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1. 发明申请

US20050245738A1 Stable bioavailable crystalline form or cefdinir and a process for the preparation thereof 审中-公开
标题翻译：稳定的生物可利用结晶形式或头孢地尼，及其制备方法
公开(公告)号：US20050245738A1
公开(公告)日：2005-11-03
申请号：US10838431
申请日：2004-05-03
申请人： Girij Singh , Himadri Sen , Dhananjai Srivastava , Himanshu Godbole , Gurvinder Singh , Pravin Mahajan , Umesh Rananaware , Sagar Nehate , Sanjay Wagh
发明人： Girij Singh , Himadri Sen , Dhananjai Srivastava , Himanshu Godbole , Gurvinder Singh , Pravin Mahajan , Umesh Rananaware , Sagar Nehate , Sanjay Wagh
IPC分类号： A61K31/545 , C07D501/00 , C07D501/18
CPC分类号： C07D501/00
摘要： The present invention relates to a stable and bioavailable crystalline form of a third generation cephalosporin antibiotic, cefdinir and a process for the preparation thereof. The present invention also relates to a pharmaceutical composition containing the novel crystalline cefdinir, useful in the treatment of maladies such as bacterial infections.
摘要翻译：本发明涉及第三代头孢菌素抗生素，头孢地尼的稳定和生物可利用的结晶形式及其制备方法。本发明还涉及含有新型结晶头孢地尼的药物组合物，其可用于治疗诸如细菌感染的疾病。

2. 发明申请

US20080071089A1 Process for the Manufacture of Rabeprazole Sodium 审中-公开
标题翻译：雷贝拉唑钠制造方法
公开(公告)号：US20080071089A1
公开(公告)日：2008-03-20
申请号：US11910089
申请日：2006-03-16
申请人： Girij Singh , Rajinder Siyan , Gurvinder Singh , Rajendra Mahale
发明人： Girij Singh , Rajinder Siyan , Gurvinder Singh , Rajendra Mahale
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A process for manufacture of amorphous Rabeprazole sodium with mean particle diameter between 10 to 55 μm said process comprising addition of Rabeprazole to aqueous sodium hydroxide; addition of ethyl alcohol to the solution; distillation of solvents from the solution thus obtained till thick mass is obtained; addition of an organic solvent to the residue to obtain a clear solution; addition of this clear solution to an anti- solvent under agitation and isolation of the product.
摘要翻译：一种平均粒径为10-55μm的无定形雷贝拉唑钠的方法，所述方法包括将雷贝拉唑加入到氢氧化钠水溶液中; 向溶液中加入乙醇; 从得到的溶液中蒸馏出溶剂，直至得到稠质; 向残余物中加入有机溶剂以获得澄清溶液; 在搅拌和分离产物的同时将这种澄清溶液加入到抗溶剂中。

3. 发明申请

US20070149604A1 Novel method for preparation of crystalline perindopril erbumine 失效
标题翻译：用于制备结晶培哚普利埃布胆碱的新方法
公开(公告)号：US20070149604A1
公开(公告)日：2007-06-28
申请号：US10576386
申请日：2003-10-21
申请人： Girij Singh , Himanshu Godbole , Sagar Nehate
发明人： Girij Singh , Himanshu Godbole , Sagar Nehate
IPC分类号： A61K31/405 , C07D209/42
CPC分类号： C07D209/42
摘要： A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in FIG. 2 The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N,N-dimethylformamide, dimethyl acetals of lower aliphatic aldehydes, dimethyl ketals of lower aliphatic ketones and 1,2-dialkoxyethane with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20° C. to 30° C., and further cooling to 0° C. to 15° C. for 30 minutes to 1 hour and finally filtering off and drying the crystals.
摘要翻译：制备式（II）的结晶培哚普利埃布林的方法，其显示如图1所示的X射线（粉末）衍射图案。 2该方法包括使式（I）培哚普利溶液在选自N，N-二甲基甲酰胺，低级脂族醛的二甲基缩醛，低级脂族酮和1,2-二烷氧基乙烷的二甲基缩酮与叔丁胺的溶剂和结晶通过将反应混合物加热回流，从而过滤热，逐渐冷却至20℃至30℃，并进一步冷却至0℃至15℃，持续30分钟至1小时，从而获得最后过滤并干燥晶体。

