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1. 发明申请

WO2008130642A3 IMPROVED PROCESS FOR PREPARING CLOPIDOGREL 审中-公开
公开(公告)号：WO2008130642A3
公开(公告)日：2008-10-30
申请号：PCT/US2008/005041
申请日：2008-04-18
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , PRAVEEN, Kompally , MISTRY, Dhirenkumar, N.
发明人： KANSAL, Vinod, Kumar , PRAVEEN, Kompally , MISTRY, Dhirenkumar, N.
IPC分类号： C07D495/04
摘要： The present invention encompasses processes for the preparation of optically pure clopidogrel camphorsulfonic acid salt without the need to isolate or recover (±) clopidogrel.

2. 发明申请

WO2008027385A3 PROCESSES FOR THE SYNTHESIS OF 5-PHENYL -1 TRITYL-1H-TETRAZOLE 审中-公开
公开(公告)号：WO2008027385A3
公开(公告)日：2008-03-06
申请号：PCT/US2007/018923
申请日：2007-08-28
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , LUNAGARIYA, Vijaykumar, D.
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , LUNAGARIYA, Vijaykumar, D.
IPC分类号： C07D257/04 , C07D403/10
摘要： Provided are processes for the synthesis of 5 -phenyl- 1-trityl-lH-tetrazole, an intermediate useful in the synthesis of irbesartan. The tritylation of 5-phenyl-lH-tetrazole is carried out using phase transfer catalysis in a biphasic solvent system.

3. 发明申请

WO2010009402A9 NILOTINIB INTERMEDIATES AND PREPARATION THEREOF 审中-公开
公开(公告)号：WO2010009402A9
公开(公告)日：2010-01-21
申请号：PCT/US2009/051001
申请日：2009-07-17
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , WANG, Yanling , LI, Jie , KANSAL, Vinod, Kumar , ZHU, Jirang , LIFSHITZ-LIRON, Revital , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , ARIYAMUTHU, Sundaraselvan , PILARSKI, Gideon , HE, Xungui
发明人： WANG, Yanling , LI, Jie , KANSAL, Vinod, Kumar , ZHU, Jirang , LIFSHITZ-LIRON, Revital , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , ARIYAMUTHU, Sundaraselvan , PILARSKI, Gideon , HE, Xungui
IPC分类号： C07D233/61 , C07D401/04 , C07D401/14
摘要： Intermediates of Nilotinib were prepared, including, for example, 3-(trifluoromethyl- 5 -(4-methyl- 1 H-imidazole- 1 -yl)-benzeneamine; 3 -(4-(pyridin-3 -yl)pyrimidin-2-ylamino)-4- methylbenzoyl halogen dihydrochloride; and N-(3-Bromo-5-trifluoromethylphenyl)-4- methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzamide. Nilotinib»3HCl and its crystalline forms are also described.

4. 发明申请

WO2009056993A2 A PROCESS FOR THE SYNTHESIS OF RAMELTEON AND ITS INTERMEDIATES 审中-公开
标题翻译：一个合成中间体及其中间体的方法
公开(公告)号：WO2009056993A2
公开(公告)日：2009-05-07
申请号：PCT/IB2008/003894
申请日：2008-11-03
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Snjay, L. , PATEL, Rakesh , JADAV, Arpan, M.
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Snjay, L. , PATEL, Rakesh , JADAV, Arpan, M.
CPC分类号： C07D307/93
摘要： A process for the preparation of ramelteon and intermediates useful in the process. The process suitable for industrial scale provides increased yield and/or greater purity with fewer process steps.
摘要翻译：用于制备在该方法中有用的拉米尔顿和中间体的方法。适用于工业规模的方法通过较少的工艺步骤提供增加的产率和/或更高的纯度。

5. 发明申请

WO2007053723A3 PROCESS FOR THE PREPARATION OF CEFDINIR 审中-公开
公开(公告)号：WO2007053723A3
公开(公告)日：2007-05-10
申请号：PCT/US2006/042745
申请日：2006-10-31
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh , WIZEL, Shlomit
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh , WIZEL, Shlomit
IPC分类号： C07D513/04
摘要： The invention relates to processes for preparing cefdinir via its potassium and cesium salts.

6. 发明申请

WO2007053722A3 CRYSTALLINE FORM OF CEFDINIR CESIUM SALT 审中-公开
公开(公告)号：WO2007053722A3
公开(公告)日：2007-05-10
申请号：PCT/US2006/042743
申请日：2006-10-31
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh
IPC分类号： C07D513/04
摘要： Provided is the cesium salt of cefdinir, processes for its preparation and its use in the preparation of cefdinir.

