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1. 发明申请

US20060122395A1 Industrial process for the synthesis of 2-substituted 1-(hydroxy-ethylidene)-1,1-bisphosfi- conic acids of high purity and the salts thereof 有权
公开(公告)号：US20060122395A1
公开(公告)日：2006-06-08
申请号：US10541866
申请日：2004-01-27
申请人： Jozsef Neu , Janos Fischer , Tamas Fodor , Jozsef Torley , Tibor Gizur , Sandor Levai , Adam Demeter , Eva Perenyi
发明人： Jozsef Neu , Janos Fischer , Tamas Fodor , Jozsef Torley , Tibor Gizur , Sandor Levai , Adam Demeter , Eva Perenyi
IPC分类号： C07F9/22
CPC分类号： C07F9/3873 , C07F9/58
摘要： Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3′-pyridyl or 2′-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.

2. 发明授权

US07612229B2 Industrial process for the synthesis of 2-substituted 1-(hydroxy-ethylidene)-1,1-bisphosfi- conic acids of high purity and the salts thereof 有权
标题翻译：用于合成高纯度的2-取代的1-（羟基 - 亚乙基）-1,1-双磷酸的工业方法及其盐
公开(公告)号：US07612229B2
公开(公告)日：2009-11-03
申请号：US10541866
申请日：2004-01-27
申请人： Jozsef Neu , Janos Fischer , Tamas Fodor , Jozsef Törley , Tibor Gizur , Sandor Levai , Adam Demeter , Eva Perenyi
发明人： Jozsef Neu , Janos Fischer , Tamas Fodor , Jozsef Törley , Tibor Gizur , Sandor Levai , Adam Demeter , Eva Perenyi
IPC分类号： C07F9/22
CPC分类号： C07F9/3873 , C07F9/58
摘要： Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3′-pyridyl or 2′-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.
摘要翻译：用于合成式（I）的高纯度2-取代-1-（羟基 - 亚乙基）-1,1-双膦酸的方法，其盐和水合物 - 其中R的含义是3'-吡啶基或2' - 氨基 - 亚乙基 - 其中R的含义如上所述，或其盐和水合物与甲酸在甲磺酸存在下，使用五氧化二磷作为试剂，在给定的情况下，所得的酸与碱成盐。

3. 发明申请

US20060178511A1 Process for the synthesis of high purity3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine 失效
标题翻译：合成高纯度3,5-二氨基-6-（2,3-二氯苯基）-1,2,4-三嗪的方法
公开(公告)号：US20060178511A1
公开(公告)日：2006-08-10
申请号：US10528379
申请日：2003-09-18
申请人： Jozsef Neu , Tibor Gizur , Jozsef Torley , Ferenc Vegh , Peter Kalvin , Gabor Tarkanyi
发明人： Jozsef Neu , Tibor Gizur , Jozsef Torley , Ferenc Vegh , Peter Kalvin , Gabor Tarkanyi
IPC分类号： C07D253/02
CPC分类号： C07D253/075 , C07C281/16
摘要： The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide. In given case the obtained crude product can be recrystallized from a proper organic solvent.
摘要翻译：本发明涉及使用2,3-二氯苯甲酰氰合成式（I）的高纯度3,5-二氨基-6-（2,3-二氯苯基）-1,2,4-三嗪的新方法，氨基胍盐为起始原料。将2,3-二氯苯甲酰氰与1-2摩尔当量的氨基胍盐在3-6摩尔当量的甲磺酸中反应，然后将得到的式（Ⅳ）加合物转化成不含氧化镁的产物。在给定情况下，所得粗产物可以从合适的有机溶剂中重结晶。

