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    • 6. 发明授权
    • Benzospiran derivatives
    • Benzospiran衍生物
    • US3932425A
    • 1976-01-13
    • US460449
    • 1974-04-12
    • Daniel Lednicer
    • Daniel Lednicer
    • C07C13/72C07C49/675C07C49/683C07C49/697C07C49/747C07C49/755C07C57/50C07C59/54C07C59/86C07C205/45C07D295/02C07D295/033C07D295/096C07D295/135C07D317/22C07D319/08
    • C07D319/08C07C205/45C07C247/00C07C45/44C07C49/675C07C49/683C07C49/697C07C49/747C07C49/755C07C57/50C07C59/54C07C59/86C07D295/033C07D295/096C07D295/135C07D317/22C07C2103/94
    • This invention relates to novel benzospiran derivatives embraced by the formula ##SPC1##Wherein the sum of A and B is at least the integer 2; A is selected from the group consisting of --(CH.sub.2).sub.n -- wherein n is 1 through 5 and --(C.sub.n H.sub.2n --.sub.2 XY)-- wherein X is selected from the group consisting of hydroxy, acetoxy, amino and acetamido and Y is hydrogen, and X when taken together with Y is selected from the group consisting of =O and =CR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; B is absent or --(CH.sub.2).sub.n -- wherein n is 1 through 3; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, ##EQU1## WHEREIN N IS 2 THROUGH 5 AND Ar is phenyl having zero through three substituents selected from the group consisting of lower alkyl of 1 through 3 carbon atoms, lower alkoxy of 1 through 3 carbon atoms, bromine, chlorine and fluorine; R.sup.1 and R.sup.2 taken together with --N
    • 本发明涉及以下式所示的新型苯并环丙兰衍生物:其中A和B的至少为整数2; A选自 - (CH 2)n - ,其中n为1至5和 - (C n H 2n-2 XY) - 其中X选自羟基,乙酰氧基,氨基和乙酰氨基,Y为氢,以及 X与Y一起选自= O和= CR 3 R 4,其中R 3和R 4选自氢和1至3个碳原子的低级烷基; B不存在或 - (CH 2)n - ,其中n为1至3; R1选自氢和1至3个碳原子的低级烷基; R 2选自氢,1至3个碳原子的低级烷基,O和 - (CH 2)n CAr,其中N为2,并且Ar为具有0至3个选自下列基团的低级烷基的苯基: 1至3个碳原子,1至3个碳原子的低级烷氧基,溴,氯和氟; R 1和R 2与-N'一起是选自未取代的和取代的吡咯烷子基,哌啶子基和六亚甲基亚氨基的饱和杂环氨基; Z选自氢,1至3个碳原子的低级烷基,1至3个碳原子的低级烷氧基,1至3个碳原子的硝基,氨基,一烷基氨基,1至4个碳原子的酰基酰胺基,溴, 氯和氟; 及其药理学上可接受的酸加成盐。 它还涉及制备上述新化合物(1)的中间体和方法及其新颖的衍生物。 新化合物(1)对人和动物的施用抑制其中枢神经系统并降低其血压。