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1.发明申请PROCESS FOR PREPARATION OF HIGH-PURITY MELOXICAM AND MELOXICAM POTASSIUM SALT 审中-公开制备高纯度麦芽糖和莫西沙姆钾盐的方法公开(公告)号：US20120035162A1
公开(公告)日：2012-02-09
申请号：US13271445
申请日：2011-10-12
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 , A61P29/00 , C07D279/16
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。
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2.发明授权Process for preparation of high-purity meloxicam and meloxicam potassium salt 有权制备高纯度美洛昔康和美洛昔康钾盐的方法公开(公告)号：US08097616B2
公开(公告)日：2012-01-17
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： C07D417/12 , A61K31/427 , A61P29/00
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 sait monohydrate is produced. Said sait 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溶液反应，由此生产出高纯度的美洛昔康钾一水合物。 随后用矿物质或有机酸处理所述食物以产生高纯度美洛昔康。
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3.发明申请Process for Preparation of High-Purity Meloxicam and Meloxicam Potassium Salt 有权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。
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![Process for preparing (1R,2S,4R)-(-)-2-[(2'-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof](/abs-image/US/2001/06/05/US06242386B1/abs.jpg.150x150.jpg)
4.发明授权Process for preparing (1R,2S,4R)-(-)-2-[(2'-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof 失效制备（1R，2S，4R） - （ - ） - 2 - [（2' - {N，N-二甲基氨基}乙氧基）] - 2- [苯基] -1,7,7-三 - [甲基 ] - 双环[2.2.1]庚烷及其药学上可接受的酸加成盐公开(公告)号：US06242386B1
公开(公告)日：2001-06-05
申请号：US09569050
申请日：2000-05-10
申请人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
发明人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
IPC分类号： C07C20900
CPC分类号： C07C213/02 , C07B2200/07 , C07C217/12 , C07C2602/42 , C07C217/02
摘要： A process for preparing (1R,2S,4R)-(−)-2-[(2′-[N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo [2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof with higher yields and higher grades of purity.
摘要翻译： 制备（1R，2S，4R） - （ - ） - 2 - [（2' - [N，N-二甲基氨基}乙氧基）] - 2- [苯基] -1,7,7-三 - [ 甲基] - 双环[2.2.1]庚烷及其药学上可接受的酸加成盐，具有更高的产率和更高等级的纯度。
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![HIGH PURITY (1R,2S,4R)-(−)-2-[(2′-{N,N-DIMETHYLAMINO}-ETHOXY)]-2-[PHENYL]-1,7,7 -TRI-[METHYL]-BICYCLO [2.2.1]HEPTANE AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF AND A PROCESS FOR THE PREPARATION OF THESE COMPOUNDS AS WELL AS MEDICAMENTS CONTAINING 1 OR MORE OF THESE COMPOUNDS AND THEIR USE](/abs-image/US/2003/09/23/US06624201B2/abs.jpg.150x150.jpg)
5.发明授权HIGH PURITY (1R,2S,4R)-(−)-2-[(2′-{N,N-DIMETHYLAMINO}-ETHOXY)]-2-[PHENYL]-1,7,7 -TRI-[METHYL]-BICYCLO [2.2.1]HEPTANE AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF AND A PROCESS FOR THE PREPARATION OF THESE COMPOUNDS AS WELL AS MEDICAMENTS CONTAINING 1 OR MORE OF THESE COMPOUNDS AND THEIR USE 有权高纯度（1R，2S，4R） - （ - ） - 2 - [（2' - （N，N-二甲基氨基） - 乙氧基）] - 2- [苯基] -1,7,7-三 - [甲基] -BICYCLO [2.2.1] HEPTANE和药物可接受的酸添加剂及其制备这些化合物的方法，作为含有这些化合物1或更多的药物及其使用的药物公开(公告)号：US06624201B2
公开(公告)日：2003-09-23
申请号：US09984542
申请日：2001-10-30
申请人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
发明人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
IPC分类号： A61K31135
CPC分类号： C07C213/02 , C07B2200/07 , C07C217/12 , C07C2602/42 , C07C217/02
摘要： The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.
