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1. 发明申请

WO2010092591A2 NOVEL CRYSTALLINE POLYMORPHS OF 5-[[(2R,3S)-2-[(1R)-1-[3,5- BIS(TRIFLUOROMETHYL) PHENYL] ETHOXY]-3-(4-FLUOROPHENYL)-4-MORPHOLINYL]METHYL]-1,2- DIHYDRO-3H-1,2,4-TRIAZOL-3-ONE AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译： 5 - [[（2R，3S）-2 - [（1R）-1- [3,5-双（三氟甲基）苯基]乙氧基] -3-（4-氟苯基）-4-吗啉基]甲基的新型结晶聚合物 ] -1,2-二氢-3H-1,2,4-三唑-3-酮及其制备方法
公开(公告)号：WO2010092591A2
公开(公告)日：2010-08-19
申请号：PCT/IN2009000370
申请日：2009-06-29
申请人： USV LTD , SATHE DHANANJAY GOVIND , BHISE NANDU BABAN , SAWANT KAMLESH DIGAMBAR , SHINDIKAR ANAND VINOD , PATIL SACHIN SHIVAJI , NAIK TUSHAR ANIL
发明人： SATHE DHANANJAY GOVIND , BHISE NANDU BABAN , SAWANT KAMLESH DIGAMBAR , SHINDIKAR ANAND VINOD , PATIL SACHIN SHIVAJI , NAIK TUSHAR ANIL
CPC分类号： C07D413/06
摘要： Disclosed herein is novel polymorph of 5-[[(2R,3S)-2-[(1R)-1-[3,5- bis(trifluoromethyl) phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3H-1,2,4- triazol-3-one, commonly known as Aprepitant or pharmaceutically acceptable salts thereof and process for preparation thereof. The present invention further relates to highly pure polymorph, Form II of Aprepitant. The present invention further relates to improved process for preparation of Aprepitant.
摘要翻译：本文公开了5 - [[（2R，3S）-2 - [（1R）-1- [3,5-双（三氟甲基）苯基]乙氧基] -3-（4-氟苯基）-4-吗啉基 ]甲基] -1,2-二氢-3H-1,2,4-三唑-3-酮，通常称为阿吡啶或其药学上可接受的盐及其制备方法。本发明还涉及高纯度的多晶型物，即Aprepitant的II型。本发明还涉及改进的制备阿吡瑞坦的方法。

2. 发明申请

WO2007105234A3 A PROCESS FOR THE PREPARATION OF ISOMERS OF 11-[3-(DIMETHYLAMINO)PROPYLIDENE]-6, 11-DIHYDRODIBENZ [b, e] OXEPIN-2-ACETIC ACID HYDROCHLORIDE AND POLYMORPHS THEREOF 审中-公开
标题翻译：制备11- [3-（二甲基氨基）丙基] -6,11-二氢苯并[b，e]氧化-2-乙酸氢氯化物及其多元醇的异构体的方法
公开(公告)号：WO2007105234A3
公开(公告)日：2008-02-21
申请号：PCT/IN2007000104
申请日：2007-03-05
申请人： USV LTD , TARUR VENKATASUBRAMANIAN RADHA , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , NAIDU AVINASH VENKATARAMAN , AHER UMESH PARASHRAM , PATIL SACHIN SHIVAJI , VARMA SUDHIR ANANGPAL , SAWANT KAMLESH DIGAMBAR , NAIK TUSHAR ANIL , AMRE RAKESH RAMCHANDRA
发明人： TARUR VENKATASUBRAMANIAN RADHA , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , NAIDU AVINASH VENKATARAMAN , AHER UMESH PARASHRAM , PATIL SACHIN SHIVAJI , VARMA SUDHIR ANANGPAL , SAWANT KAMLESH DIGAMBAR , NAIK TUSHAR ANIL , AMRE RAKESH RAMCHANDRA
IPC分类号： C07D313/12
CPC分类号： C07D313/12
摘要： The present invention relates to an improved process for the preparation of 1 1 -(Z)-[3- (Dimethylamino) propyl idene] -6, 1 l-dihydrodibenz[b,e]oxepin-2-acetic acid (Olopatadine hydrochloride) by reaction of l l-oxo-6, l l -dihydrodibenz[b,e] oxepin-2-acetic acid with Grignard reagent of l-halo-3-dimethylaminopropane and further dehydrated with or without isolation of the intermediate 1 l -(3-dimethylaminopropyl)-l l -hydroxy-6,l l- dihydrodibenz[b,e]oxepin-2-acetic acid. The present invention relates novel polymorphs of 1 1 -(Z)-[3-(Dimethylamino) propyl idene] -6, 1 l -dihydrodibenz[b,e]oxepin-2-acetic acid (Olopatadine hydrochloride). The present invention further relates to preparation of 1 1 - (E)-[3-(Dimethylamino) propylidene]-6, l l-dihydrodibenz[b,e]oxepin-2 -acetic acid hydrochloride.
摘要翻译：本发明涉及制备11-（Z） - [3-（二甲基氨基）丙基]烯-1,6-二氢二苯并[b，e]氧杂七环素-2-乙酸（盐酸奥洛他定）的改进方法，通过11-氧代-6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸与1-卤代-3-二甲基氨基丙烷的格氏试剂反应，并进一步脱水或不分离中间体11 - （3 二甲基氨基丙基）-11-羟基-6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸。本发明涉及11-（Z） - [3-（二甲基氨基）丙基]烯-1-基] -6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸（盐酸奥洛他定）的多晶型物。本发明还涉及制备11-（E） - [3-（二甲基氨基）亚丙基] -6,11-二氢二苯并[b，e]氧杂七环素-2-乙酸盐酸盐。

