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71. 发明申请

WO2009128083A1 NOVEL POLYMORPHIC FORMS OF SUNITINIB BASE 审中-公开
标题翻译： SUNITINIB基础的新型多形态
公开(公告)号：WO2009128083A1
公开(公告)日：2009-10-22
申请号：PCT/IN2008/000248
申请日：2008-04-16
申请人： NATCO PHARMA LIMITED , KONDURI, Srinivasa Krishna Murthy , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KONDURI, Srinivasa Krishna Murthy , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.
摘要翻译：本发明涉及N- [2-（二乙基氨基）乙基] -5 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基）甲基-2' 4-二甲基-1H-吡咯-3-甲酰胺 - 舒尼替尼碱（I）。本发明还涉及制备这种多晶型晶体的方法。

72. 发明申请

WO2009060463A1 AN ENVIRONMENTALLY FRIENDLY PROCESS FOR THE PREPARATION OF IMATINIB BASE 审中-公开
标题翻译：用于制备IMATINIB基础的环境友好过程
公开(公告)号：WO2009060463A1
公开(公告)日：2009-05-14
申请号：PCT/IN2007/000520
申请日：2007-11-05
申请人： NATCO PHARMA LIMITED , AMALA, Kompella , ADIBHATLA KALI SATYA, Bhujanga rao , RACHAKONDA, Sreenivas , VENKAIAH CHOWDARY, Nannapaneni
发明人： AMALA, Kompella , ADIBHATLA KALI SATYA, Bhujanga rao , RACHAKONDA, Sreenivas , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： A novel and environmentally friendly process for the preparation of highly pure (>99.8%) imatinib base of Formula (I) is disclosed. Imatinib base of this invention is suitable for conversion to pharmaceutically acceptable salts.
摘要翻译：公开了一种用于制备式（I）的高纯度（> 99.8％）伊马替尼碱的新颖且环保的方法。本发明的伊马替尼碱适于转化为药学上可接受的盐。

73. 发明申请

WO2008139492A2 A PROCESS FOR THE PREPARATION OF HIGHLY PURE RANOLAZINE BASE 审中-公开
标题翻译：制备高纯度RANOLAZINE碱的方法
公开(公告)号：WO2008139492A2
公开(公告)日：2008-11-20
申请号：PCT/IN2008/000289
申请日：2008-05-09
申请人： NATCO PHARMA LIMITED , KOMPELLA, Amala kishan , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KOMPELLA, Amala kishan , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
CPC分类号： C07D295/14
摘要： The present invention relates to an improved and novel process for the preparation of highly pure (>99.8) N-(2,6-Dimethyl phenyl)-4-[2-hydroxy-3-(2-methoxy phenoxy) propyl]-1-piperazine acetamide (Ranolazine) of formula (I) and its pharmaceutically acceptable salts process for preparation thereof.
摘要翻译：本发明涉及一种制备高纯度（> 99.8）N-（2,6-二甲基苯基）-4- [2-羟基-3-（2-甲氧基苯氧基）丙基] -1 （I）的哌嗪乙酰胺（Ranolazine）及其药学上可接受的盐制备方法。

74. 发明申请

WO2008136010A1 A PROCESS FOR THE PREPARATION OF HIGHLY PURE IMATINIB BASE 审中-公开
标题翻译：一种制备高纯度图像基质的方法
公开(公告)号：WO2008136010A1
公开(公告)日：2008-11-13
申请号：PCT/IN2007/000178
申请日：2007-05-07
申请人： NATCO PHARMA LIMITED , KOMPELLA, Amala , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KOMPELLA, Amala , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D401/14 , A61K31/505
CPC分类号： C07D401/14
摘要： A novel process for the preparation of highly pure (>99.8%) imatinib base of Formula (I) is disclosed. Highly pure imatinib base of this invention is suitable for conversion to pharmaceutically acceptable salts.
摘要翻译：公开了制备式（I）的高纯度（> 99.8％）伊马替尼碱的新方法。本发明的高纯伊马替尼碱适于转化为药学上可接受的盐。

