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1.发明公开PROCESS FOR THE PREPARATION OF AMORPHOUS FORM OF A PLATELET AGGREGATION INHIBITOR DRUG 审中-公开制造方法血小板聚集阻燃产品的无定形形式
公开(公告)号：EP1648903A2
公开(公告)日：2006-04-26
申请号：EP04743728.0
申请日：2004-06-30
发明人： KOTAY NAGY, Péter , SIMIG, Gyula , BARKOCZY, József , GREGOR, Tamás , FARKAS, Béla , VERECZKEYN DONATH, Györgyi , NAGY, Kálmán , KÖRTVELYESSY, Gyuláné , SZENT-KIRALLYI, Zsuzsanna
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02
CPC分类号： C07D495/04
摘要： The present invention relates to a new method of preparation of the polymorph form 1 of methyl (S)-(+)-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridine-5-yl-acetate hydrogensulfate of the formula (I).
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2.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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3.发明公开SUBSTITUTED ALKYL-PYRIDAZINONES FOR THE TREATMENT OF MEMORY AND LEARNING MALFUNCTIONS 审中-公开取代的烷基哒嗪酮对记忆和学习的薄弱环节处理
公开(公告)号：EP1567159A1
公开(公告)日：2005-08-31
申请号：EP03777020.3
申请日：2003-11-13
发明人： LEVAY, György , GACSALYI, István , MARKO, Bernadett , SCHMIDT,Eva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLOSNE KOVACS, Anikó , SZENASI, Gábor , WELLMANN, János , HARSING, László Gábor , BARKOCZY, József , SIMIG, Gyula , KOTAY NAGY, Péter
IPC分类号： A61K31/501 , A61P25/28
CPC分类号： A61K31/501
摘要： The compounds of the general Formula I, wherein R1 stands for hydrogen or lower alkyl; one of symbols X and Y stands for hydrogen or halogen and the other represents a group of the general Formula II, R2 is hydrogen or lower alkyl; n is 1, 2 or 3; R3 is hydrogen, lower alkyl or aryl-lower alkyl; Z is -0-; or R3 and Z together with the intermediate atoms form a piperazino ring; Q and W independently from each other stands for -CH= or -N=; and R4, R5 and R6 can be the same or different and stand for hydrogen, halogen, trifluoromethyl or lower alkoxy; or R4 and R5 together form an ethylenedioxy group) and pharmaceutically acceptable salts thereof can be used for the treatment or prophylaxis of malfunctions of memory and/or cognitive decline or prevention of decline of learning abilities.
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4.发明授权SUBSTITUTED ALKYLAMINOPYRIDAZINONE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权取代的烷基氨基哒嗪酮衍生物，其制备方法和含有该化合物的药物组合物
公开(公告)号：EP1430047B1
公开(公告)日：2005-02-09
申请号：EP02762620.9
申请日：2002-09-26
发明人： BARKOCZY, Júzsef , SIMIG, Gyula , KOTAY NAGY, Péter , LEVAY, György , GACSALYI, István , MARTONNE MARKO, Bernadett , SCHMIDT, Eva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLOSNE KOVACS, Anikú , SZENASI, Gábor , WELLMANN, János , HARSING, Lászlú, Gábor
IPC分类号： C07D401/12 , A61K31/50 , A61P25/22 , A61P25/28
CPC分类号： C07D401/12 , C07D237/22 , C07D403/12 , C07D405/12
摘要： The invention relates to new substituted alkylaminopyridazinone derivatives of the general Formula (I), (wherein R1 is hydrogen or alkyl having 1-4 carbon atoms; one of X and Y stands for hydrogen or halogen and the other represents a group of the general Formula (II), R2 is hydrogen or alkyl having 1-4 carbon atoms; n is 1, 2 or 3; R3 stands for hydrogen, alkyl having 1-4 carbon atoms or aryl-(C1-4 alkyl); Z stands for oxygen; or R3 and Z together with the groups placed between them form a piperazine ring; and R4 stands for hydrogen, halogen, trifluoromethyl or alkoxy having 1-4 carbon atoms) and pharmaceutically acceptable acid addition salts thereof. The invention compounds are useful in the treatment of anxiolytic conditions and cognitive disorders.
