公开(公告)号：US20080275241A1

公开(公告)日：2008-11-06

申请号：US12158708

申请日：2006-12-22

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Nandu Baban Bhise ,  Kamlesh Digambar Sawant ,  Tushar Anil Naik ,  Neeraj Srivastav ,  Raviraj Bhatu Deore

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Nandu Baban Bhise ,  Kamlesh Digambar Sawant ,  Tushar Anil Naik ,  Neeraj Srivastav ,  Raviraj Bhatu Deore

IPC分类号： C07D455/03

CPC分类号： C07D471/18

摘要： The present disclosure relates to a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one or Dolasetron base. It also discloses a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one mesylate or Dolasetron mesylate. Further, the present disclosure relates to a process for producing Form I of Dolasetron base, and to the novel crystalline polymorphs, Form II, III, IV and V of Dolasetron base and industrial processes for producing them.

摘要翻译： 本公开涉及制备内 - 六氢-8-（3-吲哚基羰基氧基）-2,6-亚甲基-2H-喹嗪啉-3（4H） - 酮或多拉司琼碱的方法。 还公开了制备内六氢-8-（3-吲哚基羰基氧基）-2,6-亚甲基-2H-喹嗪酮-3（4H） - 酮甲磺酸酯或甲磺酸多拉司琼的方法。 此外，本公开内容涉及制备杜拉司琼碱的形式I的方法，以及Dolasetron碱的新型结晶多晶型II，III，IV和V以及用于生产它们的工业方法。

公开(公告)号：US20080319226A1

公开(公告)日：2008-12-25

申请号：US12092657

申请日：2005-11-09

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Nandu Baban Bhise ,  Avinash Venkatraman Naidu ,  Umesh Parashram Aher ,  Sachin Shivaji Patil

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Nandu Baban Bhise ,  Avinash Venkatraman Naidu ,  Umesh Parashram Aher ,  Sachin Shivaji Patil

IPC分类号： C07C231/00

CPC分类号： C07C253/30 ,  C07C253/34 ,  C07C255/41

摘要： A process for the preparation of highly pure (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (Entacapone). It comprises condensing 3,4-dihydroxy-5-nitro benzaldehyde with N,N-diethyl cyano acetamide in an organic solvent in the presence of an organic base and an acid under reflux conditions followed by distilling off the solvent under vacuum and treating the residue with a lower aliphatic carboxylic acid at 40-8O0 C. The resulting residue is extracted with a chlorinated solvent and the solvent is distilled off under vacuum. The resulting residue is extracted with an organic solvent to obtain crude N,N-diethyl-2-cyano-3-3,4-dihydroxy-5-nitrophenyl)acrylamide. The crude product N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide formed is treated with a mixture of organic alcohol and organic acid in the molar ratio of the crude product to organic alcohol 1:5 to 15 and crude product to organic acid 1:1 to 3 under reflux conditions.

摘要翻译： 制备高纯度（E）-N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺（恩他卡朋）的方法。 它包括在有机碱和酸的存在下，在回流条件下，将3,4-二羟基-5-硝基苯甲醛与N，N-二乙基氰基乙酰胺在有机溶剂中缩合，然后在真空下蒸除溶剂，并处理残余物 与40-80℃的低级脂族羧酸反应。所得残余物用氯化溶剂萃取，真空蒸除溶剂。 所得残余物用有机溶剂萃取，得到粗N，N-二乙基-2-氰基-3-3,4-二羟基-5-硝基苯基）丙烯酰胺。 所形成的粗产物N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺以有机醇与有机酸的混合物以粗产物与有机醇的摩尔比 1:5至15，并在回流条件下将粗产物与有机酸1:1至3反应。

公开(公告)号：US20080171884A1

公开(公告)日：2008-07-17

申请号：US11908846

申请日：2005-06-03

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Narayana Rao Mantripragada ,  Rajesh Bhopalkar ,  Kamlesh Digambar Sawant ,  Dattatraya Nivrutti Chavan

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Narayana Rao Mantripragada ,  Rajesh Bhopalkar ,  Kamlesh Digambar Sawant ,  Dattatraya Nivrutti Chavan

IPC分类号： C07D209/04

CPC分类号： C07D209/24

摘要： A Polymorph Form G of Fluvastatin sodium having X-ray diffraction peak at 2θ value of 3.48 is provided. A process for the preparation of the novel polymorph Form G comprising spray drying a 3 to 10% w/v solution of Fluvastatin sodium in a solvent using a spray gun at inlet temperature of 120 to 200° C. and outlet temperature of 60 to 110° C. of the spray gun is also provided.

