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81. 发明授权

EP2606035B1 PROCES FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS 有权
标题翻译：合成取代尿素化合物的方法
公开(公告)号：EP2606035B1
公开(公告)日：2017-09-06
申请号：EP11749010.2
申请日：2011-07-28
申请人： BIAL - Portela & CA., S.A.
发明人： LEARMONTH, David Alexander , BROADBELT, Brian , WAHNON, Jorge Bruno Reis
IPC分类号： C07D233/90 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/12 , C07D405/14
CPC分类号： C07D233/90 , C07D233/60 , C07D233/61 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12

82. 发明授权

EP1907382B1 NITROCATECHOL DERIVATIVES AS COMT INHIBITORS 有权转让
标题翻译： NITROCATECHOL衍生物作为COMT抑制剂
公开(公告)号：EP1907382B1
公开(公告)日：2015-05-27
申请号：EP06769520.5
申请日：2006-07-26
申请人： Bial-Portela & CA, S.A.
发明人： LEARMONTH, David Alexander , KISS, Laszlo Erno , LEAL PALMA, Pedro Nuno , DOS SANTOS FERREIRA, Humberto , ARAÚJO SOARES DA SILVA, Patrício Manuel Vieira
IPC分类号： C07D413/04 , C07D413/14 , A61K31/421 , A61K31/4425 , A61K31/4439 , A61K31/506 , A61P25/00 , C07D417/14 , C07D413/06 , C07D401/04 , C07D213/89 , C07D407/04 , C07D271/06 , C07D271/10
CPC分类号： C07D413/14 , A61K31/4412 , C07D213/89 , C07D215/60 , C07D271/06 , C07D271/107 , C07D401/04 , C07D405/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04
摘要： New compounds of formula I are described: The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

83. 发明授权

EP2380575B1 Eslicarbazepine acetate and use 失效转让
标题翻译： Esclicarbazepin醋酸和使用
公开(公告)号：EP2380575B1
公开(公告)日：2015-02-25
申请号：EP11174415.7
申请日：2005-05-06
申请人： Bial-Portela & CA, S.A.
发明人： Vieira Araujo Soares Da Silva, Patrício Manuel , De Almeida, José Luís
IPC分类号： A61K31/55 , A61P29/00
CPC分类号： A61K31/55

84. 发明公开

EP2726454A2 PROCESS 失效
标题翻译：程序
公开(公告)号：EP2726454A2
公开(公告)日：2014-05-07
申请号：EP12738246.3
申请日：2012-06-29
申请人： Bial-Portela & CA, S.A.
发明人： BELIAEV, Alexander , WAHNON, Jorge Bruno Reis , LEARMONTH, David Alexander , MADEC, Jonathan , SCHNEIDER, Jean-Marie , MATON, William
IPC分类号： C07C311/19 , C07D403/04
CPC分类号： C07D405/04 , C07C235/80 , C07C311/16 , C07C311/17
摘要： The present invention relates to a process for preparing (R)-5-(2-(benzylamino)ethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione, and pharmaceutically acceptable salts thereof, especially the hydrochloride salt. The invention also relates to a process for making intermediates useful in the formation of said compound, and to the intermediates, per se.

85. 发明授权

EP2297042B1 CATALYTIC ASYMMETRIC HYDROGENATION 失效
标题翻译：不对称催化氢化反应
公开(公告)号：EP2297042B1
公开(公告)日：2013-07-10
申请号：EP09721339.1
申请日：2009-03-17
申请人： Bial-Portela & CA, S.A.
发明人： LEARMONTH, David Alexander , BELIAEV, Alexander , LI, Wenge
IPC分类号： C01G55/00 , C07D233/84 , C07D311/74 , C07D335/06 , C07D407/04 , C07D409/04
CPC分类号： C07D311/04 , C07D405/04 , C07F15/0053 , C07F15/008

86. 发明公开

EP2475357A1 ORAL SUSPENSION FORMULATIONS OF ESCLICARBAZEPINE ACETATE 审中-公开
标题翻译：奥兰多悬挂式安全防护罩
公开(公告)号：EP2475357A1
公开(公告)日：2012-07-18
申请号：EP10757859.3
申请日：2010-09-10
申请人： Bial-Portela & CA, S.A.
发明人： VASCONCELOS, Teófilo Cardoso de , SANTOS LIMA, Ricardo Jorge dos , CAMPOS COSTA, Rui Cerdeira de , COSTA BARROCAS, Pedro Miguel da , CASTRO PEREIRA, Lígia Sofia de
IPC分类号： A61K9/10 , A61K31/55 , A61K47/14 , A61K47/26 , A61K47/36
CPC分类号： A61K31/55 , A61K9/10
摘要： An oral suspension formulation comprising eslicarbazepine acetate and a pharmaceutically acceptable liquid vehicle.
摘要翻译：一种口服悬浮液制剂，其包含乙酸西酞西泮和药学上可接受的液体载体。

