公开(公告)号：EP2885286B1

公开(公告)日：2017-03-22

申请号：EP13748072.9

申请日：2013-08-13

申请人： Bayer Pharma Aktiengesellschaft

发明人： SIEGEL, Stephan ,  BÄURLE, Stefan ,  CLEVE, Arwed ,  HAENDLER, Bernard ,  FERNANDEZ-MONTALVAN, Amaury Ernesto ,  MÖNNING, Ursula ,  KRAUSE, Sabine ,  LEJEUNE, Pascale ,  SCHMEES, Norbert ,  BUSEMANN, Matthias ,  HOLTON, Simon ,  KUHNKE, Joachim

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/10 ,  C07D243/02 ,  A61K31/55 ,  A61P35/00 ,  A61P31/12

CPC分类号： C07D417/10 ,  A61K31/551 ,  A61K31/5513 ,  C07D243/02 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14

公开(公告)号：EP1660462B1

公开(公告)日：2008-11-19

申请号：EP04769081.3

申请日：2004-07-29

申请人： EGIS GYÓGYSZERGYÁR RT.

发明人： BARKOCZY, Jozsef ,  LING, István ,  SIMIG, Gyula ,  SZÉNÁSI, Gábor ,  GIGLER, Gábor ,  KERTÉSZ, Szabolcs ,  SZÜCS, Gyula ,  SZABÓ, Géza ,  VÉGH, Miklós ,  HÁRSING, László, Gábor

IPC分类号： C07D243/02

CPC分类号： C07D243/02

摘要： The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I),wherein R stands for a lower alkyl group or a group of the general formula -NH-R', wherein R' stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives.The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.

公开(公告)号：EP1761507A1

公开(公告)日：2007-03-14

申请号：EP05773249.7

申请日：2005-05-19

申请人： Greenpharma

发明人： BERNARD, Philippe

IPC分类号： C07D243/02 ,  A61K31/551 ,  A61P25/00

CPC分类号： C07D243/02

摘要： The invention especially relates to novel type 2,3-benzodiazepine stereospecific derivatives as inhibitors of phosphodiesterase, especially types 2 and 4, and to the applications thereof in the field of therapeutics, especially for the prevention and treatment of pathologies involving a central and/or peripheral disorder. The inventive compounds correspond especially to general formulae (I) and (II).

公开(公告)号：EP1537117B1

公开(公告)日：2007-01-17

申请号：EP03769564.0

申请日：2003-09-04

申请人： Aventis Pharma S.A.

发明人： MUSICKI, Branislav

IPC分类号： C07D487/08 ,  A61K31/4995 ,  A61P31/00 ,  C07D237/28 ,  C07D243/02

CPC分类号： C07D487/08 ,  C07D237/28 ,  C07D243/02

摘要： The invention concerns novel heterocyclic compounds of formula (1), and their salts with a base or an acid. The invention also concerns the method as well as the intermediates for preparing said compounds, and their use as medicines, in particular as anti-bacterial agents and beta-lactamase inhibitors.

公开(公告)号：EP1465879A2

公开(公告)日：2004-10-13

申请号：EP02781451.6

申请日：2002-12-12

申请人： EGIS GYOGYSZERGYAR RT.

发明人： MOLNARNE SAMU, Erika ,  SIMIG, Gyula ,  VAGO, Pál ,  GREFF, Zoltán

IPC分类号： C07D243/02 ,  C07D317/22 ,  C07D317/26

CPC分类号： C07D317/26 ,  C07C45/59 ,  C07C49/84 ,  C07D243/02 ,  C07D317/22

摘要： The invention relates to a new process for the preparation of 1-(3,4-dimethoxy-phenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodizepine of Formula (I) which comprises reacting a compound of general Formula (II) (wherein R1 and R2 independently each stands for C1-4-alkyl or together form C2-6-alkylene) with hydrazine or a hydrate or salt thereof formed with an inorganic or organic acid. 1-(3,4-dimethoxy-phenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine of the Formula I is a known anxiolytic agent. The invention also relates to new intermediates and a process for the preparation thereof.

公开(公告)号：EP0726257B1

公开(公告)日：2001-04-11

申请号：EP96101884.3

申请日：1996-02-09

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Vágo, Pál, Dr. ,  Reiter, Jozsef, Dr. ,  Gyertyán, István, Dr. ,  Gacsályi, Istvan ,  Bilkei-Gorzo, András, Dr. ,  Egyed, András, Dr. ,  Andrási, Ferenc, Dr. ,  Bakonyi, Anna, Dr. ,  Berzsensyi, Pál, Dr. ,  Botka, Péter ,  Hámori, Tamás, Dr. ,  Salamon Haskáné, Cecilia, Dr. ,  Horváth, Edit, Dr. ,  Horváth, Katalin, Dr. ,  Körösi, Jeno, Dr. ,  Máté, Györgyné, Dr. ,  Moravcsik, Imre ,  Szentkuti, Eszter, Dr. ,  Zolyomi, Gábor, Dr. ,  Blasko, Gábor, Dr. ,  Daroczi Kazoné, Klára ,  Simig, Gyula, Dr. ,  Tihanyi, Károly, Dr. ,  Bajnogel, Judit, Dr.