7. 发明申请

WO2010045565A1 PROCESS FOR THE SYNTHESIS OF RAMELTEON AND ITS INTERMEDIATES 审中-公开
标题翻译： RAMELTEON及其中间体的合成方法
公开(公告)号：WO2010045565A1
公开(公告)日：2010-04-22
申请号：PCT/US2009/061019
申请日：2009-10-16
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , JADAV, Arpan, M. , DADHANIYA, Pratish , NALAWADE, Jitendra
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , JADAV, Arpan, M. , DADHANIYA, Pratish , NALAWADE, Jitendra
IPC分类号： C07D307/77
CPC分类号： C07D307/77
摘要： The present invention provides processes and intermediates for the synthesis of ramelteon.
摘要翻译：本发明提供了用于合成苎麻的方法和中间体。

8. 发明申请

WO2009023191A2 AN IMPROVED PROCESS FOR THE PREPARATION OF CLARITHROMYCIN 审中-公开
标题翻译：改进氯雷他定的制备方法
公开(公告)号：WO2009023191A2
公开(公告)日：2009-02-19
申请号：PCT/US2008/009633
申请日：2008-08-11
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , GANDHI, Mitesh , PATEL, Rakesh
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , GANDHI, Mitesh , PATEL, Rakesh
CPC分类号： C07H17/08 , C07H1/00
摘要： The present invention includes a process involving a one-pot reaction for preparing erythromycin 9-oxime salt comprising: (a) reacting erythromycin thiocyanate with an ammonium source to obtain erythromycin free base; (b) oximating the C-9 carbonyl of the erythromycin free base by reacting the erythromycin free base with triethylamine and hydroxyl amine hydrochloride to form erythromycin oxime; and (c) reacting the erythromycin oxime obtained in step (b) with an ammonium source to obtain the erythromycin 9-oxime salt. The present invention is also drawn to a one-pot reaction for preparing clarithromycin starting with the one-pot reaction for preparing erythromycin 9-oxime salt, further comprising after step (c): (d) silylating the hydroxy groups at the oxime group, and the 2" and 4> λ positions of the erythromycin 9-oxime salt to obtain a silylated derivative; (e) methylating the hydroxy group at the 6 position of the silylated derivative using at least one methylating agent in the presence of at least one inorganic base to obtain SMOP, wherein SMOP is 6-O-methyl-2', 4"-bis(trimethylsilyl)- erythromycin A 9-O-(2-methoxyprop-2-yl)oxime; and (f) converting the SMOP into clarithromycin using at least one deoximating agent in the presence of aqueous ethanol.
摘要翻译：本发明包括一种用于制备红霉素9-肟盐的一锅反应的方法，包括：（a）将红霉素硫氰酸盐与铵源反应以获得游离红霉素的碱; （b）通过使红霉素游离碱与三乙胺和羟胺盐酸盐反应，使红霉素游离碱的C-9羰基肟化，形成红霉素肟; 和（c）使步骤（b）中获得的红霉素肟与铵源反应，得到红霉素9-肟盐。本发明还涉及从用于制备红霉素9-肟盐的一锅反应开始制备克拉霉素的一锅反应，还包括在步骤（c）之后：（d）使肟基上的羟基甲硅烷基化，和红霉素9-肟盐的2“和4”→位置，以获得甲硅烷基化衍生物;（e）使用至少一种甲基化试剂在甲硅烷基化衍生物的6位甲基化存在下，无机碱以获得SMOP，其中SMOP为6-O-甲基-2'，4“ - 双（三甲基甲硅烷基） - 红霉素A 9-O-（2-甲氧基丙-2-基）肟; 和（f）在含水乙醇的存在下使用至少一种去肟剂将SMOP转化成克拉霉素。

9. 发明申请

WO2008151170A2 PROCESS FOR THE SYNTHESIS OF RAMELTEON AND ITS INTERMEDIATES 审中-公开
标题翻译： RAMELTEON及其中间体的合成方法
公开(公告)号：WO2008151170A2
公开(公告)日：2008-12-11
申请号：PCT/US2008/065590
申请日：2008-06-02
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , RAFILOVICH, Michal , BEN MOHA-LERMAN, Elena , LIFSHITZ-LIRON, Revital
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , RAFILOVICH, Michal , BEN MOHA-LERMAN, Elena , LIFSHITZ-LIRON, Revital
IPC分类号： C07D307/77 , A61K31/343 , A61P43/00
CPC分类号： C07D307/93 , C07D307/79
摘要： The present invention provides processes and intermediates for the synthesis of ramelteon.
摘要翻译：本发明提供了用于合成苎麻的方法和中间体。

10. 发明申请

WO2007053724A2 CRYSTALLINE FORMS OF CEFDINIR POTASSIUM SALT 审中-公开
标题翻译： CEFDINIR钾盐的晶体形式
公开(公告)号：WO2007053724A2
公开(公告)日：2007-05-10
申请号：PCT/US2006/042749
申请日：2006-10-31
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh , WIZEL, Shlomit , HILDESHEIM, Jean
发明人： KANSAL, Vinod, Kumar , MISTRY, Dhirenkumar, N. , PANDEY, Saurabh , PATEL, Rakesh , WIZEL, Shlomit , HILDESHEIM, Jean
IPC分类号： C07D501/00 , A61K31/41 , A61P31/12
CPC分类号： C07D501/22 , C07D501/00
摘要： The present invention encompasses the solid state chemistry of cefdinir potassium salt.
摘要翻译：本发明包括头孢地尼钾盐的固态化学。

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