Pyrrolidine ester derivatives with oxytocin modulating activity
    9.
    发明授权
    Pyrrolidine ester derivatives with oxytocin modulating activity 有权
    吡咯烷酯衍生物与催产素调节活性

    公开(公告)号:US07189754B2

    公开(公告)日:2007-03-13

    申请号:US10471290

    申请日:2002-03-19

    IPC分类号: A61K31/40 C07D207/00

    摘要: The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1–C6-alkyl, C2–C6-alkenyl, C2–C6-alkynyl, aryl, heteroaryl, 3–8-membered cycloalkyl, acyl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1–2 further cycloalkyl or aryl or heteroaryl group

    摘要翻译: 本发明涉及式(I)的吡咯烷酯用于治疗和/或预防早产,早产和痛经的用途。 特别地,本发明涉及式(I)的吡咯烷酯的用途,特别是拮抗催产素受体。 本发明还涉及新的吡咯烷酯。 X选自CR 6,S 6,S 6,N 6,R 6,R 6, 7 ; R选自包含C 1 -C 6 -C 6烷基,C 2 -C 6 -C 6烷基,C 2 -C 6 - 烯基,C 2 -C 6炔基,饱和或不饱和的3-8元环烷基,其可以含有1-3个选自N,O,S,芳基,杂芳基的杂原子 C 1 -C 6 - 烷基芳基,C 1 -C 6 - 烷基杂芳基,C 1 -C 6 - 烷基芳基,C 1 -C 6 - R 1选自由C 1 -C 6 - C 6 - 烷基,C 2 - (C 1 -C 6)烷基组成的组或由C 1 -C 6 - C 6 - 烯基,C 2 -C 6 - 炔基,芳基,杂芳基,3-8元环烷基,酰基,C

    Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
    10.
    发明授权
    Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists 有权
    吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂

    公开(公告)号:US07115639B2

    公开(公告)日:2006-10-03

    申请号:US10480992

    申请日:2002-06-14

    CPC分类号: C07D413/04 C07D413/14

    摘要: The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group

    摘要翻译: 本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物,以及含有这种吡咯烷恶二唑衍生物的药物制剂。 所述吡咯烷衍生物可用于治疗和/或预防早产,早产和痛经。 特别地,本发明涉及显示出显着调节,特别是催产素受体拮抗剂活性的吡咯烷衍生物。 更优选地,所述化合物可用于治疗和/或预防催产素介导的疾病状态,包括早产,早产和痛经。 本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基