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1. 发明申请

WO2008078330A1 IMPROVED PROCESS FOR EPROSARTAN 审中-公开
标题翻译： EPROSARTAN的改进方法
公开(公告)号：WO2008078330A1
公开(公告)日：2008-07-03
申请号：PCT/IN2006/000507
申请日：2006-12-27
申请人： HETERO DRUGS LIMITED , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： The present invention provides an improved and commercially viable process for preparation of eprosartan and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. Thus, for example, methyl 4-[[2-butyl-5-formyl-1 H-imidazol-1-yl]methyl]benzoate is reacted with ethyl 2- carboxy-3-(2-thienyl)propionate in the presence of a base, such as piperidine or piperidinium propionate in propionic acid, in cyclohexane solvent to give ethyl ( αΕ )- α -[[2-n-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1 H -imidazol-5- yl]methylene-2-thiophene propionate substantially free of decarboxylate impurity namely, ethyl 3-(2-thienyl)propionate, which is then subjected to base hydrolysis followed by treatment with methanesulfonic acid to obtain eprosartan mesylate in high purity and in high yield.
摘要翻译：本发明提供了以高纯度和高产率制备依普罗沙坦及其药学上可接受的酸加成盐的改进和商业上可行的方法。因此，例如，4 - [[2-丁基-5-甲酰基-1H-咪唑-1-基]甲基]苯甲酸甲酯与2-羧基-3-（2-噻吩基）丙酸乙酯在碱（例如哌啶或丙酸哌啶鎓）在丙酸中的溶液中，在环己烷溶剂中反应，得到（α）-α - [[2-正丁基-1 - [[4-（甲氧基羰基）苯基]甲基] 咪唑-5-基]亚甲基-2-噻吩丙酸酯，基本上不含脱羧酸盐杂质即3-（2-噻吩基）丙酸乙酯，然后进行碱水解，然后用甲磺酸处理，得到高纯度的甲磺酸依普罗沙坦并以高产量。

2. 发明申请

WO2009013760A2 EPROSARTAN MESYLATE CRYSTALLINE PARTICLES AND A PROCESS FOR PREPARING PURE EPROSARTAN 审中-公开
标题翻译： EPROSARTAN MESYLATE晶体颗粒和纯EPROSARTAN的制备方法
公开(公告)号：WO2009013760A2
公开(公告)日：2009-01-29
申请号：PCT/IN2007/000309
申请日：2007-07-25
申请人： HETERO DRUGS LIMITED , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： The present invention relates to eprosartan mesylate particles having relatively larger surface area, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles. The present invention further relates to crystalline solid of eprosartan acetate, to a process for its preparation and to a pharmaceutical composition comprising it. The present invention also provides substantially pure eprosartan free base and process for its preparation.
摘要翻译：本发明涉及具有相对较大表面积的甲磺酸依普罗沙坦颗粒，用于制造所述结晶颗粒的方法，以及包含所述结晶颗粒的药物组合物。本发明还涉及醋酸依普罗沙坦的结晶固体，其制备方法和包含其的药物组合物。本发明还提供了基本上纯的依普罗沙坦游离碱及其制备方法。

3. 发明申请

WO2009122421A2 IMPROVED PROCESS FOR EPROSARTAN INTERMEDIATE 审中-公开
标题翻译： EPROSARTAN中间件的改进过程
公开(公告)号：WO2009122421A2
公开(公告)日：2009-10-08
申请号：PCT/IN2008/000211
申请日：2008-03-31
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , PETER PAUL RAJ, Medabalimi
IPC分类号： C07D401/04
CPC分类号： C07D409/06
摘要： The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1 H-imidazole-5-yl] methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-butyl-5-formyl-1 H-imidazole-1-yl]methyl]benzoic acid methyl ester is reacted with ethyl 2-carboxy-3-(2-thienyl) propionate in the presence of piperidinium propionate in diisopropyl ether or a mixture of n- hexane and a solvent selected from toluene and cyclohexane, optionally purifying the crude compound to obtain (E)-α-[[2-butyl-1-[[4-(methoxy carbonyl)phenyl]methyl]-1 H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester substantially free of 3-(2-thienyl) propanoic acid ethyl ester impurity.
摘要翻译：本发明提供了制备（E）-a - [[2-丁基-1 - [[4-（甲氧基羰基）苯基]甲基] -1H-咪唑-5-基]亚甲基] -2- 噻吩丙酸乙酯，产率高。因此，例如，将4 - [[2-丁基-5-甲酰基-1H-咪唑-1-基]甲基]苯甲酸甲酯与2-羧基-3-（2-噻吩基）丙酸乙酯在在二异丙基醚或正己烷和选自甲苯和环己烷的溶剂的混合物中存在丙酸哌啶酯，任选地纯化粗化合物，得到（E）-α-[[2-丁基-1 - [[4-（甲氧基羰基）苯基]甲基] -1H-咪唑-5-基]亚甲基] -2-噻吩丙酸乙酯，基本上不含3-（2-噻吩基）丙酸乙酯杂质。

