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1. 发明申请

WO2005087764A1 TETRAHYDROBENZAZEPINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS (ANTIPSYCHOTIC AGENTS) 审中-公开
标题翻译：作为DOPAMINE D3受体（抗生素代谢物）的调节剂的四氢苯并噻吩衍生物
公开(公告)号：WO2005087764A1
公开(公告)日：2005-09-22
申请号：PCT/EP2005/002635
申请日：2005-03-04
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
发明人： ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
IPC分类号： C07D413/14
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, 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. as agents to treat various aspects 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，例如，作为治疗各方面药物依赖的药剂或作为抗精神病药。

2. 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。

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

WO2006002928A1 COMPOUNDS HAVING AFFINITY FOR THE DOPAMINE D3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：多巴胺D3受体具有重要性的化合物及其在医药中的应用
公开(公告)号：WO2006002928A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/007069
申请日：2005-06-29
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
发明人： BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
IPC分类号： C07D498/04
CPC分类号： C07D513/04
摘要： Compounds of formula (I) or a salt thereof are disclosed, wherein A, m R 1 , R 2 , R 3 , q, W 1 , W 2 , R 4 and R 5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物或其盐，其中A，m R 1，R 2，R 3，q，W W 1，W 2，R 4和R 5如说明书中所定义。还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

5. 发明申请

WO2004078718A1 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：WO2004078718A1
公开(公告)日：2004-09-16
申请号：PCT/EP2004/001843
申请日：2004-02-24
申请人： GLAXO GROUP LIMITED , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
发明人： DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein R 1 is hydrogen, fluoro, chloro, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy or haloC 1-6 alkoxy; m is 0 when ==== is a double bond and m is 1 when ==== is a single bond; R 2 is hydrogen, halogen, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is -(CH 2 -CH 2 )-, -(CH=CH)-, -(CH 2 ) 3 -, -C(CH 3 ) 2 -, -(CH=CH-CH 2 )-, -(CH 2 -CH=CH)- or a group -(CHR 5 )- wherein R 5 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy or C 1-6 alkylthio; R 3 is halogen, cyano, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy, C 1-6 alkylthio, hydroxy, amino, mono- or di-C 1-6 alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC 1-6 alkyl, haloC 1-6 alkoxy, aryl, arylC 1-6 alkyl, arylC 1-6 alkyloxy, arylC 1-6 alkylthio or COOR 6 , CONR 7 R 8 or COR 9 wherein R 6 , R 7 , R 8 and R 9 are independently hydrogen or C 1-6 alkyl; p is 0, 1 or 2 or 3; R 4 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 1-6 alkanoyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, -CH 2 - or NR 10 wherein R 10 is hydrogen or C 1-6 alkyl; D is a single bond, -CH 2 -, -(CH 2 ) 2 - or -CH=CH-; and Z is -NR 11 R 12 where R 11 and R 12 are independently hydrogen or C 1-6 alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and 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是氢，氟，氯，羟基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基或卤代C 1-6烷氧基; 当====为双键时，m为0，当==为单键时，m为1; R2是氢，卤素，氰基，硝基，C1-6烷基，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 - （CH 2 -CH 2） - ， - （CH = CH） - ， - （CH 2）3 - ， - C（CH 3）2 - ， - （CH = CH-CH 2） - ， - （CH 2 -CH = CH ） - 或基 - （CHR 5） - ，其中R 5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 ; R 3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4-7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，芳基C 1-6烷基，芳基C 1-6烷氧基，芳基C 1-6烷硫基或COOR 6，CONR 7 R 8或COR 9，其中R 6，R 7，R 8和R 9独立地为氢或C 1-6烷基; p为0,1或2或3; R4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; Y是氧，硫，-CH 2 - 或NR 10，其中R 10是氢或C 1-6烷基; D是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; 并且Z为-NR 11 R 12，其中R 11和R 12独立地为氢或C 1-6烷基，或任选取代的N-连接或C连接的4至7元杂环基。还公开了化合物在治疗中的制备和用途的方法，例如抑郁和焦虑。

