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51. 发明申请

US20060276463A1 Pure levofloxacin hemihydrate and processes for preparation thereof 审中-公开
标题翻译：纯左氧氟沙星半水合物及其制备方法
公开(公告)号：US20060276463A1
公开(公告)日：2006-12-07
申请号：US10539130
申请日：2003-12-15
申请人： Tarun Sharma , Pramed Kumar , Prosenjit Bose , Yatendra Kumar
发明人： Tarun Sharma , Pramed Kumar , Prosenjit Bose , Yatendra Kumar
IPC分类号： A61K31/538 , C07D491/04
CPC分类号： C07D498/06
摘要： The invention relates to pure levofloxacin hemihydrate and a process for preparing pure levofloxacin hemihydrate. The invention also relates to pharmaceutical compositions that include the pure levofloxacin hemihydrate and use of said compositions for treating a patient in need of an antimicrobial therapy.
摘要翻译：本发明涉及纯左氧氟沙星半水合物和制备纯左氧氟沙星半水合物的方法。本发明还涉及包含纯左氧氟沙星半水合物和所述组合物用于治疗需要抗微生物治疗的患者的药物组合物。

52. 发明申请

US20060252789A1 Amorphous moxifloxacin hydrochloride 审中-公开
标题翻译：无定型莫西沙星盐酸盐
公开(公告)号：US20060252789A1
公开(公告)日：2006-11-09
申请号：US10533246
申请日：2003-10-30
申请人： Sujay Biswas , Prosenjit Bose , Yatendra Kumar
发明人： Sujay Biswas , Prosenjit Bose , Yatendra Kumar
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The invention relates to an amorphous form of moxifloxacin hydrochloride and processes for preparing amorphous moxifloxacin hydrochloride. The invention also relates to pharmaceutical compositions that include the amorphous moxifloxacin hydrochloride and use of said compositions for the treatment of bacterial infections.
摘要翻译：本发明涉及无定形形式的莫西沙星盐酸盐和制备盐酸莫西沙星的方法。本发明还涉及包含无定形莫西沙星盐酸盐和所述组合物用于治疗细菌感染的药物组合物。

53. 发明申请

US20060211761A1 Hmg-coa-reductase inhibitors 审中-公开
标题翻译： Hmg-coa还原酶抑制剂
公开(公告)号：US20060211761A1
公开(公告)日：2006-09-21
申请号：US10520726
申请日：2003-07-08
申请人： Yatendra Kumar , Ram Aryan , Jitendra Sattigeri , Mohammad Salman , Gowri Shankar , Kumar Bhushan , Bhargav Pandya , Ramnik Sharma
发明人： Yatendra Kumar , Ram Aryan , Jitendra Sattigeri , Mohammad Salman , Gowri Shankar , Kumar Bhushan , Bhargav Pandya , Ramnik Sharma
IPC分类号： A61K31/4025 , A61K31/401 , C07D405/02
CPC分类号： C07D207/34
摘要： The invention relates to particular hydroxyl and protected hydroxyl derivatives of compounds known to be useful as HMG CoA-reductase inhibitors. In particular, herein are provided hydroxyl and protected hydroxyl compounds of Formula I and their corresponding lactones.
摘要翻译：本发明涉及已知可用作HMG CoA还原酶抑制剂的化合物的特定羟基和被保护的羟基衍生物。特别地，本文提供式I的羟基和保护的羟基化合物及其相应的内酯。

54. 发明申请

US20060142574A1 Process for the preparation of ganciclovir 审中-公开
标题翻译：更昔洛韦制备方法
公开(公告)号：US20060142574A1
公开(公告)日：2006-06-29
申请号：US10532910
申请日：2003-10-31
申请人： Jayachandra Babu , Purna Ray , Chandra Khanduri , Yatendra Kumar
发明人： Jayachandra Babu , Purna Ray , Chandra Khanduri , Yatendra Kumar
IPC分类号： C07D473/10
CPC分类号： C07D473/18
摘要： The present invention relates to a process for the preparation of N2-Acetyl-9-(1,3-diace-toxy-2-propoxymethyl) guanine, referred to here as N-9 alkylated isomer of structural formula I, and to the use of this compound as an intermediate for the preparation of antiviral compound, ganciclovir.
摘要翻译：本发明涉及一种制备本文中称为结构式I的N-9烷基化异构体的N 2 - 乙酰基-9-（1,3-二乙酰氧基-2-丙氧基甲基）鸟嘌呤的方法和用途的该化合物作为制备抗病毒化合物更昔洛韦的中间体。

55. 发明授权

US07045618B2 Cefpodixime proxetil 失效
标题翻译：头孢泊肟酯
公开(公告)号：US07045618B2
公开(公告)日：2006-05-16
申请号：US10469330
申请日：2002-02-27
申请人： Yatendra Kumar , Kaptan Singh , Rakesh Kumar Arora
发明人： Yatendra Kumar , Kaptan Singh , Rakesh Kumar Arora
IPC分类号： C07D501/34
CPC分类号： C07D501/00
摘要： The present invention relates to an improved and cost effective process for the industrial manufacture of cefpodoxime proxetil. More specifically, the present invention relates to the preparation of cefpodoxime proxetil of high purity and yield. The process comprises a) dissolving impure cefpodoxime proxetil or adding a solution containing cefpodoxime proxetil into a polar organic solvent or mixture(s) thereof, optionally reducing the solvent by concentration, and adding into a non-polar organic solvent or mixture(s) thereof to precipitate the solid; and b) dissolving the solid obtained from the above step into water-miscible polar organic solvent, optionally reducing the solvent by concentration, adding it into water to obtain the pure cefpodoxime proxetil.
摘要翻译：本发明涉及一种改进和成本有效的工业制造头孢泊肟酯的方法。更具体地，本发明涉及高纯度和产率的头孢泊肟酯的制备。该方法包括：a）将不纯的头孢泊肟原料溶解或加入含有头孢泊肟酯的极性有机溶剂或其混合物，任选地通过浓缩来还原溶剂，并加入到非极性有机溶剂或其混合物中沉淀固体; b）将上述步骤得到的固体溶解于水溶性极性有机溶剂中，任选地通过浓缩来还原溶剂，将其加入水中，得到纯头孢泊肟原料。

