Patents by Inventor Michael E. Randazzo
Michael E. Randazzo 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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Publication number: 20140243517Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: AstraZeneca ABInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Patent number: 8049019Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein.Type: GrantFiled: October 27, 2009Date of Patent: November 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Boguslaw M. Mudryk, Michael E. Randazzo, Rulin Zhao
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Publication number: 20110201795Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Patent number: 7932379Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: GrantFiled: June 19, 2007Date of Patent: April 26, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Publication number: 20100113489Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin- 4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein.Type: ApplicationFiled: October 27, 2009Publication date: May 6, 2010Inventors: John V. Duncia, Boguslaw M. Mudryk, Michael E. Randazzo, Zili Xiao, Michael G. Yang, Rulin Zhao, Percy H. Carter
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Patent number: 7629351Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8,R9, R10, and are as described herein.Type: GrantFiled: July 25, 2007Date of Patent: December 8, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, John V. Duncia, Boguslaw M. Mudryk, Michael E. Randazzo, Zili Xiao, Michael G. Yang, Rulin Zhao
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Patent number: 7388098Abstract: Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and thType: GrantFiled: September 24, 2001Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: John J. Venit, Gary D. Madding, Victor W. Rosso, Francis J. Okuniewicz, Robert P. Discordia, Susanne Kiau, Atul S. Kotnis, Michael E. Randazzo, D. David Hennings, Jingyang Zhu, Jason G. Chen
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Patent number: 7375213Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: GrantFiled: December 23, 2003Date of Patent: May 20, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Publication number: 20080027084Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4 -ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein.Type: ApplicationFiled: July 25, 2007Publication date: January 31, 2008Inventors: John V. Duncia, Boguslaw M. Mudryk, Michael E. Randazzo, Zili Xiao, Michael G. Yang, Rulin Zhao, Percy H. Carter
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Publication number: 20040138439Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: ApplicationFiled: December 23, 2003Publication date: July 15, 2004Inventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Publication number: 20020111512Abstract: Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and thType: ApplicationFiled: September 24, 2001Publication date: August 15, 2002Inventors: John J. Venit, Gary D. Madding, Victor W. Rosso, Francis J. Okuniewicz, Robert P. Discordia, Susanne Kiau, Atul S. Kotnis, Michael E. Randazzo, D. David Hennings, Jingyang Zhu, Jason G. Chen
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Patent number: 6335324Abstract: Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.Type: GrantFiled: December 13, 1999Date of Patent: January 1, 2002Assignee: Bristol-Myers Squibb Co.Inventors: Gregory S. Bisacchi, William A. Slusarchyk, Uwe Treuner, James C. Sutton, Robert Zahler, Steven Seiler, David R. Kronenthal, Michael E. Randazzo, Mark D. Schwinden, Zhongmin Xu, Zhongping Shi
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Patent number: 5250734Abstract: A compound represented by the following formula (I): ##STR1## wherein R is hydrogen, methyl, ethyl, propyl, butyl, phenyl, CH.sub.2 CH(OH)CH.sub.3, CH.sub.2 CH(OH)CH(OH), CH.sub.2 CH.sub.2 CH.sub.2 -phenyl, or a group of the formula (CH.sub.2).sub.x -Ar, where x is 0 to 4 and Ar is a 6-membered ring from phenyl, pyridyl, cyclohexyl, or pyranyl, each of which may be substituted with a hydrophilic group(s), andX can be Cl, tartrate, oxalate, or quinate.Type: GrantFiled: May 28, 1992Date of Patent: October 5, 1993Assignee: Belmac CorporationInventors: Jean-Francois Rossignol, Michael E. Randazzo