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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

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。

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

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