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1. 发明授权

US08173818B2 Process for producing sulphoxide compounds 失效
标题翻译：亚砜化合物的制备方法
公开(公告)号：US08173818B2
公开(公告)日：2012-05-08
申请号：US12376631
申请日：2007-08-08
申请人： Anand Singh , Khushwant Singh , Sushil Kumar Dubey
发明人： Anand Singh , Khushwant Singh , Sushil Kumar Dubey
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Disclosed herein, a process for producing sulphoxide compound of the Formula (I) by asymmetrically oxidizing a prochiral sulphide of the Formula (II) with an effective amount of oxidizing agent in the presence of a chiral transition metal complex without using an organic solvent and base.
摘要翻译：本文公开了一种通过在手性过渡金属络合物的存在下用有效量的氧化剂不对称地氧化式（II）的前手性硫化物而制备式（I）的亚砜化合物的方法，而不使用有机溶剂和碱。

2. 发明申请

US20100179328A1 PROCESS FOR PRODUCING SULPHOXIDE COMPOUNDS 失效
标题翻译：生产硫化氧化合物的方法
公开(公告)号：US20100179328A1
公开(公告)日：2010-07-15
申请号：US12376631
申请日：2007-08-08
申请人： Anand Singh , Khushwant Singh , Sushil Kumar Dubey
发明人： Anand Singh , Khushwant Singh , Sushil Kumar Dubey
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Disclosed herein, a process for producing sulphoxide compound of the Formula (I) by asymmetrically oxidizing a prochiral sulphide of the Formula (II) with an effective amount of oxidizing agent in the presence of a chiral transition metal complex without using an organic solvent and base.
摘要翻译：本文公开了一种通过在手性过渡金属络合物的存在下用有效量的氧化剂不对称地氧化式（II）的前手性硫化物而制备式（I）的亚砜化合物的方法，而不使用有机溶剂和碱。

3. 发明授权

US07795451B2 Polymorphic forms of fluvastatin sodium and process for preparing the same 有权
标题翻译：氟伐他汀钠的多形态及其制备方法
公开(公告)号：US07795451B2
公开(公告)日：2010-09-14
申请号：US11815969
申请日：2006-02-10
申请人： Bhausaheb Chavhan , Arun Kumar Awasthi , Richa Aggarwal , Rani S. Beena , Soumendu Paul , Rajesh Kumar Thaper , Sushil Kumar Dubey
发明人： Bhausaheb Chavhan , Arun Kumar Awasthi , Richa Aggarwal , Rani S. Beena , Soumendu Paul , Rajesh Kumar Thaper , Sushil Kumar Dubey
IPC分类号： C07D209/12
CPC分类号： C07D209/10
摘要： Disclosed herein are novel polymorphic forms of Fluvastatin sodium, wherein said polymorphic forms are designated as JF, JF1, JF2, JF3 and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic forms are also disclosed. The present invention also relates to process for preparing amorphous form of Fluvastatin sodium.
摘要翻译：本文公开了氟伐他汀钠的新型多晶型物，其中所述多晶型物质命名为JF，JF1，JF2，JF3，其特征在于它们的粉末X射线衍射图，红外吸收光谱，热重分析和差示扫描量热法。还公开了制备所述多晶型物的方法。本发明还涉及制备氟伐他汀钠无定形形式的方法。