4. 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。

5. 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.

6. 发明申请

WO2006030449A1 CRYSTALLINE ALFUZOSIN BASE 审中-公开
标题翻译：水晶碱基
公开(公告)号：WO2006030449A1
公开(公告)日：2006-03-23
申请号：PCT/IN2004/000292
申请日：2004-09-16
申请人： HETERO DRUGS LIMITED , 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： C07D405/12
CPC分类号： C07D405/12
摘要： The present invention relates to crystalline alfuzosin base and processes for preparation of the said crystalline solid. Thus, for example, alfuzosin base (HPLC purity: 97%) is added to methanol and heated to reflux to form a clear solution, the solution is cooled to 25° - 30°C and stirred for 12 hours at the same temperature, the resulting solution is cooled to 10°- 15°C and stirred for 2 hours, and the resulting solid is filtered, washed with methanol and dried at 50°- 60°C for 4 hours to give 99.95% pure alfuzosin base.
摘要翻译：本发明涉及结晶阿夫唑嗪碱及其制备方法。因此，例如，将阿夫唑嗪碱（HPLC纯度：97％）加入到甲醇中并加热回流以形成澄清溶液，将溶液冷却至25℃-30℃，在相同温度下搅拌12小时，将所得溶液冷却至10〜15℃，搅拌2小时，过滤所得固体，用甲醇洗涤，在50-60℃干燥4小时，得到99.95％纯的阿夫唑嗪碱。

7. 发明申请

WO2006008749A1 PROCESS FOR PREPARING PURE CEPHALOSPORINE INTERMEDIATES 审中-公开
标题翻译：制备纯中间体中间体的方法
公开(公告)号：WO2006008749A1
公开(公告)日：2006-01-26
申请号：PCT/IN2004/000209
申请日：2004-07-16
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： C07D501/18
CPC分类号： C07D501/00
摘要： The present invention relates to a process for preparing key intermediates for cephalosporin antibiotics substantially free of undesired delta A 2 isomer. Thus, 7-aminocephalosporanic acid (7-ACA) is silylated with hexamethyldisilazane in cyclohexane at reflux temperature. (6R,7R)-3-[(Acetyloxy)methyl]-7-(trimethylsilyl)aminoceph-3-em-4-oic acid obtained is reacted with the mixture of N-methylpyrrolidine and trimethylsilyliodide in cyclohexane, desilylated with isopropyl alcohol and treated with hydrochloric acid to obtain [6R-(6a,7b)]-1-[[7-Amino-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-methylpyrrolidinium inner salt hydrochloride. [6R-(6a,7b)]-1-[[7-Amino-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-methylpyrrolidinium inner salt hydrochloride is N-acylated with syn-2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid 2-benzothiazolyl thioester (MAEM) followed by treatment with hydrochloric acid to give cefepime dihydrochloride monohydrate.
摘要翻译：本发明涉及一种制备基本上不含不需要的ΔA2异构体的头孢菌素抗生素的关键中间体的方法。因此，将7-氨基头孢烷酸（7-ACA）在环己烷中在回流温度下用六甲基二硅氮烷甲硅烷基化。（6R，7R）-3 - [（乙酰氧基）甲基] -7-（三甲基甲硅烷基）氨基头孢-3-烯-4-酸与N-甲基吡咯烷和三甲基甲硅烷基碘的混合物在环己烷中反应，用异丙醇脱甲硅烷基酯，用[6R-（6a，7b）] - [[7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-1-酮吡啶-3-基]甲基] -1-甲基吡咯烷鎓盐内盐酸盐。 [6R-（6a中，图7b）] - 1 - [[7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂双环〔4.2.0〕辛-2-烯-3-基]甲基] -1-甲基吡咯烷鎓盐内盐酸盐与顺-2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酸2-苯并噻唑基硫酯（MAEM）进行N-酰化，接着用盐酸处理，得到头孢吡肟二盐酸盐一水合物。

