公开(公告)号：US20100210848A1

公开(公告)日：2010-08-19

申请号：US12681386

申请日：2008-10-03

Applicant: Ashok Kumar ,  Dharmendra Singh ,  Nellithanath Thankachen Byju ,  Prasad Shankar Kadam ,  Harishankar Prahladkumar Vishwakarma ,  Vijay Ojha ,  Umeshkumar Suresh Ninawe

Inventor： Ashok Kumar ,  Dharmendra Singh ,  Nellithanath Thankachen Byju ,  Prasad Shankar Kadam ,  Harishankar Prahladkumar Vishwakarma ,  Vijay Ojha ,  Umeshkumar Suresh Ninawe

IPC: C07D401/12

CPC classification number: C07D401/12

Abstract: The present invention discloses novel processes for preparing optically active sulphoxide compounds of formula I by asymmetric oxidation of prochiral sulphide compounds of Formula II. More particularly, the invention discloses processes for preparation of optically active proton pump Inhibitors (PPIs) or their optically active precursor (=intermediate) compounds (Formula I) that can be converted into pharmaceutically useful PPIs.

Abstract translation: 本发明公开了通过式II的前手性硫化物化合物的不对称氧化制备式I的光学活性亚砜化合物的新方法。 更具体地，本发明公开了可转化为药学上有用的PPI的光学活性质子泵抑制剂（PPI）或其光学活性前体（=中间体）化合物（式I）的制备方法。

公开(公告)号：US20110166347A1

公开(公告)日：2011-07-07

申请号：US13062416

申请日：2009-09-09

Applicant: Ashok Kumar ,  Dharmendra Singh ,  Umesh Luthara ,  Yogesh Mohandhai Patel

Inventor： Ashok Kumar ,  Dharmendra Singh ,  Umesh Luthara ,  Yogesh Mohandhai Patel

IPC: C07D413/12 ,  C12P17/04 ,  C07D307/88

CPC classification number: C07D307/88 ,  C12P17/04

Abstract: The present invention discloses an isolation and purification process for mycophenolic acid obtained from the fermentation process. Invention further discloses preparation of sodium salt of mycophenolic acid and mycophenolate mofetil from mycophenolic acid.

Abstract translation: 本发明公开了从发酵过程获得的霉酚酸的分离纯化方法。 本发明还公开了霉酚酸的霉酚酸和霉酚酸酯的钠盐的制备。

公开(公告)号：US20100081839A1

公开(公告)日：2010-04-01

申请号：US12509145

申请日：2009-07-24

Applicant: Ashok KUMAR ,  Priti Jayesh Bhayani ,  Vaibhav Chinubhai Doshi ,  Ashvini Saxena ,  Gunjan Pramod Pathak ,  Rashmi Abhyankar ,  Sarvanan Manavalan ,  Mukesh Purohit ,  Santosh Parihar

Inventor： Ashok KUMAR ,  Priti Jayesh Bhayani ,  Vaibhav Chinubhai Doshi ,  Ashvini Saxena ,  Gunjan Pramod Pathak ,  Rashmi Abhyankar ,  Sarvanan Manavalan ,  Mukesh Purohit ,  Santosh Parihar

IPC: C07C309/19

CPC classification number: C07D495/04

Abstract: The present invention describes an improved industrial process for crystallizing out polymorph ‘Form I’ of (+) clopidogrel hydrogen sulphate (also called clopidogrel bisulphate) in) from either a Type-1 solvent or liquid characterized by comprising two or more functional groups or their mixtures thereof; or a Type-II solvent and/or solvent mixture selected from the group of methyl ethyl ketone, cyclopentylmethyl ether, dipropylglycolether, dibutylglycol ether, propylmethyl cellosolve, butylmethylcellosolve, propylethylellosolve, butylethylcellosolve or their cross combinations in a reproducible manner without detectable contamination of polymorph designated as ‘Form II’. The invention also discloses improvements in the preparation of clopidogrel free base and process for recovery and recycling of resolving agent camphor sulphonic acid.

Abstract translation: 本发明描述了一种改进的工业方法，用于从特征在于包含两个或更多个官能团的1型溶剂或液体中结晶出（+）氯吡格雷硫酸氢盐（也称为氯吡格雷硫酸氢盐））的多晶型物“I型” 其混合物; 或选自甲基乙基酮，环戊基甲基醚，二丙基乙二醇醚，二丁基二醇醚，丙基甲基溶纤剂，丁基甲基溶纤剂，丙基乙基溶纤剂，丁基甲基溶纤剂，丙基乙基醚基醚，丁基乙基溶纤剂或它们的交联组合的II型溶剂和/ 作为“形式II”。 本发明还公开了氯吡格雷游离碱的制备和分解剂樟脑磺酸的回收和回收方法的改进。

公开(公告)号：US20080103334A1

公开(公告)日：2008-05-01

申请号：US11923352

申请日：2007-10-24

Applicant: Ashok Kumar ,  Satish Rajanikant Soudagar ,  Avinash Manohar Nijasure ,  Nalinakshya Balaram Panda ,  Prashant Gautam ,  Gajendrasingh Ramsingh Thakur

