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1. 发明申请

WO2006011157A2 A NOVEL METHOD FOR THE PREPARATION OF ARYL PIPERAZINYL-HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：一种制备芳基哌嗪类杂环化合物的新方法
公开(公告)号：WO2006011157A2
公开(公告)日：2006-02-02
申请号：PCT/IN2005000205
申请日：2005-06-16
申请人： LUPIN LTD , TYAGI OM DUTT , SRIVASTAVA TUSHAR KUMAR , CHAUHAN YOGENDRA KUMAR , NALAM VASANTH KUMAR
发明人： TYAGI OM DUTT , SRIVASTAVA TUSHAR KUMAR , CHAUHAN YOGENDRA KUMAR , NALAM VASANTH KUMAR
IPC分类号： C07D417/00
CPC分类号： C07D417/12
摘要： A novel method for preparing a compound of formula (I), which comprises of coupling the piperazine derivative of formula (II), with alkyl halide containing compound of the formula (III), by heating in solvent free conditions or, optionally, in a minimum quantity of non-aqueous suspending liquid, in presence of a catalyst and a neutralizing agent to neutralize the hydrohalic acid.
摘要翻译：一种制备式（I）化合物的新方法，其包括将式（II）的哌嗪衍生物与含烷基卤的式（III）化合物偶联，通过在无溶剂条件下加热，或任选地在在催化剂和中和剂存在下，最少量的非水悬浮液，以中和氢卤酸。

2. 发明申请

WO2005094800A3 A CO-PRECIPITATED CEFEPIME COMPOSITION AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：共沉淀的头峰组合物及其制备方法
公开(公告)号：WO2005094800A3
公开(公告)日：2005-11-24
申请号：PCT/IN2005000095
申请日：2005-03-30
申请人： LUPIN LTD , TYAGI OM DUTT , CHAUHAN YOGENDRA KUMAR , SRIVASTAVA TUSHAR KUMAR
发明人： TYAGI OM DUTT , CHAUHAN YOGENDRA KUMAR , SRIVASTAVA TUSHAR KUMAR
IPC分类号： A61K31/546 , C07D501/00
CPC分类号： A61K31/546
摘要： The present invention provides a stable and sterile composition of Cefepime with a pharmaceutically acceptable non-toxic organic and inorganic base in high purity which exhibits good thermal stability which is obtained by co precipitation of composition containing non-sterile Cefepime and non-sterile pharmaceutically acceptable base. The method of preparing the co-precipitated composition of Cefepime with pharmaceutically acceptable non-toxic base comprises of, i) dissolving a composition containing mixture of non sterile Cefepime and a non sterile pharmaceutically acceptable non-toxic organic or inorganic base in water to obtain a clear aqueous solution having a pH in the range of 3.5-7 and ii) filtration of aqueous solution through 0.2 micron membrane filter and then adding the clear aqueous solution to a suitable an organic solvent followed by stirring, filtration and drying.
摘要翻译：本发明提供了具有高纯度的药学上可接受的无毒有机和无机碱的稳定且无菌的头孢吡肟组合物，其显示出良好的热稳定性，其通过共沉淀包含非无菌头孢吡肟和非无菌药学上可接受的碱。制备头孢吡肟与药学上可接受的无毒碱的共沉淀组合物的方法包括：i）将含有非无菌头孢吡肟和非无菌药学上可接受的无毒有机或无机碱的混合物的组合物溶解于水中以获得澄清的pH值为3.5-7的水溶液，和ii）通过0.2微米膜过滤器过滤水溶液，然后将澄清的水溶液加入合适的有机溶剂中，随后搅拌，过滤并干燥。

3. 发明申请

WO2009090544A2 PROCESS FOR PRODUCING AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译：生产无花果ATORVASTATIN钙的方法
公开(公告)号：WO2009090544A2
公开(公告)日：2009-07-23
申请号：PCT/IB2009000068
申请日：2009-01-15
申请人： MATRIX LAB LTD , RAO P V SRINIVAS , CHAUHAN YOGENDRA KUMAR , SRIVASTAVA TUSHAR KUMAR , RAY PURNA CHANDRA , TYAGI OM DUTT
发明人： RAO P V SRINIVAS , CHAUHAN YOGENDRA KUMAR , SRIVASTAVA TUSHAR KUMAR , RAY PURNA CHANDRA , TYAGI OM DUTT
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： Disclosed herein is an improved process for producing amorphous atorvastatin calcium and a method of packaging thereof.
摘要翻译：本文公开了一种生产无定形阿托伐他汀钙的改进方法及其包装方法。

