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1. 发明申请

WO2012098400A1 PIPERAZINE DERIVATIVES AS CAV2.2 CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：作为CAV2.2钙通道阻断剂的哌嗪衍生物
公开(公告)号：WO2012098400A1
公开(公告)日：2012-07-26
申请号：PCT/GB2012/050111
申请日：2012-01-19
申请人： CONVERGENCE PHARMACEUTICALS LIMITED , NORTON, David , ANDREOTTI, Daniele , WARD, Simon E , PROFETA, Roberto , SPADA, Simone , PRICE, Helen Susanne
发明人： NORTON, David , ANDREOTTI, Daniele , WARD, Simon E , PROFETA, Roberto , SPADA, Simone , PRICE, Helen Susanne
IPC分类号： C07D487/14 , A61K31/4985 , A61P3/14
CPC分类号： C07D471/14 , C07D487/14
摘要： The invention relates to novel piperazine compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca v 2.2 calcium channels is beneficial, i.e. in particular to treat pain.
摘要翻译：本发明涉及新型哌嗪化合物; 进行准备; 含有该化合物的药物组合物; 以及在治疗中使用化合物治疗阻断Cav2.2钙通道的疾病是有益的，即特别是治疗疼痛。

2. 发明申请

WO2009056520A1 AZABICYCLO[3.2.1]OCTANE DERIVATIVES 审中-公开
标题翻译： AZABICYCLO [3.2.1] OCTANE DERIVATIVES
公开(公告)号：WO2009056520A1
公开(公告)日：2009-05-07
申请号：PCT/EP2008/064529
申请日：2008-10-27
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , PROFETA, Roberto
发明人： ANDREOTTI, Daniele , PROFETA, Roberto
IPC分类号： C07D221/22
CPC分类号： C07D221/22
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A or W, wherein A is formula (IA) wherein p is 0, 1, 2, 3, 4 or 5 and R 5 is halogen, cyano or C 1-4 alkyl, each of them being the same or different; and W is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 5 , each of them being the same or different; R 3 is a group (P) wherein R 6 is selected from the group consisting of hydrogen, C 1-4 alkyl, haloC 1-4 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl, and n is 1 or 2; R4 is hydrogen, linear or branched C 1-4 alkyl, hydroxyl or C 1-4 alkoxy; 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，溶剂合物或前药，其中R 1是氢或C 1-4烷基; R2是A或W基团，其中A是式（IA），其中p是0,1,2,3,4或5，R 5是卤素，氰基或C 1-4烷基，它们各自相同或不同; 并且W是一个或者萘基，任选地被1或2个基团R 5取代，它们各自相同或不同; R3是一个基团（P），其中R6选自氢，C1-4烷基，卤代C 1-4烷基，C 3-6环烷基和C 3-6环烷基C 1-3烷基，n是1或2; R4是氢，直链或支链C 1-4烷基，羟基或C 1-4烷氧基; 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。

3. 发明申请

WO2007042239A1 PROLINAMIDE DERIVATIVES AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：丙酰胺衍生物作为钠通道调节剂
公开(公告)号：WO2007042239A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009731
申请日：2006-10-06
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , BERGAUER, Markus , GIOVANNINI, Riccardo , PROFETA, Roberto
发明人： ALVARO, Giuseppe , BERGAUER, Markus , GIOVANNINI, Riccardo , PROFETA, Roberto
IPC分类号： C07D207/22 , A61K31/401 , A61P25/24
CPC分类号： C07D207/22
摘要： The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
摘要翻译：本发明提供式（I）化合物，其溶剂合物，盐或前药，其可用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。

4. 发明申请

WO2007042240A1 QUATERNARY ALPHA-AMINOCARBOXAMIDE DERIVATIVES AS MODULATORS OF VOLTAGE-GATED SODIUM CHANNELS 审中-公开
标题翻译：作为电压门控通道的调节剂的季铵 - 氨基甲酰胺衍生物
公开(公告)号：WO2007042240A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009732
申请日：2006-10-06
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , BERGAUER, Markus , BONETTI, Francesca , PROFETA, Roberto
发明人： ALVARO, Giuseppe , AMANTINI, David , BERGAUER, Markus , BONETTI, Francesca , PROFETA, Roberto
IPC分类号： C07D207/16 , C07D487/10 , C07D471/10 , A61K31/40 , A61K31/407 , A61K31/435 , A61P23/00 , A61P29/00 , A61P25/08
CPC分类号： C07D207/16 , C07D471/10 , C07D487/10
摘要： The invention relates to quaternary α-aminocarboxyamide derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.
摘要翻译：本发明涉及式（I）的季α-氨基羧酰胺衍生物，其中R 1，R 2，R 3，R 3， 4，R 5，R 6，X，q和n如权利要求1中所定义，用于治疗由电压门控的调制介导的疾病和病症钠通道。

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