4. 发明授权

US07390899B2 Process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl) (1,2,4-triazine) 失效
标题翻译：合成高纯度3,5-二氨基-6-（2,3-二氯苯基）（1,2,4-三嗪）
公开(公告)号：US07390899B2
公开(公告)日：2008-06-24
申请号：US10528379
申请日：2003-09-18
申请人： Jozsef Neu , Tibor Gizur , Jozsef Törley , Janos Csabai , Ferenc Vegh , Peter Kalvin , Gabor Tarkanyi
发明人： Jozsef Neu , Tibor Gizur , Jozsef Törley , Janos Csabai , Ferenc Vegh , Peter Kalvin , Gabor Tarkanyi
IPC分类号： C07D253/075 , C07C281/16
CPC分类号： C07D253/075 , C07C281/16
摘要： The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide. In given case the obtained crude product can be recrystallized from a proper organic solvent
摘要翻译：本发明涉及使用2,3-二氯苯甲酰氰合成式（I）的高纯度3,5-二氨基-6-（2,3-二氯苯基）-1,2,4-三嗪的新方法，氨基胍盐为起始原料。将2,3-二氯苯甲酰氰与1-2摩尔当量的氨基胍盐在3-6摩尔当量的甲磺酸中反应，然后将得到的式（Ⅳ）加合物转化成不含氧化镁的产物。在给定情况下，所得粗产物可以从合适的有机溶剂中重结晶

5. 发明申请

US20090111988A1 NOVEL PROCESS FOR PRODUCTION OF 5--6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE (ZIPRASIDONE) 审中-公开
标题翻译：生产5-6-氯-1,3-二氢-2H-吲哚-2-酮（ZIPRASIDONE）的新方法
公开(公告)号：US20090111988A1
公开(公告)日：2009-04-30
申请号：US12298590
申请日：2007-05-02
申请人： Jozsef Neu , Jozsef Torley , Sandor Garadnay
发明人： Jozsef Neu , Jozsef Torley , Sandor Garadnay
IPC分类号： C07D417/14 , C07D209/34
CPC分类号： C07D417/12
摘要： The present invention provides a novel, industrially easily realisable and economically preferable process for production of pure 5-{2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one i.e., ziprasidone hydrochloride shown in the reaction scheme (II), (III), (IV), (V) and (VI). According to the invention the intermediate compound 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) is produced from 5-(2-bromoacethyl)-6-chloro-1,3-dihydro-2H-indole-2-one of Formula (IV). The highly pure ziprasidone base of Formula (II) is obtained in the reaction of 3-piperazinyl-1,2-benzisothiazol of Formula (VI) with 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) in an organic solvent or organic solvent mixture.
摘要翻译：本发明提供了一种工业上容易实现的和经济上优选的纯5- {2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基] - 乙基} -6-氯 - （II），（III），（IV），（V）和（VI）所示的齐拉昔酮盐酸盐，例如1,3-二氢-2H-吲哚-2-酮。根据本发明，式（III）的中间体化合物5-（2-溴乙基）-6-氯-1,3-二氢-2H-吲哚-2-酮由5-（2-溴代乙基）-6- （IV）的3-氯-1,3-二氢-2H-吲哚-2-酮。在式（Ⅵ）的3-哌嗪基-1,2-苯并异噻唑与5-（2-溴乙基）-6-氯-1,3-二氢-2H-哒嗪酮的反应中得到式（II）的高纯度齐拉西酮碱（III）的吲哚-2-酮在有机溶剂或有机溶剂混合物中的溶液。

