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1. 发明申请

WO2009136405A1 HIGH PURITY PALONOSETRON BASE AND ITS SOLID STATE CHARACTERISTICS 审中-公开
标题翻译：高纯度PALONOSETRON基础及其固体状态特征
公开(公告)号：WO2009136405A1
公开(公告)日：2009-11-12
申请号：PCT/IN2008/000285
申请日：2008-05-05
申请人： NATCO PHARMA LIMITED , ADIBHATLA KALI SATYA, Bhujanga rao , PULLA REDDY, Muddasani , RAVI, Janaki rama rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： ADIBHATLA KALI SATYA, Bhujanga rao , PULLA REDDY, Muddasani , RAVI, Janaki rama rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： The present invention describes the process for the preparation of pure enantiomeric form of palonosetron base of formula (I), and its solid-state characteristics of said compound.
摘要翻译：本发明描述了制备式（I）的帕洛诺司琼碱的纯对映体形式及其所述化合物的固态特性的方法。

2. 发明申请

WO2009054004A2 NOVEL PROCESS FOR THE PREPARATION OF SORAFENIB 审中-公开
标题翻译：制作SORAFENIB的新工艺
公开(公告)号：WO2009054004A2
公开(公告)日：2009-04-30
申请号：PCT/IN2008/000698
申请日：2008-10-22
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
CPC分类号： C07D213/81
摘要： A novel and improved process for the preparation of sorafenib (4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide) of formula I involving a novel intermediate of formula II as key intermediate is disclosed. Sorafenib tosylate, available in the market as Nexavar is a multiple kinase inhibitor targeting both RAF kinase and receptor tyrosine kinase that promote angiogenesis.
摘要翻译：一种新型和改进的制备式I的索拉非尼（4-（3-（4-（3-（4-氯-3-（三氟甲基）苯基）脲基）苯氧基）-N-甲基吡啶酰胺），其涉及式II的新型中间体作为关键中间人被披露。索拉非尼甲苯磺酸盐，在市场上可用，因为Nexavar是靶向促进血管生成的RAF激酶和受体酪氨酸激酶的多重激酶抑制剂。

3. 发明申请

WO2007074475A3 NOVEL POLYMORPHIC FORMS OF IBANDRONATE 审中-公开
标题翻译： IBANDRONATE的新型多晶型
公开(公告)号：WO2007074475A3
公开(公告)日：2007-09-07
申请号：PCT/IN2006000501
申请日：2006-12-21
申请人： NATCO PHARMA LTD , 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 , A61K31/663
CPC分类号： C07F9/3873
摘要： The present invention relates to novel and stable polymorphic forms of ibandronate monosodium monohydrate of formula I and processes for their preparation. Ibandronate monosodium monohydrate is useful, as bone resorption inhibitor. The novel crystalline forms are designated as Form I, Form II and the amorphous ibandronate monosodium monohydrate as Form III.
摘要翻译：本发明涉及式I的伊班膦酸单一水合物的新颖且稳定的多晶型物及其制备方法。作为骨吸收抑制剂，Ibandronate monoosodium monohydrate是有用的。新型结晶形式称为I型，II型和无定形伊班膦酸单钠一水合物，为III型。

4. 发明申请

WO2007026379A3 NOVEL CRYSTALLINE FORMS OF RISEDRONATE MONOSODIUM 审中-公开
标题翻译：新型晶体结构形式
公开(公告)号：WO2007026379A3
公开(公告)日：2007-07-12
申请号：PCT/IN2006000315
申请日：2006-08-30
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , USHA RANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , USHA RANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07F9/58
CPC分类号： C07F9/582
摘要： Present invention is related to three novel crystalline forms of risedronate monosodium of Formula (I) and processes for the preparation of same. These forms are stable and suitable for pharmaceutical formulations.
摘要翻译：本发明涉及式（I）的利塞膦酸单钠的三种新型结晶形式及其制备方法。这些形式是稳定的并且适用于药物制剂。

