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91. 发明申请

WO2010023676A3 PROCESS FOR PREPARING LAMIVUDINE POLYMORPH FORM 审中-公开
公开(公告)号：WO2010023676A3
公开(公告)日：2010-03-04
申请号：PCT/IN2008/000556
申请日：2008-09-01
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SUBASH CHANDER REDDY, Kesireddy
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SUBASH CHANDER REDDY, Kesireddy
IPC分类号： C07D411/04
摘要： The invention relates to a process for the preparation of stable lamivudine polymorph form and to a composition comprising thereof.

92. 发明申请

WO2010004571A2 PROCESS FOR PURIFICATION OF RABEPRAZOLE SODIUM 审中-公开
标题翻译：精制雷贝拉唑钠的方法
公开(公告)号：WO2010004571A2
公开(公告)日：2010-01-14
申请号：PCT/IN2008/000433
申请日：2008-07-07
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SAMBI REDDY, Jonnala
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SAMBI REDDY, Jonnala
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： There is provided a process for preparing amorphous rabeprazole sodium. Thus, for example, sodium hydroxide was dissolved in methanol. Rabeprazole was added to the solution and stirred at 25 - 35°C for 1 hour. Methanol was distilled off from the reaction mass, dichloromethane was added to the residual mass and the contents were stirred to obtain solution. The solution was added to cyclohexane. The contents were stirred at 25 - 35°C for 30 minutes, centrifuged the material and washed at 60 - 65°C to obtain amorphous rabeprazole sodium.
摘要翻译：提供了一种制备无定形雷贝拉唑钠的方法。因此，例如，将氢氧化钠溶解在甲醇中。将雷贝拉唑加入到溶液中，并在25-35℃下搅拌1小时。从反应物质中蒸出甲醇，向残余物质中加入二氯甲烷并搅拌内容物以获得溶液。将该溶液加入到环己烷中。将内容物在25-35℃搅拌30分钟，离心该物质并在60-65℃洗涤，得到无定形雷贝拉唑钠。

93. 发明申请

WO2009144734A1 PROCESS FOR PREPARATION OF TADALAFIL 审中-公开
标题翻译：制备方法
公开(公告)号：WO2009144734A1
公开(公告)日：2009-12-03
申请号：PCT/IN2008/000339
申请日：2008-05-28
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , VSV PRASAD, Valivarthi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , VSV PRASAD, Valivarthi
IPC分类号： C07D471/22 , C07D417/14
CPC分类号： C07D417/14
摘要： It has been found that tadalafil can be obtained in high purity when (6R,12aR)-methyl-1,2,3,4-tertahydro-2-chloroacetyL-1-(3,4-methylenedioxy- phenyl)-9H-pyrido[3,4-b]indole-3-carboxylate is reacted with methylamine in methanol in specific quantities for a specific reaction time. It has also been found that (6R,12aR)-methyl-1,2,3,4-tertahydro-2-chloroacetyl-1-(3,4-methylenedioxy- phenyl)-9H-pyrido[3,4-b]indole-3-carboxylate, the key intermediate in the preparation of tadalafil, may be obtained in higher yield from D-Tryptophan methyl ester without isolationg intermediate as solid.
摘要翻译：已经发现，当（6R，12aR） - 甲基-1,2,3,4-四氢-2-氯乙酰基-L-（3,4-亚甲二氧基 - 苯基）-9H-吡啶并[ [3,4-b]吲哚-3-羧酸乙酯与甲胺在甲醇中反应特定反应时间。还已经发现，（6R，12aR） - 甲基-1,2,3,4-四氢-2-氯乙酰基-1-（3,4-亚甲二氧基 - 苯基）-9H-吡啶并[3,4-b] 吲哚-3-羧酸盐是制备他达拉非的关键中间体，可以从没有分离出中间体作为固体的D-色氨酸甲酯以更高的产率获得。

94. 发明申请

WO2009125416A3 PROCESS FOR PREPARATION OF VALSARTAN INTERMEDIATE 审中-公开
公开(公告)号：WO2009125416A3
公开(公告)日：2009-10-15
申请号：PCT/IN2008/000227
申请日：2008-04-07
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , RAMAKRISHNA REDDY, Matta
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , RAMAKRISHNA REDDY, Matta
IPC分类号： C07C253/30 , C07C253/34 , C07C255/58
摘要： The present invention provides a process for preparation of a key intermediate of valsartan in a pure form and use of this intermediate for the preparation of valsartan or a pharmaceutically acceptable salt in pure form.

