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51. 发明授权

US07960558B2 Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof 有权
标题翻译：用于合成ACE抑制剂的药物中间体及其用途
公开(公告)号：US07960558B2
公开(公告)日：2011-06-14
申请号：US12300545
申请日：2007-05-11
申请人： Márta Porcs-Makkay , Gyula Simig , Tibor Mezei , Angéla Veressné Pandur , Gyula Lukács
发明人： Márta Porcs-Makkay , Gyula Simig , Tibor Mezei , Angéla Veressné Pandur , Gyula Lukács
IPC分类号： C07D263/44 , C07D209/52 , C07D209/42 , C07C69/96
CPC分类号： C07K5/0222 , A61K38/00 , C07C271/22 , C07D209/42 , C07D263/44
摘要： The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.
摘要翻译：通式（I）的化合物，其中R 1是芳基或烷基; R2代表烷基; R3表示烷基或芳烷基，是有价值的药物中间体，其可以通过使通式（IV）化合物（其中R 1和R 2的定义如上所述）与至少2摩尔当量的通式（VI）（其中X表示卤素或叔丁氧羰基氧基，R3如上定义）。通式（II）的已知化合物（其中R1和R2如上定义）通过使通式（I）的化合物与亚硫酰氯反应来制备。通式（I）的化合物是可用于合成药物活性成分的新中间体，特别是在制备ACE抑制剂中。依那普利，培哚普利或雷米普利。

52. 发明授权

US07951798B2 Polymorphs of olanzapine hydrochloride 失效
标题翻译：盐酸奥氮平的多晶型物
公开(公告)号：US07951798B2
公开(公告)日：2011-05-31
申请号：US10553908
申请日：2004-04-22
申请人： János Pethö , József Barkóczy , Péter Kótay Nagy , Gyula Simig , Zsuzsa Szent-Királlyi
发明人： János Pethö , József Barkóczy , Péter Kótay Nagy , Gyula Simig , Zsuzsa Szent-Királlyi
IPC分类号： A61P25/18 , A61K31/551 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to new crystalline forms I, II and III of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]-benzodiazepine hydrochloride, a process for the preparation thereof and pharmaceutical compositions containing the same. Said new polymorphic forms are useful as active ingredients for the treatment of psychotic conditions.
摘要翻译：本发明涉及2-甲基-4-（4-甲基哌嗪-1-基）-10H-噻吩并[2,3-b] [1,5] - 苯并二氮杂盐酸盐的新结晶形式I，II和III，其制备方法和含有该组合物的药物组合物。所述新的多晶型物可用作治疗精神病状态的活性成分。

53. 发明授权

US07786129B2 Piperazine derivatives of dialkyl oxindoles 失效
标题翻译：二氢羟吲哚的哌嗪衍生物
公开(公告)号：US07786129B2
公开(公告)日：2010-08-31
申请号：US11596473
申请日：2005-05-11
申请人： Balázs Volk , József Barkóczy , Gyula Simig , Tibor Mezei , Rita Kapillerné Dezsöfi , Endréné Flórian , István Gacsályi , Katalin Pallagi , Gábor Gigler , György Lévay , Krisztina Móricz , Csilla Leveleki , Nóra Sziray , Gábor Szénási , András Egyed , László Gábor Hársing
发明人： Balázs Volk , József Barkóczy , Gyula Simig , Tibor Mezei , Rita Kapillerné Dezsöfi , Endréné Flórian , István Gacsályi , Katalin Pallagi , Gábor Gigler , György Lévay , Krisztina Móricz , Csilla Leveleki , Nóra Sziray , Gábor Szénási , András Egyed , László Gábor Hársing
IPC分类号： A61K31/4045 , C07D209/34 , C07D401/12 , C07D405/12
CPC分类号： C07D403/12 , C07D209/34 , C07D401/12 , C07D405/12
摘要： The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R2 represents hydrogen or halogen; R3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R4 stands for alkyl having 1-7 carbon atom(s); R5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R6, R7 and R8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R6 and R7 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.
摘要翻译：本发明涉及通式（I）的新的3,3-二取代吲哚-2-酮衍生物，其中R1代表氢，卤素，具有1-7个碳原子的烷基或亚磺酰氨基; R2代表氢或卤素; R3表示氢，具有1-7个碳原子的烷基，任选地带有芳基取代基或任选携带一个或两个卤素取代基的芳基; R4代表具有1-7个碳原子的烷基; R 5表示通式（IIa）或（IIb）的基团，其中Q和W各自表示氮或CH; R6，R7和R8各自表示氢，卤素，三氟甲基，具有1-7个碳原子的烷基或烷氧基，或R6和R7一起表示亚乙二氧基; m为0,1或2; a是单，双或三键; n为0,1或2; 和其药学上可接受的酸加成盐，其可用于治疗或预防中枢神经系统疾病，胃肠系统和心血管系统。

