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11. 发明授权

US08350030B2 Process for producing 5-fluoro-1-(2R, 5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine 有权
标题翻译： 5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的制备方法
公开(公告)号：US08350030B2
公开(公告)日：2013-01-08
申请号：US12746739
申请日：2008-12-05
申请人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
发明人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.
摘要翻译：本文公开了5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶及其药学上可接受的盐的改进方法。

12. 发明授权

US08329952B2 Process for the preparation of O-desmethylvenlafaxine succinate polymorphic forms 有权
标题翻译： O-去甲基蓝法素琥珀酸酯多形态的制备方法
公开(公告)号：US08329952B2
公开(公告)日：2012-12-11
申请号：US12669487
申请日：2008-07-15
申请人： Ramakoteswara Rao Jetti , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohana Vamsi Krishna Vadlamudi , Prasanth Kumar Barik , Om Dutt Tyagi
发明人： Ramakoteswara Rao Jetti , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohana Vamsi Krishna Vadlamudi , Prasanth Kumar Barik , Om Dutt Tyagi
IPC分类号： C07C211/00
CPC分类号： C07C213/10 , C07B2200/13 , C07C2601/14 , C07C215/64
摘要： The present invention relates to process for the preparation of novel crystalline Desmethylvenlafaxine succinate polymorphic Forms-A, B. The present invention also relates to novel processes for the preparation of 0-Desmethylvenlafaxine succinate polymorphic Forms-(I), (II), (III) and amorphous.
摘要翻译：本发明涉及制备新的结晶Desmetvenlafaxine琥珀酸多晶型A，B的方法。本发明还涉及制备O-去甲基文拉法辛琥珀酸多晶型的新方法 - （I），（II），（III ）和无定形。

13. 发明授权

US08258312B2 Process for preparing pure valsartan 有权
标题翻译：纯缬沙坦制备方法
公开(公告)号：US08258312B2
公开(公告)日：2012-09-04
申请号：US12666476
申请日：2008-06-26
申请人： Om Dutt Tyagi , Jakka Devendra Rao , Katukuri Aravind Kumar , Dammalapati Ventaka Lakshmi Narasimha Rao
发明人： Om Dutt Tyagi , Jakka Devendra Rao , Katukuri Aravind Kumar , Dammalapati Ventaka Lakshmi Narasimha Rao
IPC分类号： C07D249/00
CPC分类号： C07D257/04
摘要： An improved process for the preparation of substantially pure valsartan employing suitable reagents such as chelating agent and reaction conditions.
摘要翻译：使用合适试剂如螯合剂和反应条件制备基本上纯的缬沙坦的改进方法。

14. 发明申请

US20100197932A1 PROCESS FOR PREPARING PURE VALSARTAN 有权
标题翻译：制备纯粹瓦斯塔坦的方法
公开(公告)号：US20100197932A1
公开(公告)日：2010-08-05
申请号：US12666476
申请日：2008-06-26
申请人： Om Dutt Tyagi , Jakka Devendra Rao , Katukuri Aravind Kumar , Dammalapati Ventaka Lakshmi Narasimha Rao
发明人： Om Dutt Tyagi , Jakka Devendra Rao , Katukuri Aravind Kumar , Dammalapati Ventaka Lakshmi Narasimha Rao
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： An improved process for the preparation of substantially pure valsartan employing suitable reagents such as chelating agent and reaction conditions.
摘要翻译：使用合适试剂如螯合剂和反应条件制备基本上纯的缬沙坦的改进方法。

15. 发明申请

US20090227787A1 PROCESS FOR THE PREPARATION OF CEFIXIME 有权
标题翻译：制备CEFIXIME的方法
公开(公告)号：US20090227787A1
公开(公告)日：2009-09-10
申请号：US11722422
申请日：2005-12-19
申请人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
发明人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
IPC分类号： C07D501/04
CPC分类号： C07D501/04
摘要： The present invention provides an improved process for the preparation of Cefixime of formula (I), a cephalosporine antibiotic with an improved quality in regard to color and solubility.
摘要翻译：本发明提供了一种制备式（I）的头孢克肟的改进方法，头孢菌素抗生素在颜色和溶解度方面具有改进的质量。