95. 发明申请

WO2009125415A1 AMORPHOUS FORM OF SILDENAFIL CITRATE 审中-公开
标题翻译：硅酸钙的非晶形式
公开(公告)号：WO2009125415A1
公开(公告)日：2009-10-15
申请号：PCT/IN2008/000226
申请日：2008-04-07
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , VSV PRASAD, Valivarthi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , VSV PRASAD, Valivarthi
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to a novel amorphous form of sildenafil citrate, to a process for the preparation thereof and to a composition comprising thereof.
摘要翻译：本发明涉及一种新型无定形形式的西地那非柠檬酸盐，其制备方法及其组合物。

96. 发明申请

WO2010089753A2 NOVEL POLYMORPHS OF LOPINAVIR 审中-公开
标题翻译： LOPINAVIR的新型POLYMORPHS
公开(公告)号：WO2010089753A2
公开(公告)日：2010-08-12
申请号：PCT/IN2009/000083
申请日：2009-02-06
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SUBASH CHANDER REDDY, Kesireddy
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SUBASH CHANDER REDDY, Kesireddy
IPC分类号： C07D239/10
CPC分类号： C07D239/10
摘要： The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100 °C for 10 hours to give lopinavir desolvated crystalline form H1.
摘要翻译：本发明提供一种新型的洛匹那韦的环己烷溶剂合物形式及其制备方法。本发明还提供了一种新型脱盐结晶形式的洛匹那韦，其制备方法和含有它的药物组合物。因此，例如，将洛匹那韦环己烷溶剂化物在100℃下加热10小时，得到脱蛋白脱水结晶形式H1。

97. 发明申请

WO2010052726A1 NOVEL POLYMORPH OF MOXIFLOXACIN HYDROCHLORIDE 审中-公开
标题翻译：莫西沙星氢氯化物的新型聚合物
公开(公告)号：WO2010052726A1
公开(公告)日：2010-05-14
申请号：PCT/IN2008/000759
申请日：2008-11-06
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , MADHAN MOHAN REDDY, Musku , BHARATH REDDY, Deevireddy
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , MADHAN MOHAN REDDY, Musku , BHARATH REDDY, Deevireddy
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel polymorph of moxifloxacin hydrochloride, processes for its preparation and to pharmaceutical compositions containing it. Thus, for example moxifloxacin hydrochloride is suspended in methanol and water and the p H is adjusted to 1.0 - 2.0 with concentrated hydrochloric acid at 25 °C and the separated solid is collected and dried to obtain moxifloxacin hydrochloride monohydrate polymorph IV.
摘要翻译：本发明涉及盐酸莫西沙星的新型多晶型物，其制备方法和含有它的药物组合物。因此，例如将莫西沙星盐酸盐悬浮在甲醇和水中，用浓盐酸在25℃下将pH调节至1.0-2.0，收集分离的固体并干燥，得到盐酸莫西沙星一水合物多晶型IV。

