Patents by Inventor Harold Mastalerz

Harold Mastalerz 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).

  • Isofuranone compounds useful as HPK1 inhibitors
    Patent number: 11166959
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CH or N; Y is CR5 or N; and R1, R2, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds to modulate or inhibit the enzymatic activity of hematopoietic progenitor kinase 1 (HPK1), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: November 9, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Erika M. V. Araujo, Yan Chen, Bireshwar Dasgupta, Andrew P. Degnan, Matthew D. Hill, Godwin Kwame Kumi, Harold A. Mastalerz, Mark D. Wittman, Bradley C. Pearce, Guifen Zhang
  • ISOFURANONE COMPOUNDS USEFUL AS HPK1 INHIBITORS
    Publication number: 20200390776
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CH or N; Y is CR5 or N; and R1, R2, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds to modulate or inhibit the enzymatic activity of hematopoietic progenitor kinase 1 (HPK1), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
    Type: Application
    Filed: November 5, 2018
    Publication date: December 17, 2020
    Inventors: Erika M.V. Araujo, Yan Chen, Bireshwar Dasgupta, Andrew P. Degnan, Matthew D. Hill, Godwin Kwame Kumi, Harold A. Mastalerz, Mark D. Wittman, Bradley C. Pearce, Guifen Zhang
  • Substituted dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-ones as RIPK3 inhibitors
    Patent number: 10301306
    Abstract: Compounds having Formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK3 modulation. All the variables defined herein.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: May 28, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Amy C. Hart, William J. Pitts, Harold Mastalerz, Junqing Guo, Gregory D. Brown
  • SUBSTITUTED DIHYDRO-1H-PYRROLO[3,2-C]PYRIDIN-4(5H)-ONES AS RIPK3 INHIBITORS
    Publication number: 20170362219
    Abstract: Compounds having Formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK3 modulation. All the variables defined herein.
    Type: Application
    Filed: December 14, 2015
    Publication date: December 21, 2017
    Inventors: Amy C. HART, William J. PITTS, Harold MASTALERZ, Junqing GUO, Gregory D. BROWN
  • Imidazotriazinecarbonitriles useful as kinase inhibitors
    Patent number: 9556178
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: January 31, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • IMIDAZOTRIAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20160108050
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: December 21, 2015
    Publication date: April 21, 2016
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer lnghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann, Yong Zhang, Libing Chen, Bin Chen, John S. Tokarski, Ashvinikumar V. Gavai
  • Imidazotriazinecarbonitriles useful as kinase inhibitors
    Patent number: 9273057
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 1, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann, Yong Zhang, Libing Chen, Bin Chen, John S. Tokarski, Ashvinikumar V. Gavai
  • IMIDAZOTRIAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20150210697
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: July 30, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann, Yong Zhang, Libing Chen, Bin Chen, John S. Tokarski, Ashvinikumar V. Gavai
  • IMIDAZOTRIAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Imidazotriazinecarbonitriles useful as kinase inhibitors
    Patent number: 8940736
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Carbazole and carboline kinase inhibitors
    Patent number: 8815840
    Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: August 26, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
  • IMIDAZOTRIAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20140018319
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8592579
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: November 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20120302747
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: August 7, 2012
    Publication date: November 29, 2012
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • CARBAZOLE AND CARBOLINE KINASE INHIBITORS
    Publication number: 20120058988
    Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Application
    Filed: December 17, 2009
    Publication date: March 8, 2012
    Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20110124623
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: January 28, 2011
    Publication date: May 26, 2011
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20110039838
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Application
    Filed: October 25, 2010
    Publication date: February 17, 2011
    Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7879855
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: February 1, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Pyrrolotriazine compounds as kinase inhibitors
    Patent number: 7846931
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: September 24, 2008
    Date of Patent: December 7, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
  • PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH
    Publication number: 20100137319
    Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
    Type: Application
    Filed: February 5, 2010
    Publication date: June 3, 2010
    Inventors: Harold Mastalerz, Dolatral M. Vyas, George L. Trainor, Ashvinikumar V. Gavai