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1. 发明申请

WO2004043465A1 SUBSTITUTED ALKYL-PYRIDAZINONES FOR THE TREATMENT OF MEMORY AND LEARNING MALFUNCTIONS 审中-公开
标题翻译：用于治疗记忆和学习功能障碍的替代性阿奇霉素
公开(公告)号：WO2004043465A1
公开(公告)日：2004-05-27
申请号：PCT/HU2003/000096
申请日：2003-11-13
申请人： EGIS GYÓGYSZERGYÁR RT. , LÉVAY, György , GACSÁLYI, István , MARKÓ, Bernadett , SCHMIDT, Éva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLÓSNÉ KOVÁCS, Anikó , SZÉNÁSI, Gábor , WELLMANN, János , HÁRSING, László Gábor , BARKÓCZY, József , SIMIG, Gyula , KÓTAY NAGY, Péter
发明人： LÉVAY, György , GACSÁLYI, István , MARKÓ, Bernadett , SCHMIDT, Éva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLÓSNÉ KOVÁCS, Anikó , SZÉNÁSI, Gábor , WELLMANN, János , HÁRSING, László Gábor , BARKÓCZY, József , SIMIG, Gyula , KÓTAY NAGY, Péter
IPC分类号： A61K31/501
CPC分类号： A61K31/501
摘要： The compounds of the general Formula I, wherein R 1 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, R 2 is hydrogen or lower alkyl; n is 1, 2 or 3; R 3 is hydrogen, lower alkyl or aryl-lower alkyl; Z is -0-; or R 3 and Z together with the intermediate atoms form a piperazino ring; Q and W independently from each other stands for -CH= or -N=; and R 4 , R 5 and R 6 can be the same or different and stand for hydrogen, halogen, trifluoromethyl or lower alkoxy; or R 4 and R 5 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.
摘要翻译：通式I的化合物，其中R 1代表氢或低级烷基; 符号X和Y之一代表氢或卤素，另一个表示通式II的基团，R 2是氢或低级烷基; n为1,2或3; R 3是氢，低级烷基或芳基 - 低级烷基; Z为-0-; 或R 3和Z与中间原子一起形成哌嗪子基环; Q和W彼此独立地代表-CH =或-N =; R 4，R 5和R 6可以相同或不同，代表氢，卤素，三氟甲基或低级烷氧基; 或R 4和R 5一起形成亚乙二氧基）及其药学上可接受的盐可用于治疗或预防记忆功能障碍和/或认知衰退或预防学习能力下降。

2. 发明申请

WO2003027078A1 SUBSTITUTED ALKYLAMINOPYRIDAZINONE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：取代的烷基氨基吡啶酮衍生物，其制备方法和含有该衍生物的药物组合物
公开(公告)号：WO2003027078A1
公开(公告)日：2003-04-03
申请号：PCT/HU2002/000097
申请日：2002-09-26
申请人： EGIS GYÓGYSZERGYÁR RT. , BARKÓCZY, József , SIMIG, Gyula , KÓTAY NAGY, Péter , LÉVAY, György , GACSÁLYI, István , MARTONNÉ MARKÓ, Bernadett , SCHMIDT, Éva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLÓSNÉ KOVÁCS, Anikó , SZÉNÁSI, Gábor , WELLMANN, János , HÁRSING, László Gábor
发明人： BARKÓCZY, József , SIMIG, Gyula , KÓTAY NAGY, Péter , LÉVAY, György , GACSÁLYI, István , MARTONNÉ MARKÓ, Bernadett , SCHMIDT, Éva , EGYED, András , KOMPAGNE, Hajnalka , LEVELEKI, Csilla , MIKLÓSNÉ KOVÁCS, Anikó , SZÉNÁSI, Gábor , WELLMANN, János , HÁRSING, László Gábor
IPC分类号： C07D237/22
CPC分类号： C07D401/12 , C07D237/22 , C07D403/12 , C07D405/12
摘要： New substituted alkylaminopyridazinone derivatives of the general Formula (I), (wherein R 1 is hydrogen or alkyl having 1-4 carbon atoms; X is hydrogen or halogen; R 2 is hydrogen or alkyl having 1-4 carbon atoms; n is 1, 2 or 3; Q and W independently from each other stand for -N= or -CH=; and R 4 and R 5 independently from each other represent hydrogen, halogen, trifluoromethyl or alkoxy having 1-4 carbon atoms) and pharmaceutically acceptable acid addition salts thereof possess useful anxiolytic and cognition enhancing properties.
摘要翻译：新的取代的通式（I）的烷基氨基哒嗪酮衍生物，其中R1是氢或具有1-4个碳原子的烷基; X是氢或卤素; R2是氢或具有1-4个碳原子的烷基; n是1,2或 3; Q和W彼此独立地代表-N =或-CH =;且R4和R5彼此独立地表示氢，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，具有有用的抗焦虑和认知增强特性。