56. 发明申请

US20060040915A1 Process for the preparation of cefdinir 审中-公开
标题翻译：头孢地尼的制备方法
公开(公告)号：US20060040915A1
公开(公告)日：2006-02-23
申请号：US10513004
申请日：2002-04-26
申请人： Yatendra Kumar , Mohan Prasad , Ashok Prasad , Shailendra Singh , Neela Kumar
发明人： Yatendra Kumar , Mohan Prasad , Ashok Prasad , Shailendra Singh , Neela Kumar
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/22 , C07D501/00
摘要： The present invention relates to a process for the preparation of cefdinir on an industrial scale.
摘要翻译：本发明涉及以工业规模制备头孢地尼的方法。

57. 发明申请

US20050154231A1 Tamsulosin derivative 失效
标题翻译：坦索罗辛衍生物
公开(公告)号：US20050154231A1
公开(公告)日：2005-07-14
申请号：US11016264
申请日：2004-12-17
申请人： Yatendra Kumar , Ram Aryan , Radhakrishnan Shankar , Kumar Bhushan , Anita Chugh
发明人： Yatendra Kumar , Ram Aryan , Radhakrishnan Shankar , Kumar Bhushan , Anita Chugh
IPC分类号： A61K31/18 , A61P13/08 , C07C303/40 , C07C311/37
CPC分类号： C07C311/37 , C07C303/40
摘要： The optically active compound, R (−)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-hydroxybenzenesulfonamide in good optical purity, a metabolite of the α1-adrenergic blocking agent tamsulosin, and methods for the preparation thereof. Pharmaceutical compositions including the optically active compound and methods of treatment comprising administration of an effective α1-adrenergic antagonistic amount of such compositions to mammals.
摘要翻译：具有良好光学纯度的旋光活性化合物R（ - ） - 5- [2 - [[2-（2-乙氧基苯氧基）乙基]氨基]丙基] -2-羟基苯磺酰胺是α< SUB-肾上腺素能阻断剂坦洛新，及其制备方法。包括光学活性化合物的药物组合物和治疗方法包括向哺乳动物施用有效的α1 - 肾上腺素能拮抗剂量的这种组合物。

58. 发明授权

US06602999B1 Amorphous form of cefpodoxime proxetil 失效
标题翻译：无定形形式的头孢泊肟酯
公开(公告)号：US06602999B1
公开(公告)日：2003-08-05
申请号：US10048354
申请日：2002-05-21
申请人： Yatendra Kumar , Rakesh Kumar Arora , Kaptan Singh
发明人： Yatendra Kumar , Rakesh Kumar Arora , Kaptan Singh
IPC分类号： C07D50134
CPC分类号： C07D501/00
摘要： A novel process for the production of an improved amorphous form of cefpodoxime proxetil [(6R-[6&agr;,7&bgr;(Z))]-7-{E(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid-1-[[(1-methylethoxy)carboxylic acid-1-[[(1-methylethoxy)carbonyl]oxy]ethyl ester, is described.
摘要翻译：一种改进的无定形形式的头孢泊肟原料[（6R- [6α，7beta（Z））] - 7- {E（2-氨基-4-噻唑基）（甲氧基亚氨基）乙酰基]氨基] -3 - （甲氧基甲基）-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸-1 - [[（1-甲基乙氧基）羧酸-1 - [[（1 - 甲基乙氧基）羰基]氧基]乙酯。

59. 发明授权

US5939564A Process of lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的过程
公开(公告)号：US5939564A
公开(公告)日：1999-08-17
申请号：US055572
申请日：1998-04-06
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50.degree. C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.
摘要翻译：在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中的新方法使用非常温和的反应条件。改进的方法包括通过在无水条件下从环境温度至溶剂回流的温度加热，将开环羟基酸形式的他汀类药物溶解在有机溶剂中，以产生溶液，用温和的催化剂处理溶液温度为约环境温度至50℃，并向溶液中加入水，使得内酯形式的他汀类从反应混合物中结晶。反应中使用的温和催化剂是有机碱与有机或无机酸的盐，例如吡啶氢溴酸盐，吡啶盐酸盐或吡啶鎓对甲苯磺酸盐。有机溶剂包括低级链烷醇，非醇极性溶剂或两者的混合物。

60. 发明授权

US5763646A Process for manufacturing simvastatin from lovastatin or mevinolinic acid 失效
标题翻译：从洛伐他汀或甲维林酸生产辛伐他汀的方法
公开(公告)号：US5763646A
公开(公告)日：1998-06-09
申请号：US816573
申请日：1997-03-13
申请人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30 , C07C67/02
CPC分类号： C07D309/30
摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.
摘要翻译：以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基，然后关闭开放的吡喃酮环以产生辛伐他汀。在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

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