6. 发明授权

US5543562A Non-hygroscopic monoammonium salts of phosphonic acids or phosphinic acids 失效
标题翻译：膦酸或次膦酸的非吸湿性单铵盐
公开(公告)号：US5543562A
公开(公告)日：1996-08-06
申请号：US422265
申请日：1995-04-14
申请人： Fulgencio Powell Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Jan os Repasi , Agota Repasine Veres , Jozsef Vigh , Istvanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
发明人： Fulgencio Powell Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Jan os Repasi , Agota Repasine Veres , Jozsef Vigh , Istvanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
IPC分类号： A01N33/00 , A61K38/22 , A01N25/00 , A01N57/20 , A61K38/00 , A61L27/00 , A61P27/02 , C07F9/30 , C07F9/38 , C07K7/08 , C07K14/52 , C07K14/575 , C07K14/65 , A01N57/02 , A01N57/12
CPC分类号： C07K14/65 , A01N57/20 , C07F9/301 , C07F9/3813 , A61K38/00
摘要： A solid, non-hygroscopic salt of the Formula (I) ##STR1## wherein R.sup.1 is hydroxy or alkyl;A is C.sub.1 to C.sub.4 alkyl-amino or an amino-alkyl group containing a primary or a secondary amino group; andB is ammonium ion or an alkyl-substituted ammonium ion, which is substantially free of a diammonium salt ##STR2##
摘要翻译：式（I）的固体，非吸湿盐其中R 1是羟基或烷基; A是C1-C4烷基 - 氨基或含有伯或仲氨基的氨基 - 烷基; （B）是铵离子或烷基取代的铵离子，其基本上不含二铵盐（V）

7. 发明申请

US20080306271A1 Novel Process for Production of Highly Pure Polymorph (I) Donepezil Hydrochloride 审中-公开
标题翻译：用于生产高纯度多晶型物（I）盐酸多奈哌齐的新方法
公开(公告)号：US20080306271A1
公开(公告)日：2008-12-11
申请号：US12094304
申请日：2006-12-18
申请人： Jozsef Neu , Istvan Greiner , Janos Csabai , Sandor Garadnay
发明人： Jozsef Neu , Istvan Greiner , Janos Csabai , Sandor Garadnay
IPC分类号： C07D211/32
CPC分类号： C07D211/02 , C07D211/32
摘要： The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan-1-one hydrochloride is saturated using Pd carbon to get 4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine at more than 97% HPLC purity. In the crystallization step donepezil-hydrochloride is crystallized from an aqueous alcoholic solvent to get Polymorph (I) in at least 99.95% HPLC purity.
摘要翻译：本发明提供了一种工业上可实现的和经济上优选的生产高纯度1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-基]甲基哌啶盐酸盐的方法，即盐酸多奈哌齐在以下反应方案中，在多晶型（I）形态晶体形式中。（I）在该方法的关键步骤之一中，在氢化期间，使用Pd碳饱和5,6-二甲氧基2-（吡啶-4-亚乙基）茚满-1-酮盐酸盐，得到4 - [（5,6 - 二甲氧基-1-茚满酮）-2-基] - 甲基哌啶，HPLC纯度高于97％。在结晶步骤中，盐酸多奈哌齐从含水醇溶剂中结晶得到至少99.95％HPLC纯度的多晶型物（I）。

8. 发明授权

US5410075A Non-hygroscopic monoammonium salts of phosphonic and phosphinic acids 失效
标题翻译：膦酸和次膦酸的非吸湿性单铵盐
公开(公告)号：US5410075A
公开(公告)日：1995-04-25
申请号：US192414
申请日：1994-02-04
申请人： Fulgencio Powell Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Janos Repasi , Agota Repasine Veres , Jozsef Vigh , Istvanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
发明人： Fulgencio Powell Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Janos Repasi , Agota Repasine Veres , Jozsef Vigh , Istvanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
IPC分类号： A01N33/00 , A61K38/22 , A01N25/00 , A01N57/20 , A61K38/00 , A61L27/00 , A61P27/02 , C07F9/30 , C07F9/38 , C07K7/08 , C07K14/52 , C07K14/575 , C07K14/65 , A01N57/02 , A01N57/12
CPC分类号： C07K14/65 , A01N57/20 , C07F9/301 , C07F9/3813 , A61K38/00
摘要： A solid, non-hygroscopic salt of the Formula (I) ##STR1## wherein R.sup.1 is dydroxy or alkyl;A is C.sub.1 to C.sub.4 alkyl-amino or an amino-alkyl group containing a primary or a secondary amino group; andB is ammonium ion or an alkyl-substituted ammonium ion, which is substantially free of a diammonium salt ##STR2##
摘要翻译：式（I）的固体，非吸湿盐其中R 1是二羟基或烷基; A是C1-C4烷基 - 氨基或含有伯或仲氨基的氨基 - 烷基; B是铵离子或烷基取代的铵离子，其基本上不含二铵盐

