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1. 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。

2. 发明申请

WO2012001694A1 PROCESS FOR OLMESARTAN MEDOXOMIL 审中-公开
标题翻译： OLMESARTAN MEDOXOMIL的方法
公开(公告)号：WO2012001694A1
公开(公告)日：2012-01-05
申请号：PCT/IN2010/000441
申请日：2010-06-28
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
IPC分类号： C07D257/04
CPC分类号： C07D405/14
摘要： The present invention provides a process for the preparation of substantially pure trityl olmesartan medoxomil. The present invention also provides a process for purification of trityl olmesartan medoxomil. The present invention further provides a process for purification of olmesartan medoxomil.
摘要翻译：本发明提供了制备基本上纯的三苯甲基奥美沙坦酯的方法。本发明还提供了三苯甲基奥美沙坦酯的纯化方法。本发明还提供了一种纯化奥美沙坦酯的方法。

3. 发明申请

WO2011132194A1 PROCESS FOR THE PREPARATION OF RALOXIFENE HYDROCHLORIDE 审中-公开
标题翻译：制备雷洛芬芬氢氯化物的方法
公开(公告)号：WO2011132194A1
公开(公告)日：2011-10-27
申请号：PCT/IN2010/000247
申请日：2010-04-19
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VASMI KRISHNA, Bandi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VASMI KRISHNA, Bandi
IPC分类号： C07D407/00
CPC分类号： C07D333/56
摘要： The present invention provides an improved process for the preparation of α-(3- methoxyphenylthio)-4-methoxyacetophenone. The present invention also provides a process for the preparing free flowing solid of 6-methoxy-2-(4-methoxyphenyl)- benzo[b]-thiophene. The present invention further provides a process for the preparation of substantially pure 6-methoxy-2-(4-methoxyphenyl)-benzo[b]-thiophene. The present invention further provides a process for purification of raloxifene hydrochloride.
摘要翻译：本发明提供了制备α-（3-甲氧基苯硫基）-4-甲氧基苯乙酮的改进方法。本发明还提供了制备6-甲氧基-2-（4-甲氧基苯基） - 苯并[b]噻吩的自由流动固体的方法。本发明还提供了制备基本上纯的6-甲氧基-2-（4-甲氧基苯基） - 苯并[b]噻吩的方法。本发明还提供了盐酸雷洛昔芬的纯化方法。

4. 发明申请

WO2011121592A1 PROCESS FOR IRBESARTAN SUBSTANTIALLY FREE OF DIMMER IMPURITY 审中-公开
标题翻译： IRBESARTAN的工艺大大减少了不必要的重量
公开(公告)号：WO2011121592A1
公开(公告)日：2011-10-06
申请号：PCT/IN2010/000199
申请日：2010-03-29
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
IPC分类号： C07D257/00 , C07D257/04
CPC分类号： C02F1/14 , C02F1/30 , C02F1/32 , C02F2001/007 , C02F2201/008 , C02F2209/003 , C02F2209/02 , C02F2303/04 , F24S23/77 , F24S25/00 , Y02A20/212 , Y02E10/47
摘要： The present invention provides a process for the preparation of irbesartan substantially free of 3-((2'-(1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H- tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one (or) 3- ((2'-(2-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2H-tetrazol-5-yl)biphenyl-4- yl)methyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one impurity.
摘要翻译：本发明提供了制备基本上不含3 - （（2' - （1 - （（2' - （1H-四唑-5-基）联苯-4-基）甲基）-1H-四唑的厄贝沙坦的方法噻唑-5-基）联苯-4-基）甲基）-2-丁基-1,3-二氮杂螺[4.4]壬-1-烯-4-酮（或）3 - （（2' - （2 - （（ 2' - （1H-四唑-5-基）联苯-4-基）甲基）-2H-四唑-5-基）联苯-4-基）甲基）-2-丁基-1,3-二氮杂螺[4.4] 非1-烯-4-酮杂质。

5. 发明申请

WO2009157001A2 PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL 审中-公开
标题翻译：制备CANDESARTAN CILEXETIL的方法
公开(公告)号：WO2009157001A2
公开(公告)日：2009-12-30
申请号：PCT/IN2008/000399
申请日：2008-06-24
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： C07D403/10
CPC分类号： C07D403/10
摘要： There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2'-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl] methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co- distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0°C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil.
摘要翻译：提供了一种制备坎地沙坦酯的方法，所述方法包括在钯催化剂存在下，用氢气将三苯甲基坎地沙坦酯在醇中氢化。将甲苯和甲醇的混合物加入到1-（环己氧基羰基氧基）乙基-2-乙氧基-1 - [[2' - （N-三苯基甲基四唑-5-基）联苯-4-基]甲基]苯并咪唑-7-羧酸甲酯和在大气压下，在钯碳存在下，在室温下氢化直到氢吸收停止。在硅藻土床上过滤，用甲苯和甲醇的混合物洗涤床，收集滤液并浓缩。用乙腈共蒸馏，加入乙腈，在室温下搅拌，冷却至0℃。搅拌，过滤，用冷乙腈洗涤，干燥得到坎地沙坦酯。

6. 发明申请

WO2011125062A1 PROCESS FOR THE PREPARATION OF MEMANTINE HYDROCHLORIDE 审中-公开
标题翻译：制备氯化氢的方法
公开(公告)号：WO2011125062A1
公开(公告)日：2011-10-13
申请号：PCT/IN2010/000230
申请日：2010-04-08
申请人： HETERO RESEARCH FOUNDATION , PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
发明人： PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , MURALIDHARA REDDY, Dasari , RAJI REDDY, Rapolu , RAMAKRISHNA REDDY, Matta , VAMSI KRISHNA, Bandi
IPC分类号： A01N33/02 , A61K31/13
CPC分类号： C07C231/22 , C07C17/06 , C07C209/62 , C07C209/84 , C07C231/10 , C07C2603/74 , C07C233/06 , C07C211/38 , C07C23/46
摘要： The present invention provides an improved process for the preparation of 1-bromo-3,5-dimethyladamantane. The present invention also provides a process for preparing free flowing solid of 1-acetamido-3,5-dimethyladamantane. The present invention further provides a process for the preparation of memantine hydrochloride substantially free of 1-amino-3,5,7-trimethyladamantane hydrochloride and/or 1-amino-3-methyladamantane hydrochloride impurity.
摘要翻译：本发明提供了制备1-溴-3,5-二甲基金刚烷的改进方法。本发明还提供了制备1-乙酰氨基-3,5-二甲基金刚烷的自由流动固体的方法。本发明还提供了制备基本上不含1-氨基-3,5,7-三甲基金刚烷盐酸盐和/或1-氨基-3-甲基金刚烷盐酸盐杂质的美金刚盐酸盐的方法。

7. 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.

8. 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。

9. 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.

10. 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。

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