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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。