54. 发明申请

US20100168087A1 BENZO[1,2,3]THIADIAZINE DERIVATES 审中-公开
标题翻译：苯并[1,2,3]噻二嗪衍生物
公开(公告)号：US20100168087A1
公开(公告)日：2010-07-01
申请号：US12377771
申请日：2007-08-13
申请人： Marta Porcs-Makkay , Gyula Lukacs , Gabor Kapus , Istvan Gacsalyi , Gyula Simig , Gyoergy Levay , Tibor Mezei , Miklos Vegh , Szabolcs Kertesz , Jozsef Barkoczy , Csilla Leveleki , Laszlo Gabor Harsing
发明人： Marta Porcs-Makkay , Gyula Lukacs , Gabor Kapus , Istvan Gacsalyi , Gyula Simig , Gyoergy Levay , Tibor Mezei , Miklos Vegh , Szabolcs Kertesz , Jozsef Barkoczy , Csilla Leveleki , Laszlo Gabor Harsing
IPC分类号： A61K31/5415 , C07D285/16 , A61P25/00
CPC分类号： C07D285/16
摘要： The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system.
摘要翻译：本发明涉及通式（I）的新的苯并[1,2,3]噻二嗪-1,1-二氧化物衍生物，含有这些化合物的药物及其在药物中的用途。通式（I）的苯并[1,2,3]噻二嗪-1,1-二氧化物衍生物适用于预防或治疗中枢神经系统疾病。

55. 发明申请

US20090215757A1 Process for Preparation of High-Purity Meloxicam and Meloxicam Potassium Salt 有权
标题翻译：高纯度美洛昔康和美洛昔康钾盐的制备方法
公开(公告)号：US20090215757A1
公开(公告)日：2009-08-27
申请号：US11793548
申请日：2005-12-16
申请人： Tibor Mezei , Gyula Simig , Enikó Molnár , Gyula Lukács , Márta Porcs-Makkay , Balázs Volk , Valéria Hofmanné Fekete , Kálmán Nagy , Norbert Mesterházy , György Krasznai , Györgyi Vereczkeyné Donáth , Gyuláné Körtvélyessy , Éva Pécsi
发明人： Tibor Mezei , Gyula Simig , Enikó Molnár , Gyula Lukács , Márta Porcs-Makkay , Balázs Volk , Valéria Hofmanné Fekete , Kálmán Nagy , Norbert Mesterházy , György Krasznai , Györgyi Vereczkeyné Donáth , Gyuláné Körtvélyessy , Éva Pécsi
IPC分类号： A61K31/5415 , C07D417/12
CPC分类号： C07D417/12
摘要： The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam.
摘要翻译：本发明提供了制备式（II）的高纯度美洛昔康的方法。美洛昔康原始产物与氢氧化钾或碳酸钾的溶液反应，由此生产出高纯度的美洛昔康钾盐一水合物。随后用矿物或有机酸处理所述盐，得到高纯度美洛昔康。