3. 发明申请

WO2007125542A3 A PROCESS FOR PREPARATION OF ADAPALENE 审中-公开
标题翻译：一种制备ADAPALENEN的方法
公开(公告)号：WO2007125542A3
公开(公告)日：2007-12-27
申请号：PCT/IN2007000145
申请日：2007-04-09
申请人： USV LTD , TARUR RADHAKRISHNAN VENKATASUB , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , PATNEKAR SUBODH SHASHIKANT , PATIL SACHIN SHIVAJI
发明人： TARUR RADHAKRISHNAN VENKATASUB , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , PATNEKAR SUBODH SHASHIKANT , PATIL SACHIN SHIVAJI
IPC分类号： A61K31/192 , A61P17/10 , C07C41/16 , C07C43/225 , C07C51/09 , C07C65/26 , C07C67/343
CPC分类号： C07C67/343 , C07C41/16 , C07C51/09 , C07C51/412 , C07C2603/74 , C07C65/26 , C07C69/94 , C07C43/225
摘要： The present invention discloses a process for preparation of highly pure Adapalene, chemically designated as 6-[3-(l-adamantyl)-4-methoxy phenyl]-2-naphthoic acid (I) comprising: a) reacting 1-adamantanol with 4-bromophenol (II) in presence of sulphonic acid with or without the use of organic solvent to give 2-(l-adamantyl)-4- bromophenol (III); b) alkylating compound of formula(III) with dimethylsulphate in presence of base in organic solvent to obtain 2-(l-adamantyl)-4-bromoanisole (IV); c) C-C coupling the compound of formula (IV) with methyl-6-bromo-2- naphthoate using magnesium, purified zinc chloride and NiCl 2 -DPPE in THF at a temperature of 40-60°C tO obtain methyl ester of 6-[3-(l- adamantyl)-4-methoxy phenyl] -2-naphthoic acid (V); d) purifying crude methyl ester of 6-[3-(l-adamantyl)-4-methoxy phenyl]-2- naphthoic acid (V) using a mixture of organic solvent to obtain pure compound (V); e) hydrolyzing the compound (V) with a solution of alkali in organic solvent to obtain metal salt of 6-[3-(l-adamantyl)-4-methoxy phenyl] -2-naphthoic acid (VI); f) acidifying metal salt of adapalene (VI) using organic or inorganic acid to obtain crude adapalene (I) and g) recrystallizing the crude adapalene (I) using a mixture of organic solvents to obtain pure adapalene (I).
摘要翻译：本发明公开了一种制备高纯度阿达帕林的方法，化学名为6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（I），其包括：a）使1-金刚烷醇与4 （II）在有或没有使用有机溶剂的情况下在磺酸存在下反应，得到2-（1-金刚烷基）-4-溴酚（III）; b）在碱的存在下，在有机溶剂中，用式（III）的化合物与硫酸二甲酯烷基化，得到2-（1-金刚烷基）-4-溴苯甲醚（Ⅳ）; c）在40-60℃的温度下，使用镁，纯化氯化锌和NiCl 2 -DPPE在THF中将式（Ⅳ）化合物与6-溴-2-萘甲酸甲酯偶联，得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的甲酯。 d）使用有机溶剂的混合物纯化6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的粗甲酯，得到纯的化合物（V）; e）用碱在有机溶剂中的溶液水解化合物（V），得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（Ⅵ）的金属盐。 f）使用有机或无机酸酸化阿达帕林（VI）的金属盐，得到粗制阿达帕林（I），和g）使用有机溶剂的混合物重结晶粗制阿达帕林（I），得到纯的阿达帕林（I）。

