Patents by Inventor Madhup K. Dhaon
Madhup K. Dhaon 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: 8129521Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at ?30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated.Type: GrantFiled: February 23, 2010Date of Patent: March 6, 2012Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Y. Chen
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Publication number: 20100204466Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at ?30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated.Type: ApplicationFiled: February 23, 2010Publication date: August 12, 2010Inventors: Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Chen
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Patent number: 7700614Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at ?30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated.Type: GrantFiled: December 14, 2005Date of Patent: April 20, 2010Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Chen
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Publication number: 20080167335Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at ?30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated.Type: ApplicationFiled: December 14, 2005Publication date: July 10, 2008Inventors: Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Y. Chen
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Patent number: 6512114Abstract: The present invention provides a process for the synthesis of Midazolam I from a compound of formula II, using thermodynamic, basic workup conditions. Additional steps to isolate the pure bulk product follow.Type: GrantFiled: June 30, 1999Date of Patent: January 28, 2003Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, Grant L. Esser, Deborah A. Davis, Ashok V. Bhatia
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Publication number: 20010014738Abstract: The present invention relates to a process for the synthesis of a compound having the formula I, 1Type: ApplicationFiled: June 30, 1999Publication date: August 16, 2001Inventors: MADHUP K. DHAON, PARVIZ LABIB, DEBORAH A. DAVIS, GRANT L. ESSER
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Patent number: 6262260Abstract: The present invention provides a process for the synthesis of compounds of formula (II) or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 23, 2000Date of Patent: July 17, 2001Assignee: Abbott LaboratoriesInventor: Madhup K. Dhaon
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Patent number: 6191285Abstract: The present invention provides an improved process for producing ketorolac tromethamine. The preferred method utilizes a three-part solvent system, comprising isopropanol, ethyl acetate and water.Type: GrantFiled: December 7, 1998Date of Patent: February 20, 2001Assignee: Abbott LaboratoriesInventors: Grant L. Esser, Marazban H. Vandrevala, Madhup K. Dhaon, Ameen F. Ghannam, Dragan Obradovich
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Patent number: 5698676Abstract: A process of synthesizing a peptide using an alkylene oxide as an acid scavenger is provided. A process of the present invention can be used in a solid phase or solution phase synthetic process where peptide synthesis occurs by the sequential addition of N-.alpha.-amino-Boc-protected residues followed by acid deprotection of that N-.alpha.-amino protecting group and scavenging of the acid.Type: GrantFiled: November 30, 1995Date of Patent: December 16, 1997Assignee: Abbott LaboratoriesInventor: Madhup K. Dhaon
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Patent number: 5547937Abstract: This invention discloses that certain fragments of a pulmonary surfactant protein exhibit unexpected surface activity. These protein fragments are useful in preparing formulations for the treatment of respiratory distress syndrome.Type: GrantFiled: August 29, 1994Date of Patent: August 20, 1996Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, Edwin O. Lundell, Virender K. Sarin, Constance H. Baxter, Darryl R. Absolom
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Patent number: 5312985Abstract: A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvyl-phenylalanine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.Type: GrantFiled: April 8, 1993Date of Patent: May 17, 1994Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, John A. Houbion
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Patent number: 5283260Abstract: A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvylphenyl al anine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.Type: GrantFiled: April 8, 1993Date of Patent: February 1, 1994Assignee: Abbott LaboratoriesInventors: Robert H. Miller, Nickki L. Parlet, Kent L. Cipollo, Madhup K. Dhaon, John A. Houbion, Edwin O. Lundell
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Patent number: 5256697Abstract: A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvyl-phenylalanine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.Type: GrantFiled: April 16, 1992Date of Patent: October 26, 1993Assignee: Abbott LaboratoriesInventors: Robert H. Miller, Nickki L. Parlet, Kent L. Cipollo, Madhup K. Dhaon, John A. Houbion, Edwin O. Lundell