摘要翻译： 本发明涉及通式（I）的新的取代的烷基氨基哒嗪酮衍生物，其中R 1是氢或具有1-4个碳原子的烷基; X和Y中的一个代表氢或卤素，另一个代表通式 （II）中，R2是氢或具有1-4个碳原子的烷基; n是1,2或3; R3代表氢，具有1-4个碳原子的烷基或芳基 - （C1-4烷基）; Z代表氧 ;或者R3和Z与它们之间的基团一起形成哌嗪环; R4代表氢，卤素，三氟甲基或具有1-4个碳原子的烷氧基）及其药学上可接受的酸加成盐。 本发明化合物可用于治疗抗焦虑症和认知障碍。
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5.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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6.发明公开SUBSTITUTED ALKYLAMINOPYRIDAZINONE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权取代ALKYLAMINOPYRIDAZINONDERIVATE，其制造方法SAME和药物制剂
公开(公告)号：EP1430047A1
公开(公告)日：2004-06-23
申请号：EP02762620.9
申请日：2002-09-26
发明人： BARKOCZY, Júzsef , SIMIG, Gyula , KOTAY NAGY, Péter , LEVAY, György , GACSALYI, István , MARTONNE MARKO, Bernadett , SCHMIDT, Eva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLOSNE KOVACS, Anikú , SZENASI, Gábor , WELLMANN, János , HARSING, Lászlú, Gábor
IPC分类号： C07D401/12 , A61K31/50 , A61P25/22 , A61P25/28
CPC分类号： C07D401/12 , C07D237/22 , C07D403/12 , C07D405/12
摘要： The invention relates to new substituted alkylaminopyridazinone derivatives of the general Formula (I), (wherein R1 is hydrogen or alkyl having 1-4 carbon atoms; one of X and Y stands for hydrogen or halogen and the other represents a group of the general Formula (II), R2 is hydrogen or alkyl having 1-4 carbon atoms; n is 1, 2 or 3; R3 stands for hydrogen, alkyl having 1-4 carbon atoms or aryl-(C1-4 alkyl); Z stands for oxygen; or R3 and Z together with the groups placed between them form a piperazine ring; and R4 stands for hydrogen, halogen, trifluoromethyl or alkoxy having 1-4 carbon atoms) and pharmaceutically acceptable acid addition salts thereof. The invention compounds are useful in the treatment of anxiolytic conditions and cognitive disorders.
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7.发明公开
公开(公告)号：EP1417206A1
公开(公告)日：2004-05-12
申请号：EP02755381.7
申请日：2002-07-24
发明人： BARKOCZY, Jozsef , KOTAY NAGY, Péter , SIMIG, Gyula , LEVAY, György , GACSALYI, István , EGYED, András , RACZNE BAJNOGEL, Judit , PALLAGI, Katalin , SCHMIDT, Eva , SZENASI, Gábor , MIKLOSNE KOVACS, Aniko , WELLMANN, János
IPC分类号： C07D413/14 , A61K31/50
CPC分类号： C07D413/14
摘要： The invention refers to novel 2H-pyridazine-3-one derivatives of the formula I, pharmaceutical compositions containing the same and a process for the preparation of the active ingredient. The novel compounds possess neuroleptic effect and can be used, primarily, for the treatment of schizophrenia. In formula I, R stands for a hydrogen atom or a C1-4 alkyl group, X and Y represent, independently, a hydrogen atom, a halogen atom or a group of the formula II, with the proviso that one of X and Y means always a group of the formula II, and then the other one stands for a hydrogen atom or a halogen atom, wherein in formula II n has a value of 1 or 2.
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8.发明公开POLYMORPH SALT OF A PYRIDAZINONE DERIVATIVE FOR THE TREATMENT OF ARRHYTHMIA 审中-公开甲哒嗪酮衍生物，用于治疗心律失常多态性SALT
公开(公告)号：EP1417179A1
公开(公告)日：2004-05-12
申请号：EP02755384.1
申请日：2002-07-26
IPC分类号： C07D237/22 , A61K31/50
CPC分类号： C07D237/22
摘要： The invention relates to the new crystalline form I 5-chloro-4-[3-[N-[2-(3,4-dimethoxy-phenyl)-ethyl]-N-methylamino]-propylamino]-3-[2H]-pyridazinone fumarate, a process for the preparation thereof, pharmaceutical compositions containing the same and the use of said new polymorph for the treatment of arrhythmia.
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9.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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10.发明公开
公开(公告)号：EP1644381A1
公开(公告)日：2006-04-12
申请号：EP04743729.8
申请日：2004-06-30
发明人： KOTAY NAGY, Péter , SIMIG, Gyula , BARKOCZY, József , GREGOR, Tamás , FARKAS, Béla , VERECZKEYNE DONATH, Györgyi , NAGY, Kálmán , KÖRTVELYESSY, Gyuláné , SZENT-KIRALLYI, Zsuzsanna
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to a new method of preparation of the polymorph form 1 of methyl (S)-(+)-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridine-5-yl-acetate hydrogensulfate of the formula (I).
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