摘要翻译： 本发明涉及高纯度（1R，2S，4R） - （ - ） - 2 - [（2' - （N，N-二甲基氨基） - 乙氧基）] - 2- [苯基] - [甲基] - 双环[2.2.1]庚烷及其药学上可接受的酸加成盐，其含有不超过0.2％（1R，3S，4R）-3 - [（2' - （N，N-二甲基氨基） - 乙基 ）] - 1,7,7-三 - [甲基] - 双环[2.2.1]庚烷-2-酮和/或其药学上可接受的酸加成盐。此外，本发明涉及制备 这些化合物。此外，本发明涉及含有1种以上这些化合物及其用途的药剂。
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![High purity (1R,2S,4R)-(-)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof](/abs-image/US/2002/01/01/US06335469B1/abs.jpg.150x150.jpg)
6.发明授权High purity (1R,2S,4R)-(-)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof 失效高纯度（1R，2S，4R） - （ - ） - 2 - [（2' - {N，N-二甲基氨基}乙氧基）] - 2- [苯基] -1,7,7-三 - [甲基] - 双环[2.2.1]庚烷及其药学上可接受的酸加成盐公开(公告)号：US06335469B1
公开(公告)日：2002-01-01
申请号：US09569046
申请日：2000-05-10
申请人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
发明人： Gyula Lukács , Gyula Simig , Tibor Mezei , Zoltán Budai , Márta Porcs-Makkay , György Krasznai , Kálmán Nagy , Györgyi Donáth Vereczkey , Tibor Szabó , Norbert Németh , János Szulágyi
IPC分类号： C07C21500
CPC分类号： C07C213/02 , C07B2200/07 , C07C217/12 , C07C2602/42 , C07C217/02
摘要： The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.
摘要翻译： 本发明涉及高纯度（1R，2S，4R） - （ - ） - 2 - [（2' - （N，N-二甲基氨基） - 乙氧基）] - 2- [苯基] - [甲基] - 双环[2.2.1]庚烷及其药学上可接受的酸加成盐，其含有不超过0.2％（1R，3S，4R）-3 - [（2' - （N，N-二甲基氨基） - 乙基 ）] - 1,7,7-三 - [甲基] - 双环[2.2.1]庚烷-2-酮和/或其药学上可接受的酸加成盐。此外，本发明涉及制备 这些化合物。此外，本发明涉及含有1种以上这些化合物及其用途的药剂。
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7.发明授权Process for the preparation of amorphous form of a platelet aggregation inhibitor drug 失效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：US07396931B2
公开(公告)日：2008-07-08
申请号：US10562978
申请日：2004-06-30
申请人： Péter Kótay Nagy , Gyula Simig , József Barkóczy , Tamás Gregor , Béla Farkas , Györgyi Vereczkeyné Donáth , Kálmán Nagy , Gyuláné Körtvélyessy , Zsuzsanna Szent-Királlyi
发明人： Péter Kótay Nagy , Gyula Simig , József Barkóczy , Tamás Gregor , Béla Farkas , Györgyi Vereczkeyné Donáth , Kálmán Nagy , Gyuláné Körtvélyessy , Zsuzsanna Szent-Királlyi
IPC分类号： C07D471/02
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
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8.发明授权Process for the preparation of 3-{2-′4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido′1,2-methyl-4h-pyrido′,2-a!pyrimidin-4-one 有权制备3- {2' - （6-氟-1,2-苯并异恶唑-3-基）-1-哌啶基乙基} -6,7,8,9-四氢-2-甲基-4H- 吡啶并[1,2-methyl-4h-pyrido]，2-a]嘧啶-4-酮公开(公告)号：US07307168B2
公开(公告)日：2007-12-11
申请号：US10495362
申请日：2002-11-13
申请人： László Pongó , József Reiter , Gyula Simig , Gábor Berecz , György Clementis , Péter Slégel , János Szulágyi , László Koncz , Györgyi Vereczkeyné Donáth , Kálmán Nagy , Gyuláné Körtvélyessy
发明人： László Pongó , József Reiter , Gyula Simig , Gábor Berecz , György Clementis , Péter Slégel , János Szulágyi , László Koncz , Györgyi Vereczkeyné Donáth , Kálmán Nagy , Gyuláné Körtvélyessy
IPC分类号： C07D239/70
CPC分类号： C07D471/04
摘要： The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.