98. 发明申请

WO2008026216A2 PROCESS FOR PURIFICATION OF APREPITANT 审中-公开
标题翻译：净化方法
公开(公告)号：WO2008026216A2
公开(公告)日：2008-03-06
申请号：PCT/IN2006/000312
申请日：2006-08-28
申请人： HETERO DRUGS LIMITED , PARTHASARADHI, Reddy, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SRINIVASA RAO, Thungathurthy
发明人： PARTHASARADHI, Reddy, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SRINIVASA RAO, Thungathurthy
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[I (RS)- [3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl- methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having mean particle size of less than about 11.5 microns, process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having the content of diastereomeric impurity of 1.1 % is dissolved in ethyl acetate at 700C, the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0 - 50C to give pure aprepitant substantially free of diastereomeric impurity.
摘要翻译：本发明涉及一种获得基本上不含不期望的非对映体异构体的纯阿拉米特的方法，即5- [2（S） - [I（RS） - [3,5-双（三氟甲基） - 苯基） - 乙氧基] -3- （S） - （4-氟苯基） - 吗啉-4-基 - 甲基] -3,4-二氢-2H-1,2,4-三唑-3-酮。本发明进一步提供了一种改进的制备阿瑞匹坦晶型II的方法。本发明还涉及新型无定形形式的阿拉米特，其制备方法和包含它的药物组合物。本发明还涉及具有小于约11.5微米的平均粒度的制剂，其制备方法和包含其的药物组合物。因此，例如，将具有1.1％非对映异构体杂质的阿瑞消制剂在70℃下溶于乙酸乙酯中，通过蒸馏除去乙酸乙酯将溶液浓缩至初始体积的一半，在0-50℃收集所得固体，得到基本上不含非对映异构体杂质的纯APR。

99. 发明申请

WO2007054951A1 PROCESS FOR AMORPHOUS ESOMEPRAZOLE 审中-公开
标题翻译：异辛醚的方法
公开(公告)号：WO2007054951A1
公开(公告)日：2007-05-18
申请号：PCT/IN2005/000367
申请日：2005-11-14
申请人： HETERO DRUGS LIMITED , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a commercially viable process for preparation of amorphous esomeprazole. Thus, amorphous esomeprazole is prepared by suspending esomeprazole in water and then subjecting the suspension to lyophilization at -70°C.
摘要翻译：本发明涉及用于制备无定形艾美拉唑的商业上可行的方法。因此，通过将艾美拉唑悬浮在水中，然后使该悬浮液在-70℃下冻干来制备无定形艾美拉唑。

100. 发明申请

WO2006117794A1 A NOVEL CRYSTALLINE FORM OF CEFDINIR 审中-公开
标题翻译： CEFDINIR的新型晶体形式
公开(公告)号：WO2006117794A1
公开(公告)日：2006-11-09
申请号：PCT/IN2005/000135
申请日：2005-05-02
申请人： HETERO DRUGS LIMITED , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , MURALI, Nagabelli
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , MURALI, Nagabelli
IPC分类号： C07D501/22
CPC分类号： C07D501/00
摘要： The present invention relates to a novel crystalline form of cefdinir, process for its preparation and to a pharmaceutical composition containing it. Thus, cefdinir is added to water at 20 - 25 ° C and then hydrochloric acid (18 %) is added at 20 - 25 ° C to get a clear solution. To the solution activated carbon is added at 20 - 25 ° C, stirred for 30 minutes, filtered through hyflo bed and washed with water. Then the pH of the filtrate is adjusted to 6.5 with saturated bicarbonate solution at 5 - 8 ° C, stirred for clear solution, activated carbon is added and stirred for 30 minutes at 5 - 8 ° C. The reaction mass is filtered through hyflo bed, washed with water, 1:1 sulfuric acid is dumped to the above solution at 5 - 8 ° C (pH: 2.8) and then stirred for 60 minutes at 3 - 5 ° C. The resulting solid is filtered, washed with water and dried at 40 ° C under vacuum to give cefdinir form H.
摘要翻译：本发明涉及一种新型的头孢地尼结晶形式，其制备方法和含有它的药物组合物。因此，将cefdinir加入到20-25℃的水中，然后在20-25℃加入盐酸（18％），得到澄清溶液。向溶液中加入活性炭，在20-25℃下搅拌30分钟，通过hyflo过滤，并用水洗涤。然后用5-8℃的饱和碳酸氢盐溶液将滤液的pH调节至6.5，搅拌至澄清溶液，加入活性炭并在5-8℃下搅拌30分钟 ℃。将反应物质通过悬浮床过滤，用水洗涤，在5-8℃（pH = 2.8）将1:1硫酸倾倒到上述溶液中，然后在3℃下搅拌60分钟 -5℃。将所得固体过滤，用水洗涤，并在40℃真空干燥，得到头孢地尼甲型H.

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