4. 发明申请

WO2006109323B1 PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES 审中-公开
标题翻译： [2-甲基-5-苯基-3-（哌嗪-1-基]乙基]]吡咯衍生物的制备
公开(公告)号：WO2006109323B1
公开(公告)日：2006-11-30
申请号：PCT/IN2006000115
申请日：2006-04-05
申请人： LUPIN LTD , ARORA SUDERSHAN KUMAR , SINHA NEELIMA , JAIN SANJAY , UPADHAYAYA RAM SHANKAR , TYAGI OM DUTT , NALAM VASANTH , CHAUHAN YOGENDRA KUMAR
发明人： ARORA SUDERSHAN KUMAR , SINHA NEELIMA , JAIN SANJAY , UPADHAYAYA RAM SHANKAR , TYAGI OM DUTT , NALAM VASANTH , CHAUHAN YOGENDRA KUMAR
IPC分类号： C07D207/50 , A61K31/4025 , A61P31/06
CPC分类号： C07D207/50 , C07D207/335 , C07D401/04 , C07D401/12
摘要： A process for the preparation of compounds of Formula (I) and their pharmaceutically acceptable acid addition salt wherein R 1 is phenyl or substituted phenyl, R 3 is selected from a group of formula (a), n = 0-2 and X = -NCH 3 , CH 2 , S, SO, or SO 2 wherein R 2 and R 5 are as defined herein.
摘要翻译：制备式（I）化合物及其药学上可接受的酸加成盐的方法，其中R 1是苯基或取代的苯基，R 3 3选自式（a），n = 0-2和X = -NCH 3，CH 2，S，SO或SO 2其中R R 2和R 5如本文所定义。

5. 发明申请

WO2008152653A3 AN IMPROVED PROCESS FOR THE PREPARATION OF TAMSULOSIN HYDROCHLORIDE 审中-公开
标题翻译：一种改进制备TAMSULOSIN HYDROCHLORIDE的方法
公开(公告)号：WO2008152653A3
公开(公告)日：2010-04-29
申请号：PCT/IN2008000367
申请日：2008-06-10
申请人： MATRIX LAB LTD , TYAGI OM DUTT , RAY PURNA CHANDRA , RAO KONUDULA BABU , CHAUHAN YOGENDRA KUMAR , NARAYANA BANDLAMUDI VEERA , REDDY DOSARALA SIVA PRASAD
发明人： TYAGI OM DUTT , RAY PURNA CHANDRA , RAO KONUDULA BABU , CHAUHAN YOGENDRA KUMAR , NARAYANA BANDLAMUDI VEERA , REDDY DOSARALA SIVA PRASAD
IPC分类号： C07C311/37 , C07C209/08 , C07C209/16
CPC分类号： C07C311/37 , C07B2200/07 , C07C303/40
摘要： The invention relates an improved process for preparing the (R)-(-)5-[2-[[2-(2-ethoxyphenoxyethyl]amino]propyl]-2-methoxybenzenesulfonamide of Formula (I): and its pharmaceutically acceptable salts.
摘要翻译：本发明涉及制备式（I）所示的（R） - （ - ） - [ - （ - ） - [ - [ - （ - ） - [ - [ - （（2-乙氧基苯氧基乙基）氨基]丙基] -2-甲氧基苯磺酰胺及其药学上可接受的盐。

