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1.发明公开NOVEL 2,3-BENZODIAZEPINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 有权“NEW 2,3-苯并二氮杂衍生物及其药物组合物含有这些化合物作为活性含有”
公开(公告)号：EP1351942A1
公开(公告)日：2003-10-15
申请号：EP01271364.0
申请日：2001-12-19
发明人： LING, István , BARKOCZY, Jozsef , SIMIG, Gyula , GREFF, Zoltán , RATKAI, Zoltán , SZABO, Géza , VEGH, Miklos , GIGLER, Gábor , SZENASI, Gábor , MARTONNE MARKO, Bernadett , LEVAY, György , HARSING, Lászlo, Gábor
IPC分类号： C07D243/02 , A61K31/551 , A61P25/00
CPC分类号： C07D243/02
摘要： The invention refers to novel 2,3-benzodiazepine derivatives of formula (I) and pharmaceutical compositions containing the same as the active ingredient. The novel compounds have antipasmodic, muscle relaxant and neuroprotective activities. In formula I; X represents a hydrogen atom, a chloro atom or a methoxy group; Y stands for a hydrogen atom or a halo atom; Z means a methyl group or a chloro atom; R is a C1-4 alkyl group or a group of the formula -NR1R2, wherein R?1 and R2¿ represent, independently, a hydrogen atom, a C¿1-4? alkyl group, a C1-4 alkoxy group or a C?3-6¿ cycloalkyl group.
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2.发明公开1,3-DIOXOLO/4,5-H//2,3/BENZODIAZEPINE DERIVATIVES AS AMPA/KAINATE RECEPTOR INHIBITORS 有权1-3二氧杂环戊烯/ 4.5-H // 2,3-苯并二氮杂衍生物作为AMPA /红藻氨酸受体抑制剂
公开(公告)号：EP1015457A1
公开(公告)日：2000-07-05
申请号：EP98939782.3
申请日：1998-08-07
发明人： BARKOCZY, Júzsef , CSELENYAK, Judit , RATKAI, Zoltán , SIMIG, Gyula , BALAZS, Lászlo , DOMAN, Imre , KOTAY NAGY, Péter , GREFF, Zoltán , SERES, Péter , SZABO, Géza , GACSALYI, István , GIGLER, Gábor , GYERTYAN, István , LEVAY, György , KOVACS, Attila , SIMO, Annamária , SZABADOS, Tamás , EGYED, András , VEGH, Miklos , TIHANYI, Károly
IPC分类号： C07D491/04 , A61K31/55
CPC分类号： C07D491/04
摘要： The invention refers to 1,3-dioxolo-/4,5-h//2,3/benzodiazepine derivatives of formula (I), a process for preparing these compounds and to pharmaceutical compositions containing these active substances, which are used to selectively inhibit Ampa/Kainate receptors.
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3.发明授权NOVEL 2,3-BENZODIAZEPINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 有权“NEW 2,3-苯并二氮杂衍生物及其药物组合物含有这些化合物作为活性含有”
公开(公告)号：EP1351942B1
公开(公告)日：2004-07-21
申请号：EP01271364.0
申请日：2001-12-19
发明人： LING, István , BARKOCZY, Jozsef , SIMIG, Gyula , GREFF, Zoltán , RATKAI, Zoltán , SZABO, Géza , VEGH, Miklos , GIGLER, Gábor , SZENASI, Gábor , MARTONNE MARKO, Bernadett , LEVAY, György , HARSING, Lászlo, Gábor
IPC分类号： C07D243/02 , A61K31/551 , A61P25/00
CPC分类号： C07D243/02
摘要： The invention refers to novel 2,3-benzodiazepine derivatives of formula (I) and pharmaceutical compositions containing the same as the active ingredient. The novel compounds have antipasmodic, muscle relaxant and neuroprotective activities. In formula I; X represents a hydrogen atom, a chloro atom or a methoxy group; Y stands for a hydrogen atom or a halo atom; Z means a methyl group or a chloro atom; R is a C1-4 alkyl group or a group of the formula -NR1R2, wherein R?1 and R2¿ represent, independently, a hydrogen atom, a C¿1-4? alkyl group, a C1-4 alkoxy group or a C?3-6¿ cycloalkyl group.