4. 发明申请

US20080300408A1 Process for Preparing a Pure Polymorphic Form of 3-Pyridyl-1-Hydroxyethylidine-1, 1-Bisphosphonic Acid Sodium Salt 审中-公开
标题翻译：制备3-吡啶基-1-羟基乙基-1,1-二膦酸钠盐的纯多形态的方法
公开(公告)号：US20080300408A1
公开(公告)日：2008-12-04
申请号：US11718857
申请日：2006-08-21
申请人： Satish Chandra Pandey , Khushi Ram , Manoj Kumar Singh , Rajesh Kumar Thaper , Sushil Kumar Dubey
发明人： Satish Chandra Pandey , Khushi Ram , Manoj Kumar Singh , Rajesh Kumar Thaper , Sushil Kumar Dubey
IPC分类号： C07F9/58
CPC分类号： C07F9/58
摘要： This process in general relates to the novel process for preparing polymorphic forms of 3-pyridyl-1-hydroxyethylidine-1,1-bisphosphonic acid sodium salt (Risedronate Sodium) in particular risedronate Form A and B employing a solvent system in an appropriate ratio. An improved process for preparation of risedronic acid is also disclosed in the present invention.
摘要翻译：该方法一般涉及使用适当比例的溶剂体系制备3-吡啶基-1-羟基乙基-1,1-二膦酸钠盐（利塞膦酸钠）的多晶形式的新方法，特别是利塞膦酸盐A和B型。本发明还公开了改进的利塞膦酸制备方法。

5. 发明授权

US06717007B1 Regiospecific synthesis of phosphonous acids 失效
标题翻译：膦酸的区域特异性合成
公开(公告)号：US06717007B1
公开(公告)日：2004-04-06
申请号：US10088381
申请日：2002-08-05
申请人： Sushil Kumar Dubey , Venkat Rajgopal , Anil Vir Singh , Saswata Lahiri , Mukesh Jagannath Wani
发明人： Sushil Kumar Dubey , Venkat Rajgopal , Anil Vir Singh , Saswata Lahiri , Mukesh Jagannath Wani
IPC分类号： C07F928
CPC分类号： C07F9/48
摘要： An improved regiospecific synthesis of organic phosphonous acids, comprising of hydrophosphorylation of an olefin with hydrophosphorous acid in the presence of an inorganic persulfate, which acts as a source of free radicals at a pH ranging from 4.5 to 7.0, in which the orientation of addition is anti-Markonikoff. The process enables production of organic phosphonous acids at lower temperature and atmospheric pressure under milder pH conditions for better regioselectivity in hydrophosphorylation and obtain the phosphonous acid with good yield and purity following simple isolation procedure. Phosphonous acids obtained by the process are commercially valuable as effective detergents and wetting agents, lubricants and lubricant additives, plasticizers for plastics and resins, corrosion inhibitors, chemicals including insecticides and pesticides, cobalt extractants and as key intermediates for preparation of commercially important angiotensin converting enzyme (ACE) inhibitors.
摘要翻译：改进的有机膦酸的区域特异性合成，其包括在无机过硫酸盐存在下与氢亚磷酸的烯烃的磷酸化作用，其在4.5至7.0的pH范围内作为自由基的来源，其中添加取向为反Markonikoff。该方法能够在较低温度和大气压下在较温和的pH条件下生产有机膦酸，以在氢磷酸化中获得更好的区域选择性，并通过简单的分离程序获得良好的产率和纯度的膦酸。通过该方法获得的亚磷酸作为有效的洗涤剂和润湿剂，润滑剂和润滑剂添加剂，用于塑料和树脂的增塑剂，腐蚀抑制剂，包括杀虫剂和农药的化学品，钴提取剂和作为制备商业上重要的血管紧张素转化酶的关键中间体是有商业价值的（ACE）抑制剂。

6. 发明授权

US08420846B2 Process for producing (S)-3-[(1-dimethylamino)ethyl] phenyl-N-ethyl-N-methyl-carbamate via novel intermediates 有权
标题翻译：通过新型中间体制备（S）-3 - [（1-二甲基氨基）乙基]苯基-N-乙基-N-甲基 - 氨基甲酸酯的方法
公开(公告)号：US08420846B2
公开(公告)日：2013-04-16
申请号：US13060666
申请日：2009-08-25
申请人： Shailendra Kumar Dubey , Vikas Bansal , Kamaljeet Pannu , Sushil Kumar Dubey
发明人： Shailendra Kumar Dubey , Vikas Bansal , Kamaljeet Pannu , Sushil Kumar Dubey
IPC分类号： C07C303/28 , C07C309/73 , C07C271/42 , C07C269/00
CPC分类号： C07C309/73 , C07B2200/07 , C07C213/00 , C07C269/00 , C07C215/50 , C07C271/44
摘要： Disclosed herein are novel intermediates and process for large scale production of (S)-3-[(1-dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate (rivastigmine) or its pharmaceutically acceptable salts employing the novel intermediates. Further provided are methods for producing the novel intermediates thereof.
摘要翻译：本文公开了新型中间体和用于大规模生产（S）-3 - [（1-二甲基氨基）乙基]苯基-N-乙基-N-甲基 - 氨基甲酸酯（利伐斯的明）或其药学上可接受的盐的新型中间体的方法。还提供了制备其新型中间体的方法。