9. 发明授权

US5324708A Non-hygroscopic monoammonium salts of phosphonic and phosphinic acids 失效
标题翻译：膦酸和次膦酸的非吸湿性单铵盐
公开(公告)号：US5324708A
公开(公告)日：1994-06-28
申请号：US869925
申请日：1992-04-16
申请人： Fulgencio P. Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Janos Repasi , Agota R. Veres , Jozsef Vigh , Istavanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
发明人： Fulgencio P. Moreno , Laszlo Litkei , Vilmos Galamb , Imre Gulyas , Janos Repasi , Agota R. Veres , Jozsef Vigh , Istavanne Koczka , Edit Fehervari , Laszlone Roka , Laszlone Pethe , Jozsef Neu
IPC分类号： A01N33/00 , A61K38/22 , A01N25/00 , A01N57/20 , A61K38/00 , A61L27/00 , A61P27/02 , C07F9/30 , C07F9/38 , C07K7/08 , C07K14/52 , C07K14/575 , C07K14/65 , A01N25/34 , A01N57/02 , A01N57/12
CPC分类号： C07K14/65 , A01N57/20 , C07F9/301 , C07F9/3813 , A61K38/00
摘要： A solid, non-hygroscopic salt of the Formula (I) ##STR1## wherein R.sup.1 is hydroxy or alkyl;A is C.sub.1 to C.sub.4 alkyl-amino or an amino-alkyl group containing a primary or a secondary amino group; andB is ammonium ion or an alkyl-substituted ammonium ion, which is substantially free of a diammonium salt ##STR2##
摘要翻译：式（I）的固体，非吸湿盐其中R 1是羟基或烷基; A是C1-C4烷基 - 氨基或含有伯或仲氨基的氨基 - 烷基; B是铵离子或烷基取代的铵离子，其基本上不含二铵盐

10. 发明申请

US20090093635A1 PROCESS FOR MAKING POLYMORPH FROM I OF (S) - (+) -METHYL-ALPHA- (2-CHLOROPHENYL) -6, 7-DYHIDRO-THIENO- [3, 2-c] PYRIDINE-5 (4H) -ACETATE HYDROGEN SULFATE 审中-公开
标题翻译：制备（S） - （+） - 甲基 - （2-氯苯基）-6,7-二氢 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸氢硫酸酯的聚异戊二烯的方法
公开(公告)号：US20090093635A1
公开(公告)日：2009-04-09
申请号：US12282037
申请日：2006-03-08
申请人： Sandor Garadnay , Istvan Greiner , Jozsef Neu
发明人： Sandor Garadnay , Istvan Greiner , Jozsef Neu
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of the pharmaceutically applicable polymorph Form I of (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]-pyridine-5(4H)-acetate hydrogen sulfate of formula I; by reacting (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate and sulfuric acid in the presence of solvents which comprises dissolving (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate in an ether; mixing this solution with a solution of a C6-C11 alcohol and sulfuric acid; and recovering the so obtained compound of formula I from the mother liquor.
摘要翻译：本发明涉及制备（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二苯并噻吩并[3,2-c] 式I的吡啶-5（4H） - 乙酸盐硫酸氢盐; 通过使（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二氯 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯和硫酸在溶剂存在下反应其包括在醚中溶解（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二氯 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯; 将该溶液与C6-C11醇和硫酸的溶液混合; 并从母液中回收如此得到的式I化合物。

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