3. 发明申请

WO2005109987A3 3-(((4-PHENYL)-PIPERAZINE-1-YL)-ALKYL)-3-ALKYL-1, 3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
公开(公告)号：WO2005109987A3
公开(公告)日：2005-11-24
申请号：PCT/HU2005/000052
申请日：2005-05-11
申请人： EGIS GYÓGYSZERGYÁR RT. , VOLK, Balázs , BARKÓCZY, József , SIMIG, Gyula , MEZEI, Tibor , KAPILLERNÉ DEZSŐFI, Rita , FLÓRIAN, Endréné , GACSÁLYI, István , PALLAGI, Katalin , GIGLER, Gábor , LÉVAY, György , MÓRICZ, Krisztina , LEVELEKI, Csilla , SZIRAY, Nóra , SZÉNÁSI, Gábor , EGYED, András , HÁRSING, László Gábor
发明人： VOLK, Balázs , BARKÓCZY, József , SIMIG, Gyula , MEZEI, Tibor , KAPILLERNÉ DEZSŐFI, Rita , FLÓRIAN, Endréné , GACSÁLYI, István , PALLAGI, Katalin , GIGLER, Gábor , LÉVAY, György , MÓRICZ, Krisztina , LEVELEKI, Csilla , SZIRAY, Nóra , SZÉNÁSI, Gábor , EGYED, András , HÁRSING, László Gábor
IPC分类号： C07D209/34 , C07D401/12 , C07D403/12 , A61K31/4045 , A61K31/4458 , A61K31/506 , A61P25/24
摘要： The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R 1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R 2 represents hydrogen or halogen; R 3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R 4 stands for alkyl having 1-7 carbon atom(s); R 5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R 6 , R 7 and R 8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R 6 and R 7 together represent ethylenedioxy; m is 0, 1, or 2; a is a single, double or triple bond; n is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof which are useful in the treatment or prophylaxis of diseases of the central nervous system, the gastrointestinal system and the cardiovascular system.

4. 发明申请

WO2010089616A1 OPTICALLY ACTIVE 3-[(PHENYLPIPERAZIN-1-YL)ALKYL]-3- ALKYL-OXINDOLE DERIVATIVES HAVING CNS ACTIVITY 审中-公开
标题翻译：具有CNS活性的3 - [（苯基哌嗪-1-基）烷基] -3-烷氧基衍生物的光学活性
公开(公告)号：WO2010089616A1
公开(公告)日：2010-08-12
申请号：PCT/HU2010/000014
申请日：2010-02-05
申请人： EGIS GYÓGYSZERGYÁR NYILVÁNOSAN MŰKÖDŐ RÉSZVÉNYTÁRSASÁG , VOLK, Balázs , BARKÓCZY, József , GACSALYI, István , FOGASSY, Elemér , SCHINDLER, József , GIGLER, Gábor , KOMPAGNE, Hajnalka , NAGYNÉ GYÖNÖS, Ildikó , PALLAGI, Katalin , PORCS-MAKKAY, Márta , SZÉNÁSI, Gábor , MEZEI, Tibor , LUKÁCS, Gyula , LÉVAY, György , EGYED, András , HÁRSING, László Gábor
发明人： VOLK, Balázs , BARKÓCZY, József , GACSALYI, István , FOGASSY, Elemér , SCHINDLER, József , GIGLER, Gábor , KOMPAGNE, Hajnalka , NAGYNÉ GYÖNÖS, Ildikó , PALLAGI, Katalin , PORCS-MAKKAY, Márta , SZÉNÁSI, Gábor , MEZEI, Tibor , LUKÁCS, Gyula , LÉVAY, György , EGYED, András , HÁRSING, László Gábor
IPC分类号： C07D209/34 , A61K31/4045 , A61P25/18
CPC分类号： C07D209/34
摘要： The present invention relates to the enantiomers of 5,7-dichloro-3-{4-[4-(4- chlorophenyl)-piperazin-1-yl]butyl} -3-ethyl- 1,3-dihydro-2H-indol-2-one of the Formula (II) pharmaceutically acceptable salts thereof, process for the preparation thereof, medicinal products containing said enantiomers and the use thereof and their pharmaceutically acceptable salts in the treatment of the disorders of the central nervous system.
摘要翻译：本发明涉及5,7-二氯-3- {4- [4-（4-氯苯基） - 哌嗪-1-基]丁基} -3-乙基-1,3-二氢-2H-吲哚的对映异构体其中式（II）的药学上可接受的盐，其制备方法，含有所述对映异构体的药物及其用途及其药学上可接受的盐在治疗中枢神经系统疾病中的用途。

