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1. 发明申请

WO2004005256A3 SUBSTITUTED 4-PHENYL-PIPERIDIN-AMIDES AS TACHYKININ ANTAGONISTS AND SEROTONIN REPTAKE INHIBITORS 审中-公开
标题翻译：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
公开(公告)号：WO2004005256A3
公开(公告)日：2004-10-14
申请号：PCT/EP0307127
申请日：2003-07-02
申请人： GLAXO GROUP LTD , ALVARO GIUSEPPE , CARDULLO FRANCESCA , DI FABIO ROMANO , GIOVANNINI RICCARDO , PIGA ELISABETTA , TRANQUILLINI MARIA ELVIRA
发明人： ALVARO GIUSEPPE , CARDULLO FRANCESCA , DI FABIO ROMANO , GIOVANNINI RICCARDO , PIGA ELISABETTA , TRANQUILLINI MARIA ELVIRA
IPC分类号： A61K31/451 , A61K31/55 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
CPC分类号： C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
摘要： 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 .
摘要翻译：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。

2. 发明申请

WO2004005255A1 N-BENZYL-3-PHENYL-3-HETEROCYCLYL-PROPIONAMIDE COMPOUNDS AS TACHYKININ AND/ OR SEROTONIN REUPTAKE INHIBITORS 审中-公开
标题翻译：作为TACHYKININ和/或SEROTONIN REUPTAKE抑制剂的N-苄基-3-苯基-3-间苯二甲酰胺化合物
公开(公告)号：WO2004005255A1
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007126
申请日：2003-07-02
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , CARDULLO, Francesca , D'ADAMO, Lucilla , PIGA, Elisabetta , SERI, Catia
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , D'ADAMO, Lucilla , PIGA, Elisabetta , SERI, Catia
IPC分类号： C07D211/14
CPC分类号： C07D207/08 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/535 , C07D207/20 , C07D211/34 , C07D211/38 , C07D211/70 , C07D213/56 , C07D265/30
摘要： The present invention relates to heterocyclic derivatives of formula (1) wherein R 1 represents a 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms, or R 1 represents a 4,5 or 6 membered heterocyclic group, wherein saids 5 or 6 membered heteroaryl or the 4,5 or 6 membered heterocyclic group may optionally be substituted by one to three substituents, which may be the same or different, selected from (CH 2 ) p R 6 , wherein p is zero or an integer from 1 to 4 and wherein R and R 2 - R 6 are each as defined in the description and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（1）的杂环衍生物，其中R 1表示5或6元杂芳基，其中5元杂芳基含有至少一个选自氧，硫或氮的杂原子和6元杂芳基含有1至3个氮原子，或R 1表示4,5或6元杂环基，其中所述5或6元杂芳基或4,5或6元杂环基可以任选被一至三个取代基取代，相同或不同，选自（CH 2）p R 6，其中p为0或1至4的整数，并且其中R和R 2 -R 6各自如说明书中所定义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速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

3. 发明申请

WO2004005256A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004005256A2
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007127
申请日：2003-07-02
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
IPC分类号： C07D211/34
CPC分类号： C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
摘要： 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 .
摘要翻译：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。

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