IPC分类号： C07D243/02 ,  C07D491/04 ,  C07D403/06 ,  C07D409/06 ,  C07D405/06 ,  A61K31/55 ,  C07D493/04

CPC分类号： C07D405/06 ,  C07D243/02 ,  C07D491/04 ,  C07D493/04

公开(公告)号：EP1062210A1

公开(公告)日：2000-12-27

申请号：EP99909935.1

申请日：1999-03-09

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： WANNAMAKER, Marion, W. ,  CHARIFSON, Paul ,  LAUFFER, David, J. ,  MULLICAN, Michael, D.

IPC分类号： C07D243/02 ,  A61K31/55 ,  C07D401/14 ,  C07D405/12 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D243/02 ,  C07D401/14 ,  C07D405/12

摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme ('ICE') inhibitors represented by formula (I), wherein Y is (a) or (b). This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-η production and methods for treating interleukin-1, apoptosis-, and interferon-η-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

公开(公告)号：EP0478195B1

公开(公告)日：1999-05-26

申请号：EP91308404.2

申请日：1991-09-13

申请人： ROHM AND HAAS COMPANY

发明人： Egan, Anne Ritchie ,  Michelotti, Enrique Luis ,  Ross, Ronald, Jr. ,  Wilson, Willie Joe

IPC分类号： C07D237/14 ,  C07D237/26 ,  C07D409/04 ,  C07D273/04 ,  C07D213/26 ,  C07D215/22 ,  C07D243/02 ,  C07D285/18 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06

CPC分类号： C07D213/64 ,  A01N43/40 ,  A01N43/42 ,  A01N43/54 ,  A01N43/58 ,  A01N43/60 ,  A01N43/62 ,  A01N43/653 ,  A01N43/80 ,  A01N43/82 ,  A01N43/88 ,  C07D213/85 ,  C07D215/227 ,  C07D231/12 ,  C07D233/56 ,  C07D237/04 ,  C07D237/18 ,  C07D237/26 ,  C07D237/32 ,  C07D237/36 ,  C07D239/36 ,  C07D243/02 ,  C07D249/08 ,  C07D273/04 ,  C07D285/34 ,  C07D401/04 ,  C07D403/04 ,  C07D405/06 ,  C07D405/10 ,  C07D409/04 ,  C07D409/06 ,  C07D413/06 ,  C07F7/0812

公开(公告)号：EP0726256A1

公开(公告)日：1996-08-14

申请号：EP96101883.5

申请日：1996-02-09

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Vágo, Pál, Dr. ,  Reiter, Jozsef, Dr. ,  Gyertyán, István, Dr. ,  Gigler, Gábor ,  Andrási, Ferenc, Dr. ,  Bakonyi, Anna, Dr. ,  Berzsensyi, Pál, Dr. ,  Botka, Péter ,  Birkás Faiglne, Erzsébet, Dr. ,  Hámori, Tamás, Dr. ,  Horváth, Edit, Dr. ,  Horváth, Katalin, Dr. ,  Korösi, Jeno, Dr. ,  Máté, Györgyné, Dr. ,  Moravcsik, Imre ,  Somogyi, Györgyi ,  Szentkuti, Eszter, Dr. ,  Zolyomi, Gábor, Dr.

IPC分类号： C07D243/02 ,  C07D491/04 ,  C07D405/06 ,  A61K31/55

CPC分类号： C07D405/06 ,  C07D243/02 ,  C07D491/04 ,  C07D493/04

摘要： 2,3-Benzodiazepine derivatives of general formula

wherein

R represents hydrogen or C 1-4 -alkanoyl,
R 1 stands for phenyl, optionally carrying 1 to 3 identical or different substituent(s) selected from the group consisting of halogen, nitro, amino, C 1-4 -alkylamino,(C 1-4 -alkyl)-amino, C 1-4 -alkanoylamino, C 1-4 -alkyl, C 1-4 -alkoxy, methylenedioxy and hydroxy; or naphthyl, optionally carrying a substituent selected from the group consisting of hydroxy, C 1-4 -alkyl and C 1-4 -alkoxy;
R 2 stands for hydrogen or C 1-4 -alkyl;
R 3 and R 4 independently represent C 1-4 -alkyl or
R 3 and R 4 together form methylene,
as well as acid addition salts and stereoisomers and mixtures thereof, and their use for preparing medicaments, particularly for the treatment of central nervous system disorders.