5. 发明申请

WO2008146063A1 NEW BENZOFURAN DERIVATIVES AS SELECTIVE 5HT6 RECEPTOR INHIBITORS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：作为选择性5HT6受体抑制剂的新型苯并呋喃衍生物及其制备方法
公开(公告)号：WO2008146063A1
公开(公告)日：2008-12-04
申请号：PCT/HU2008/000060
申请日：2008-05-30
申请人： EGIS GYÓGYSZERGYÁR Nyilvánosan Müködö Részvénytársagág , RIVÓ, Endre , PRAUDA, Ibolya , REITER, József , BARKÓCZY, József , GACSÁLYI, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
发明人： RIVÓ, Endre , PRAUDA, Ibolya , REITER, József , BARKÓCZY, József , GACSÁLYI, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
IPC分类号： A61K31/343 , A61K31/496 , C07D307/83 , C07D405/12 , A61P9/00 , A61P25/00
CPC分类号： C07D307/86
摘要： The present invention relates to new selective 5HT 6 receptor binding benzofuran derivatives of general formula (I) wherein, Z represents a hydrogen atom, C 1-4 acyl group, C 1-6 alkyl sulfonyl group, phenyl sulfonyl group substituted with one or more halogen atom; or naphthyl sulfonyl group optionally substituted with a halogen atom, tetrahydro naphthyl sulfonyl group, (lS)(+)-10-camphor-sulfonyl group, (lR)(-)-10-camphor-sulfonyl group or benzofuranyl sulfonyl group, substituted with a halogen atom and C 1 -4 alkyl group, Y represents C 2-6 alkylene group, R 1 and R 2 represent, independently, a hydrogen atom, C 1-4 alkyl group, benzyl group, or together with one or more halogen atoms, trifluoromethyl group, or C 1-4 alkoxy group substituted 4-phenyl-piperazine-l-yl group; and/or their pharmaceutically suitable acid addition salts, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.
摘要翻译：本发明涉及通式（I）的新的选择性5HT6受体结合苯并呋喃衍生物，其中Z表示氢原子，C1-4酰基，C1-6烷基磺酰基，被一个或多个卤素原子取代的苯基磺酰基; 或（R）（ - ） - 10-樟脑磺酰基，或被苯并呋喃基磺酰基取代的苯并呋喃基磺酰基，或者被卤素原子取代的萘基磺酰基，四氢萘基磺酰基，（1S）（+） - 10-樟脑磺酰基，（1R）卤素原子和C1〜4烷基，Y表示C2-6亚烷基，R1和R2独立地表示氢原子，C1-4烷基，苄基或与一个或多个卤素原子一起形成的三氟甲基，或C 1-4烷氧基取代的4-苯基 - 哌嗪-1-基; 和/或其药学上合适的酸加成盐，用于制备所述化合物的方法，含有所述化合物的药物组合物及其在治疗和/或预防中枢神经系统和心血管系统疾病中的用途。