16. 发明授权

US07511135B2 Method for manufacture of ceftiofur 失效
标题翻译：头孢噻呋的制造方法
公开(公告)号：US07511135B2
公开(公告)日：2009-03-31
申请号：US10532194
申请日：2003-10-27
申请人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar , Yuvaraj Atmaram Chavan
发明人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar , Yuvaraj Atmaram Chavan
IPC分类号： C07D501/36
CPC分类号： C07D417/14
摘要： A process for preparation of ceftiofur of formula (I) having purity greater than 97% is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic acid-2-benzothiazolyl thioester of formula (II), with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III) in the presence of a mixture of an water-immiscible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (I) substantially free of impurities by, a) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase, b) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, and c) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a anti-solvent.
摘要翻译：公开了制备具有大于97％纯度的式（I）头孢噻呋的方法。该方法包括使式（II）的[2-（2-氨基噻唑-4-基）] - 2-顺式 - 甲氧基亚氨基乙酸-2-苯并噻唑基硫代酯与7-氨基-3-（2-呋喃基羰硫基甲基）-3 （III）的头孢-4-羧酸在水不混溶的惰性有机溶剂和水的混合物存在下，在有机碱的存在下，分离式（I）的头孢噻呋基本上不含杂质， a）向反应混合物中加入水，并在水相中选择性地分配有机相中的杂质和与碱的盐形式的头孢噻呋（I），b）以含有头孢噻呋（I）的形式酸化含有头孢噻呋在含有水混溶性和与水不混溶的有机溶剂的混合物存在下，在含有碱或碱土金属盐的饱和水溶液的存在下，将碱与碱反应，从而将头孢噻吩（I）有机相，和c）分离高纯度和实质的头孢噻呋（I）通过蒸发有机溶剂或通过加入抗溶剂沉淀而不含杂质。

17. 发明授权

US07335767B2 Method for preparation of ceftiofur and salts thereof 失效
标题翻译：头孢噻呋及其盐的制备方法
公开(公告)号：US07335767B2
公开(公告)日：2008-02-26
申请号：US10694619
申请日：2003-10-27
申请人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar
发明人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar
IPC分类号： C07D501/36
CPC分类号： C07D501/00
摘要： A process for preparation of ceftiofur sodium of formula (Ib) possessing high stability and having purity of more than 97% and substantially free of impurities, is disclosed. The process comprises: i) reacting cefotaxime or its salts or its esters of formula (VI) wherein R3 is hydrogen, an alkali or alkaline earth metal, or an easily hydrolysable ester, with thiofuroic acid, employed in a molar proportion of 1.5 to 3.0 moles per mole of compound (VI), in the presence of acetonitrile as solvent and in the presence of large excess of methanesulfonic acid, employed in molar proportions of 12 to 18 moles per mole of compound (VI), and at a temperature of between −5° C. to 30° C. to give after necessary neutralization of the alkali or alkaline earth metal or removal of the ester group of the 4-carboxylic acid function, wherever applicable, ceftiofur of formula (Ia), possessing high stability and having purity of more than 97% and substantially free of impurities; ii) converting the ceftiofur of formula (Ia) thus obtained to its salt with an organic amine by treating a solution of ceftiofur in a mixture of water and a water-miscible organic solvent with an organic amine, at a temperature ranging from −10° C. to 10° C.; iii) reacting of the amine salt thus obtained with a sodium metal carrier in a mixture of water and water-miscible organic solvent and in presence of sodium hydrogen sulfite to give ceftiofur sodium of formula (Ib).
摘要翻译：公开了制备具有高稳定性和纯度大于97％且基本上不含杂质的式（Ib）头孢噻呋钠的方法。该方法包括：i）将头孢噻肟或其盐或其其中R 3为氢的式（VI）的酯，碱金属或碱土金属或易水解的酯与硫代呋喃酸反应，摩尔比例为1.5-3.0摩尔/摩尔化合物（Ⅵ），在乙腈作为溶剂的存在下，在大量过量的甲磺酸的存在下，摩尔比例为12至18摩尔/摩尔化合物（Ⅵ ），并且在-5℃至30℃的温度下进行，必要时中和碱金属或碱土金属或除去4-羧酸官能团的酯基（如果适用的话），式（Ia），具有高稳定性，纯度大于97％，基本上不含杂质; ii）通过在-10℃的温度范围内用有机胺处理水与水混溶性有机溶剂的混合物中的头孢噻肟溶液，将有机胺衍生的式（Ia）头孢噻吩转化为其盐 ℃至10℃。 iii）将由此得到的胺盐与水和水混溶性有机溶剂的混合物中的钠金属载体与亚硫酸氢钠的混合物反应，得到式（Ib）的头孢噻肟钠。

