷基, R 3和R 4与相邻的氮原子一起形成环,X表示氢,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-OR 5(其中R 5 表示氢,酰基或任选取代的酰氨基),m表示0〜2的整数,n表示1〜6的整数,其盐表示阻断5-羟色胺S受体,钙竞争效应,利尿作用, 和抗血栓形成作用,可用于预防和治疗缺血性心脏病,血栓形成和高血压。