6. 发明申请

WO2008142706A3 NOVEL PROCESS FOR THE SYNTHESIS OF PIOGLITAZONE AND ITS SALTS THEREOF 审中-公开
标题翻译：用于合成PIOGLITAZONE及其盐的新方法
公开(公告)号：WO2008142706A3
公开(公告)日：2009-12-03
申请号：PCT/IN2008000315
申请日：2008-05-19
申请人： MATRIX LAB LTD , TYAGI OM DUTT , RAY PURNA CHANDRA , RAO KONUDULA BABU , CHAUHAN YOGENDRA KUMAR , NALLA RAJA MAHENDAR REDDY , PRASAD GADAMSETTY
发明人： TYAGI OM DUTT , RAY PURNA CHANDRA , RAO KONUDULA BABU , CHAUHAN YOGENDRA KUMAR , NALLA RAJA MAHENDAR REDDY , PRASAD GADAMSETTY
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Present invention relates to an improved process for the preparation of thiazolidinedione derivatives. Further the invention provides the hydrogenation of acid addition salt of benzylidene compound with less reducing agent under low Hydrogen gas pressure to get substantially pure thiazolidinedione derivatives with improved yields.
摘要翻译：本发明涉及一种制备噻唑烷二酮衍生物的改进方法。此外，本发明提供了在低氢气压力下用较少还原剂氢化亚苄基化合物的酸加成盐，以获得基本上纯的噻唑烷二酮衍生物，其产率提高。

7. 发明申请

WO2008126105A2 IMPROVED PROCESS FOR THE PREPARATION OF ZOPICLONE AND IT'S ENANTIOMERICALLY ENRICHED ISOMER 审中-公开
标题翻译：改进的ZOPICLONE及其具有良好特征的异构体的方法
公开(公告)号：WO2008126105A2
公开(公告)日：2008-10-23
申请号：PCT/IN2008000239
申请日：2008-04-10
申请人： MATRIX LAB LTD , TYAGI OM DUTT , SRIVASTAVA TUSHAR KUMAR , PRASAD VELLANKI SIVA RAM , RAGHO RANE DNYANDEV , DURGA RAO BANDI NAGA , SRINIVAS REDDY DAGGULA
发明人： TYAGI OM DUTT , SRIVASTAVA TUSHAR KUMAR , PRASAD VELLANKI SIVA RAM , RAGHO RANE DNYANDEV , DURGA RAO BANDI NAGA , SRINIVAS REDDY DAGGULA
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2- yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo [3,4-b] pyrazine is reacted with 1-chloro- carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro- pyrrolo- [3,4-b] - pyrazine of the intermediate which can be converted to racemic Zopiclone.
摘要翻译：本发明涉及一种改良的佐匹克隆及其对映体富集异构体（依佐替普）的制备方法。 6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢吡咯并[3,4-b]吡嗪在碱存在下与1-氯 - 羰基-4-甲基哌嗪反应土壤金属碳酸盐，氢氧化物或氧化物在溶剂介质中给予佐匹克隆。将其与光学活性酸在水和水混溶性有机溶剂的混合物中反应，随后加工得到依佐替普。本发明还涉及将（R）或（S）佐匹克隆转化成6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢 - 吡咯并[3 ，4-b] - 吡嗪，其可以转化为外消旋佐匹克隆。

8. 发明申请

WO2004039811A3 A METHOD FOR MANUFACTURE OF CEFTIOFUR 审中-公开
标题翻译：一种制造CEFTIOFUR的方法
公开(公告)号：WO2004039811A3
公开(公告)日：2004-08-12
申请号：PCT/IN0300345
申请日：2003-10-27
申请人： LUPIN LTD , TYAGI OM DUTT , RICHHARIYA SANTOSH KUMAR , PAWAR RAJESH KUMAR RAMCHANDRA , CHAVAN YUVARAJ ATMARAM
发明人： TYAGI OM DUTT , RICHHARIYA SANTOSH KUMAR , PAWAR RAJESH KUMAR RAMCHANDRA , CHAVAN YUVARAJ ATMARAM
IPC分类号： C07D417/14 , C07D501/36
CPC分类号： C07D417/14
摘要： A process for preparation of ceftiofur of formula (I) of high purity and substantially free from impurities is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic acid-2-benzothiazolyl thioester of formula (II), with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III) in the presence of a mixture of an water-immescible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (I) substantially free of impurities by, d) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase, e) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, and f) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a co-solvent.
摘要翻译：公开了一种制备高纯度且基本上不含杂质的式（I）头孢噻呋的方法。该方法包括使式（II）的[2-（2-氨基噻唑-4-基）] - 2-顺式 - 甲氧基亚氨基乙酸-2-苯并噻唑基硫酯与7-氨基-3-（2-呋喃羰基硫甲基）-3 （III）的头孢烯-4-羧酸在水不可渗透的惰性有机溶剂和水的混合物存在下并且在有机碱存在下反应并分离基本上不含杂质的式（I）头孢噻呋， d）向反应混合物中加入水并选择性分配有机相中的杂质和与水相中的碱形成盐形式的头孢噻呋（I），e）将含有头孢噻呋（I）的水相酸化成形式在含有水混溶性和水不混溶性有机溶剂的混合物存在下，在含碱金属盐或碱土金属盐的饱和水溶液存在下，将所述碱与盐分离，以将头孢噻呋（I）分配到有机相，和f）分离高纯度和基本的头孢噻呋（I） y通过蒸发有机溶剂而不含杂质或通过加入共溶剂沉淀。