摘要翻译： 本发明涉及制备3- {2- [4-（6-氟-1,2-苯并异恶唑-3-基）-1-哌啶基]乙基} -6,7,8,9-四氢 -2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮及其药学上可接受的酸加成盐，使式（II）的肟在 将碱金属氢氧化物，碱金属碳酸盐或碱式C 1-4醇盐在惰性有机溶剂中的存在，将由此获得的式I的碱转化为酸加成盐或使得碱 式I的酸加成盐或其酸加成盐，其中通式（XIV）的卤素衍生物（其中Hal为卤素）与式（Ⅴ）的哌啶肟衍生物或其酸加成盐在式 碱，并通过式II的肟的闭环使用形成C 1-4烷基 - 烷醇作为惰性溶剂。 本发明的方法能够经济地制备具有适用于制药目的的纯度的产品。
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9.发明授权Optically active carbamates, process for preparation thereof and use thereof as pharmaceutical intermediates 失效光学活性氨基甲酸酯，其制备方法及其作为药物中间体的用途公开(公告)号：US07851627B2
公开(公告)日：2010-12-14
申请号：US12096636
申请日：2006-12-08
申请人： Tibor Mezei , Enikö{umlaut over ( )} Molnar , Péter Trinka , Ferenc Bartha , Zoltán Katona , Györgyi Vereczekeyné Donath , Kálmán Nagy , Lászlö Pongo , Gyula Lukacs , Márta Porcs-Makkay , Zsuzsanna Évinger , Gyula Simig
发明人： Tibor Mezei , Enikö{umlaut over ( )} Molnar , Péter Trinka , Ferenc Bartha , Zoltán Katona , Györgyi Vereczekeyné Donath , Kálmán Nagy , Lászlö Pongo , Gyula Lukacs , Márta Porcs-Makkay , Zsuzsanna Évinger , Gyula Simig
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07D295/073 , C07D295/185
摘要： The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
摘要翻译： 本发明涉及式（IV）的1 - [（4-氯苯基） - 苯基甲基] -4-（2,2,2-三氯乙氧基羰基） - 哌嗪及其旋光异构体，其制备方法和 制备1-（4-氯苯基） - 苯基甲基 - 哌嗪的式（Ⅳ）化合物及其旋光异构体及其盐。 1-（4-氯苯基） - 苯基甲基 - 哌嗪及其旋光异构体是制备非镇静抗组胺型活性药物成分的重要中间体。
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公开(公告)号：US20130030183A1
公开(公告)日：2013-01-31
申请号：US13517339
申请日：2010-12-21
申请人： Márta Porcs-Makkay , Tamás Gregor , Balázs Volk , Gábor Németh , József Barkóczy , Bálint Nyulasi , Tibor Mezei , György Ruzsics , Angéla Pandur , Erika Szilágyi , Kálmán Nagy , Péter Slégel , Enikö Molnár , Jözsef Debreczeni
发明人： Márta Porcs-Makkay , Tamás Gregor , Balázs Volk , Gábor Németh , József Barkóczy , Bálint Nyulasi , Tibor Mezei , György Ruzsics , Angéla Pandur , Erika Szilágyi , Kálmán Nagy , Péter Slégel , Enikö Molnár , Jözsef Debreczeni
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.
摘要翻译： 本发明的目的是制备2-乙酰氧基-5-（2-氟-α-环丙基 - 羰基 - 苄基）-4,5,6,7-四氢-4H-噻吩并[3 ，（II）的5,6,7,7a-四氢-4H-噻吩并[3,2-c]吡啶-2-酮与式（I）的化合物（2-c]吡啶（普拉格雷） ）与式（III）的2-溴-1-环丙基-2-（2-氟苯基） - 乙酮或式（IIIa）的2-氯-1-环丙基-2-（2-氟苯基） - 乙酮 并且形成式（Ⅳ）化合物的乙酰化反应，其中反应在有机碱存在下与乙酰化试剂进行而不分离式（Ⅳ）化合物。 偶联和乙酰化在相同的有机碱如三乙胺，N，N-二异丙基 - 乙胺或吡啶的存在下进行。 在该方法结束时，式（I）的普拉格雷通过从有机溶剂或溶剂混合物中重结晶来纯化。
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