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    • 1. 发明申请
    • THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR
    • 作为PROSTAGLANDIN F受体的调节剂的噻唑烷羧酰胺衍生物
    • WO2003082278A1
    • 2003-10-09
    • PCT/EP2003/050083
    • 2003-03-27
    • APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.PAGE, PatrickJORAND-LEBRUN, CatherineQUATTROPANI, AnnaPOMEL, VincentSCHWARZ, MatthiasHAMELIN, EstelleTHOMAS, Russell J.
    • PAGE, PatrickJORAND-LEBRUN, CatherineQUATTROPANI, AnnaPOMEL, VincentSCHWARZ, MatthiasHAMELIN, EstelleTHOMAS, Russell J.
    • A61K31/426
    • C07D417/12A61K31/426A61K31/427C07D277/06C07D417/14Y02P20/582
    • The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. G is selected from the group consisting of C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, C 1 -C 6 Alkyl cycloalkyl, C 1 -C 6 -alkyl heteroaryl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl or -heterocyclo­alkyl, said cycloalkyl or aryl or heteroaryl groups may be fused with cycloalkyl or aryl or heteroaryl groups. R 1 is selected from the group consisting of aryl, heteroaryl, C 3 -C 8 -cycloalkyl or - heterocyclo-alkyl, said (hetero)cycloalkyl or aryl or heteroaryl groups may be fused with (hetero)cycloalkyl or aryl or heteroaryl groups. R 2 is selected from the group consisting of H, carboxy, acyl, alkoxycarbonyl, amino­carbonyl, C 1 -C 5 -alkyl carboxy, C 1 -C 5 -alkyl acyl, C 1 -C 5 -alkyl alkoxycarbonyl, C 1 -C 5 -alkyl aminocarbonyl, C 1 -C 5 -alkyl acyloxy, C 1 -C 5 -alkyl acylamino, C 1 -C 5 -alkyl ureido, C 1 -C 5 alkyl amino, C 1 -C 5 -alkyl alkoxy, C 1 -C 5 -alkyl sulfanyl, C 1 -C 5 -alkyl sulfinyl, C 1 -C 5 -alkyl sulfonyl, C 1 -C 5 -alkyl sulfonylamino, C 1 -C 5 -alkyl sulfonyloxy, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, C 1 -C 6 -alkyl aryl, C 2 -C 6 -alkyl heteroaryl, C 1 -C 6 -alkyl cycloalkyl, C 1 -C 6 -alkyl heterocycloalkyl, C 2 -C 6 -alkenyl aryl, C 2 -C 6 -alkenyl heteroaryl, C 2 -C 6 -alkynyl aryl, or C 2 -C 6 -alkynyl heteroaryl.
    • 本发明涉及式(II)的噻唑烷羧酰胺衍生物,其用于治疗和/或预防早产,早产,痛经和用于在剖宫产分娩前停止劳动。 G选自C1-C6-烷基芳基,C1-C6-烷基杂芳基,C1-C6烷基环烷基,C1-C6-烷基杂芳基,芳基,杂芳基,C3-C8-环烷基或 - 杂环烷基,所述环烷基 或芳基或杂芳基可与环烷基或芳基或杂芳基稠合。 R 1选自芳基,杂芳基,C 3 -C 8 - 环烷基或 - - 杂环烷基,所述(杂)环烷基或芳基或杂芳基可与(杂)环烷基或芳基或杂芳基稠合。 R 2选自H,羧基,酰基,烷氧基羰基,氨基羰基,C 1 -C 5 - 烷基羧基,C 1 -C 5 - 烷基酰基,C 1 -C 5 - 烷基烷氧基羰基,C 1 -C 5 - 烷基氨基羰基,C 1 C 1 -C 5烷基酰氧基,C 1 -C 5烷基酰氨基,C 1 -C 5烷基脲基,C 1 -C 5烷基氨基,C 1 -C 5烷基烷氧基,C 1 -C 5烷基硫烷基,C 1 -C 5烷基亚磺酰基, 烷基磺酰基,C 1 -C 5 - 烷基磺酰基氨基,C 1 -C 5 - 烷基磺酰氧基,C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,C 2 -C 6炔基,芳基,杂芳基,C 3 -C 8 - 环烷基,杂环烷基,C 1 -C 6 烷基芳基,C 2 -C 6烷基杂芳基,C 1 -C 6烷基环烷基,C 1 -C 6烷基杂环烷基,C 2 -C 6烯基芳基,C 2 -C 6链烯基杂芳基,C 2 -C 6炔基芳基或C 2 -C 6 - 炔基杂芳基。
    • 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。