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    • 6. 发明公开
    • Derivatives of N-(2-pyrrolidinylmethyl)-benzamide, process for their preparation, intermediates and a pharmaceutical preparation
    • N-(2-吡咯烷基甲基)苯甲酰胺的衍生物,它们的制备方法,中间体和药物制剂。
    • EP0156776A1
    • 1985-10-02
    • EP85850022.6
    • 1985-01-21
    • Astra Läkemedel Aktiebolag
    • Bengtsson, Karl StefanHögberg, ThomasJohansson, Lars GeorgeDe Paulis, TomasStröm, Hans Eric PeterWidman, Marianne ElisabetÖgren, Sven Ove
    • C07D207/09C07C65/21C07C101/72A61K31/40
    • C07D207/08C07C65/21
    • Novel therapeutically active compounds of the formula
      wherein

      Z , being Z 1 , Z 2 or Z 3 , is the same or different and selected among OH, OR', NH 2 , NR 2 4 , NHR', SH, SR 4 and OR 4 wherein R' is a formyl group, an acyl group, an alkoxycarbonyl group or a mono- or dialkylcarbamoyl group and R 4 is a lower alkyl group,
      R 2 is a hydrogen, a halogen, a lower alkyl or a lower trifluoroalkyl group,
      R 3 is a hydrogen atom, a lower alkyl group, an alkenyl group, an alkynyl group or a phenyl group, which phenyl group could optionally be substituted by one or more of fluoro, chloro, bromo, trifluoromethyl, methyl, ethyl, methoxy or ethoxy in the ortho, meta or para positions, or optionally substituted by methylenedioxy, provided that at least one of Z 1 , Z 2 and Z 3 is a group OR 4 and further provided that when Z 2 is OH or NH 2 , Z' is NR 2 4 , NHR 4 , SH, SR 4 or OR' or a physiologically acceptable salt or optical isomer thereof, intermediates and methods for their preparation, pharmaceutical preparations containing the compounds and methods for their therapeutical use.
    • 下式的新的治疗活性化合物 worin Z是ž<1>,Z <2>或Z <3>是相同的或不同的,并且其中选择OH,OR <1>,NH 2,NR 2 <4> ,NHR <4>,SH,SR <4>和或<4> worin - [R <1>为甲酰基到酰基烷氧基羰基或单 - 或二烷基氨基甲基,且R <4>是低级烷基 基,R <2>为氢,卤素,低级烷基或低级三氟烷基,R <3>是氢原子,低级烷基,链烯基的苯基,在炔基或苯基,其中 组可以任选地被一个或多个氟,氯,溴,三氟甲基,甲基,乙基,甲氧基或乙氧基的邻位的,金属或对位,或通过亚甲二氧基OPTIONALLY substituiertem被substituiertem,提供确实Z中至少一个<1> ,Z <2>和Z <3>的基团或<4>和进一步提供确实当Z <2>是OH或NH 2,Z <1>为NR 2 <4>,NHR <4>,SH,SR < 4>或或<4>或其生理上可接受的盐或其旋光异构体,中间体和方法及其 制剂,药物制剂含有所述化合物和方法及其治疗用途。