摘要翻译： 提供了在2θ值为3.48时具有X射线衍射峰的氟伐他汀钠的多晶型物G. 一种用于制备新型多晶型物G的方法，包括使用喷枪在入口温度为120-200℃，出口温度为60-110℃下，使溶剂中的氟伐他汀钠3至10％w / v溶液喷雾干燥 也提供了喷枪的°C。

公开(公告)号：US07847112B2

公开(公告)日：2010-12-07

申请号：US10569036

申请日：2004-07-16

申请人： Narayana Rao Mantripragada ,  Dhananjay Govind Sathe ,  Venkatasubramanian Radhakrishnan Tarur ,  Kamlesh Digambar Sawant ,  Gautam Ramjibhai Patel

发明人： Narayana Rao Mantripragada ,  Dhananjay Govind Sathe ,  Venkatasubramanian Radhakrishnan Tarur ,  Kamlesh Digambar Sawant ,  Gautam Ramjibhai Patel

IPC分类号： C07C50/00 ,  A61K31/12 ,  A01N35/00

CPC分类号： C07C50/32 ,  C07C46/10

摘要： Novel crystalline forms of anti Pneumocystis carinii compound (2-[4-(4-Chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone) commonly known as Atovaquone and methods for producing the same is disclosed herein. This also provides pharmaceutical compositions comprising the said polymorphs of Atovaquone and method of treating Pneumocystis carinii pneumonia, the method comprising administering to a warm blooded animal an effective amount of a product-by-process composition of matter comprising polymorphic forms of Atovaquone.

摘要翻译： 通常称为Atovaquone的抗卡氏肺囊虫化合物（2- [4-（4-氯苯基）环己基] -3-羟基-1,4-萘醌）的新型结晶形式及其制备方法公开。 这也提供了包含所述Atovaquone多晶型物和治疗卡氏肺囊虫肺炎的方法的药物组合物，该方法包括向温血动物施用有效量的包含多佐型酮的多形态物质的逐步产物组合物。

公开(公告)号：US20090304797A1

公开(公告)日：2009-12-10

申请号：US12304148

申请日：2007-06-22

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Narayana Rao ,  Kamles Digambar Sawant ,  Sasi Kumar Mohan Thoovara ,  Bhupendra Shaligram Rane

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Narayana Rao ,  Kamles Digambar Sawant ,  Sasi Kumar Mohan Thoovara ,  Bhupendra Shaligram Rane

IPC分类号： A61K9/14 ,  C07D257/04 ,  A61K31/41 ,  A61P9/12

CPC分类号： A61K9/145 ,  A61K31/41

摘要： The present invention relates to process for preparing micronized Valsartan with particle size distribution of d10 less than 5μ, d50 less than 10μ and d90 less than 20μ preferably d90

摘要翻译： 本发明涉及具有d10小于5mu，d50小于10mu和d90小于20mu，优选d90 <10mu的粒度分布的微粉化缬沙坦的方法。

公开(公告)号：US07439365B2

公开(公告)日：2008-10-21

申请号：US10879816

申请日：2004-06-29

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Avinash Venkatraman Naidu ,  Umesh Parashram Aher

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Avinash Venkatraman Naidu ,  Umesh Parashram Aher

IPC分类号： C07D211/02

CPC分类号： C07D211/32 ,  C07D211/22

摘要： The present invention relates to the oxalate salt of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine, commonly known as Donepezil, and its method of preparation.

摘要翻译： 本发明涉及通常称为多奈哌齐的1-苄基-4 - [（5,6-二甲氧基-1-二氢茚酮）-2-基]甲基哌啶的草酸盐及其制备方法。

公开(公告)号：US08187634B2

公开(公告)日：2012-05-29

申请号：US12377129

申请日：2007-08-31

申请人： Deepak Anant Hegde ,  Varsha Shashank Choudhary ,  Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Harish Kashinath Mondkar ,  Samadhan Daulat Patil ,  Sasikumar Mohan Thoovara ,  Yogesh Sharad Bhide

发明人： Deepak Anant Hegde ,  Varsha Shashank Choudhary ,  Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Harish Kashinath Mondkar ,  Samadhan Daulat Patil ,  Sasikumar Mohan Thoovara ,  Yogesh Sharad Bhide

IPC分类号： A61K31/785 ,  A61K9/28 ,  A61P13/12 ,  C08G61/02

CPC分类号： A61K31/785 ,  A61K9/284 ,  A61K9/2846 ,  A61K9/2866 ,  C08F8/02 ,  C08F8/08 ,  C08F126/02

摘要： Disclosed herein is an improved process for preparation of Sevelamer hydrochloride having phosphate binding capacity of 4.7 to 6.4 mmol/g. Further, the invention discloses Sevelamer hydrochloride compositions and a novel process for preparation of said compositions comprising high shear non-aqueous granulation.