18. 发明授权

US08304578B2 Process for producing 1-[2-(dimethylamino)-1-(4-phenol)ethyl]cyclohexanol 有权
标题翻译： 1- [2-（二甲基氨基）-1-（4-苯酚）乙基]环己醇的制备方法
公开(公告)号：US08304578B2
公开(公告)日：2012-11-06
申请号：US12810791
申请日：2008-12-26
申请人： Om Dutt Tyagi , Saswata Lahiri , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohan Vamsi Krishna Vadlamudi , Venkata Bala Kishore Sarma Inupakutika , Surya Nageswara Rao Achanta
发明人： Om Dutt Tyagi , Saswata Lahiri , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohan Vamsi Krishna Vadlamudi , Venkata Bala Kishore Sarma Inupakutika , Surya Nageswara Rao Achanta
IPC分类号： C07C213/02
CPC分类号： C07C215/64 , C07C2601/14
摘要： The present invention relates to an improved, process for large scale production of 1-[2-(dimethylamino)-1-(4-phenol)ethyl]cyclohexanol (O-desmethylvenlafaxine) or its pharmaceutically acceptable salts with increased yield and minimal impurities.
摘要翻译：本发明涉及一种改进的大规模生产1- [2-（二甲基氨基）-1-（4-苯酚）乙基]环己醇（O-去甲基文拉法呢）或其药学上可接受的盐的方法，其具有增加的产率和最小的杂质。

19. 发明授权

US08008478B2 Process for the preparation of cefixime 有权
标题翻译：头孢克肟的制备方法
公开(公告)号：US08008478B2
公开(公告)日：2011-08-30
申请号：US11722422
申请日：2005-12-19
申请人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
发明人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
IPC分类号： C07D501/22
CPC分类号： C07D501/04
摘要： The present invention provides an improved process for the preparation of Cefixime of formula (I), a cephalosporine antibiotic with an improved quality in regard to color and solubility. This process includes: (i) reaction of 7-β-(4-chloro-2-alkoxycarbonyl methoxyimino-3-oxobutyromido)-3-cephem-4-carboxylic acid (V) with thiourea at pH 5.0 to 6.0 at temperature 25-40° C. in water, (ii) carbon treatment to the reaction mixture in presence of sodium dithionite or ethylenediaminetetraacetic acid (EDTA) followed by filtration, (iii) acidification of the filtrate obtained in step (ii) to pH 2.0 to 3.0 with acid at 50-80° C. to give cefixime ester (IV) (iv) alkaline hydrolysis of cefixime ester of formula (IV) in water followed by acidification to pH 5.0 to 6.0, (v) precipitation of cefixime (I) by adding ketone solvent followed by acidification to pH 2.0 to 3 and (vi) isolation of solid.
摘要翻译：本发明提供了一种制备式（I）的头孢克肟的改进方法，头孢菌素抗生素在颜色和溶解度方面具有改进的质量。该方法包括：（i）在温度25℃下，将7-和bgr-（4-氯-2-烷氧基羰基甲氧基亚氨基-3-氧代丁酰基）-3-头孢烯-4-羧酸（V）与硫脲在pH5.0至6.0下的反应 -40℃，（ii）在连二亚硫酸钠或乙二胺四乙酸（EDTA）存在下对反应混合物进行碳处理，然后过滤，（iii）将步骤（ii）中获得的滤液酸化至pH 2.0至3.0 （IV）的头孢克肟酯在水中碱性水解，然后酸化至pH 5.0至6.0，（v）头孢克肟（I）的沉淀通过加入酮溶剂，然后酸化至pH 2.0至3，和（vi）固体分离。

20. 发明申请

US20100286447A1 PROCESS FOR PRODUCING 1-[2-(DIMETHYLAMINO)-1-(4-PHENOL)ETHYL]CYCLOHEXANOL 有权
标题翻译： 1- [2-（二甲基氨基）-1-（4-苯酚）乙基]环己醇的制备方法
公开(公告)号：US20100286447A1
公开(公告)日：2010-11-11
申请号：US12810791
申请日：2008-12-26
申请人： Om Dutt Tyagi , Saswata Lahiri , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohan Vamsi Krishna Vadlamudi , Venkata Bala Kishore Sarma Inupakutika , Surya Nageswara Rao Achanta
发明人： Om Dutt Tyagi , Saswata Lahiri , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohan Vamsi Krishna Vadlamudi , Venkata Bala Kishore Sarma Inupakutika , Surya Nageswara Rao Achanta
IPC分类号： C07C213/02 , C07C213/10
CPC分类号： C07C215/64 , C07C2601/14
摘要： The present invention relates to an improved, process for large scale production of 1-[2-(dimethylamino)-1-(4-phenol)ethyl]cyclohexanol (O-desmethylvenlafaxine) or its pharmaceutically acceptable salts with increased yield and minimal impurities.
摘要翻译：本发明涉及一种改进的大规模生产1- [2-（二甲基氨基）-1-（4-苯酚）乙基]环己醇（O-去甲基文拉法呢）或其药学上可接受的盐的方法，其具有增加的产率和最小的杂质。

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