5. 发明申请

WO2005063717A1 AN IMPROVED PROCESS FOR THE PREPARATION OF ZOLEDRONIC ACID 审中-公开
标题翻译：一种改进的制备ZOLEDRONIC酸的方法
公开(公告)号：WO2005063717A1
公开(公告)日：2005-07-14
申请号：PCT/IN2004/000392
申请日：2004-12-20
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , USHA RANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , USHA RANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D233/54
CPC分类号： C07D233/54 , C07F9/65061
摘要： The invention disclosed in this application relates to an improved process for the preparation of zoledronic acid of formula (I) given below which comprises heating at a temperature in the range of 50-80 °C a solution of imidazol-1-ylacetic acid hydrochloride with ortho-phosphoric acid in a solvent medium where boiling point of the solvent used in lesser or close to that of phosphorous trichloride, adding phosphorous trichloride to the reaction mass slowly over a period of 2-3hr at a temperature in the range of 50-80 °C, keeping the resulting reaction mass at a temperature in the range of 50-80 °C for a period of 1-6hr, adding hydrochloric acid to the reaction mass and keeping the reaction mass at a temperature in the range of 60-120 °C, separating the organic solvent from the reaction mass while it is still hot, and diluting the aqueous layer containing zoledronic acid with water miscible solvent. Zoledronic acid is widely used as a bone resorption inhibitor.
摘要翻译：本申请中公开的本发明涉及一种制备下式给出的式（I）唑来膦酸的改进方法，该方法包括在50-80℃的温度下加热咪唑-1-基乙酸盐酸盐与在溶剂介质中使用邻磷酸，其溶剂沸点低于或接近三氯化磷，在反应物质中缓缓加入三氯化磷，温度范围为50-80℃ 将所得反应物质保持在50-80℃的温度下1-6小时，向反应物料中加入盐酸并将反应物料保持在60-120℃的温度范围内 ℃，同时将有机溶剂与反应物质分离，同时用水混溶的溶剂稀释含有唑来膦酸的水层。唑来膦酸广泛用作骨吸收抑制剂。

6. 发明申请

WO0185692A3 AN IMPROVED PROCESS FOR THE PREPARATION OF QUINOLONE DERIVATIVES 审中-公开
标题翻译：改进喹诺酮衍生物的制备方法
公开(公告)号：WO0185692A3
公开(公告)日：2002-06-06
申请号：PCT/IN0100042
申请日：2001-03-19
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07C229/34 , C07D215/56 , C07C225/16
CPC分类号： C07C229/34 , C07C2601/02 , C07D215/56
摘要： This invention relates to an improved process for the preparation of quinolone drugs of the formula (I), wherein R=C1-C6 alkyl, C3-C6 cycloalklyl, aryl, substituted aryl, NR R =diarylamino, arylalkylamino, C1-C6-dialkylamino, piprazinyl, N or C alkyl (C1-C6) substituted piperazinyl, morpholino, pyrrolidinyl, substituted pyrrolidinyl, aralkyl, substituted aralkyl etc. Some of the compounds falling within the formula (I) are ciprofloxacin, enrofloxin, pefloxacin, etc. These compounds are useful as antibacterial drugs. The process of the present invention for preparation of compound of formula (I) comprises in enhancing the reactivity of the displaceable halogen (X) in the compound of the formula (II) towards various amines of formula (III) wherein R = as defined for compound of formula (I), R =COOR (R =C1-C6 alkyl, aryl, aralkyl), nitrile a carboxamide (-CONR R , R and R = C1-C6 alkyl, C3-C6 cycloalkyl, aralkyl), X = Cl, Br, F; NR R = as defined above by introducing a nitro group ortho to the displaceable halo group and subsequently removing the nitro group in a conventional manner. The process of the present invention enhances the yield of the compound of the formula (I) and also improves the quality of the prepared compound.
摘要翻译：本发明涉及制备式（I）的喹诺酮药物的改进方法，其中R = C 1 -C 6烷基，C 3 -C 6环烷基，芳基，取代的芳基，NR 1 R 2 =二芳基氨基，芳基烷基氨基 C 1 -C 6 - 二烷基氨基，哌嗪基，N或C烷基（C 1 -C 6）取代的哌嗪基，吗啉代，吡咯烷基，取代的吡咯烷基，芳烷基，取代的芳烷基等。属于式（I）的化合物中的一些是环丙沙星，enrofloxin，这些化合物可用作抗菌药物。用于制备式（I）化合物的本发明的方法包括提高式（II）化合物中的可置换卤素（X）对式（III）的各种胺的反应性，其中R =如式（I）化合物，R 3 = COOR 6（R 6 = C 1 -C 6烷基，芳基，芳烷基），腈甲酰胺（-CONR 7 R 8，R 7）和R 8 = C 1 -C 6烷基，C 3 -C 6环烷基，芳烷基），X = Cl，Br，F; NR 1 R 2 =如上所定义，通过在可置换卤素基团的邻位引入硝基并随后以常规方式除去硝基。本发明的方法提高了式（I）化合物的产率，并提高了制备的化合物的质量。

