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1. 发明申请

WO2003066635A1 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2003066635A1
公开(公告)日：2003-08-14
申请号：PCT/EP2003/001308
申请日：2003-02-10
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano , TRANQUILLINI, Maria, Elvira , SPADA, Simone
发明人： ALVARO, Giuseppe , DI FABIO, Romano , TRANQUILLINI, Maria, Elvira , SPADA, Simone
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/445
摘要： The present invention relates to piperidine derivatives of formula (I): R represents halogen or C 1-4 alkyl; R 1 represents C 1-4 alkyl; R 2 or R 3 independently represent hydrogen or C 1-4 alkyl; R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R 5 represents hydrogen , C 1-4 alkyl or C 3-7 cycloalkyl; R 6 is hydrogen and R 7 is a radical of formula (W): R 6 is a radical of formula (W) and R 7 is hydrogen; X represents CH 2 , NR 5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of condition mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物：R代表卤素或C 1-4烷基; R1表示C1-4烷基; R2或R3独立地表示氢或C1-4烷基; R 4表示三氟甲基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或卤素; R5代表氢，C1-4烷基或C3-7环烷基; R6是氢，R7是式（W）的基团：R6是式（W）的基团，R7是氢; X表示CH 2，NR 5或O; Y表示氮，Z表示CH或Y表示CH，Z表示氮; A表示C（O）或S（O）q，条件是当Y为氮且Z为CH时，A不为S（O）q; m为0或1〜3的整数; n为1〜3的整数， p和q独立地为1至2的整数; 及其药学上可接受的盐和溶剂化物。其制备方法及其用于治疗由速激肽介导的病症。

2. 发明申请

WO2005049600A1 BETA-LACTAMS FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的BETA-LACTAMS
公开(公告)号：WO2005049600A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012772
申请日：2004-11-10
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
发明人： ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I) wherein ---- represents a single or a double bond; R represents a radical selected from formulae i), ii), iii) and iv) in which R 1 is halogen, cyano, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R 2 represents hydrogen or C 1-4 alkyl; R 3 represents hydrogen, hydroxy or C 1-4 alkyl; R 4 represents hydrogen or R 4 together with R 3 represents =0 or =CH 2 ; R 5 represents phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, hydroxy, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC 1-4 alkyl; R 6 and R 7 independently represent hydrogen, cyano, C 1-4 alkyl; R 8 is (CH 2 )rR 10 ; R 9 represents hydrogen, halogen, C 3-7 cycloalkyl, hydroxy, nitro, cyano or C 1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C 1-4 alkoxy; R 10 represents hydrogen or C 3-7 cycloalkyl; n represents 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（I）的新化合物，其中----表示单键或双键; R表示选自式i），ii），iii）和iv）中的基团，其中R 1为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数 ; R2代表氢或C1-4烷基; R3表示氢，羟基或C1-4烷基; R4表示氢或R4，R3表示= 0或= CH2; R5表示苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，C 1-4烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）qC 1-4烷基; R6和R7独立地表示氢，氰基，C1-4烷基; R8为（CH2）rR10; R9代表氢，卤素，C3-7环烷基，羟基，硝基，氰基或任选被一个或两个选自卤素，氰基，羟基或C 1-4烷氧基的基团取代的C 1-4烷基; R 10表示氢或C 3-7环烷基; n表示1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，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。

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。

4. 发明申请

WO2010063663A1 N-{[(IR,4S,6R-3-(2-PYRIDINYLCARBONYL)-3-AZABICYCLO [4.1.0]HEPT-4-YL] METHYL}-2-HETEROARYLAMINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： N - {[（1R，4S，6R-3-（2-吡啶基]苄基] -3-亚氨基] [4.1.0] HEPT-4-YL]甲基} -2-叔丁基胺衍生物及其用途
公开(公告)号：WO2010063663A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/066017
申请日：2009-11-30
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
发明人： ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/55 , A61P25/22 , A61P25/24 , A61P3/04
CPC分类号： C07D401/14
摘要： This invention relates to N -{[(1 R ,4 S ,6 R )-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N - {[（1R，4S，6R）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物及其作为药物。