9. 发明申请

WO2006109324A3 PROCESSES FOR PREPARATION OF AMORPHOUS CEFEPIME ACID ADDITION SALTS 审中-公开
标题翻译：制备非晶形磷酸添加剂的方法
公开(公告)号：WO2006109324A3
公开(公告)日：2007-04-05
申请号：PCT/IN2006000125
申请日：2006-04-12
申请人： LUPIN LTD , TYAGI OM DUTT , MEHARE KISHOR GULABRAO , DESHMUKH SANJAY
发明人： TYAGI OM DUTT , MEHARE KISHOR GULABRAO , DESHMUKH SANJAY
IPC分类号： C07D501/00 , A61K31/545
CPC分类号： C07D501/00 , C07D501/56
摘要： The present invention provides processes for the preparation amorphous form of Cefepime acid addition salt in high purity which exhibits very good thermal stability on storage. The processes are simple and cost-effective. The selective solvent precipitation method comprises of: (a) dissolving cefepime acid addition salt or solvates thereof in a polar solvent, (b) addition of less polar solvent to the solution obtained in step (a) to precipitate out cefepime acid addition salt followed by isolation of solid by filtration and drying or alternatively, (a) dissolving cefepime acid addition salt or solvates thereof in a polar solvent, (b) addition of the solution obtained in step (a) to less polar solvent to precipitate out cefepime acid addition salt followed by isolation of solid by filtration and drying. The further method involves spray drying of solution of cefepime acid addition salt or solvates thereof prepared in a polar solvent.
摘要翻译：本发明提供了高纯度制备非晶态Cefepime酸加成盐的方法，其在储存时表现出非常好的热稳定性。流程简单，成本效益高。选择性溶剂沉淀法包括：（a）将头孢吡肟酸加成盐或溶剂合物溶解在极性溶剂中，（b）向步骤（a）获得的溶液中加入极性极少的溶剂，沉淀出头孢吡肟酸加成盐，通过过滤和干燥分离固体，或者（a）将头孢吡肟酸加成盐或溶剂合物溶解在极性溶剂中，（b）将步骤（a）中获得的溶液加入到极性较小的溶剂中以沉淀出头孢吡肟酸加成盐然后通过过滤和干燥分离固体。另外的方法包括喷雾干燥在极性溶剂中制备的头孢吡肟酸加成盐或溶剂合物溶液。

10. 发明申请

WO2009087679A3 PROCESS FOR PREPARING POLYMORPHIC FORMS OF (S)-6-CHLORO-(CYCLOPROPYLETHYNYL)-1,4-DIHYDRO-4-(TRIFLUOROMETHYL)-2H-3,1-BENZOXAZIN-2-ONE 审中-公开
标题翻译：制备（S）-6-氯 - （环丙基乙基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶型的方法
公开(公告)号：WO2009087679A3
公开(公告)日：2010-01-21
申请号：PCT/IN2008000860
申请日：2008-12-24
申请人： MATRIX LAB LTD , TYAGI OM DUTT , JETTI RAM K R , RAMIREDDY B A
发明人： TYAGI OM DUTT , JETTI RAM K R , RAMIREDDY B A
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： Disclosed herein is a novel process for preparing polymorphic Forms of (S)-6- chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2- one referred as M1, I, II, ß, and ?.
摘要翻译：本文公开了一种制备（S）-6-氯 - （环丙基乙炔基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶形式的新颖方法，称为M1， I，II，ß和？

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