75. 发明申请

WO2008102369A1 NOVEL POLYMORPHS OF ERLOTINIB HYDROCHLORIDE AND METHOD OF PREPARATION 审中-公开
标题翻译： ERLOTINIB氢氯化物的新型多聚体及其制备方法
公开(公告)号：WO2008102369A1
公开(公告)日：2008-08-28
申请号：PCT/IN2007/000407
申请日：2007-09-11
申请人： NATCO PHARMA LIMITED , JYOTHI PRASAD, Ramanadham , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： JYOTHI PRASAD, Ramanadham , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D239/94 , A61K31/517 , A61P35/00
CPC分类号： C07D239/94
摘要： The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.
摘要翻译：本发明涉及盐酸埃洛替尼的三种新型结晶形式及其制备方法。盐酸埃洛替尼是式（I）的N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺盐酸盐。本发明提供了称为Form-M，Form-N和Form-P的盐酸埃罗替尼的稳定新型结晶形式及其制备方法。盐酸埃洛替尼可用作治疗人类过度增生性疾病如癌症的药物。

76. 发明申请

WO2008096368A3 A NOVEL PROCESS FOR PRODUCTION OF RECOMBINANT HUMAN G-CSF 审中-公开
公开(公告)号：WO2008096368A3
公开(公告)日：2008-08-14
申请号：PCT/IN2008/000067
申请日：2008-02-04
申请人： NATCO PHARMA LIMITED , DASARI, Venkata, Krishna, Rao , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： DASARI, Venkata, Krishna, Rao , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07K14/535
摘要： The present invention relates to Recombinant human Granulocyte Colony Stimulating Factor (G-CSF) and describes a novel process for high-level expression, a simple, economically feasible, largely scalable production of rhG-CSF- from bacterial cells. The invention comprises of the development of transcriptional and translational conditions of G-CSF gene to improve the level of protein expression resulting in the increase of specific and volumetric product yield. The specific product yield in batch mode fermentation is 68mg/L/OD and the level of protein expression is 45% on total cellular protein. The volumetric product yield in fed batch mode fermentation is 4.2 g/L.

77. 发明申请

WO2008090565A1 NOVEL THERMODYNAMICALLY STABLE POLYMORPHIC FORM-L OF LETROZOLE 审中-公开
标题翻译：新型热稳定性多晶型的LETROZOLE
公开(公告)号：WO2008090565A1
公开(公告)日：2008-07-31
申请号：PCT/IN2007/000112
申请日：2007-03-20
申请人： NATCO PHARMA LIMITED , KOMPELLA, Amala kishan , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KOMPELLA, Amala kishan , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/04
CPC分类号： C07D249/08
摘要： The present invention relates to a novel crystalline Form L of letrozole and a process for preparing the same. Letrozole is useful for the first-line treatment in post-menopausal women with hormone receptor positive (or) locally advanced (or) metastatic breast cancer.
摘要翻译：本发明涉及来曲唑的新型结晶形式L及其制备方法。来曲唑对于具有激素受体阳性（或）局部晚期（或）转移性乳腺癌的绝经后妇女的一线治疗是有用的。

78. 发明申请

WO2008007390A2 AN IMPROVED PROCESS FOR PURIFICATION OF ZOLMITRIPTAN 审中-公开
标题翻译：改进ZOLMITRIPTAN的改进方法
公开(公告)号：WO2008007390A2
公开(公告)日：2008-01-17
申请号：PCT/IN2007/000267
申请日：2007-06-29
申请人： NATCO PHARMA LIMITED , KOMPELLA, Amala, Kisham , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KOMPELLA, Amala, Kisham , RACHAKONDA, Sreenivas , ADIBHATLA KALI SATYA, Bhujanga, Rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention relates to an improved and novel process for the purification of the Zolmitriptan (I) to get highly pure drug substance of greater than 99.8% purity. Zolmitriptan is a 5HT 1 -like receptor agonist useful in the treatment and prophylaxis of migraine and is chemically known as (S)-4-[(3-[2-(Dimethylamino) ethyl]-1H-indol-5-yl] methyl]-2-oxazolidinone (I). A novel method of purification of the drug substance Zolmitriptan (I) is developed and is described.
摘要翻译：本发明涉及一种改进和新颖的Zolmitriptan（I）纯化方法，以获得纯度高于99.8％的高纯度药物。佐米替曲坦是一种可用于治疗和预防偏头痛的5HT 1 - 样受体激动剂，化学上称为（S）-4 - [（3- [2-（二甲基氨基）乙基] 吲哚-5-基]甲基] -2-恶唑烷酮（I）。开发并描述了药物物质Zolmitriptan（I）的新型纯化方法。

