Patents by Inventor Milind Gharpure

Milind Gharpure has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 11447443
    Abstract: The present invention provides an improved process for preparation of L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) (Droxidopa) and its salts; comprising (a) reaction of the aldehyde compound (III) (as described herein) with Metal complex (II) (as described herein), and (h) hydrolysis of the compound (IV) obtained from step (a) in presence of acid. The present invention also relates to a novel intermediates metal chiral complex (IV) for the preparation of Droxidopa.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: September 20, 2022
    Assignee: PIRAMAL PHARMA LIMITED
    Inventors: Milind Gharpure, Ashutosh Jagtap, Changdev Raut, Nainesh Kansagara, Jaisankar Krishnapillai, Nirmal Kumar Manoharan, Navnath Patil
  • Patent number: 11312740
    Abstract: The present invention relates to an industrially feasible and economically viable process for preparation of SGLT2 inhibitors of formula X in significantly high yield and purity.
    Type: Grant
    Filed: May 9, 2018
    Date of Patent: April 26, 2022
    Assignee: PIRAMAL PHARMA LIMITED
    Inventors: Milind Gharpure, Sanjay Kumar Sharma, Sandesh Vishwasrao, Prasad Vichare, Dipak Varal
  • Patent number: 11198703
    Abstract: The present invention relates to an industrially feasible and economically viable process for preparation of Bexagliflozin of formula V in significantly high yield and purity.
    Type: Grant
    Filed: May 9, 2018
    Date of Patent: December 14, 2021
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Milind Gharpure, Sanjay Kumar Sharma, Sandesh Vishwasrao, Prasad Vichare, Dipak Varal
  • Patent number: 11192848
    Abstract: The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3 4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.
    Type: Grant
    Filed: January 3, 2019
    Date of Patent: December 7, 2021
    Assignee: PIRAMAL PHARMA LIMITED
    Inventors: Milind Gharpure, Ashutosh Jagtap, Changdev Raut, Navnath Patil, Prashant Ladkat, Jaisankar Krishnapillai, Nirmal Kumar Manoharan, Kumaravel Kandasamy
  • Patent number: 10428033
    Abstract: The present invention provides an improved process for preparation of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine; commonly known as vortioxetine (referred to as the compound (I)) and pharmaceutically acceptable salts thereof; wherein the process comprises reaction of 2-((2,4-dimethylphenyl)thio)aniline (II) with bis(2-alkyl)amine (IIIa) or its salt in the presence of a cyclic amide solvent.
    Type: Grant
    Filed: February 14, 2018
    Date of Patent: October 1, 2019
    Assignee: Piramal Enterprises Limited
    Inventors: Milind Gharpure, Sanjay Kumar Sharma, Nainesh Kansagara
  • Patent number: 10428097
    Abstract: The present invention relates to a novel process for the preparation of intermediate of fosaprepitant dimeglumine. The present invention particularly relates to a process for the preparation of fosaprepitant dibenzyl ester, an intermediate of fosaprepitant dimeglumine, which is simple, easy to handle on commercial scale and efficient.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: October 1, 2019
    Assignee: Piramal Enterprises Limited
    Inventors: Milind Gharpure, Prashant Ladkat, Navnath Shinde, Ashutosh Jagtap
  • Patent number: 10196400
    Abstract: The present invention provides an improved process for preparation of the substantially pure (3aR,7aR)-4?-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1?-piperazin]-1?-ium methanesulfonate (referred to as compound-II), which is useful as a key intermediate for the synthesis of lurasidone ((3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione). The process comprises reaction of the compound-III (as described herein) with the compound-IV (as described herein) in the presence of a solvent mixture selected from an alcohol and water; and a base The improved process for the preparation of compound II provides the product with total amount of unreacted compound-IV as impurity in less than 0.06% and the product with HPLC purity as ?99.8%. The process further refers purification of Lurasidone hydrochloride, wherein the product contains the residual acetone <5000 ppm.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: February 5, 2019
    Assignee: Piramal Enterprises Limited
    Inventors: Milind Gharpure, Shashi Kant Tiwari, Ganesh Wagh, Galge Revanappa, Manikrao Warpe, Yogesh Zalte, Dhileepkumar Krishnmurthy
  • Patent number: 10150745
    Abstract: The present invention provides an improved process for the preparation of 8-chloro-1-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoate (IIIa) and 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoic acid (V).
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: December 11, 2018
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Ashutosh Jagtap, Milind Gharpure, Navnath Shinde, Navnath Patil, Chirag Shah, Changdev Raut, Dhileepkumar Krishnmurthy
  • Patent number: 10144703
    Abstract: A process for the preparation of 5-(3,4-dimethoxyphenylethyl) methyl-amino-2-(3,4-dimethoxyphenyl)-2-isopropyl valeronitrile, which is known as Verapamil is described. A process for improving the purity of verapamil and therefore of its hydrochloride represented as the compound of formula I, by efficient removal of the impurities formed, affording a product of purity greater than 99% is described.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: December 4, 2018
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Dhileep Kumar Krishnamurthy, Milind Gharpure, Narender Rao Somisetti, Murali Rajappa, Rajshekar Aareddy, Damodhar Kasireddy
  • Publication number: 20180230116
    Abstract: The present invention provides an improved process for preparation of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine; commonly known as vortioxetine (referred to as the compound (I)) and pharmaceutically acceptable salts thereof; wherein the process comprises reaction of 2-((2,4-dimethylphenyl)thio)aniline (II) with bis(2-alkyl)amine (IIIa) or its salt in the presence of a cyclic amide solvent.
    Type: Application
    Filed: February 14, 2018
    Publication date: August 16, 2018
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Milind Gharpure, Sanjay Kumar Sharma, Nainesh Kansagara
  • Patent number: 9056813
    Abstract: The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA.
    Type: Grant
    Filed: January 17, 2013
    Date of Patent: June 16, 2015
    Assignee: Glenmark Generics Limited
    Inventors: Milind Gharpure, Krishna Narawade, Prem Chand, Shekhar Bhaskar Bhirud
  • Publication number: 20150018578
    Abstract: The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA
    Type: Application
    Filed: January 17, 2013
    Publication date: January 15, 2015
    Applicant: Glenmark Generics Limited
    Inventors: Milind Gharpure, Krishna Narawade, Prem Chand, Shekhar Bhirud
  • Publication number: 20060293296
    Abstract: A process for the preparation of cefpodoxime proxetil of high purity conforming to pharmacopoeial specifications.
    Type: Application
    Filed: December 20, 2002
    Publication date: December 28, 2006
    Inventors: Milind Gharpure, Sanjay Deshmukh, Asok Saha, Rajendra Mahale
  • Publication number: 20060149055
    Abstract: A process for obtaining cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises addition of a solution of methanesulfonic acid in water to a solution of impure cefpodoxime proxetil of formula (I) in an organic solvent to form the corresponding cefpodoxime proxetil methanesulfonate of formula (II1), followed by addition of a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II1) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II1) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.
    Type: Application
    Filed: January 6, 2003
    Publication date: July 6, 2006
    Inventors: Milind Gharpure, Sanjay Deshmukh, Rajendra Mahale