7. 发明申请

WO2009098715A4 NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI -CANCER AGENTS 审中-公开
标题翻译：新型吡唑并[3,4-d]嘧啶衍生物作为抗癌剂
公开(公告)号：WO2009098715A4
公开(公告)日：2009-12-10
申请号：PCT/IN2009000037
申请日：2009-01-12
申请人： NATCO PHARMA LTD , KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PILLI RAMAKRISHNA , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA , VENKAIAH CHOWDARY NANNAPANENI
发明人： KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PILLI RAMAKRISHNA , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA RAO , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to substituted pyrazolo [3,4-d] pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo [3,4-d] pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti- proliferative effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及式（I）的取代的吡唑并[3,4-d]嘧啶衍生物或其药学上可接受的盐，其具有抗增殖活性如抗癌活性并因此可用于治疗方法的人体或动物体。本发明还涉及制备取代的吡唑并[3,4-d]嘧啶衍生物的方法，含有该化合物的药物组合物及其在制备用于在温血动物中产生抗增殖作用的药物中的用途，像人这样的热血动物。

8. 发明申请

WO2009098715A3 NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI -CANCER AGENTS 审中-公开
标题翻译：新型吡咯并[3,4-D]吡啶衍生物作为抗体剂
公开(公告)号：WO2009098715A3
公开(公告)日：2009-10-15
申请号：PCT/IN2009000037
申请日：2009-01-12
申请人： NATCO PHARMA LTD , KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PILLI RAMAKRISHNA , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA , VENKAIAH CHOWDARY NANNAPANENI
发明人： KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PILLI RAMAKRISHNA , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA RAO , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to substituted pyrazolo [3,4-d] pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo [3,4-d] pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti- proliferative effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及具有抗增殖活性如抗癌活性的式（I）的取代吡唑并[3,4-d]嘧啶衍生物或其药学上可接受的盐，因此可用于治疗方法的人体或动物体。本发明还涉及制备取代的吡唑并[3,4-d]嘧啶衍生物的方法，用于制备含有该化合物的药物组合物及其在制备用于在温暖的药物中产生抗增殖作用的药物中的用途，流血的动物如人。

