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    Pyrrolidine derivatives as oxytocin antagonists
    10.
    发明授权
    Pyrrolidine derivatives as oxytocin antagonists 失效
    吡咯烷衍生物作为催产素拮抗剂

    公开(公告)号：US07557136B2

    公开(公告)日：2009-07-07

    申请号：US10547032

    申请日：2004-02-16

    申请人： Matthias Schwarz ,  Catherine Jorand-Lebrun ,  Delphine Valognes

    发明人： Matthias Schwarz ,  Catherine Jorand-Lebrun ,  Delphine Valognes

    IPC分类号： A61K31/40 ,  A61K31/4245 ,  A61K31/4184 ,  C07D207/14 ,  C07D271/06 ,  C07D403/06

    CPC分类号： C07D413/06 ,  C07D207/22

    摘要： The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R1is selected from the group comprising or consisting of H and C1-C6-alkyl; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C1-C6 alkyl aryl, heteroaryl, C1-C6 alkyl heteroaryl, C2-C6-alkenyl, C2-C6-alkenyl aryl, C2-C6 alkenyl heteroaryl, C2-C6-alkynyl, C2-C6-alkynyl aryl, C2C6-alkynyl heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyl heterocycloalkyl, CIC6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyl alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, C1-C6-alkyl ureido, amino, C1-C6-alkyl amino, sulfonyloxy, C1-C6 alkyl sulfonyloxy, sulfonyl, C1-C6-alkyl sulfonyl, sulfinyl, C1-C6-alkyl sulfinyl, C1-C6alkyl sulfanyl, C1-C6-alkyl sulfonylamino.

    摘要翻译： 本发明涉及式（I）的新型吡咯烷衍生物，其几何异构体，其作为对映异构体的光学活性形式，diastercomers，它们的混合物及其外消旋体形式及其盐，其中：R 1选自包括或 由H和C 1 -C 6 - 烷基组成; R 2选自氢，C 1 -C 6 - 烷基，C 1 -C 6烷基芳基，杂芳基，C 1 -C 6烷基杂芳基，C 2 -C 6 - 烯基，C 2 -C 6烯基芳基，C 2 -C 6烯基杂芳基 ，C 2 -C 6 - 炔基芳基，C 2 -C 6炔基杂芳基，C 3 -C 8环烷基，杂环烷基，C 1 -C 6烷基环烷基，C 1 -C 6烷基杂环烷基，CIC 6烷基羧基，酰基，C 1 -C 6 - 烷基酰基，C 1 -C 6烷基酰氧基，C 1 -C 6烷基烷氧基，烷氧基羰基，C 1 -C 6烷基烷氧基羰基，氨基羰基，C 1 -C 6烷基氨基羰基，C 1 -C 6烷基酰基氨基，C 1 -C 6烷基脲基，氨基 ，C 1 -C 6烷基氨基，磺酰氧基，C 1 -C 6烷基磺酰氧基，磺酰基，C 1 -C 6烷基磺酰基，亚磺酰基，C 1 -C 6烷基亚磺酰基，C 1 -C 6烷基硫烷基，C 1 -C 6烷基磺酰基氨基。