6. 发明申请

WO2003089409A1 COMPOUNDS HAVING AFFINITY AT 5HT2C RECEPTOR AND USE THEREOF IN THERAPY 审中-公开
标题翻译：在5HT2C受体中具有亲和力的化合物及其治疗用途
公开(公告)号：WO2003089409A1
公开(公告)日：2003-10-30
申请号：PCT/EP2003/004180
申请日：2003-04-17
申请人： GLAXO GROUP LIMITED , DAMIANI, Federica , HAMPRECHT, Dieter , JAXA-CHAMIEC, Albert, Andrzej , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
发明人： DAMIANI, Federica , HAMPRECHT, Dieter , JAXA-CHAMIEC, Albert, Andrzej , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38 , C07D211/76 , C07D211/88 , C07D401/12
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: wherein R 1 is hydrogen, hydroxy, fluoro, chloro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy or haloC 1-6 alkoxy; m is 0 when ======= is a double bond and m is 1 when ======= is a single bond; R 2 is hydrogen, halogen, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is -(CH 2 -CH 2 )-, -(CH=CH)-, -(CH 2 ) 3 -, -C(CH 3 ) 2 -, -(CH=CH-CH 2 )-, -(CH 2 -CH=CH)- or a group -(CHR 5 )- wherein R 5 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy or C 1-6 alkylthio; R 3 is halogen, cyano, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy, C 1-6 alkylthio, hydroxy, amino, mono- or di-C 1-6 alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC 1-6 alkyl, haloC 1-6 alkoxy, aryl, arylC 1-6 alkyl, arylC 1-6 alkyloxy, arylC 1-6 alkylthio or COOR 6 , CONR 7 R 8 or COR 9 wherein R 6 , R 7 , R 8 and R 9 are independently hydrogen or C 1-6 alkyl; p is 0, 1 or 2 or 3; R 4 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 1-6 alkanoyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, -CH 2 - or NR 10 wherein R 10 is hydrogen or C 1-6 alkyl; D is a single bond, -CH 2 -, -(CH 2 ) 2 - or -CH=CH-; and Z is an optionally substituted C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, an optionally substituted N-linked 4 to 7 membered heterocyclic group, or Z is -NR 11 R 12 where R 11 and R 12 are independently hydrogen or C 1-6 alkyl. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐：其中R 1是氢，羟基，氟，氯，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基或卤代C 1-6烷氧基; 当<=======>是双键时，m为0，当<=======>为单键时，m为1; R2是氢，卤素，氰基，硝基，C1-6烷基，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 - （CH 2 -CH 2） - ， - （CH = CH） - ， - （CH 2）3 - ， - C（CH 3）2 - ， - （CH = CH-CH 2） - ， - （CH 2 -CH = CH ） - 或基 - （CHR 5） - ，其中R 5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 ; R 3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4-7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，芳基C 1-6烷基，芳基C 1-6烷氧基，芳基C 1-6烷硫基或COOR 6，CONR 7 R 8或COR 9，其中R 6，R 7，R 8和R 9独立地为氢或C 1-6烷基; p为0,1或2或3; R4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; Y是氧，硫，-CH 2 - 或NR 10，其中R 10是氢或C 1-6烷基; D是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; Z为含有至少一个氮原子，任意取代的N-连接的4-7元杂环基的任意取代的C连接的4至7元杂环基，或Z为-NR 11 R 12，其中R 11和R 12独立地为氢或C 1-6烷基。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁和焦虑。

7. 发明申请

WO2003042228A1 MACROLIDES 审中-公开
标题翻译：大环内酯类
公开(公告)号：WO2003042228A1
公开(公告)日：2003-05-22
申请号：PCT/GB2002/005101
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , PLIVA D.D. , ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4" position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的4“位取代的14或15元大环内酯及其药学上可接受的盐和溶剂化物，其制备方法及其在治疗或预防人体全身或局部细菌感染中的用途或动物体。

8. 发明公开

EP1453846A1 MACROLIDES 有权
标题翻译：具有抗菌活性的14至15肢体大环内酯类
公开(公告)号：EP1453846A1
公开(公告)日：2004-09-08
申请号：EP02779670.5
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , Pliva - Istrazivacki Institutd.o.o.
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , STIMAC, Vlado , TIBASCO, Jessica , SCHOENFELD, Wolfgang
IPC分类号： C07H17/08 , A61K31/70 , A61P31/04
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4' position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

9. 发明授权

EP1751163B1 BENZAZEPINE COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF 有权
标题翻译：苯并氮杂随着对多巴胺D3受体及其用途AFFINITY
公开(公告)号：EP1751163B1
公开(公告)日：2011-08-10
申请号：EP05756061.7
申请日：2005-05-31
申请人： GLAXO GROUP LIMITED
发明人： BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D487/04 , C07D498/04 , C07D513/04 , A61K31/55 , A61P25/18
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) and salts thereof are disclosed: wherein A, R1, m, R2, n, R3, R4, q, W1, W2, R5 and R6 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.

10. 发明公开

EP1599445A1 COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF 有权
标题翻译： AN 5HT 2C受体活性化合物和用途
公开(公告)号：EP1599445A1
公开(公告)日：2005-11-30
申请号：EP04713874.8
申请日：2004-02-24
申请人： GLAXO GROUP LIMITED
发明人： DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
IPC分类号： C07D207/26 , C07D207/38 , A61K31/40
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ==== is a double bond and m is 1 when ==== is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, 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 -(CH2-CH2)-, -(CH=CH)-, -(CH2)3-, -C(CH3)2-, -(CH=CH-CH2)-, -(CH2-CH=CH)- or a group -(CHR5)- wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 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, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 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; Y is oxygen, sulfur, -CH2- or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, -CH2-, -(CH2)2- or -CH=CH-; and Z is -NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.

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