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1. 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。

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

WO2004099143A1 CYCLIC AMINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：循环胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：WO2004099143A1
公开(公告)日：2004-11-18
申请号：PCT/EP2004/005005
申请日：2004-05-07
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , ARISTA, Luca , CARDULLO, Francesca , D'ADAMO, Lucilla , FERIANI, Aldo , GIOVANNINI, Riccardo , SERI, Catia
发明人： ALVARO, Giuseppe , ARISTA, Luca , CARDULLO, Francesca , D'ADAMO, Lucilla , FERIANI, Aldo , GIOVANNINI, Riccardo , SERI, Catia
IPC分类号： C07D211/34
CPC分类号： C07D405/04 , C07D211/34 , C07D405/12
摘要： A compound of formula (I) wherein R represents a radical selected from i) ii) iii) iv) where the substituents R1, R2, R3, R4, R4, R 7 and the indices m, n and p are as defined in the description; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them 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：式（I）化合物，其中R表示选自i）ii）iii）iv）中的基团，其中取代基R 1，R 2，R 3，R 4，R 4，R 7和索引m，n和p如说明书中所定义 ; 或其药学上可接受的盐和溶剂合物; 其制备方法用于含有它们的药物组合物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。

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

WO2008113795A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008113795A1
公开(公告)日：2008-09-25
申请号：PCT/EP2008/053194
申请日：2008-03-18
申请人： GLAXO GROUP LIMITED , BERTHELEME, Nicolas , BRADLEY, Daniel, Marcus , CARDULLO, Francesca , MERLO, Giancarlo , POZZAN, Alfonso , SCOTT, Jaqueline, Sandra , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BERTHELEME, Nicolas , BRADLEY, Daniel, Marcus , CARDULLO, Francesca , MERLO, Giancarlo , POZZAN, Alfonso , SCOTT, Jaqueline, Sandra , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10 , A61K31/416 , A61P25/00 , C07D231/12 , C07D231/54 , C07D493/04
CPC分类号： C07D231/56 , C07D231/12 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10 , C07D493/04
摘要： Compound of formula (I) and salts thereof are provided: wherein A, R 1 , R, R 2 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中A，R 1，R 2，R 2如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

6. 发明申请

WO2010007032A1 PIPERIDINE BASED UREAS AS NK1 ANTAGONISTS 审中-公开
标题翻译：作为NK1拮抗剂的基于哌啶的UREAS
公开(公告)号：WO2010007032A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/058937
申请日：2009-07-13
申请人： GLAXO WELLCOME MANUFACTURING PTE LTD , ALVARO, Giuseppe , CARDULLO, Francesca , CASTIGLIONI, Emiliano
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , CASTIGLIONI, Emiliano
IPC分类号： C07D401/04 , A61K31/454 , A61P1/08 , A61P25/20 , A61P25/22 , A61P25/24
CPC分类号： C07D401/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein n is 1 or 2; useful in the treatment of conditions for which antagonism of NK1 receptor is beneficial.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中n为1或2; 可用于治疗NK1受体的拮抗作用有利的条件。

7. 发明申请

WO2010066658A1 COMPOUNDS WHICH POTENTIATE THE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：可能拮抗AMPA受体的化合物及其在医药中的应用
公开(公告)号：WO2010066658A1
公开(公告)日：2010-06-17
申请号：PCT/EP2009/066476
申请日：2009-12-07
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CARDULLO, Francesca , MARSHALL, Howard , MARZORATI, Paola , POZZAN, Alfonso , WARD, Simon, E
发明人： BRADLEY, Daniel, Marcus , CARDULLO, Francesca , MARSHALL, Howard , MARZORATI, Paola , POZZAN, Alfonso , WARD, Simon, E
IPC分类号： C07D207/26 , C07D213/63 , C07D213/74 , C07D231/12 , C07D233/58 , C07D471/04 , C07D495/04 , A61K31/4184 , A61P25/18
CPC分类号： C07D213/63 , C07D207/26 , C07D213/74 , C07D231/12 , C07D233/58 , C07D471/04 , C07D495/04
摘要： A compound of Formula (I) or a salt thereof are provided: wherein R is defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物或其盐：其中R在说明书中定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

8. 发明申请

WO2008092887A1 I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： I-OXA-3-AZASPIRO（4.5）Decan-2-ONE和1-OXA-3,8-DIAZASPIRO（4.5）Decan-2-ONE衍生物用于治疗排卵病
公开(公告)号：WO2008092887A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051110
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ 1 or nitrogen; Z 1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C 4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ 1 , compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
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合物，式（I）其中R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; W是-CZ 1 N或氮; Z 1是氢，C 1 -C 4烷基; A是可以被一个或多个卤素取代的5元杂芳基，吡嗪，嘧啶或喹啉或喹唑啉：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或可被一个或多个取代基取代的5-10元芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 条件是当W是-CZ 1时，式（I）的化合物具有反式立体化学; 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NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

9. 发明申请

WO2006087169A1 COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：可能的谷氨酸受体的化合物及其在医药中的应用
公开(公告)号：WO2006087169A1
公开(公告)日：2006-08-24
申请号：PCT/EP2006/001342
申请日：2006-02-13
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , ARISTA, Luca , CARDULLO, Francesca , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： ANDREOTTI, Daniele , ARISTA, Luca , CARDULLO, Francesca , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D213/61 , C07D213/42 , C07D317/58 , C07D333/20 , C07D213/65 , C07D277/64 , A61K31/4418 , A61K31/36 , A61K31/381 , A61K31/426 , A61P25/18
CPC分类号： C07D277/64 , C07D213/42 , C07D213/61 , C07D213/65 , C07D317/58 , C07D333/20
摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及通过式（I）的新化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

10. 发明申请

WO2009043883A1 AZABICYCLO [3. 1. O] 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：WO2009043883A1
公开(公告)日：2009-04-09
申请号：PCT/EP2008/063166
申请日：2008-10-01
申请人： Glaxo Group Limited , BERTANI, Barbara , CARDULLO, Francesca , DAMBRUOSO, Paolo , MARZORATI, Paola , MICHELI, Fabrizio , PASQUARELLO, Alessandra , SERI, Catia , TEDESCO, Giovanna
发明人： BERTANI, Barbara , CARDULLO, Francesca , DAMBRUOSO, Paolo , MARZORATI, Paola , MICHELI, Fabrizio , PASQUARELLO, Alessandra , SERI, Catia , TEDESCO, Giovanna
IPC分类号： C07D403/14 , C07D413/14 , C07D417/14 , C07D491/052 , A61K31/513 , A61P25/00
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R 1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be 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 , and n is 1 or 2; 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R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被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，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5，n为1或2; 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。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

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