87. 发明公开

EP2413913A2 PHARMACEUTICAL FORMULATIONS COMPRISING NITROCATECHOL DERIVATIVES AND METHODS OF MAKING THE SAME 有权
标题翻译：含有硝基去氧醇衍生物的药物制剂及其制备方法
公开(公告)号：EP2413913A2
公开(公告)日：2012-02-08
申请号：EP10714386.9
申请日：2010-03-31
申请人： Bial-Portela & CA, S.A.
发明人： VASCONCELOS, Teófilo Cardoso de , LIMA, Ricardo Jorge dos Santos , BARROCAS, Pedro Miguel da Costa , PEREIRA, Lígia Sofia de Castro , COSTA, Rui Cerdeira de Campos
IPC分类号： A61K9/16 , A61K31/00 , A61K9/48
CPC分类号： A61K9/1623 , A61K9/4858 , A61K31/4439
摘要： The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and other derivatives thereof and methods of making the same.
摘要翻译：本公开涉及包含至少一种选自如本文定义的式I的硝基儿茶酚衍生物和其盐，酯，水合物，溶剂合物和其它衍生物的活性药物成分及其制备方法的组合物和药物制剂。

88. 发明公开

EP2386303A1 Eslicarbazepine acetate and methods of use 审中-公开
标题翻译： Esclicarbazepin-Acetat和Verwendungsverfahren
公开(公告)号：EP2386303A1
公开(公告)日：2011-11-16
申请号：EP11174413.2
申请日：2005-05-06
申请人： Bial-Portela & CA, S.A.
发明人： Vieira Araujo Soares Da Silva, Patrício Manuel , De Almeida, José Luís
IPC分类号： A61K31/55 , A61P25/06
CPC分类号： A61K31/55
摘要： The present disclosure relates to the treatment of migraine with eslicarbazepine acetate. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate.
摘要翻译：本公开涉及用醋酸西酞替啶治疗偏头痛。本公开还涉及制备包含醋酸巴西平的药物组合物的方法。

89. 发明授权

EP1915346B1 ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE 无效转让
标题翻译：奥卡西平不对称催化还原
公开(公告)号：EP1915346B1
公开(公告)日：2011-08-17
申请号：EP06726863.1
申请日：2006-04-21
申请人： Bial-Portela & CA, S.A.
发明人： LEARMONTH, David, Alexander , GRASA, Gabriela, Alexandra , ZANOTTI-GEROSA, Antonio
IPC分类号： C07D223/22
CPC分类号： C07D223/28 , A61K31/55 , C07D223/22
摘要： A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

90. 发明公开

EP2319836A1 Asymmetric catalytic reduction of oxcarbazepine 有权
标题翻译：不对称性卡塔西泮
公开(公告)号：EP2319836A1
公开(公告)日：2011-05-11
申请号：EP11152286.8
申请日：2006-04-21
申请人： Bial-Portela & CA, S.A.
发明人： Learmonth, David Alexander , Grasa, Gabriela Alexandra , Zanotti-Gerosa, Antonio
IPC分类号： C07D223/22
CPC分类号： C07D223/28 , A61K31/55 , C07D223/22
摘要： A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B):

wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
摘要翻译：制备（S） - （+） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺或（R） - （ - ） - 10,11-二氢 - 公开了在催化剂和氢化物源的存在下还原奥卡西平，10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺。催化剂由[RuX 2（L）] 2（其中X是氯，溴或碘）和L是芳基或芳基 - 脂族配体与式（A）或式（B）的配体组合制备：其中R 1选自C 1-6烷氧基和C 1-6烷基，n为0至5的数，当n为2至5的数时，R 1可以相同或不同，并且R 2 是烷基，取代的烷基，芳基，取代的芳基，烷芳基或取代的烷芳基。氢化物源是NR 3 R 4 R 5和甲酸，[R 3 R 4 R 5 NH] [OOCH]和任选的甲酸或[M] [OOCH] x和甲酸，其中R 3，R 4 R 5为C 1-6烷基，M为碱金属或碱土金属，x为1或2.在此过程中，维持6.5至8的pH。

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