56. 发明申请

US20080021016A1 Combined Pharmaceutical Composition for the Inhibition of the Decline of Cognitive Functions 审中-公开
标题翻译：用于抑制认知功能下降的组合药物组合物
公开(公告)号：US20080021016A1
公开(公告)日：2008-01-24
申请号：US10592461
申请日：2004-03-12
申请人： Gyorgy Levay , Istvan Gacsalyi , Laszlo Harsing , Gyula Simig
发明人： Gyorgy Levay , Istvan Gacsalyi , Laszlo Harsing , Gyula Simig
IPC分类号： A61K31/135 , A61K31/13 , A61K31/4015 , A61K31/437 , A61K31/55 , A61P25/28
CPC分类号： A61K45/06 , A61K31/135 , A61K31/355 , A61K31/4015 , A61K31/445 , A61K31/475 , A61K31/55 , A61K2300/00
摘要： The invention relates to a combined pharmaceutical composition for the inhibition of the decline of cognitive functions comprising as A) component (1R,2S,4R)-(-)-2-[N,N-(dimethylaminoethoxy)]-2-phenyl-1,7,7-trimethylbicyclo]-2-phenyl-1.7.-trimethylbicyclo[2.2.1]heptane of the formula (I) or a pharmaceutically acceptable acid addition salt thereof and as B) component a nootropic, an inhibitor of the acetylcholinesterase enzyme and/or a further pharmaceutical active ingredient which exhibits a beneficial effect on the cognitive processes in admixture with suitable inert pharmaceutical carriers and/or auxiliary agents. The combined pharmaceutical composition according to the present invention can be particularly used for the treatment of Alzheimer disease or other diseases showing similar symptoms, diseases accompanied by malfunctions of intellectual abilities (e.g. mental decline in schizophrenia), mental decline in elderly (dementias in elderly), Korsakoff syndrome, Huntington syndrome, Parkinson syndrome or mental decline produced by alcoholism.
摘要翻译：本发明涉及用于抑制认知功能下降的组合药物组合物，其包含A）成分（1R，2S，4R） - （ - ） - 2- [N，N-（二甲基氨基乙氧基）] -2-苯基 - （I）的1,7,7-三甲基双环] -2-苯基-1,7-三甲基双环[2.2.1]庚烷或其药学上可接受的酸加成盐和作为B）组分的向异性，乙酰胆碱酯酶的抑制剂酶和/或另外的药物活性成分，其与合适的惰性药物载体和/或辅助剂混合显示对认知过程的有益作用。根据本发明的组合药物组合物可以特别用于治疗阿尔茨海默氏病或类似症状的其他疾病，伴有智力障碍的疾病（例如精神分裂症的精神下降），老年人精神衰退（老年痴呆症），Korsakoff综合征，亨廷顿综合症，帕金森综合征或酒精中毒引起的精神衰弱。

57. 发明申请

US20070232619A1 Piperazine Derivatives of Dialkyl Oxindoles 失效
标题翻译：二烷基吲哚的哌嗪衍生物
公开(公告)号：US20070232619A1
公开(公告)日：2007-10-04
申请号：US11596473
申请日：2005-05-11
申请人： Balazs Volk , Jozsef Barkoczy , Gyula Simig , Tibor Mezei , Rita Dezsofi , Endrene Florian , Istvan Gacsalyi , Katalin Pallagi , Gabor Gigler , Gyorgy Levay , Krisztina Moricz , Csilla Leveleki , Nora Sziray , Gabor Szenasl , Andras Egyed , Laszlo Harsing
发明人： Balazs Volk , Jozsef Barkoczy , Gyula Simig , Tibor Mezei , Rita Dezsofi , Endrene Florian , Istvan Gacsalyi , Katalin Pallagi , Gabor Gigler , Gyorgy Levay , Krisztina Moricz , Csilla Leveleki , Nora Sziray , Gabor Szenasl , Andras Egyed , Laszlo Harsing
IPC分类号： A61K31/496 , C07D403/02 , C07D403/14
CPC分类号： C07D403/12 , C07D209/34 , C07D401/12 , C07D405/12
摘要： The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R2 represents hydrogen or halogen; R3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R4 stands for alkyl having 1-7 carbon atom(s); R5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R6, R7 and R8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R6 and R7 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.
摘要翻译：本发明涉及通式（I）的新的3,3-二取代吲哚-2-酮衍生物，其中R 1代表氢，卤素，具有1-7个碳原子的烷基（ s）或磺酰胺基; R 2表示氢或卤素; R 3表示氢，具有1-7个碳原子的烷基，任选地带有芳基取代基或任选地带有一个或两个卤素取代基的芳基; R 4代表具有1-7个碳原子的烷基; R 5表示通式（IIa）或（IIb）的基团，其中Q和W各自表示氮或CH; R 6，R 7和R 8均代表氢，卤素，三氟甲基，具有1-7个碳原子的烷基或烷氧基，，或R 6和R 7一起代表亚乙二氧基; m为0,1或2; a是单，双或三键; n为0,1或2; 和其药学上可接受的酸加成盐，其可用于治疗或预防中枢神经系统疾病，胃肠系统和心血管系统。