9. 发明申请

WO2009010988A1 AN IMPROVED, INDUSTRIALLY VIABLE PROCESS FOR THE PREPARATION OF HIGH PURITY PALIPERIDONE 审中-公开
标题翻译：改进的高效PALIPERIDONE的改进的，工业上可行的方法
公开(公告)号：WO2009010988A1
公开(公告)日：2009-01-22
申请号：PCT/IN2008/000446
申请日：2008-07-14
申请人： NATCO PHARMA LIMITED , RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D471/04 , A61K31/517 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to an improved and industrially viable process for the preparation of high purity ≥ 99.8% chemical of paliperidone of formula-I (3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetra-hydro-9-hydroxy-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one), involving the novel intermediate, 3-(2- hydroxyethyl)-2-methyl-9-(phenylmethoxy)-4H-Pyrido[l,2-a]pyrimidin-4-one of formula-II. All intermediates encountered in the synthetic pathway of present invention are isolated by simple crystallization techniques in high pure. Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders and is marketed under the brand name INVEGA.
摘要翻译：本发明涉及一种改进的和工业上可行的方法，用于制备高纯度= 99.8％的利培酮的式I（3- [2- [4-（6-氟-1,2-苯并异恶唑-3-基））-1-哌啶基]乙基] -6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮），其涉及新的中间体，3-（2-羟基乙基）-2-甲基-9-（苯基甲氧基）-4H-吡啶并[1,2-a]嘧啶-4-酮。在本发明的合成途径中遇到的所有中间体通过高纯度的简单结晶技术分离。帕立酮可用作治疗精神病性疾病的抗精神病药物，并以品牌名称INVEGA上市。

10. 发明申请

WO2009010987A1 AN IMPROVED PROCESS FOR THE PREPARATION OF PURE PALONOSETRON HYDROCHLORIDE 审中-公开
标题翻译：用于制备纯PALONOSETRON HYDROCHLORIDE的改进方法
公开(公告)号：WO2009010987A1
公开(公告)日：2009-01-22
申请号：PCT/IN2008/000313
申请日：2008-05-16
申请人： NATCO PHARMA LIMITED , RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D453/02 , A61K31/439 , A61P1/08
CPC分类号： C07D453/02
摘要： The present invention relates to an improved and industrially viable process for the preparation of high purity >99.8% chemical and >99.8% chiral of palonosetron hydrochloride of formula-I ((3as)-2[(3s)-1-azabicyclo [2.2.2] oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinoline-1-one monohydrochloride) obtained from reduction of 2-[(S)-1-azabicyclo[2.2.2]oct-3-yl]-2,4,5,6-tetrahydro-1H-benz[de]iso-quinolin-1-one hydrochloride of formula-VI. In the prior art compound of formula-VI or its base are used in the catalytic hydrogenation. But the selection of solvents like acetic acid or THF rendered them commercially not viable due to low yield and low purity of palonosetron hydrochloride. In the present process simple solvent like methanol and readily available palladium-on-carbon were used to increase the yield and purity of palonosetron hydrochloride. Palonosetron Hydrochloride is useful as anti-emetic agent during the chemotherapy of treatment of cancer patients and is marketed under the brand names 'Aloxi' and 'Onicit'.
摘要翻译：本发明涉及一种改进和工业上可行的制备式I（（3as）-2 [（3s）-1-氮杂双环[2.2]的盐酸帕洛诺司琼的高纯度> 99.8％化学和99.8％手性的方法。 2]辛-3-基] -2,3,3a，4,5,6-六氢-1H-苯并[de]异喹啉-1-酮单盐酸盐）由还原2 - [（S）-1-氮杂双环 [2.2.2]辛-3-基] -2,4,5,6-四氢-1H-苯并[de]异喹啉-1-酮盐酸盐。在现有技术中，将式VI或其碱的化合物用于催化氢化。但是由于盐酸帕洛诺司琼的产率低，纯度低，所以选择乙酸或THF等溶剂使得它们在商业上不可行。在本方法中，使用简单的溶剂如甲醇和易于获得的钯 - 碳来提高盐酸帕洛诺司琼的产率和纯度。在盐酸帕洛诺司琼治疗癌症患者化疗期间，可用作止吐剂，并以“Aloxi”和“Onicit”品牌销售。

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