6. 发明申请

WO2008146064A1 NEW BENZOFURAN DERIVATIVES AS SELECTIVE 5HT7 RECEPTOR INHIBITORS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：作为选择性5HT7受体抑制剂的新型苯佐衍生物及其制备方法
公开(公告)号：WO2008146064A1
公开(公告)日：2008-12-04
申请号：PCT/HU2008/000061
申请日：2008-05-30
申请人： EGIS GYÓGYSZERGYÁR , PRAUDA, Ibolya , RIVÓ, Endre , REITER, József , BARKÖCZY, József , GACSÁLYL, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
发明人： PRAUDA, Ibolya , RIVÓ, Endre , REITER, József , BARKÖCZY, József , GACSÁLYL, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
IPC分类号： C07D307/86 , C07D405/12 , A61K31/4525 , A61P25/00
CPC分类号： C07D405/12 , C07D307/86
摘要： The present invention relates to new selective 5HT 7 receptor binding benzofuran derivatives of general formula (I), wherein X represents a halogen atom or SO 2 NR 1 R 2 group, wherein R 1 and R 2 represent, independently, a hydrogen atom, C 1-6 alkyl group, C 3-6 cycloalkyl group, phenyl group substituted with one or more halogen atom(s) or 1,7.7-trimethyl-bicyclo[2,2,1]hept-2-yl group, Y represents C 2-6 alkylene group, optionally substituted with hydroxy group, A represents carbon atom, nitrogen atom or CH group, B represents CH or CH 2 group, Q represents C 1-4 alkyl group, a phenyl group optionally substituted with one or more halogen atom(s), C 1-4 alkoxy group or trifluoromethyl group; phenylamino group substituted with a halogen atom or trifluoromethyl group; pyridine heterocycle; benzisoxazole or benzisothiazole heterocycle, optionally substituted with a halogen atom; benzimidazole or benzimidazolone heterocycle, optionally substituted with a halogen atom or trifluoromethyl group on the benzene ring, or optionally substituted on one of the N atoms with an C 1-4 alkyl group; benzodioxane heterocycle, optionally substituted with a halogen atom on the benzene ring; pyridazinone heterocycle substituted with a halogen atom; dibenzothiazepine heterocycle or Q together with groups A and B represents a thiophene ring and their pharmaceutically suitable acid addition salts, with the proviso that if Y represents 2-hydroxy propylene group, A represents a carbon atom, B represents CH group, and Q represents 3-trifluoro-methyl-phenyl group, then X does not represent bromo atom. The invention extends to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.
摘要翻译：本发明涉及通式（I）的新的选择性5HT7受体结合苯并呋喃衍生物，其中X表示卤素原子或SO2NR1R2基团，其中R1和R2独立地表示氢原子，C1-6烷基，C3-6 环烷基，被一个或多个卤素原子或1,7,7-三甲基 - 双环[2,2,1]庚基取代的苯基，Y表示任选被羟基取代的C 2-6亚烷基 A表示碳原子，氮原子或CH基，B表示CH或CH2基，Q表示C1-4烷基，任选被一个或多个卤素原子取代的苯基，C 1-4烷氧基或三氟甲基 ; 被卤素原子或三氟甲基取代的苯基氨基; 吡啶杂环; 苯并异恶唑或苯并异噻唑杂环，任选被卤素原子取代; 苯并咪唑或苯并咪唑酮杂环，任选被苯环上的卤素原子或三氟甲基取代，或任选地在一个N原子上被C 1-4烷基取代; 苯并二恶烷杂环，任选被苯环上的卤素原子取代; 用卤素原子取代的哒嗪酮杂环; 二苯并硫氮杂环或Q与A和B组一起代表噻吩环及其药学上合适的酸加成盐，条件是如果Y表示2-羟基丙基，则A表示碳原子，B表示CH基，Q表示3 三氟甲基 - 苯基，则X不表示溴原子。本发明涉及生产所述化合物的方法，含有所述化合物的药物组合物及其在治疗和/或预防中枢神经系统和心血管系统疾病中的用途。

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