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1. 发明公开

EP1102751A4 NOVEL BI- AND TRI-CYCLIC AZA COMPOUNDS AND THEIR USES 审中-公开
标题翻译：二和三环氮杂化合物和它们的应用
公开(公告)号：EP1102751A4
公开(公告)日：2005-06-22
申请号：EP99939698
申请日：1999-08-05
申请人： UNIV GEORGETOWN
发明人： KOZIKOWSKI ALAN P , SMITH MILES P
IPC分类号： C07D487/08 , A61K31/437 , A61K31/46 , A61P1/14 , A61P3/04 , A61P15/10 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D451/02 , C07D471/08 , C07D471/18 , C07D487/18 , C07D221/02 , C07D215/36 , C07D221/22 , C07D453/00 , C07D455/00 , C07D491/00 , C07D498/00 , C07D513/00
CPC分类号： C07D451/02 , C07D471/08

2. 发明授权

EP0266730B1 Esters of hexadydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and related compounds 失效
标题翻译：六氢-8-羟基-2,6-亚甲基-2H-喹嗪-3（4H） - 酮和相关化合物的酯。
公开(公告)号：EP0266730B1
公开(公告)日：1994-08-10
申请号：EP87116119.6
申请日：1987-11-02
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Gittos, Maurice Ward
IPC分类号： C07D455/00 , C07D471/18 , A61K31/445
CPC分类号： C07D471/18

3. 发明授权

EP2595966B1 SYNTHESIS OF CYCLOPENTAQUINAZOLINES 有权转让
公开(公告)号：EP2595966B1
公开(公告)日：2020-10-28
申请号：EP11809966.2
申请日：2011-07-15
申请人： BTG International Limited
发明人： KERSCHEN, James, Alan , BRIDGES, Alexander, James , DALZIEL, Sean, Mark , DAPREMONT, Olivier , KIM, Hyunjung , THOMPSON, Andrew, S. , ZELLER, James, Robert
IPC分类号： C07D239/70 , C07D455/00

4. 发明公开

EP2176226A1 METHOD FOR MAKING TETRABENAZINE COMPOUNDS 审中-公开
标题翻译：制备四氮杂苯胺化合物的方法
公开(公告)号：EP2176226A1
公开(公告)日：2010-04-21
申请号：EP08770100.9
申请日：2008-06-04
申请人： GENERAL ELECTRIC COMPANY
发明人： RISHEL, Michael James , AMARASINGHE, Kande Kankananamalage Dayarathna , DINN, Sean Richard , JOHNSON, Bruce Fletcher
IPC分类号： C07D217/00 , C07D217/24 , C07D455/00
CPC分类号： C07D455/06 , C07D217/16 , C07D217/18 , Y02P20/55
摘要： A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps of reacting a nucleophilic alkenyl species with aldehyde compound II and oxidizing the resultant allylic alcohol to provide enone III. The protecting group P1 on the tetrahydroisoquinoline nitrogen is removed and the resultant deprotected intermediate is induced to undergo an amino cyclization reaction to provide a product TBZ compound having structure I. The method may be used to prepare either enantiomeric form of tetrabenazine; (+)-tetrabenazine or (-)-tetrabenazine. Alternatively the method may be adapted to provide a mixture enriched in one tetrabenazine enantiomer, a racemic mixture, or a diastereomeric mixture of tetrabenazine compounds. In addition, the present invention provides novel synthetic intermediate compositions which may be used to prepare either or both enantiomers of tetrabenazine, derivatives of tetrabenazine, and analogs of tetrabenazine.
摘要翻译：制备具有结构I的丁苯那嗪化合物（TBZ化合物）的方法包括使亲核烯基物质与醛化合物II反应并氧化所得烯丙醇以提供烯酮III的步骤。除去四氢异喹啉氮上的保护基团P1，并将所得脱保护中间体进行氨基环化反应，得到具有结构I的产物TBZ化合物。该方法可用于制备丁苯那嗪的对映体形式; （+） - 丁苯那嗪或（ - ） - 丁苯那嗪。或者，该方法可适于提供富含一种丁苯那嗪对映异构体，外消旋混合物或丁苯那嗪化合物的非对映异构混合物的混合物。此外，本发明提供了新的合成中间体组合物，其可用于制备丁苯那嗪的任一种或两种对映体，丁苯那嗪的衍生物和丁苯那嗪的类似物。

5. 发明公开

EP0339669A1 Process for preparing indole-3-carboxylic acid esters of trans-hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one 失效
标题翻译： Verfahren zur Herstellung von Indol-3-carbonsäureesternvon trans-Hexahydro-8- hydroxy-2,6-methano-2H-chinolizin-3-（4H） - 。
公开(公告)号：EP0339669A1
公开(公告)日：1989-11-02
申请号：EP89107764.6
申请日：1989-04-28
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Anzeveno, Peter B.
IPC分类号： C07D455/00 , C07D471/18
CPC分类号： C07D455/00
摘要： The present invention describes a process for preparing indole-3-carboxylic acid esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one which comprises reacting 5-hydroxy-8-azatricyclo[5.3.1.0 3,8 ]undecan-10-one with the mixed anhydride of trifluoroacetic acid and an appropriate indole-3-carboxylic acid.
摘要翻译：本发明描述了制备六氢-8-羟基-2,6-亚甲基-2H-喹嗪啉-3（4H） - 酮的吲哚-3-羧酸酯的方法，该方法包括使5-羟基-8-氮杂三环[5.3 .1.0,3,8>]十一烷-10-酮与三氟乙酸的混合酸酐和合适的吲哚-3-羧酸反应。

6. 发明授权

EP1490361B1 POLYCYCLIC COMPOUNDS AS POTENT ALPHA2-ADRENOCEPTOR ANTAGONISTS 有权
标题翻译：多环化合物作为有效的α-2-肾上腺素受体拮抗剂
公开(公告)号：EP1490361B1
公开(公告)日：2007-10-03
申请号：EP03712185.2
申请日：2003-04-03
申请人： ORION CORPORATION
发明人： DIN BELLE, David , JOKELA, Reija , TOLVANEN, Arto , HAAPALINNA, Antti , KARJALAINEN, Arto , SALLINEN, Jukka , RATILAINEN, Jari
IPC分类号： C07D455/00 , C07D471/04 , C07D491/147 , C07D495/14 , A61K31/55 , A61K31/4375 , A61P3/06 , A61P3/10 , A61P9/02 , A61P15/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： C07D455/00 , A61K31/4375 , A61K31/55 , C07D471/14 , C07D491/14
摘要： The invention provides a compound of formula I, wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of alpha-2 adrenoceptors are indicated to be effective.

7. 发明公开

EP1490361A1 POLYCYCLIC COMPOUNDS AS POTENT ALPHA2-ADRENOCEPTOR ANTAGONISTS 有权
标题翻译：多环化合物作为有效的α-2-肾上腺素受体拮抗剂
公开(公告)号：EP1490361A1
公开(公告)日：2004-12-29
申请号：EP03712185.2
申请日：2003-04-03
申请人： ORION CORPORATION
发明人： DIN BELLE, David , JOKELA, Reija , TOLVANEN, Arto , HAAPALINNA, Antti , KARJALAINEN, Arto , SALLINEN, Jukka , RATILAINEN, Jari
IPC分类号： C07D455/00 , C07D471/04 , C07D491/147 , C07D495/14 , A61K31/55 , A61K31/4375 , A61P3/06 , A61P3/10 , A61P9/02 , A61P15/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： C07D455/00 , A61K31/4375 , A61K31/55 , C07D471/14 , C07D491/14
摘要： The invention provides a compound of formula I, wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of alpha-2 adrenoceptors are indicated to be effective.

8. 发明公开

EP1102751A1 NOVEL BI- AND TRI-CYCLIC AZA COMPOUNDS AND THEIR USES 审中-公开
标题翻译：二和三环氮杂化合物和它们的应用
公开(公告)号：EP1102751A1
公开(公告)日：2001-05-30
申请号：EP99939698.9
申请日：1999-08-05
申请人： Georgetown University
发明人： KOZIKOWSKI, Alan, P. , SMITH, Miles, P.
IPC分类号： C07D221/02 , C07D221/22 , C07D215/36 , C07D451/02 , C07D453/00 , C07D455/00 , C07D471/18 , C07D491/00 , C07D498/00 , C07D513/00
CPC分类号： C07D451/02 , C07D471/08
摘要： The present invention provides tropane-derived monoamine neurotransmitter re-uptake inhibitors which predictably exhibit selectivity for either the serotonin or dopamine transporter, pharmaceutical compositions thereof and methods for their use. The serotonin-selective re-uptake inhibitors are particularly useful for treating neurological disorders associated with the serotonergic neural system of the brain, such as depression, with significantly reduced side-effects. The dopamine-selective re-uptake inhibitors are particularly useful for treating disorders associated with dopamine re-uptake and/or acetylcholine release.

9. 发明公开

EP0266730A1 Esters of hexadydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and related compounds 失效
标题翻译：六氢-8-羟基-2,6-亚甲基-2H-二氢喹啉酮-3（4H） - 酯和Verbindungen酯。
公开(公告)号：EP0266730A1
公开(公告)日：1988-05-11
申请号：EP87116119.6
申请日：1987-11-02
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Gittos, Maurice Ward
IPC分类号： C07D455/00 , C07D471/18 , A61K31/445
CPC分类号： C07D471/18
摘要： The present invention is directed to a group of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3-(4H)-one and related compounds. The compounds are prepared from the appropriate carboxylic acids and alcohols by standard procedures or, where steric factors are significant, a new process which makes use of heavy metal salts of super acids can be used. The compounds involved are useful in the treatment of migraine and similar disorders and in cytotoxic drug-induced vomiting.
摘要翻译：本发明涉及一组六氢-8-羟基-2,6-亚甲基-2H-喹诺嗪-3（4H） - 酮及相关化合物的酯。这些化合物是通过标准方法由适当的羧酸和醇制备的，或者其中空间因素是显着的，可以使用利用超级酸的重金属盐的新方法。涉及的化合物可用于治疗偏头痛和类似疾病以及细胞毒性药物诱导的呕吐。

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