Inventor： Ashok Kumar ,  Satish Rajanikant Soudagar ,  Avinash Manohar Nijasure ,  Nalinakshya Balaram Panda ,  Prashant Gautam ,  Gajendrasingh Ramsingh Thakur

IPC: C07C61/08

CPC classification number: C07C227/40 ,  C07B2200/13 ,  C07C227/04 ,  C07C227/42 ,  C07C229/28 ,  C07C2601/14

Abstract: A process for preparation of gabapentin comprising a step of obtaining 1,1-cyclohexane diacetic acid monoamide from 1,1-cyclohexane diacetic acid anhydride, wherein said reaction is characterized by the use of ammonia precursor or pre-generated ammonia-isopropanol solution. The invention further discloses preparation of gabapentin and isolation of gabapentin in polymorphic Form II with high yield and purity.

Abstract translation: 一种制备加巴喷丁的方法，包括从1,1-环己烷二乙酸酐获得1,1-环己烷二乙酸单酰胺的步骤，其中所述反应的特征在于使用氨前体或预生成的氨 - 异丙醇溶液。 本发明进一步公开了加巴喷丁的制备，并以高产率和纯度分离多形态II型加巴喷丁。

公开(公告)号：US09492406B2

公开(公告)日：2016-11-15

申请号：US14430007

申请日：2013-09-20

Applicant: IPCA Laboratories Limited

Inventor： Ashok Kumar ,  Dharmendra Singh ,  Pramilkumar Mathur ,  Thankachen Byju Nellithanath ,  Gaurav Sahal ,  Rakesh Kumar Bhasin ,  Durga Prasad Samantaray

IPC: A61K9/08 ,  A61K31/55 ,  A61K31/122 ,  A61K47/10 ,  A61K31/155 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48

CPC classification number: A61K31/155 ,  A61K9/146 ,  A61K9/2027 ,  A61K9/2077 ,  A61K9/4866 ,  A61K31/122 ,  Y02A50/411 ,  A61K2300/00

Abstract: The present invention relates to a novel pharmaceutical composition having enhanced bioavailability through improved aqueous dissolution of poorly water soluble drugs, and to a method for preparing it. The invention more particularly relates to an oral pharmaceutical composition containing active ingredients of poor aqueous solubility, more specifically, antiparasitic and antipneumocystic drug Atovaquone alone or in combination with Proguanil.

Abstract translation: 本发明涉及通过改善水溶性差的药物的水溶性而具有增强的生物利用度的新型药物组合物及其制备方法。 本发明更具体地涉及含有水溶性差的活性成分的口服药物组合物，更具体而言，涉及单独或与Proguanil组合的抗寄生虫和抗肺囊虫药物Atovaquone。

公开(公告)号：US20120136062A1

公开(公告)日：2012-05-31

申请号：US13388729

申请日：2010-08-20

Applicant: Ashok Kumar ,  Dharmendra Singh ,  Pramilkumar Mathur ,  Vitthal Syryabhan Buchude

Inventor： Ashok Kumar ,  Dharmendra Singh ,  Pramilkumar Mathur ,  Vitthal Syryabhan Buchude

IPC: A61K31/155 ,  A61P33/06 ,  A61P33/02 ,  C07C279/18

CPC classification number: C07C279/26 ,  C07C50/32

Abstract: Disclosed are complexes of an antipneumocystic compound and an antimalarial compound, processes for their preparation, pharmaceutical compositions and methods of using said complexes or compositions for the treatment and/or prophylaxis of parasitic infections.

Abstract translation: 公开了抗肺囊虫化合物和抗疟疾化合物的复合物，其制备方法，药物组合物和使用所述复合物或组合物用于治疗和/或预防寄生虫感染的方法。

公开(公告)号：US07615571B2

公开(公告)日：2009-11-10

申请号：US11324349

申请日：2006-01-03

Applicant: Sanjay Tukaram Gunjal ,  Dilip Uttam Jadhav ,  Ashok Kumar ,  Mathur Arpana ,  Nalinakshya Balaram Panda ,  Satish Rajanikant Soudagar

Inventor： Sanjay Tukaram Gunjal ,  Dilip Uttam Jadhav ,  Ashok Kumar ,  Mathur Arpana ,  Nalinakshya Balaram Panda ,  Satish Rajanikant Soudagar

IPC: A61K31/403 ,  C07D209/12

CPC classification number: C07D209/42

Abstract: New compounds useful as synthetic intermediates to synthesize perindopril, a new process for synthesizing perindopril, and new salts of perindopril.