摘要翻译： 通式的2,3-苯并二氮杂衍生物 worinřdarstellt氢或C 1-4烷酰基，R 1代表苯基，任选地携带1至选自卤素，硝基中选择的3个相同或不同的取代基（多个）， 氨基，C 1-4烷基氨基，（C 1-4烷基）氨基，C 1-4烷酰基氨基，C1-4烷基，C1-4烷氧基，亚甲二氧基和羟基; 或萘基，任选带有选自羟基，C 1-4烷基和C 1-4烷氧基中选出的取代基; R2代表氢或C 1-4烷基; R3和R4代表unabhängigC 1-4烷基或R 3和R 4一起形成亚甲基，以及酸加成盐和立体异构和它们的混合物，以及它们用于制备药物，特别是用于中枢神经系统疾病的治疗中的用途。

公开(公告)号：EP0512419A1

公开(公告)日：1992-11-11

申请号：EP92107402.7

申请日：1992-05-04

申请人： EGIS GYOGYSZERGYAR

发明人： Somogyi, György ,  Botka, Péter ,  Hámori, Tamás, Dr. ,  Körösi, Jenó, Dr. ,  Kiss, Csilla ,  Bidlo née Iglói, Mária, Dr. ,  Balogh, Tibor, Dr. ,  Horváth, Gyula, Dr. ,  Simay, Antal, Dr. ,  Gyenge, Rózsa, Dr. ,  Moravcsik, Imre ,  Orbán, Ernö, Dr. ,  Uskert née Dievald, Emilia, Dr.

IPC分类号： C07D243/02

CPC分类号： C07D243/02

摘要： According to an aspect of the invention there is provided for a process for the preparation of 1-[3'-(chloro)-phenyl]-4-[methyl[-7,8-di-[methoxy]-5 H -2,3-benzodiazepine of formula

in high purity and in a quality suitable for pharmaceutical purposes by reacting 1 mole of 2-(acetonyl)-3'-(chloro)-4,5-di-(methoxy)-benzophenone of formula

with 3 to 7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents, at a temperature from 15°C to 85°C, and subsequently recrystallizing the crude product from an aliphatic alcohol containing 1 to 5 carbon atom(s), which is carried out in the absence of air oxygen.
According to another aspect of the invention there is provided for a process for preparing purified 1-[3'-(chloro)-phenyl]-4-[methyl]-7,8-di-[methoxy]-5 H -2,3-benzodiazepine of formula I from such containing contamination(s) of formula

and/or particularly formula

in which first the contaminated 1-[3'-(chloro)-phenyl]-4-[methyl]-7,8-di-[methoxy]-5 H -2,3-benzodiazepine of formula I is treated with a solvent and an alkali hydroxide, alkali carbonate or alkali alcoholate and thereafter the compound 1-[3'-(chloro)-phenyl]-4-[methyl]-7,8-di-[methoxy]-5 H -2,3-benzodiazepine of formula I is crystallized from the obtained solution.

摘要翻译： 根据本发明的一个方面，提供了制备1- [3' - （氯） - 苯基] -4- [甲基[-7,8-二 - [甲氧基] -5H- 具有高纯度和适合于药物目的的式的3-苯并二氮杂，其通过使1摩尔式（I）的2-（丙酮基）-3' - （氯）-4,5-二（甲氧基） - 二苯甲酮 ＆lt; CHEM＆gt;在有机溶剂或有机溶剂的混合物中，在15℃〜85℃的温度下，使用3〜7摩尔水合肼，然后从含有1〜5个碳原子的脂肪醇中重结晶粗产物 原子，其在不存在空气氧的情况下进行。 根据本发明的另一方面，提供了制备纯化的1- [3' - （氯） - 苯基] -4- [甲基] -7,8-二 - [甲氧基] -5H- 苯并二氮杂从这样的含有式CHEM的污染物和/或特别是式CHEM>中首先将被污染的1- [3' - （氯） - 苯基] -4- [甲基] -7 ，式I的8-二 - [甲氧基] -5H-2,3-苯并二氮杂用溶剂和碱金属氢氧化物，碱金属碳酸盐或碱性醇化物处理，然后将化合物1- [3' - （氯） - 苯基] 从所得溶液中结晶式I的4- [甲基] -7,8-二 - [甲氧基] -5H-2,3-苯并二氮杂。