Patents by Inventor Mukund K. Gurjar
Mukund K. Gurjar 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).
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Patent number: 9643914Abstract: A process for preparation of diethyl 2-aetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.Type: GrantFiled: November 14, 2014Date of Patent: May 9, 2017Assignee: EMCURE PHARMACEUTICALS LIMITEDInventors: Mukund K. Gurjar, Narendra K. Tripathy, Kaliaperumal Neelakandan, Prasad P. Panchabhai, Nandala Srinivas, Prabhakaran Balasubramanian, Sandip B. Buchude, Balaji R. Mugale, Pravin P. Ahirrao, Samit S. Mehta
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Publication number: 20160289166Abstract: A process for preparation of diethyl 2-aetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.Type: ApplicationFiled: November 14, 2014Publication date: October 6, 2016Inventors: Mukund K. GURJAR, Narendra K. THIPATHY, Kaliaperumal NEELAKANDAN, Prasad P. PANCHABHAI, Nandala SRINIVAS, Prabhakaran BALASUBRAMANIAN, Sandip B. BUCHUDE, Balaji R. MUGALE, Pravin P. AHIRRAO, Samit S. MEHTA
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Patent number: 8686165Abstract: The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions.Type: GrantFiled: November 2, 2010Date of Patent: April 1, 2014Assignee: Emcure Pharmaceuticals LimitedInventors: Mukund K. Gurjar, Swapnil P. Sonawane, Pankaj S. Patil, Samit S. Mehta
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Publication number: 20110105598Abstract: The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions.Type: ApplicationFiled: November 2, 2010Publication date: May 5, 2011Applicant: Emcure Pharmaceuticals LimitedInventors: Mukund K. GURJAR, Swapnil P. SONAWANE, Pankaj S. PATIL, Samit S. MEHTA
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Publication number: 20110046416Abstract: The present invention provides a simple method for preparation of benzphetamine and its acid addition salt comprising reaction of methamphetamine hydrochloride of formula (III) with benzyl chloride and treating the isolated benzphetamine of formula (II) with an acid dissolved in an organic solvent to provide benzphetamine acid addition salt, more specifically, benzphetamine hydrochloride of formula (I).Type: ApplicationFiled: August 18, 2010Publication date: February 24, 2011Applicant: Emcure Pharmaceuticals LimitedInventors: Mukund K. Gurjar, Narendra K. Tripathy, Kiran A. Bapat, Vemavarapu P.K.V. Rao, Satyjeet B. Biswas, Samit S. Mehta
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Patent number: 7576234Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: December 16, 2005Date of Patent: August 18, 2009Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Patent number: 7294718Abstract: Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.Type: GrantFiled: December 9, 2004Date of Patent: November 13, 2007Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
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Patent number: 7285676Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: March 21, 2005Date of Patent: October 23, 2007Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 7179937Abstract: The invention relates to the use of derivatives of cyclopentenone for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of derivatives of cyclopentenone for the inhibition and/or prevention of cancer of the colon, pancreas, larynx, ovary, duodenum, kidney, oral cavity, prostate, lung, endothelial cells and leukemias.Type: GrantFiled: December 4, 2002Date of Patent: February 20, 2007Assignee: Dabur Research FoundationInventors: Mukund K. Gurjar, Radhika D. Wakharkar, Gautam R. Desiraju, Ashwini Nangia, Jhillu Singh Yadav, Anand C. Burman, Rama Mukherjee, Hanumant Bapu Rao Borate, Srivari Chandrasekhar, Manu Jaggi, Anuo T. Singh, Kamal Kapoor, Sanjay Sarkhel, K. V. V. M. Sairam
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Patent number: 7038073Abstract: A method of preparing a 2-alkyl amino acid involves the aziridination of an alkylacrylate and the opening of the aziridine ring by addition of a side chain. This method can result in the preparation of enantiomeric excess of a 2-alkyl amino acid. The invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: May 15, 2003Date of Patent: May 2, 2006Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 7002036Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: May 15, 2003Date of Patent: February 21, 2006Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Patent number: 6903220Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: May 15, 2003Date of Patent: June 7, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 6875882Abstract: There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.Type: GrantFiled: May 15, 2003Date of Patent: April 5, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
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Patent number: 6875883Abstract: There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzaldehyde or 2,4-dimethoxybenzaldehyde. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.Type: GrantFiled: May 15, 2003Date of Patent: April 5, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
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Patent number: 6861532Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkylcysteine involves condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, followed by alkylating the 2-arylthiazoline-4-carboxylic acid at the 4-position. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine.Type: GrantFiled: May 15, 2003Date of Patent: March 1, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda, Joseph Cherian
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Patent number: 6846932Abstract: A process for the preparation of pharmaceutically acceptable salts of chiral Amlodipine namely S(?) Amlodipine and R(+) Amlodipine from without isolation of a free base from with optical purity rank between 96-99% is described in the present invention. The process comprises resolving RS amlodipine base using of L(+) or D(?) tartaric acid to obtain salt of corresponding to the acid used in ee rang from 96-99%.Type: GrantFiled: November 20, 2003Date of Patent: January 25, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Rohini R. Joshi, Ramesh A. Joshi, Nilesh B. Karade, Mukund K. Gurjar
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Patent number: 6846958Abstract: Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.Type: GrantFiled: May 15, 2003Date of Patent: January 25, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
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Patent number: 6818786Abstract: The present invention relates to a process for the preparation of ethyl 3-ethoxy-4-ethoxycarbonyl-phenylacetate having formula 1 Ethyl 3-ethoxy-4-ethoxycarbonyl-phenylacetate (1) is an important key intermediate for the synthesis of repaglinide (2) an oral hypoglycemic agentType: GrantFiled: March 31, 2003Date of Patent: November 16, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Uttam R. Kalkote, Mukund K. Gurjar, Shreerang V. Joshi, Suresh M. Kadam, Sanjay J. Naik
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Publication number: 20040192955Abstract: The present invention relates to a process for the preparation of ethyl 3-ethoxy-4-ethoxycarbonyl-phenylacetate having formula 1.Type: ApplicationFiled: March 31, 2003Publication date: September 30, 2004Inventors: Uttam R. Kalkote, Mukund K. Gurjar, Shreerang V. Joshi, Suresh M. Kadam, Sanjay J. Naik
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Publication number: 20040024224Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: February 5, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra