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    • 9. 发明申请
    • THERAPEUTIC APPLICATION OF PERHYDROISOINDOLE DERIVATIVES AS AN ANTI-EMETIC
    • 过敏性衍生物作为抗肿瘤药物的治疗应用
    • WO1995009628A1
    • 1995-04-13
    • PCT/FR1994001160
    • 1994-10-05
    • RHONE-POULENC RORER S.A.GARRET, ClaudeLOUVEL, Erik
    • RHONE-POULENC RORER S.A.
    • A61K31/40
    • C07D409/06A61K31/40C07D209/44
    • Novel therapeutic application of perhydroisoindole derivatives of general formula (I), wherein the radicals R are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3; R1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl, or heterocyclyl which can be substituted; R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted aklyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R3 is phenyl which can be substituted in position 2; R4 is OH or fluorine if R5 is H, or R4 and R5 are OH, or R4 and R5 form a bond in their isomer forms. The antiemetic drug produced from the above-mentioned derivatives or optionally their salts, when they exist, can be used for curative and preventive treatments.
    • 通式(I)的全氢异吲哚衍生物的新型治疗应用,其中基团R是可以被卤素原子取代的苯基或位置2或3的甲基; R1是任选取代的苯基,环己二烯基,萘基,茚基或可被取代的杂环基; R2是H,卤素,OH,烷基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,烷氧基,烷硫基,酰氧基,羧基,任选取代的烷基氧羰基,苄氧羰基,氨基或酰氨基; R3是可以在2位被取代的苯基; R4是OH或氟,如果R5是H,或R4和R5是OH,或R4和R5以其异构体形式形成键。 由上述衍生物或任选的其盐形成的止吐药可以用于治疗和预防性治疗。