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    • 6. 发明授权
    • Inhibitor of vascular permeability enhancer
    • 血管通透性增强剂的抑制剂
    • US5604210A
    • 1997-02-18
    • US456723
    • 1995-06-01
    • Akinobu NagaokaTetsuji ImamotoTsuneo AsanoYoshihiro SugiuraGiichi Goto
    • Akinobu NagaokaTetsuji ImamotoTsuneo AsanoYoshihiro SugiuraGiichi Goto
    • A61K31/52A61K31/70
    • A61K31/7076
    • The present invention relates to prevention or treatment a brain edema, an intracranial hemorrhage and a cerebral infarction by administering a pharmaceutically effective amount of a compound or a pharmaceutically acceptable salt thereof, for inhibiting a vascular permeability enhancer, which the compound is of the formula: ##STR1## wherein A is halogen, --X--R.sup.3 in which X is O, S, NH or NHNH, and R.sup.3 is H, acyl, a hydrocarbon group or an aromatic heterocyclic group, or --Y.dbd.R.sup.4 in which Y is N or NHN, and R.sup.4 is a divalent hydrocarbon group, and R.sup.1 is H, halogen, a hydrocarbon group, a heterocyclic group or --Z--R.sup.5 in which Z is O, S or NH, and R.sup.5 is H, a hydrocarbon group or an aromatic heterocyclic group;R.sup.2 is H, halogen, a hydrocarbon group or a heterocyclic group;B is --W--R.sup.6 in which W is CH.sub.2, CO or CS, and R.sup.6 is OH, alkoxy, acyloxy, alkylsulfinyl, alkylsulfonyl, phosphoric acid or amino, or B together with E form a cyclic phosphoric ester; andD and E are H, amino, azido, halogen or OH.
    • 本发明涉及通过施用药学有效量的化合物或其药学上可接受的盐来抑制血管通透性增强剂来预防或治疗脑水肿,颅内出血和脑梗死,该化合物具有下式: (I)其中A是卤素,X-R 3,其中X是O,S,NH或NHNH,R 3是H,酰基,烃基或芳族杂环基,或-Y = R 4,其中 Y是N或NHN,R4是二价烃基,R1是H,卤素,烃基,杂环基或-Z-R5,其中Z是O,S或NH,R5是H,烃 基团或芳族杂环基团; R2是H,卤素,烃基或杂环基; B为-W-R 6,其中W为CH 2,CO或CS,R 6为OH,烷氧基,酰氧基,烷基亚磺酰基,烷基磺酰基,磷酸或氨基,或B与E一起形成环状磷酸酯; 并且D和E是H,氨基,叠氮基,卤素或OH。