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1. 发明申请

WO2006108701A1 3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： 3-（1,2,4-TRIAZOL-3YLALKYL）AZABRICLO（3.1.0）作为DOPAMINE D3受体的调节剂的HEXANE衍生物
公开(公告)号：WO2006108701A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003554
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/497 , A61P25/00 , C07D409/14
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R 1 is independently 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 5; " each R 2 is independently hydrogen, fluorine or C 1-4 alkyl; " n is 2, 3, 4, or 5; " R 3 is C 1-4 alkyl; " R 4 is hydrogen, or a C 1-4 alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which 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, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ;or R 4 is a -SR 6 group; " R 5 is selected from a group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally 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 6 is C 1-4 alkyl or -CH 2 C 3-4 cycloalkyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1. 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, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其中“G选自：苯基，吡啶基，苯并噻唑基和吲唑基”; p是0-5的整数; “R 1”独立地选自：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 5;每个R 2独立地是氢，氟或C 1-4烷基; “n为2,3,4或5;”R 3为C 1-4烷基; “R”4是氢或C 1-4烷基，苄基，苯基，杂环基，5或6元杂芳基或8至11元双环基团，其中任何基团任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，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烷基，烷酰基和SF 5;或R 4是-SR 6 C 6;选择“R 5” 由以下组成的组：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基和2-吡咯烷基，并且这种基团任选被取代通过一个或两个选自以下的取代基：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 6”是C 1-4烷基或-CH 2 -SO 3 -S-环烷基;当R 相对于与分子的其余部分的连接键，R 1不在氯原子的邻位存在这样的R 1，并且当R _{1 对应于R 5，p为1.它们的制备方法，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，作为多巴胺D的调节剂 > 3受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。}

2. 发明申请

WO2004089897A1 COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF 审中-公开
标题翻译：在5HT2C受体上具有活性的化合物及其用途
公开(公告)号：WO2004089897A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003678
申请日：2004-04-05
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio , TERRENI, Silvia
发明人： BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio , TERRENI, Silvia
IPC分类号： C07D209/46
CPC分类号： C07D209/46
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1 6alkylthio, hydroxy, amino, mono or di C1 6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, -COOR3, -COR4 (wherein R3 and R4, are independently hydrogen or C1-6alkyl) or -COR5 (wherein R5 is amino, mono or di C1 6alkylamino or an N-linked 4 to 7 membered heterocyclic group); p is 0, 1 or 2 or 3; Q is a 6- membered aromatic group or a 6-membered heteroaromatic group; A is -(CH2-CH2)-, -(CH=CH)-, or a group -(CHR7)- wherein R7 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1 6alkylthio; R2 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1 6alkylthio, amino, mono or di C1 6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is oxygen, sulfur, -CH2- or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, -CH2-, -(CH2)2- or -CH=CH-; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is -NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, such as for depression or anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中R 1是卤素，氰基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基，C 1-6烷硫基，羟基，氨基，单或二C 1-6烷基氨基， N-连接的4至7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，-COOR 3，-COR 4（其中R 3和R 4独立地为氢或C 1-6烷基）或-COR 5（其中R 5为氨基，单或二C 1-6烷基氨基或N-连接的4至7元杂环基）; p为0,1或2或3; Q是6-元芳基或6元杂芳基; A是 - （CH 2 -CH 2） - ， - （CH = CH） - 或 - （CHR 7） - ，其中R 7是氢，卤素，羟基，氰基，硝基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基或C 1-6烷硫基; R2是氢，卤素，羟基，氰基，硝基，C1-6烷基，C1-6烷酰基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二C 1-6烷基氨基或N-连接的4至7元杂环基; X是氧，硫，-CH 2 - 或NR 8，其中R 8是氢或C 1-6烷基; Y是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; Z为任选取代的N-连接的杂环基或含有至少一个氮的C连接的4至7元杂环基，或Z为-NR 9 R 10，其中R 9和R 10独立地为氢或C 1-6烷基。还公开了其在治疗中的制备方法及其用途，例如抑郁症或焦虑症。

3. 发明申请

WO2005118549A2 COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF 审中-公开
标题翻译：具有DOPAMINE D3受体的亲和性的化合物及其用途
公开(公告)号：WO2005118549A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/005965
申请日：2005-05-31
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D223/16
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) and salts thereof are disclosed: wherein A, R 1 , m, R 2 , n, R 3 , R 4 , q, W 1 , W 2 , R 5 and R 6 are as defined in the description. Methods of preparing the compounds and uses thereof in medicine, for example in the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物及其盐：其中A，R1，m，R2，n，R3，R4，q，W1，W2，R5和R6如说明书中所定义。还公开了制备化合物的方法及其在医药中的用途，例如治疗精神分裂症或药物依赖性。

4. 发明申请

WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZ Y Y O O O O S S S S S S S S S S S S S S S S S S S S S S S S S S
公开(公告)号：WO2005080382A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001940
申请日：2005-02-21
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R 1 is independently 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; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which 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; R 5 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 a 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; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1; 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 or as antipsychotic agents.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐，其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p为0〜5的整数; R 1独立地选自：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; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; R5是选自以下的部分：异恶唑基，-CH 2 -N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基，任选地被一个或多个选自以下的两个取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 它们的制备方法，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，作为多巴胺D3受体的调节剂。治疗药物依赖或作为抗精神病药。

