Patents by Inventor Eric P. Gillis

Eric P. Gillis 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: 10752577
    Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
    Type: Grant
    Filed: January 23, 2019
    Date of Patent: August 25, 2020
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Junqi Li, Eric P. Gillis
  • Publication number: 20200055839
    Abstract: Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
    Type: Application
    Filed: January 2, 2018
    Publication date: February 20, 2020
    Inventors: Makonen BELEMA, Michael S. BOWSHER, Jeffrey A. DESKUS, Kyle J. EASTMAN, Eric P. GILLIS, David B. FRENNESSON, Christiana IWUAGWU, John F. KADOW, B. Narasimhulu NAIDU, Kyle E. PARCELLA, Kevin M. PEESE, Mark G. SAULNIER, Prasanna SIVAPRAKASAM
  • Patent number: 10538555
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: January 21, 2020
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Michael Matthew Miller, Claudio Mapelli, Martin Patrick Allen, Michael S. Bowsher, Eric P. Gillis, David R. Langley, Eric Mull, Maude A. Poirier, Nishith Sanghvi, Li-Qiang Sun, Daniel J. Tenney, Kap-Sun Yeung, Juliang Zhu, Kevin W. Gillman, Qian Zhao, Katharine A. Grant-Young, Paul Michael Scola, Lyndon A. M. Cornelius
  • Publication number: 20200016136
    Abstract: Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
    Type: Application
    Filed: January 2, 2018
    Publication date: January 16, 2020
    Inventors: Michael S. BOWSHER, Jeffrey DESKUS, Kyle J. EASTMAN, Eric P. GILLIS, David B. FRENNESSON, Christiana IWUAGWU, B. Narasimhulu NAIDU, Kyle E. PARCELLA, Kevin M. PEESE, Mark G. SAULNIER, Prasanna SIVAPRAKASAM
  • Patent number: 10450347
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: October 22, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael Matthew Miller, Martin Patrick Allen, Ling Li, Claudio Mapelli, Maude A. Poirier, Li-Qiang Sun, Qian Zhao, Eric Mull, Eric P. Gillis, Paul Michael Scola
  • Publication number: 20190315676
    Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
    Type: Application
    Filed: January 23, 2019
    Publication date: October 17, 2019
    Inventors: Martin D. Burke, Junqi Li, Eric P. Gillis
  • Patent number: 10358463
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: July 23, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael Matthew Miller, Martin Patrick Allen, Ling Li, Michael S. Bowsher, Eric P. Gillis, Eric Mull, Qian Zhao, Li-Qiang Sun, David R. Langley, Paul Michael Scola
  • Patent number: 10239824
    Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: March 26, 2019
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Junqi Li, Eric P. Gillis
  • Patent number: 10143746
    Abstract: The present disclosure provides novel macrocyclic compounds which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: December 4, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin Patrick Allen, Eric P. Gillis, David R. Langley, Michael Matthew Miller, Eric Mull, Li-Qiang Sun, Kap-Sun Yeung, Katharine A. Grant-Young, Nicholas A. Meanwell, Paul Michael Scola
  • Patent number: 9944678
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: April 17, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Li-Qiang Sun, Qian Zhao, Eric P. Gillis, Michael Matthew Miller, Martin Patrick Allen, Eric Mull, Paul Michael Scola
  • Patent number: 9908900
    Abstract: Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of building blocks, such as building blocks containing complex and/or pharmaceutically important structures, and/or provide simple or complex protected organoboronic acid building blocks. A first method includes reacting an imino-di-carboxylic acid and an organoboronate salt. A second method includes reacting a N-substituted morpholine dione and an organoboronic acid.
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: March 6, 2018
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Graham R. Dick, David M. Knapp, Eric P. Gillis, Jenna A. Klubnick
  • Patent number: 9879046
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: January 30, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael Matthew Miller, Martin Patrick Allen, Michael S. Bowsher, Kenneth M. Boy, Eric P. Gillis, David R. Langley, Eric Mull, Li-Qiang Sun, Kap-Sun Yeung, Patrick C. Reid, Paul Michael Scola
  • Patent number: 9862733
    Abstract: Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: January 9, 2018
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Eric P. Gillis, Steven G. Ballmer
  • Publication number: 20170369530
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: August 9, 2017
    Publication date: December 28, 2017
    Inventors: Michael Matthew Miller, Claudio Mapelli, Martin Patrick Allen, Michael S. Bowsher, Kenneth M. Boy, Eric P. Gillis, David R. Langley, Eric Mull, Maude A. Poirier, Nishith Sanghvi, Li-Qiang Sun, Daniel J. Tenney, Kap-Sun Yeung, Juliang Zhu, Patrick C. Reid, Paul Michael Scola
  • Patent number: 9850283
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: December 26, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael Matthew Miller, Claudio Mapelli, Martin Patrick Allen, Michael S. Bowsher, Kenneth M. Boy, Eric P. Gillis, David R. Langley, Eric Mull, Maude A. Poirier, Nishith Sanghvi, Li-Qiang Sun, Daniel J. Tenney, Kap-Sun Yeung, Juliang Zhu, Patrick C. Reid, Paul Michael Scola
  • Patent number: 9845317
    Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: December 19, 2017
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
  • Publication number: 20170283463
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: March 31, 2017
    Publication date: October 5, 2017
    Inventors: Michael Matthew Miller, Martin Patrick Allen, Ling Li, Michael S. Bowsher, Eric P. Gillis, Eric Mull, Qian Zhao, Li-Qiang Sun, David R. Langley, Paul Michael Scola
  • Publication number: 20170283462
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: March 21, 2017
    Publication date: October 5, 2017
    Inventors: Michael Matthew Miller, Martin Patrick Allen, Ling Li, Claudio Mapelli, Maude A. Poirier, Li-Qiang Sun, Qian Zhao, Eric Mull, Eric P. Gillis, Paul Michael Scola
  • Publication number: 20170260237
    Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: September 11, 2014
    Publication date: September 14, 2017
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Michael Matthew Miller, Claudio Mapelli, Martin Patrick Allen, Michael S. Bowsher, Eric P. Gillis, David R. Langley, Eric Mull, Maude A. Poirier, Nishith Sanghvi, Li-Qiang Sun, Daniel J. Tenney, Kap-Sun Yeung, Juliang Zhu, Kevin W. Gillman, Qian Zhao, Katharine A. Grant-Young, Paul Michael Scola, Lyndon A.M. Cornelius
  • Publication number: 20170252432
    Abstract: The present disclosure provides novel macrocyclic compounds which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: March 1, 2017
    Publication date: September 7, 2017
    Inventors: Martin Patrick Allen, Eric P. Gillis, David R. Langley, Michael Matthew Miller, Eric Mull, Li-Qiang Sun, Kap-Sun Yeung, Katharine A. Grant-Young, Nicholas A. Meanwell, Paul Michael