Patents Assigned to Apicore, LLC
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Publication number: 20140343282Abstract: Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: May 16, 2014Publication date: November 20, 2014Applicant: Apicore, LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Sanjay F. Thakor, Rajesh A Patel
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Publication number: 20140235870Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.Type: ApplicationFiled: April 29, 2014Publication date: August 21, 2014Applicant: Apicore, LLCInventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Muralikrishna Madala, Sanjay Thakor
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Patent number: 8748631Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.Type: GrantFiled: May 24, 2012Date of Patent: June 10, 2014Assignee: Apicore, LLCInventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Murali Krishna Madala, Sanjay F. Thakor
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Publication number: 20130310600Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: ApplicationFiled: July 25, 2013Publication date: November 21, 2013Applicant: APICORE, LLCInventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
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Publication number: 20130237707Abstract: Pharmaceutical-grade compounds containing cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine having a purity >99.0% by HPLC with less than 0.5% of trans-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine are provided.Type: ApplicationFiled: April 30, 2013Publication date: September 12, 2013Applicant: Apicore, LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Talluri Buhshaiah Chowdari, Chirag Vasantlal Shah
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Patent number: 8450487Abstract: Methods are provided for making pharmaceutical-grade cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and pharmaceutically acceptable salts thereof by isomerizing racemic 2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine to cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and subsequent purification of the C-MSOQ by salt formation with inexpensive and commercially available material such as sulfuric acid. Purification methods are disclosed which employ an organic solvent/water system and recrystallization with an organic solvent such as acetone.Type: GrantFiled: June 8, 2010Date of Patent: May 28, 2013Assignee: Apicore, LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Talluri Buhshaiah Chowdari, Chirag Vasantlal Shah
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Publication number: 20130023671Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.Type: ApplicationFiled: May 24, 2012Publication date: January 24, 2013Applicant: APICORE, LLCInventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Murali Krishna Madala, Sanjay F. Thakor
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Publication number: 20120078007Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: ApplicationFiled: December 2, 2011Publication date: March 29, 2012Applicant: APICORE, LLCInventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
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Publication number: 20110301352Abstract: Methods are provided for making pharmaceutical-grade cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and pharmaceutically acceptable salts thereof by isomerizing racemic 2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine to cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and subsequent purification of the C-MSOQ by salt formation with inexpensive and commercially available material such as sulfuric acid. Purification methods are disclosed which employ an organic solvent/water system and recrystallization with an organic solvent such as acetone.Type: ApplicationFiled: June 8, 2010Publication date: December 8, 2011Applicant: APICORE, LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Talluri Buhshaiah Chowdari, Chirag Vasantlal Shah
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Publication number: 20100094044Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: ApplicationFiled: December 21, 2009Publication date: April 15, 2010Applicant: APICORE, LLCInventors: RAVISHANKER KOVI, SATYAM NAMPALLI, PETER XAVIER THARIAL
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Patent number: 7662992Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: GrantFiled: July 25, 2008Date of Patent: February 16, 2010Assignee: Apicore, LLCInventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
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Publication number: 20080293963Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: ApplicationFiled: July 25, 2008Publication date: November 27, 2008Applicant: Apicore, LLCInventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
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Publication number: 20080281127Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.Type: ApplicationFiled: May 11, 2007Publication date: November 13, 2008Applicant: Apicore, LLCInventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
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Patent number: 7446227Abstract: A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.Type: GrantFiled: December 11, 2006Date of Patent: November 4, 2008Assignee: Apicore, LLCInventors: Satyam Nampalli, Brijesh Patel, Peter Xavier Tharial, Ravishanker Kovi
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Publication number: 20080242892Abstract: A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.Type: ApplicationFiled: June 13, 2008Publication date: October 2, 2008Applicant: APICORE, LLCInventors: Satyam Nampalli, Brijesh Patel, Peter Xavier Tharial, Ravishanker Kovi
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Publication number: 20080139848Abstract: A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.Type: ApplicationFiled: December 11, 2006Publication date: June 12, 2008Applicant: Apicore, LLCInventors: Satyam S. Nampalli, Brijesh Patel, Peter Xavier Tharial, Ravishanker Kovi