5. 发明申请

WO2010063662A1 N-{[(IR,4S,6R-3-(2-PYRIDINYLCARBONYL)-3-AZABICYCLO [4.1.0] HEPT-4-YL] METHYL}-2-HETEROARYLAMINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： N - {[（1R，4S，6R-3-（2-吡啶基]苄基] -3-亚氨基] [4.1.0] HEPT-4-YL]甲基} -2-叔丁基胺衍生物及其用途
公开(公告)号：WO2010063662A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/066016
申请日：2009-11-30
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
发明人： ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/55 , A61P25/22 , A61P25/24 , A61P3/04
CPC分类号： C07D401/06 , C07D401/14
摘要： This invention relates to N -{[(1 S ,4 S ,6 S )-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N - {[（1S，4S，6S）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物及其作为药物。

6. 发明申请

WO2003066621A1 PIPERIDINE DERIVATIVES AND THEIR USE AS ANTAGONISTS OF TACHYKININS 审中-公开
标题翻译：哌啶衍生物及其作为TACHYKININS的拮抗剂的用途
公开(公告)号：WO2003066621A1
公开(公告)日：2003-08-14
申请号：PCT/GB2003/000501
申请日：2003-02-05
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano
发明人： ALVARO, Giuseppe , DI FABIO, Romano
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to piperidine derivatives of formula (1) Wherein R represents halogen or C 1-4 alkyl; R 1 represents hydrogen or C 1-4 alkyl; R 2 represents hydrogen, C 1-4 alkyl; R 3 represents hydrogen, C 1-4 alkyl;R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R 5 represents hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl, C(O)R 6 or S(O) 2 R 6 ;R 6 represents C 1-4 alkyl or C 3-7 cycloalkyl; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p is an integer from 1 to 2; X and Y are independently C(O) or CH 2 ; provided that i) X and Y are not both C(O) and ii) when X and Y are both CH 2 and p is 1, R 5 is not hydrogen, C 1-4 alkyl or C(O)R 6 ; and pharmaceutically acceptable salts and solvates thereof, the process for their preparation and their use in the treatment of condition mediated by tachykinins.
摘要翻译：本发明涉及式（1）的哌啶衍生物，其中R代表卤素或C 1-4烷基; R1代表氢或C1-4烷基; R2代表氢，C1-4烷基; R3表示氢，C1-4烷基; R4表示三氟甲基，C1-4烷基，C1-4烷氧基，三氟甲氧基或卤素; R5表示氢，C1-4烷基，C3-7环烷基，C（O）R6或S（O）2R6; R6表示C 1-4烷基或C3-7环烷基; m为0或1〜3的整数; n为1〜3的整数， p是从1到2的整数; X和Y独立地为C（O）或CH 2; 条件是i）X和Y不同时为C（O），和ii）当X和Y均为CH 2且p为1时，R 5不为氢，C 1-4烷基或C（O）R 6; 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。

7. 发明申请

WO2009130232A1 PYRAZOLO [1, 5 -A] PYRAZINE DERIVATIVES AS ANTAGONISTS OF V1B RECEPTORS 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪衍生物作为V1B受体的拮抗剂
公开(公告)号：WO2009130232A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054780
申请日：2009-04-22
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
发明人： DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or salts thereof: wherein R is -X-[CH 2 ] n CR 4 R 5 -Y; or a group G; G is one of the groups selected form the list consisting of G1, G2, G3, G4, G5, G6, G7, G8, G9, G10, G11 and G12, and the rest of the variables are as specified in the claims, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as antagonists of V1b receptors, e.g. to treat depression and anxiety.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R是-X- [CH2] nCR4R5-Y; 或G组; G是从由G1，G2，G3，G4，G5，G6，G7，G8，G9，G10，G11和G12组成的列表中选择的组之一，其余变量如权利要求中所述，对于它们的制备，在这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为V1b受体的拮抗剂，例如治疗抑郁症和焦虑症。