Abstract translation: 用作合成中间体的新化合物可合成培哚普利，一种合成培哚普利的新方法和培哚普利的新盐。

公开(公告)号：US07547791B2

公开(公告)日：2009-06-16

申请号：US11666330

申请日：2004-10-26

Applicant: Ashok Kumar ,  Dharmendra Singh ,  Atul Jadhav ,  Navinchandra Darpan Pandya ,  Shankar Deepak Panmand ,  Ramsingh Gajendrasingh Thakur

Inventor： Ashok Kumar ,  Dharmendra Singh ,  Atul Jadhav ,  Navinchandra Darpan Pandya ,  Shankar Deepak Panmand ,  Ramsingh Gajendrasingh Thakur

IPC: C07D233/00

CPC classification number: C07D403/06

Abstract: A one-pot industrial process for preparing 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazole-1-yl)methyl]-4H-carbazol-4-one of Formula-(I) from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one of Formula-(IV) involves reaction of Formula (IV) with HNR1R2 salt and paraformaldehyde, where R1,R2 are independently alkyl groups or together forms a cyclic alkyl group, in a solvent system of acetic acid and hydrocarbon solvent to form a crude mixture of intermediate compounds of Formula (III) and (VIII), which is converted to ondansetron (Formula (I)) without isolation by reaction with 2methyimidazole in a suitable solvent system in the same pot.

Abstract translation: 制备式为1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮的一锅工业方法 - （Ⅳ）的1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮包括式（Ⅳ）与HNR1R2盐和多聚甲醛的反应，其中R 1，R 2为 独立地烷基或一起形成环烷基，在乙酸和烃溶剂的溶剂体系中形成式（III）和（VIII）的中间体化合物的粗混合物，其被转化成昂丹司琼（式（I）） 而不通过与2-甲基咪唑在同一锅中合适的溶剂体系中反应而分离。

公开(公告)号：US20110230501A1

公开(公告)日：2011-09-22

申请号：US13119648

申请日：2009-09-23

Applicant: Anil Pareek

Inventor： Anil Pareek

IPC: A61K31/4965 ,  A61K31/4706 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00

CPC classification number: A61K31/155 ,  A61K31/427 ,  A61K31/4706 ,  A61K31/64 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed herein is a pharmaceutical composition comprising Hydroxychloroquine or its pharmaceutically acceptable salt and at least one antidiabetic compound, useful in the treatment of diabetes mellitus.

Abstract translation: 本文公开了包含羟氯喹或其药学上可接受的盐和至少一种可用于治疗糖尿病的抗糖尿病化合物的药物组合物。

公开(公告)号：US07629465B2

公开(公告)日：2009-12-08

申请号：US10591657

申请日：2005-03-04

Applicant: Ashok Kumar ,  Ketan Dhansukhlal Vyas ,  Sanjay Govind Barve ,  Priti Jayesh Bhayani ,  Sanjay Nandavadekar ,  Chirag Hasmukh Shah ,  Sandeep Madhavrao Burudkar ,  Lavkesh Dayashankar Kushwaha

Inventor： Ashok Kumar ,  Ketan Dhansukhlal Vyas ,  Sanjay Govind Barve ,  Priti Jayesh Bhayani ,  Sanjay Nandavadekar ,  Chirag Hasmukh Shah ,  Sandeep Madhavrao Burudkar ,  Lavkesh Dayashankar Kushwaha

IPC: C07D471/02

CPC classification number: C07D495/04

Abstract: An improved process for the manufacture of Clopidogrel starting from 2-(2-thienyl) ethylamine, which eliminates the isolation of an unstable intermediate like 2-(2-thienyl) ethyl formimine by subjecting it to a one pot cyclization to get 4, 5, 6, 7-tetrahydrothieno (3,2-c) pyridine of Formula II and further reacting with halo-compound of Formula III (where X is Cl or Br) at 20 to 90° C. temperature characterized in a solvent like water and/or dichloroethane in presence of organic or inorganic bases is disclosed herein. This invention further discloses a process for resolution of racemic Clopidogrel into its optical antipodes and converting the dextroclopidogrel base into its known polymorphs namely ‘Form I’ or ‘Form II’ in solvents selected from methyl propyl ketone, methyl isopropyl ketone, diethyl ketone or their mixture thereof, mixture of ethyl acetate and methyl propyl ketone, mixture of ethyl acetate and methyl isopropyl ketone, or mixture of ethyl acetate and diethyl ketone or ethyl acetate.

Abstract translation: 从2-（2-噻吩基）乙胺开始制备氯吡格雷的改进方法，其通过使其进行一锅环化以得到4,5，消除了不稳定中间体如2-（2-噻吩基）乙基甲酰胺的分离 ，6,7-四氢噻吩并（3,2-c）吡啶，并在20至90℃下进一步与式III的卤代化合物（其中X为Cl或Br）反应，其特征在于溶剂如水和 /或二氯乙烷在有机或无机碱的存在下公开。 本发明还公开了一种将外消旋氯吡格雷分解成其光学对映体并将右旋氯吡格雷碱转化成已知的多晶型物，即在甲基丙基酮，甲基异丙基酮，二乙基酮或它们的溶剂中选择的“I型”或“II型” 其混合物，乙酸乙酯和甲基丙基酮的混合物，乙酸乙酯和甲基异丙基酮的混合物，或乙酸乙酯和二乙基酮或乙酸乙酯的混合物。