摘要翻译： 本文公开了一种改进的具有4.7至6.4mmol / g的磷酸盐结合能力的盐酸司维拉姆的制备方法。 此外，本发明公开了盐酸司维拉姆组合物和用于制备包含高剪切非水性造粒物的所述组合物的新方法。

公开(公告)号：US20100092421A1

公开(公告)日：2010-04-15

申请号：US12620931

申请日：2009-11-18

申请人： Deepak Anant Hegde ,  Varsha Shashank Choudhary ,  Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Harish Kashinath Mondkar ,  Samadhan Daulat Patil ,  Sasikumar Mohan Thoovara ,  Yogesh Sharad Bhide

发明人： Deepak Anant Hegde ,  Varsha Shashank Choudhary ,  Venkatasubramanian Radhakrishnan Tarur ,  Dhananjay Govind Sathe ,  Harish Kashinath Mondkar ,  Samadhan Daulat Patil ,  Sasikumar Mohan Thoovara ,  Yogesh Sharad Bhide

IPC分类号： A61K31/785 ,  A61P13/12 ,  C08G61/02

CPC分类号： A61K31/785 ,  A61K9/284 ,  A61K9/2846 ,  A61K9/2866 ,  C08F8/02 ,  C08F8/08 ,  C08F126/02

摘要： Disclosed herein is an improved process for preparation of Sevelamer hydrochloride having phosphate binding capacity of 4.7 to 6.4 mmol/g. Further, the invention discloses Sevelamer hydrochloride compositions and a novel process for preparation of said compositions comprising high shear non-aqueous granulation.

摘要翻译： 本文公开了一种改进的具有4.7至6.4mmol / g的磷酸盐结合能力的盐酸司维拉姆的制备方法。 此外，本发明公开了盐酸司维拉姆组合物和用于制备包含高剪切非水性造粒物的所述组合物的新方法。

公开(公告)号：US20080076928A1

公开(公告)日：2008-03-27

申请号：US11412294

申请日：2006-04-27

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Dhanajay Govind Sathe ,  Avinash Vankatraman Naidu ,  Kamiesh Digamber Sawant ,  Tushar Anil Naik ,  Umesh Parashram Aher ,  Sachin Shivali Patil

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Dhanajay Govind Sathe ,  Avinash Vankatraman Naidu ,  Kamiesh Digamber Sawant ,  Tushar Anil Naik ,  Umesh Parashram Aher ,  Sachin Shivali Patil

IPC分类号： C07D221/00

CPC分类号： C07D211/32

摘要： New salts of donepezil, and new polymorphic forms of donepezil and its salts, and methods to prepare both the amorphous form and various polymorphic forms of donepezil or its salts.

摘要翻译： 多奈哌齐的新盐和多奈哌齐及其盐的新型多晶型物，以及制备多奈哌齐或其盐的无定形形式和多种形式的方法。

公开(公告)号：US20090209764A1

公开(公告)日：2009-08-20

申请号：US12418803

申请日：2009-04-06

申请人： Venkatasubramanian Radhakrishnan Tarur ,  Suresh Mahadev Kadam ,  Anil Purushottam Joshi ,  Sachin Baban Gavhane

发明人： Venkatasubramanian Radhakrishnan Tarur ,  Suresh Mahadev Kadam ,  Anil Purushottam Joshi ,  Sachin Baban Gavhane

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： A process for the preparation of imiquimod comprising oxidation of 1-Isobutyl-1H-imidazo quinoline quinoline (II) afforded 1-Isobutyl-1H-imidazo-[4,5-c]-quinoline-5-N-oxide (III) which is isolated in pure form as its hydrochloride salt (IV) followed by conversion to 4-chloro derivative (V) and conversion to corresponding 4-iodo derivative (VI) which is a new intermediate. This new intermediate in convened to imiquimod (VIII) and purified via its novel maleate salt.

摘要翻译： 一种制备咪喹莫特的方法，其包括1-异丁基-1H-咪唑并喹啉喹啉（II）的氧化，得到1-异丁基-1H-咪唑并[4,5-c] - 喹啉-5-氧化物（III），其中 以其盐酸盐（IV）的形式分离，然后转化为4-氯衍生物（V），转化为相应的新的中间体4-碘衍生物（VI）。 这种新的中间体被召集到咪喹莫特（VIII）并通过其新的马来酸盐进行纯化。