8. 发明申请

WO2009016084A1 SPIRO CYCLOPENTANE COMPOUNDS USEFUL AS ANTAGONISTS OF THE H1-RECEPTOR 审中-公开
标题翻译：螺旋环化合物可用作H1受体拮抗剂
公开(公告)号：WO2009016084A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059682
申请日：2008-07-24
申请人： GLAXO GROUP LIMITED , CASTIGLIONI, Emiliano , DI FABIO, Romano , GIANOTTI, Massimo , MESIC, Milan , PAVONE, Francesca , RAST, Slavko , STASI, Luigi, Piero
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , GIANOTTI, Massimo , MESIC, Milan , PAVONE, Francesca , RAST, Slavko , STASI, Luigi, Piero
IPC分类号： C07C211/38 , A61K31/131 , A61P25/00
CPC分类号： C07C211/38 , C07C2603/94
摘要： This invention relates to novel spiro cyclopentane derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
摘要翻译：本发明涉及式（I）的新型螺环戊烷衍生物或其药学上可接受的盐，用于治疗中枢神经系统（CNS）的疾病和病症，特别是睡眠障碍。

9. 发明申请

WO2008031772A1 AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE 审中-公开
标题翻译：单一化合物作为单体反应的抑制剂
公开(公告)号：WO2008031772A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059381
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D221/04 , A61K31/435 , A61P25/00
CPC分类号： C07D221/04
摘要： The present invention relates to novel compounds of formula (I)´, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 18 , each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R 15 ) p , which can be the same or different; p is an integer from 0 to 5; R 3 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 4 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 5 is hydrogen or C 1-4 alkyl; R 7 is hydrogen or C 1-4 alkyl; or is a group X, X 1 , X 2 or X 3 ; wherein X is (IV) X 1 is (V) X 2 is (VI) and X 3 is (VII) R 6 is hydrogen or C 1-4 alkyl; or is a group X or X 1 ; R 9 is C 1-4 alkyl; R 10 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; R 11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 13 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 15 is selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 16 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 17 is hydrogen or C 1-4 alkyl; R 18 is selected from a group consisting of: halog
摘要翻译：本发明涉及新的式（I）化合物，其药学上可接受的盐，前药或溶剂合物：其中R 1是氢或C 1-4烷基; R 2是基团A，K或W，其中A是（II）K是任选被1或2个基团R 18取代的a或β萘基，每个他们是相同或不同的; 并且W是（III），并且其中G是5,6-元单环杂芳基或8至11元杂芳基双环基团; 这样的G可以被相同或不同的（R 15） p是0至5的整数; R 3 3选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 4选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 5是氢或C 1-4烷基; R 7是氢或C 1-4烷基; 或者为X，X 1，X 2或X 3; 其中X是（Ⅳ）ⅩⅢ是（Ⅴ）ⅩⅥ是（Ⅵ），ⅩⅢ是（Ⅶ） 6是氢或C 1-4烷基; 或者是X或X 1族; R 9是C 1-4烷基; R 10选自：氢，卤素，羟基，氰基，C 1-4 - 烷基，卤代C 1-4 - 烷基 C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 8; R 8是5-6元杂环基团，其可以被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4烷基卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; R 11选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 12选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 13选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基 C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 8; R 14选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 15选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4个碳原子的烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 16是氢，C 1-4烷基，C 3-6环烷基或C 3-6环烷基C _{1-3 烷基; R 17是氢或C 1-4烷基; R 18选自：卤素}

10. 发明申请

WO2007113232A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113232A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053074
申请日：2007-03-30
申请人： Glaxo Group Limited , BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11 -membered heteroaryl bicyclic group; A is a group P1 or a group P2 Wherein p is an integer ranging from 0 to 5; R 1 is halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1- 4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 6 ; and when p is an integer ranging from 2 to 5, each R 1 may be the same or different; R 2 is hydrogen or C 1-4 alkyl; n is 3, 4, 5 or 6; R 6 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R 6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1- 4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1- 4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4- alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl, haloC 1-4 alkoxy and SF 5 ; R 5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; R 7 is hydrogen or C 1-2 alkyl; R' is H, C 1-4 alkyl or C 1-4 alkanoyl; R" is defined as R'; R' and R" taken together with the interconnecting nitrogen atom may form a 5-, 6- membered saturated or unsaturated heterocyclic ring; wherein at least one of R 4 and R 5 is hydrogen; and wherein only one R 2 group may be different from hydrogen; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5-或6-元单环杂芳基或8-至11元杂芳基双环基团 A是基团P1或基团P2，其中p是0至5的整数; R 1是卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷基，烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R 2是氢或C 1-4烷基; n为3,4,5或6; R 6是选自以下的部分：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧代-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基和这样的R 6 C 6基团任选地被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4 - >一

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