5. 发明申请

WO2007022933A1 TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂的三唑衍生物
公开(公告)号：WO2007022933A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008200
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D413/14 , C07D403/14 , A61K31/4196 , A61P25/18
CPC分类号： C07D403/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R 1 is independently 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 or SF 5 ; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is S or -CH 2 -; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which 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 and C 1-4 alkanoyl; R 5 is isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1- 4alkoxy and C 1-4 alkanoyl; 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 substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中：G是5-或6-元杂芳族基团，或是含有一个或两个独立选择的杂原子的9或10元双环杂芳族基团氮和氧，其中G不是吡啶基，吲唑基或苯并噻唑基; p为0〜4的整数。 R 1独立地选自：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烷酰基或SF 5 N; 或对应于基团R 5; R 2是氢或C 1-4烷基; n为2或3; X是S或-CH 2 - ; R 3是C 1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被 1,2,3或4个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1 -4个烷氧基和C 1-4烷酰基; R 5是异恶唑基，-CH 2 N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中各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烷基，卤代C 1-4 - 烷基，C 1 - 烷氧基和C 1-4烷酰基; 其制备方法，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，作为多巴胺D 3受体的调节剂，例如。治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

6. 发明申请

WO2009109608A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2009109608A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052567
申请日：2009-03-05
申请人： GLAXO GROUP LIMITED , BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04 , A61K31/435 , A61P25/00
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04
摘要： The invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及式（I）化合物，其制备方法，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5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE）再吸收抑制剂。

7. 发明申请

WO2008074716A1 AZABICYCLIC COMPOUNDS AS SEROTONINE, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译：作为丝氨酸，多巴胺和诺贝那韦再摄入抑制剂的化学式
公开(公告)号：WO2008074716A1
公开(公告)日：2008-06-26
申请号：PCT/EP2007/063841
申请日：2007-12-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , MICHELI, Fabrizio , TERRENI, Silvia
发明人： BONANOMI, Giorgio , MICHELI, Fabrizio , TERRENI, Silvia
IPC分类号： C07D209/52 , A61K31/403 , A61P25/18
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of Formula (I)' or pharmaceutically acceptable salts or a solvates thereof: wherein A is and K is a mono or bicyclic aryl group; R 1 is selected from a group consisting of: halogen, C 1-4 alkyl and C 1-4 alkoxy, and such R 1 may assume different meanings on the basis of p value; p is an integer from 0 to 5; R 2 is a group P wherein P is and R 3 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-3 alkyl, haloC 1-2 alkyl or an optionally substituted phenyl group; X is oxygen, -NR 8 - or sulphur; n is 0 or 1; R 7 is hydrogen or methyl; R 4 is hydrogen or methyl; R 5 is hydrogen or C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; and R 8 is hydrogen or C 1-4 alkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物：其中A是且K是单或双环芳基; R 1选自由以下组成的组：卤素，C 1-4烷基和C 1-4 - 烷氧基，并且这样的R _{1 可以在p值的基础上具有不同的含义; p是0至5的整数; R 2是基团P，其中P是且R 3是氢，C 1-4烷基，C 3-6，环烷基，C 3-6环烷基C 1-3烷基，卤代C 1-12烷基或任选取代的苯基; X是氧，-NR 8 - 或硫; n为0或1; R 7是氢或甲基; R 4是氢或甲基; R 5是氢或C 1-4烷基; R 6是氢或C 1-4烷基; 并且R 8是氢或C 1-4烷基; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，它们的制备方法，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应用。}

8. 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

9. 发明申请

WO2006133946A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：WO2006133946A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005768
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/435 , A61K31/41 , A61P25/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: (I), 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, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：（I）其制备方法，用于这些方法的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D的调节剂 > 3个受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

10. 发明申请

WO2007022935A1 AZABICYCLO [3.1.0] HEXYLPHENYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：亚氨基胆碱[3.1.0]作为DOPAMINE D3受体的调节剂的HEXYLPHENYL衍生物
公开(公告)号：WO2007022935A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008202
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , PRANDI, Adolfo , TERRENI, Silvia
发明人： GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , PRANDI, Adolfo , TERRENI, Silvia
IPC分类号： C07D209/52 , A61K31/403 , A61P25/00
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: Formula (IA), wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: -SO 2 NR 5 -, -SO 2 CR 2 R 3 -, - CR 2 R 3 SO 2 - and -NR 5 SO 2 -; R 1 is hydrogen, C 1-6 alkyl, haloC 1-6 alkyl or C 2-6 alkylene; R 2 and R 3 are independently hydrogen or C 1-6 alkyl; R 4 is hydrogen, halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; R 5 is hydrogen, C 1-6 alkyl, or a phenyl optionally substituted by R 4 ; and R 6 is hydrogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; 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 substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（IA）化合物或其盐：式（IA），其中：A相对于环丙基在间位或对位位于苯基上，并且选自由以下组成的组：-SO 2 NR 5 - ， - SO 2 R 2 R 3 R 3 - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - ; R 1是氢，C 1-6烷基，卤代C 1-6 - 烷基或C 2-6 - 亚烷基 ; R 2和R 3独立地是氢或C 1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6 烷氧基或卤代C 1-6烷氧基; R 5是氢，C 1-6烷基或任选被R 4取代的苯基; R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷基，C 1-6烷基，烷氧基或卤代C 1-6烷氧基; 其制备方法，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，作为多巴胺D 3受体的调节剂，例如。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

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