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1. 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。

2. 发明申请

WO2007013097A8 IMPROVED PROCESS FOR THE PREPARATION OF IBANDRONATE SODIUM 审中-公开
标题翻译：改进IBANDRONATE SODIUM的制备方法
公开(公告)号：WO2007013097A8
公开(公告)日：2007-12-06
申请号：PCT/IN2006000251
申请日：2006-07-17
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
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：本发明公开了用于制备伊班膦酸或其单钠盐的改进和商业化方法。根据方法，将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。将式-X的酸化合物与无色三氯化磷和亚磷酸二膦酰化，随后进行水解，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Ia的伊班膦酸钠单钠为白色结晶固体。本发明方法使用简单的原料，并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。伊班膦酸钠的总收率高于式Ⅱ的腈中间体的60％以上。伊班膦酸盐被广泛用作骨吸收抑制剂。

3. 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。

4. 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。

5. 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。

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

WO2009057139A3 NOVEL 4-(TETRAZOL-5-YL)-QUINAZOLINE DERIVATIVES AS ANTI CANCER AGENTS 审中-公开
标题翻译：新型4-（四唑-5-基） - 喹唑啉衍生物作为抗癌药物
公开(公告)号：WO2009057139A3
公开(公告)日：2009-09-24
申请号：PCT/IN2008000708
申请日：2008-10-28
申请人： NATCO PHARMA LTD , KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA , VENKAIAH CHOWDARY NANNAPANENI
发明人： KONAKANCHI DURGA PRASAD , PULA SUBBA RAO , ANANTHANENI LAKSHMI , PULLA REDDY MUDDASANI , ADIBHATLA KALI SATYA BHUJANGA RAO , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07D239/72 , A61K31/498 , A61P35/00 , C07D239/86 , C07D239/94 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D403/04 , C07D239/72 , C07D239/86 , C07D239/94 , C07D401/14 , C07D403/14
摘要： The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline 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 4-(tetrazol-5-yl)-quinazoline 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（例如抗癌活性）的式-I的取代的4-（四唑-5-基） - 喹唑啉衍生物或其药学上可接受的盐，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4-（四唑-5-基） - 喹唑啉衍生物的方法，含有该化合物的药物组合物及其在制备药物中的用途，所述药物用于在温血动物如男人。

8. 发明申请

WO2009054004A3 PROCESS FOR THE PREPARATION OF SORAFENIB 审中-公开
标题翻译：制备SORAFENIB的方法
公开(公告)号：WO2009054004A3
公开(公告)日：2009-07-02
申请号：PCT/IN2008000698
申请日：2008-10-22
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： C07D213/81 , A61K31/44
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），其涉及新的公式（Ⅱ）作为关键中间体。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。

9. 发明申请

WO2007039919A8 CRYSTALLINE FORMS OF ANASTROZOLE 审中-公开
标题翻译：晶体的晶体形式
公开(公告)号：WO2007039919A8
公开(公告)日：2007-12-06
申请号：PCT/IN2006000401
申请日：2006-10-06
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , SAMBASIVA RAO TALASILA , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , SAMBASIVA RAO TALASILA , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00
CPC分类号： C07D249/08
摘要： The present invention relates to novel crystalline forms of anastrozole and processes for their preparation. Anastrozole is useful, as an anti-neoplastic agent in treatment of breast cancer. The novel forms have been designated by us as Forms I & Form II.
摘要翻译：本发明涉及阿那曲唑的新型结晶形式及其制备方法。阿那曲唑作为乳腺癌治疗中的抗肿瘤药物是有用的。这些小说形式已被我们指定为表格I和表格II。

10. 发明申请

WO2008075376A8 POLYMORPHIC FORMS OF BORTEZOMIB AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： BORTEZOMIB的多晶形式及其制备方法
公开(公告)号：WO2008075376A8
公开(公告)日：2010-04-15
申请号：PCT/IN2007000561
申请日：2007-12-03
申请人： NATCO PHARMA LTD , RAVI JANAKI RAMA RAO , PULLA REDDY MUDDASANI , ADIBATLA KALI SATYA BHUJANGA R , VENKAIAH CHOWDARY NANNAPANENI
发明人： RAVI JANAKI RAMA RAO , PULLA REDDY MUDDASANI , ADIBATLA KALI SATYA BHUJANGA RAO , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07F5/02 , A61K31/69
CPC分类号： C07F5/025
摘要： The present invention relates to two novel and stable polymorphic forms, namely Form I and Form II of bortezomib (1) and processes for the preparation of these forms. Bortezomib is an anti-neoplastic agent used in the treatment of multiple myeloma.
摘要翻译：本发明涉及两种新颖且稳定的多晶型物，即硼替佐米（1）的I型和II型以及这些形式的制备方法。硼替佐米是用于治疗多发性骨髓瘤的抗肿瘤剂。

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