79. 发明申请

WO2007013097A1 IMPROVED PROCESS FOR THE PREPARATION OF IBANDRONATE SODIUM 审中-公开
标题翻译：改进的IBANDRONATE SODIUM制备方法
公开(公告)号：WO2007013097A1
公开(公告)日：2007-02-01
申请号：PCT/IN2006/000251
申请日：2006-07-17
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07F9/38
CPC分类号： C07F9/3873
摘要： Present invention discloses an improved and commercial process for the preparation of ibandronic acid or its monosodium salt. According to the process 3-N-methylaminopropionitrile is reacted with n-pentylbromide to get the tertiary amine of formula-II. Hydrolysis of the nitrile compound of formula-II with hydrochloric acid gave the b-alanine derivative of formula-X. Bis-phosphonylation of the acid compound of formula-X with phorphorous trichloride and phosphorous acid, followed by water hydrolysis gave aqueous ibandronic acid. Treatment of this with sodium hydroxide, followed by dilution of the aqueous solution with methanol gave ibandronate monosodium of formula-Ia as white crystalline solid. Present process utilizes simple raw materials and avoids the column chromatography technique used in the prior art process for isolation of ibandronic acid. Overall yield of ibandronate is more than 60% from the nitrile intermediate of formula-II. Ibandronate is widely used as bone resorption inhibitor.
摘要翻译：本发明公开了制备伊班膦酸或其单钠盐的改进的和商业的方法。根据该方法，使3-N-甲基氨基丙腈与正戊基溴反应得到式-II的叔胺。用盐酸水解式-II的腈化合物，得到式-X的β-丙氨酸衍生物。用无机三氯化磷和亚磷酸将式-X的酸化合物双膦酰化，然后水解，得到伊班膦酸水溶液。用氢氧化钠处理，然后用甲醇稀释水溶液，得到式I-a的伊班膦酸一钠，为白色结晶固体。本发明方法利用简单的原料并且避免了用于分离伊班膦酸的现有技术方法中使用的柱色谱技术。来自式-II的腈中间体的伊班膦酸盐的总收率超过60％。伊班膦酸钠广泛用作骨吸收抑制剂。

80. 发明申请

WO2006137083A1 IMPROVED PROCESS FOR THE PREPARATION OF RIZATRIPTAN BENZOATE 审中-公开
标题翻译：制备RIZATRIPTAN苯甲酸酯的改进方法
公开(公告)号：WO2006137083A1
公开(公告)日：2006-12-28
申请号：PCT/IN2006/000199
申请日：2006-06-13
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , SATYASRINIVAS, Hanumara , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , SATYASRINIVAS, Hanumara , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： Present invention discloses an improved and commercially viable process for the preparation of rizatriptan benzoate of formula (I). According to the present process the hydrazone intermediate derived from the phenylhydrazine of formula- (III) and 4- dimethylaminobutyraldehyde diethyl acetal is gradually heated to 60-70 °C in aqueous sulfuric acid medium and maintained for 3-4hr to get rizatriptan with less dimeric impurity of formula (X). The resultant rizatriptan is isolated and converted into the pharmaceutically acceptable benzoate salt. Present process produces less percentage of dimeric (less than 3 %) or polymeric impurities compared to the prior art process and more yield of rizatriptan. Rizatriptan benzoate produced according to the present process has more than 99.5 % purity with less than 0.1% dimeric impurity of formula (X) by HPLC. Rizatriptan benzoate is useful for the treatment of migraine.
摘要翻译：本发明公开了一种用于制备式（I）的利扎曲坦苯甲酸酯的改进且商业可行的方法。根据本发明方法，将由式（III）的苯肼衍生的腙中间体和4-二甲基氨基丁醛二乙基缩醛在硫酸水溶液中逐渐加热至60-70℃，保持3-4小时，得到较少二聚的利扎曲坦式（X）的杂质。所得的利扎曲普兰分离并转化成药学上可接受的苯甲酸盐。与现有技术的方法相比，目前的方法产生的二聚（少于3％）或聚合物杂质的百分比较低，并且利扎曲普坦的产量更高。根据本发明制备的利扎曲坦苯甲酸酯通过HPLC具有大于99.5％的纯度，小于0.1％的式（X）二聚杂质。利马曲坦苯甲酸酯可用于治疗偏头痛。

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