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    • 7. 发明申请
    • PYRROLIDINE ESTER DERIVATIVES WITH OXYTOCIN MODULATING ACITVITY
    • 具有氧化调节作用的吡咯烷酮衍生物
    • WO2002074741A1
    • 2002-09-26
    • PCT/EP2002/003005
    • 2002-03-19
    • APPLIED RESEARCH SYSTEMS ARS HOLDING NVSCHWARZ, MatthiasQUATTROPANI, AnnaSCHEER, AlexanderDORBAIS, JérômePOMEL, Vincent
    • SCHWARZ, MatthiasQUATTROPANI, AnnaSCHEER, AlexanderDORBAIS, JérômePOMEL, Vincent
    • C07D207/20
    • C07D401/10A61K31/401C07D207/22C07D403/10
    • 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 antagonise the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR 6 R 7 , NOR 6 , NNR 6 R 7 ;R is selected from the group comprising or consisting of C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, saturated or unsaturated 3-8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl. R 1 is selected from the group comprising or consisting of C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, acyl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1-2 further cycloalkyl or aryl or heteroaryl group.
    • 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 R 7,NOR 6,NNR 6 R 7; R选自C 1 -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,C 1 -C 6烷基芳基,C 1 -C 6烷基杂芳基的杂原子。 R 1选自由C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 炔基,芳基,杂芳基,3-8元环烷基,酰基,C 1 -C 6 - 烷基芳基 ,C 1 -C 6烷基杂芳基,所述环烷基或芳基或杂芳基可与1-2个其它环烷基或芳基或杂芳基稠合。