4. 发明申请

WO2014167577A2 "SYNTHESIS OF DABIGATRAN" 审中-公开
标题翻译： “DABIGATRAN的合成”
公开(公告)号：WO2014167577A2
公开(公告)日：2014-10-16
申请号：PCT/IN2014000188
申请日：2014-03-25
申请人： USV LTD
发明人： PATKAR LAXMIKANT NARHARI , MONDKAR HARISH KASHINATH , AROTE NITIN DNYANESHWAR , PATIL SACHIN SHIVAJI , JADHAV TANAJI SHAMRAO , HAGAVANE NITIN NIVRUTTI , BOPALKAR RAJESH GANPAT
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07C271/20
摘要： The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-l-methyl-lH-benzimidazole-5-yl) carbonyl] -(2-pyridinyl) amino} propanoate and Ethyl-3-{[(2-dichloromethyl-l-methyl -lH-benzimidazole-5-yl)carbonyl]- (2-pyridinyl) amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及制备达比加群酯或其药学上可接受的盐的方法。本发明涉及新的化合物，特别是3 - {[（2-甲酰基-1-甲基-1H-苯并咪唑-5-基）羰基] - （2-吡啶基）氨基}丙酸乙酯和3- { [（2-二氯甲基-1-甲基-1H-苯并咪唑-5-基）羰基] - （2-吡啶基）氨基}丙酸乙酯及其制备方法。本发明还涉及这些新化合物在制备达比加群酯或其药学上可接受的盐中的用途。

5. 发明专利

CA2907839C SYNTHESIS OF DABIGATRAN 未知
公开(公告)号：CA2907839C
公开(公告)日：2021-11-23
申请号：CA2907839
申请日：2014-03-25
申请人： USV LTD
发明人： PATKAR LAXMIKANT NARHARI , MONDKAR HARISH KASHINATH , AROTE NITIN DNYANESHWAR , PATIL SACHIN SHIVAJI , JADHAV TANAJI SHAMRAO , HAGAVANE NITIN NIVRUTTI , BOPALKAR RAJESH GANPAT
IPC分类号： C07D401/12 , A61K31/4439
摘要： The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-l-methyl-lH-benzimidazole-5-yl) carbonyl] -(2-pyridinyl) amino} propanoate and Ethyl-3-{[(2-dichloromethyl-l-methyl -lH-benzimidazole-5-yl)carbonyl]- (2-pyridinyl) amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.

6. 发明专利

DE602005017204D1 未知
公开(公告)号：DE602005017204D1
公开(公告)日：2009-11-26
申请号：DE602005017204
申请日：2005-11-09
申请人： USV LTD
发明人： TARUR VENKATASUBRAMANIAN RADHA , SATHE DHANANJAY GOVIND , BHISE NANDU BABAN , NAIDU AVINASH VENKATRAMAN , AHER UMESH PARASHRAM , PATIL SACHIN SHIVAJI
IPC分类号： C07C253/30 , C07C255/41
摘要： A process for the preparation of highly pure (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (Entacapone). It comprises condensing 3,4-dihydroxy-5-nitro benzaldehyde with N,N-diethyl cyano acetamide in an organic solvent in the presence of an organic base and an acid under reflux conditions followed by distilling off the solvent under vacuum and treating the residue with a lower aliphatic carboxylic acid at 40-8O0 C. The resulting residue is extracted with a chlorinated solvent and the solvent is distilled off under vacuum. The resulting residue is extracted with an organic solvent to obtain crude N,N-diethyl-2-cyano-3-3,4-dihydroxy-5-nitrophenyl)acrylamide. The crude product N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide formed is treated with a mixture of organic alcohol and organic acid in the molar ratio of the crude product to organic alcohol 1:5 to 15 and crude product to organic acid 1:1 to 3 under reflux conditions.

7. 发明专利

IN1117MU2013A "SYNTHESIS OF DABIGATRAN" 未知
公开(公告)号：IN1117MU2013A
公开(公告)日：2015-05-01
申请号：IN1117MU2013
申请日：2013-03-25
申请人： USV LTD
发明人： PATKAR LAXMIKANT NARHARI , MONDKAR HARISH KASHINATH , AROTE NITIN DNYANESHWAR , PATIL SACHIN SHIVAJI
IPC分类号： C07D213/75
摘要： The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-]-methy]-lH-ben2imidazole-5-yl) carbonyl] -(2-pyridinyl) amino} propanoate and Ethyl-3-{[(2-dichloromethyl-l-methyl -lH-benzimidazole-5-yl)carbonyl]- (2-pyridinyl) amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.

8. 发明专利

CA2907839A1 SYNTHESIS OF DABIGATRAN 未知
公开(公告)号：CA2907839A1
公开(公告)日：2014-10-16
申请号：CA2907839
申请日：2014-03-25
申请人： USV LTD
发明人： PATKAR LAXMIKANT NARHARI , MONDKAR HARISH KASHINATH , AROTE NITIN DNYANESHWAR , PATIL SACHIN SHIVAJI , JADHAV TANAJI SHAMRAO , HAGAVANE NITIN NIVRUTTI , BOPALKAR RAJESH GANPAT
IPC分类号： C07D401/12 , A61K31/4439
摘要： The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-l-methyl-lH-benzimidazole-5-yl) carbonyl] -(2-pyridinyl) amino} propanoate and Ethyl-3-{[(2-dichloromethyl-l-methyl -lH-benzimidazole-5-yl)carbonyl]- (2-pyridinyl) amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.

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