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4.发明公开POLYMORPHS OF A 1-PYRROLE DERIVATIVE, INTERMEDIATE FOR THE PREPARATION OF ATORVASTATIN 有权阿托伐他汀的多晶型物制备1-吡咯衍生物中间体的新形式
公开(公告)号：EP1430049A1
公开(公告)日：2004-06-23
申请号：EP02758667.6
申请日：2002-09-13
发明人： BARKOCZY, Júzsef , SIMIG, Gyula , GREFF, Zoltán , KOTAY NAGY, Péter , SZENT KIRALLYI, Zsuzsa , BARTHA, Ferenc , VERECZKEYNE DONATH, Györgyi , NAGY, Kálmán
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： The invention relates to new crystalline forms I and II of (4R-cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluoro-phenyl)-5-(1-methyl-ethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester of the Formula (I) and a process for the preparation thereof. The new polymorphs of the present invention are useful pharmaceutical intermediates which can be used in the preparation of the hydroxymethyl-glutaryl coenzyme (HMG- COA) reducing enzyme inhibitor having the INN (International Non-proprietory Name) atorvastatin.
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5.发明授权1,3-DIOXOLO/4,5-H//2,3/BENZODIAZEPINE DERIVATIVES AS AMPA/KAINATE RECEPTOR INHIBITORS 有权1-3二氧杂环戊烯/ 4.5-H // 2,3-苯并二氮杂衍生物作为AMPA /红藻氨酸受体抑制剂
公开(公告)号：EP1015457B1
公开(公告)日：2003-11-26
申请号：EP98939782.3
申请日：1998-08-07
发明人： BARKOCZY, Júzsef , CSELENYAK, Judit , RATKAI, Zoltán , SIMIG, Gyula , BALAZS, Lászlo , DOMAN, Imre , KOTAY NAGY, Péter , GREFF, Zoltán , SERES, Péter , SZABO, Géza , GACSALYI, István , GIGLER, Gábor , GYERTYAN, István , LEVAY, György , KOVACS, Attila , SIMO, Annamária , SZABADOS, Tamás , EGYED, András , VEGH, Miklos , TIHANYI, Károly
IPC分类号： C07D491/04 , A61K31/55
CPC分类号： C07D491/04
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公开(公告)号：EP1200442B8
公开(公告)日：2003-08-20
申请号：EP00944129.6
申请日：2000-07-04
发明人： GREFF, Zoltán , SZAB , Géza , BARK CZY, József , R TKAI, Zoltán , BLASK , Gábor , SIMIG, Gyula , GIGLER, Gábor , MARTONN MARK , Bernadett , L VAY, György , TIHANYI, Károly , EGYED, András , SIM , Annamária
IPC分类号： C07D491/04 , A61K31/551 , A61P25/00
CPC分类号： C07D491/04
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7.发明公开SALTS OF 2,2-DIMETHYL-1,3-DIOXANE INTERMEDIATES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开2,2-二甲基-1,3- DIOXANINTERMEDIATEN和方法盐类及其
公开(公告)号：EP1178980A1
公开(公告)日：2002-02-13
申请号：EP00927612.2
申请日：2000-05-05
发明人： KOTAY NAGY, Péter , GREFF, Zoltán , BARKOCZY, Jozsef , SIMIG, Gyula , BALAZS, Lászlo , DOMAN, Imre , RATKAI, Zoltán , SERES, Péter , BARTHA, Ferenc , VERECZKEYNE DONATH, Györgyi , NAGY, Kálmán
IPC分类号： C07D319/06
CPC分类号： C07D319/06
摘要： The invention relates to salts of (4R-cis) -(1,1-dimethyl -ethyl) -6-(2-aminoethyl) -2,2-dimethyl -1,3-dioxane -4-acetate of formula (I) formed with organic acids. The new salts according to the invention are stable and can be easily purified by recrystallization. The new salts of the invention are valuable pharmaceutical intermediates which can be used e.g. in the preparation of the hypolipidemic agent having the generic (INN) name atorvastatin. The invention further relates to the preparation of the new salts of the compound of formula (I).
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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
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.
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