4. 发明申请

US20060058347A1 Crystalline form for quinapril hydrochloride and process for preparing the same 失效
标题翻译：喹那普利盐酸盐的结晶形式及其制备方法
公开(公告)号：US20060058347A1
公开(公告)日：2006-03-16
申请号：US10538858
申请日：2002-12-16
申请人： Girij Singh , Govind Rawat , Vilas Dhake , Sagar Nehate
发明人： Girij Singh , Govind Rawat , Vilas Dhake , Sagar Nehate
IPC分类号： A61K31/47 , C07D217/06
CPC分类号： C07D217/26
摘要： A novel crystalline form of quinapril hydrochloride of formula (I) An amorphous form of quinapril hydrochloride substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications formed from the said novel crystalline form of quinapril hydrochloride of formula (I). The crystalline quinapril hydrochloride is in the form nitroalkane solvate in which the nitroalkane is nitromethane, nitroethane and nitropropane. Each such nitroalkane solvate having particular characteristic X-ray diffraction patterns. A process for preparation of amorphous form of quinapril hydrochloride, substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications, using the novel crystalline quinapril hydrochloride as an intermediate. The process involves obtaining free base compound of formula (V) by adjusting the pH of a solution of the benzyl ester maleate salt of quinapril of formula (V) between 7.5-8.5 in a mixture of water and an organic solvent; catalytic hydrogenation of this compound (V) in an alcoholic solvent in the presence of concentrated hydrochloric acid or hydrogen chloride dissolved in an alcoholic solvent and in the presence of catalytic amounts of Pd/C to obtain a residue containing formula (I); crystallization of the said residue by evaporating the alcoholic solvent from a nitroalkane solvent to give crystalline quinapril hydrochloride, associated with a solvate of the nitroalkane solvent, and drying the crystalline quinapril hydrochloride nitroalkane solvate at a temperature between 40° C. and 45° C. under vacuum to give amorphous quinapril hydrochloride of formula (I).
摘要翻译：式（I）的盐酸喹那普利的新型结晶形式

5. 发明申请

US20060149056A1 Stable bioavailable crystalline form of cefdinir and a process for the preparation thereof 审中-公开
标题翻译：头孢地尼的稳定的生物可利用结晶形式及其制备方法
公开(公告)号：US20060149056A1
公开(公告)日：2006-07-06
申请号：US11365915
申请日：2006-03-02
申请人： Girij Singh , Himadri Sen , Dhananjai Srivastava , Himanshu Godbole , Gurvinder Singh , Pravin Mahajan , Umesh Rananaware , Sagar Nehate , Sanjay Wagh
发明人： Girij Singh , Himadri Sen , Dhananjai Srivastava , Himanshu Godbole , Gurvinder Singh , Pravin Mahajan , Umesh Rananaware , Sagar Nehate , Sanjay Wagh
IPC分类号： C07D501/14
CPC分类号： C07D501/00
摘要： The present invention relates to a stable and bioavailable crystalline form of a third generation cephalosporin antibiotic, cefdinir and a process for the preparation thereof. The present invention also relates to a pharmaceutical composition containing the novel crystalline cefdinir, useful in the treatment of maladies such as bacterial infections.
摘要翻译：本发明涉及第三代头孢菌素抗生素，头孢地尼的稳定和生物可利用的结晶形式及其制备方法。本发明还涉及含有新型结晶头孢地尼的药物组合物，其可用于治疗诸如细菌感染的疾病。

6. 发明申请

US20060276659A1 Process for preparation of perindopril and salts thereof 有权
标题翻译：培哚普利及其盐的制备方法
公开(公告)号：US20060276659A1
公开(公告)日：2006-12-07
申请号：US10547243
申请日：2003-02-28
申请人： Debashish Datta , Girij Singh , Himanshu Godbole , Rajinder Siyan
发明人： Debashish Datta , Girij Singh , Himanshu Godbole , Rajinder Siyan
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , C07C227/32 , C07C227/34 , C07C229/12
摘要： A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.
摘要翻译：制备式（II）的培哚普利及其盐的方法，其简单，安全的方便和成本有效。该方法包括式（I）化合物，其中X是氯或溴与式（Ⅶ）化合物反应，其中A表示双环系统的六元环是饱和或不饱和的，得到式（Ⅷ）化合物），其中A如上所定义，然后将由此获得的式（VIII）化合物进行催化氢化，得到式（II）的培哚普利。上述制造培哚普利的方法将特别避免使用通常用于制造的有害化学物质如光气或昂贵的偶联剂如二环己基碳二亚胺和1-羟基苯并三唑。该方法也不需要任何催化剂的干预，并且不需要任何碱性或酸性反应条件。重要的是，该方法提供了高度立体选择性地给予符合药代动力学规范的在分子的所有五个手性中心具有（S） - 构型的培哚普利（II）的培哚普利的培哚普利。本发明还涉及制备式（I）化合物的方法，还涉及制备式（III）化合物的N - [（S）-1-甲氧基丁基] - （S） - 丙氨酸的方法，处理。

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