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    • 1. 发明申请
    • SUBSTITUTED 4-PHENYL-PIPERIDIN-AMIDES AS TACHYKININ ANTAGONISTS AND SEROTONIN REPTAKE INHIBITORS
    • 作为TACHYKININ拮抗剂和丝氨酸蛋白酶抑制剂的取代的4-苯基 - 哌啶
    • WO2004005256A3
    • 2004-10-14
    • PCT/EP0307127
    • 2003-07-02
    • GLAXO GROUP LTDALVARO GIUSEPPECARDULLO FRANCESCADI FABIO ROMANOGIOVANNINI RICCARDOPIGA ELISABETTATRANQUILLINI MARIA ELVIRA
    • ALVARO GIUSEPPECARDULLO FRANCESCADI FABIO ROMANOGIOVANNINI RICCARDOPIGA ELISABETTATRANQUILLINI MARIA ELVIRA
    • A61K31/451A61K31/55A61P25/18A61P25/22A61P25/24A61P43/00C07D211/34C07D211/64C07D223/04C07D223/06
    • C07D211/34C07D211/64C07D223/04C07D223/06
    • The present invention relates to cyclic amine derivatives of formula(I) (I)whereinR represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy;R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy;R2 represents hydrogen or C1-4 alkyl;R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl;R5 represents trifluoromethyl, S(O)t C 1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano;R6 represents hydrogen or (CH2)rR7;R7 represents hydrogen, C3-7 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2 , OC(O)NR9R8 , NR8C(O)R9 or C(O)NR9R8;R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4;n represents 1 or 2;p is zero or an integer from 1 to 3;q is an integer from 1 to 3;r is an integer from 1 to 4;t is 0 , 1 or 2 ;provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein .
    • 本发明涉及式(I)(I)的环胺衍生物,其中R表示卤素,C 1-4烷基,氰基,C 1-4烷氧基,三氟甲基或三氟甲氧基; R 1表示氢,卤素,C 3-7环烷基,羟基,硝基, 氰基或C 1-4烷氧基; R 2表示氢或C 1-4烷基; R 3和R 4独立地表示氢,氰基,C 1-4烷基或R 3与R 4一起代表C 3-7环烷基 R5代表三氟甲基,S(O)t C 1-4烷基,C 1-4烷基,C 1-4烷氧基,三氟甲氧基,卤素或氰基; R 6表示氢或(CH 2)r R 7; R 7表示氢,C 3-7环烷基, NH(C 1-4烷基OC 1-4烷氧基),NH(C 1-4烷基),N(C 1-4烷基)2,OC(O)NR 9 R 8,NR 8 C(O)R 9或C(O)NR 9 R 8; R 9和R 8独立地表示氢, -4-烷基或C 3-7环烷基; m表示0或1〜4的整数; n表示1或2; p表示0或1〜3的整数,q表示1〜3的整数,r表示1〜4的整数,t表示0, 1或2;条件是当m为0时,p为2,q,r和n为1,R1,R2,R3,R4,R5和R7为氢,R为氯,R5不为碘; 及其药学上可接受的盐和溶剂合物; 其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白的用途。
    • 3. 发明申请
    • CHEMICAL COMPOUNDS
    • 化学化合物
    • WO2004005256A2
    • 2004-01-15
    • PCT/EP2003/007127
    • 2003-07-02
    • GLAXO GROUP LIMITEDALVARO, GiuseppeCARDULLO, FrancescaDI FABIO, RomanoGIOVANNINI, RiccardoPIGA, ElisabettaTRANQUILLINI, Maria, Elvira
    • ALVARO, GiuseppeCARDULLO, FrancescaDI FABIO, RomanoGIOVANNINI, RiccardoPIGA, ElisabettaTRANQUILLINI, Maria, Elvira
    • C07D211/34
    • C07D211/34C07D211/64C07D223/04C07D223/06
    • The present invention relates to cyclic amine derivatives of formula(I) (I)whereinR represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy;R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy;R2 represents hydrogen or C1-4 alkyl;R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl;R5 represents trifluoromethyl, S(O)t C 1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano;R6 represents hydrogen or (CH2)rR7;R7 represents hydrogen, C3-7 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2 , OC(O)NR9R8 , NR8C(O)R9 or C(O)NR9R8;R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4;n represents 1 or 2;p is zero or an integer from 1 to 3;q is an integer from 1 to 3;r is an integer from 1 to 4;t is 0 , 1 or 2 ;provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein .
    • 本发明涉及式(I)(I)的环胺衍生物,其中R代表卤素,C 1-4烷基,氰基,C 1-4烷氧基,三氟甲基或三氟甲氧基; R 1代表氢,卤素, 氰基或C1-4烷基; R2代表氢或C1-4烷基; R3和R4独立地代表氢,氰基,C1-4烷基或R3 与R 4一起代表C 3-7环烷基; R 5代表三氟甲基,S(O)t C 1-4烷基,C 1-4烷基,C 1-4烷氧基,三氟甲氧基,卤素或氰基; R 6代表氢或(CH 2)r R 7; R 7 (C 1-4烷基),N(C 1-4烷基)2,OC(O)NR 9 R 8,NR 8 C(O)R 9或C(O)NR 9 R 8; R9和R8独立地表示氢,C1-4烷基或C3-7环烷基; m表示0或1至4的整数; n表示1或2; p为0或1至3的整数; q为1至3的整数; r为1至4的整数; t为0, 1或2;条件是当m为0时,p为2,q,r和n表示1,R1,R2,R3,R4,R5和R7是氢并且R是氯,R5不是碘; 及其药学上可接受的盐和溶剂合物; 它们的制备方法以及它们在治疗由粘着激肽介导的病症和/或通过选择性抑制血清素再摄取转运蛋白中的用途。