58. 发明申请

US20070219209A1 Piperazine Derivatives Of Alkyl Oxindoles 审中-公开
标题翻译：烷基氧吲哚的哌嗪衍生物
公开(公告)号：US20070219209A1
公开(公告)日：2007-09-20
申请号：US11596466
申请日：2005-05-10
申请人： Balazs Volk , Jozsef Barkoczy , Gyula Simig , Tibor Mezei , Rita Kapillerne Dezsofi , Istvan Gacsalyi , Katalin Pallagi , Gabor Gigler , Gyorgy Levay , Krisztina Moricz , Csilla Leveleki , Nora Sziray , Gabor Szenasi , Andras Egyed , Laszlo Harsing
发明人： Balazs Volk , Jozsef Barkoczy , Gyula Simig , Tibor Mezei , Rita Kapillerne Dezsofi , Istvan Gacsalyi , Katalin Pallagi , Gabor Gigler , Gyorgy Levay , Krisztina Moricz , Csilla Leveleki , Nora Sziray , Gabor Szenasi , Andras Egyed , Laszlo Harsing
IPC分类号： C07D209/34 , A61K31/40 , A61P25/00
CPC分类号： C07D209/34
摘要： The present invention is concerned with new indol-2-one derivatives of the general Formula (I). The new compounds are useful for the treatment or prevention of the disorders of the central nervous system or the cardiovascular system.
摘要翻译：本发明涉及通式（I）的新的吲哚-2-酮衍生物。新化合物可用于治疗或预防中枢神经系统疾病或心血管系统。

59. 发明申请

US20070117837A1 Process for the preparation of amorphous form of a platelet aggregation inhibitor drug 失效
标题翻译：制备无定形形式的血小板聚集抑制剂药物的方法
公开(公告)号：US20070117837A1
公开(公告)日：2007-05-24
申请号：US10562978
申请日：2004-06-30
申请人： Peter Kotay Nagy , Gyula Simig , Jozsef Barkoczy , Tamas Gregor , Bela Farkas , Gyorgyi Vereczekeyne Donath , Kalman Nagy , Gyulane Kortvelyessy , Zsuzsanna Szent-Kirallyi
发明人： Peter Kotay Nagy , Gyula Simig , Jozsef Barkoczy , Tamas Gregor , Bela Farkas , Gyorgyi Vereczekeyne Donath , Kalman Nagy , Gyulane Kortvelyessy , Zsuzsanna Szent-Kirallyi
IPC分类号： A61K31/4743 , C07D498/02
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).
摘要翻译：本发明涉及一种制备（S） - （+） - （2-氯苯基）-2-（6,7-二氢-4H-噻吩并[3,2-c] 式（I）的吡啶-5-基乙酸酯硫酸氢盐。

60. 发明授权

US5716986A Oxaindene derivatives and process for the preparation thereof 失效
标题翻译：氧化烯衍生物及其制备方法
公开(公告)号：US5716986A
公开(公告)日：1998-02-10
申请号：US671515
申请日：1996-06-27
申请人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
发明人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
IPC分类号： C07D307/79 , A61K31/34 , A61K31/343 , A61K31/445 , A61K31/535 , A61P1/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D307/91 , C07D307/93
CPC分类号： C07D307/91 , C07D307/93
摘要： This invention relates to new oxaindene derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The compounds according to the invention are characterized by the general formula (1) ##STR1## wherein R.sup.1 represents lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or lower C.sub.3-6 cycloalkyl, R.sup.2 stands for hydrogen, lower C.sub.1-4 alkyl or lower C.sub.3-6 cycloalkyl, R.sup.3 stands for hydrogen, lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or benzyloxy, X denotes hydrogen, an aliphatic C.sub.1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C.sub.1-4 -alkoxy group(s) or a group of the formula R.sup.5 R.sup.6 N--R.sup.7 --, wherein R.sup.7 represents lower C.sub.1-4 alkylene and R.sup.5 and R.sup.6 each represent lower C.sub.1-4 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group, A and B together form an ethylene or a vinylene group, and n is 1, 2 or 3, and have a strong 5-lipoxygenase (5-LO) enzyme inhibiting activity.
摘要翻译：本发明涉及新的氧杂茚衍生物，其制备方法和包含其的药物组合物。根据本发明的化合物的特征在于通式（1）其中R 1表示低级C 1-4烷基，低级C 1-4烷氧基或低级C 3-6环烷基，R 2表示氢，低级C 1〜 4烷基或低级C3-6环烷基，R3代表氢，低级C1-4烷基，低级C1-4烷氧基或苄氧基，X表示氢，脂族C1-4酰基或苯甲酰基或萘甲酰基，任选被1或更多的硝基或C 1-4 - 烷氧基或式R 5 R 6 N-R 7 - 的基团，其中R 7表示低级C 1-4亚烷基，R 5和R 6各自表示低级C 1-4烷基，或者R 5和R 6连同它们所连接的氮原子形成哌啶基或吗啉基，A和B一起形成乙烯或亚乙烯基，n为1,2或3，具有强的5-脂氧合酶（5-LO）酶抑制活性。

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