7. 发明申请

US20110184167A1 PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES 失效
标题翻译：制备纤维素及其中间体的方法
公开(公告)号：US20110184167A1
公开(公告)日：2011-07-28
申请号：US13016235
申请日：2011-01-28
申请人： Nitin Gupta , Vishal Handa , Abir Kumar Pal , Hemant Kumar Singh , Saswata Lahiri , Sushil Kumar Dubey
发明人： Nitin Gupta , Vishal Handa , Abir Kumar Pal , Hemant Kumar Singh , Saswata Lahiri , Sushil Kumar Dubey
IPC分类号： C07D498/12 , C07D407/12
CPC分类号： C07D498/18 , C07D319/06
摘要： Novel intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).
摘要翻译：新型中间体，其制备方法及其在制备治疗有效的抗肿瘤药物中的用途，特别是式（I）的替西罗莫司。

8. 发明授权

US07078532B2 Process for manufacture of fosinopril sodium 失效
标题翻译：生产福辛普利钠的方法
公开(公告)号：US07078532B2
公开(公告)日：2006-07-18
申请号：US10297224
申请日：2001-08-17
申请人： Sushil Kumar Dubey , Saswata Lahiri , Anil Vir Singh
发明人： Sushil Kumar Dubey , Saswata Lahiri , Anil Vir Singh
IPC分类号： C07F9/553
CPC分类号： C07F9/572
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.
摘要翻译：本发明公开了一种在两个步骤中合成作为高纯度的单一所需异构体的福辛普利的方法，包括（a）以四种非对映异构体的混合物制备福辛普利，和（b）通过形成从所述混合物中分离所需的异构体的碱金属盐，随后结晶。

9. 发明申请

US20060122401A1 Process for manufacture of fosinopril sodium 审中-公开
公开(公告)号：US20060122401A1
公开(公告)日：2006-06-08
申请号：US11270358
申请日：2005-11-09
申请人： Sushil Kumar Dubey , Saswata Lahiri , Anil Singh
发明人： Sushil Kumar Dubey , Saswata Lahiri , Anil Singh
IPC分类号： C07F9/547
CPC分类号： C07F9/572
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.

10. 发明申请

US20110301189A1 STABLE PHARMACEUTICAL COMPOSITIONS OF RAPAMYCIN ESTERS 审中-公开
标题翻译： RAPAMYCIN ESTER的稳定药用组合物
公开(公告)号：US20110301189A1
公开(公告)日：2011-12-08
申请号：US13151721
申请日：2011-06-02
申请人： Dhiraj Khattar , Rajesh Khanna , Poonam Singla , Abhilasha Yadav , Vinay Gupta , Rajesh Kini , Sushil Kumar Dubey
发明人： Dhiraj Khattar , Rajesh Khanna , Poonam Singla , Abhilasha Yadav , Vinay Gupta , Rajesh Kini , Sushil Kumar Dubey
IPC分类号： A61K31/436 , A61P35/00 , C07D491/153
CPC分类号： A61K9/0019 , A61K31/436 , A61K47/10 , A61K47/12
摘要： A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same.
摘要翻译：雷帕霉素酯的稳定药物组合物，特别是不含抗氧化剂的3-羟基-2-（羟甲基）-2-甲基丙酸的雷帕霉素42-酯及其制备方法。

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