8. 发明申请

WO2004099183A1 NOVEL POLYMORPHS OF PANTOPRAZOLE SODIUM 审中-公开
标题翻译：潘多芬钠的新型聚合物
公开(公告)号：WO2004099183A1
公开(公告)日：2004-11-18
申请号：PCT/IN2003/000177
申请日：2003-05-06
申请人： HETERO DRUGS LIMITED , 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： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to novel polymorphs of pantoprazole sodium, to processes for their preparation and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及泮托拉唑钠的新型多晶型物，其制备方法和含有它们的药物组合物。

9. 发明申请

WO2009040825A1 A PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE ESOMEPRAZOLE 审中-公开
标题翻译：一种制备完全纯化的异喹诺酮的方法
公开(公告)号：WO2009040825A1
公开(公告)日：2009-04-02
申请号：PCT/IN2007/000433
申请日：2007-09-25
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 provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. Thus, for example, a compound containing a mixture of 1-(S)-camphorsulfonyl-5-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1 H-benzimidazole and 1-(S)-camphorsulfonyl-6-methoxy-2-[(3,5- dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1 H-benzimidazole is hydrolyzed with barium hydroxide, isolated the resulting esomeprazole barium salt followed by neutralization with an acid to yield substantially enantiomerically pure esomeprazole in neutral form and then converted into its pharmaceutically acceptable salts.
摘要翻译：本发明提供了一种改进的和商业可行的制备基本上为中性形式的对映体纯的埃索美拉唑或作为其药学上可接受的盐或其溶剂化物包括水合物的方法。因此，例如，含有1-（S） - 樟脑磺酰基-5-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （S） - 亚磺酰基] - 1 H-苯并咪唑和1-（S） - 樟脑磺酰基-6-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （S） - 亚磺酰基] -1H-苯并咪唑水解用氢氧化钡分离得到的艾美拉唑钡盐，然后用酸中和，得到基本上为中性形式的对映体纯的埃索美拉唑，然后转化为其药学上可接受的盐。

10. 发明申请

WO2006134607A1 CEFDINIR PROCESS 审中-公开
标题翻译： CEFDINIR过程
公开(公告)号：WO2006134607A1
公开(公告)日：2006-12-21
申请号：PCT/IN2005/000199
申请日：2005-06-15
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 provides an improved process for the preparation of high assayed cefdinir. Thus, crude cefdinir is added to water at 25 - 30°C and then 18% hydrochloric acid is slowly added to form a clear solution. The solution is cooled to -5°C and stirred for 5 minutes at -5°C to +5°C. Then temperature of the mass is raised to 35 - 38°C, stirred for 15 minutes at the same temperature. To the reaction mass eno carbon is added at 35 - 38°C and stirred for 30 minutes at 35 - 38°C. Then the contents are filtered on hiflo bed and washed with water. The filtrate is then cooled to 25°C, the pH is slowly adjusted to 2.6 with saturated sodium bicarbonate solution and stirred for 60 minutes at 25 - 30°C. Filtered the solid, washed with water and dried at 40°C under vacuum to give high assayed cefdinir.
摘要翻译：本发明提供了制备高分辨头孢地尼的改进方法。因此，将粗头孢非尼加入到25-30℃的水中，然后缓慢加入18％盐酸以形成澄清溶液。将溶液冷却至-5℃，并在-5℃至+ 5℃下搅拌5分钟。然后将质量的温度升高至35-38℃，在相同温度下搅拌15分钟。向反应物质中，在35-38℃下加入碳，在35-38℃下搅拌30分钟。然后将内容物在床上过滤并用水洗涤。然后将滤液冷却至25℃，用饱和碳酸氢钠溶液将pH缓慢调节至2.6，并在25-30℃下搅拌60分钟。过滤固体，用水洗涤，并在40℃真空干燥，得到高度测定的头孢地尼。

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