Patents Assigned to Gilead Connecticut, Inc.
  • Pyridone and aza-pyridone compounds and methods of use
    Patent number: 10344040
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: July 9, 2019
    Assignees: GILEAD CONNECTICUT, INC., GENENTECH INC.
    Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
  • Polymorph of Syk inhibitors
    Patent number: 10266539
    Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.
    Type: Grant
    Filed: October 19, 2017
    Date of Patent: April 23, 2019
    Assignee: Gilead Connecticut, Inc.
    Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
  • Imidazopyridines Syk inhibitors
    Patent number: 10092583
    Abstract: Certain imidazopyridines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: October 9, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
  • Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
    Patent number: 10093684
    Abstract: Certain imidazopyrazines of Formula I and pharmaceutical compositions thereof are provided herein: Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: October 9, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Douglas G. Stafford, Jianjun Xu
  • Pyridone and aza-pyridone compounds and methods of use
    Patent number: 10053469
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: August 21, 2018
    Assignees: GILEAD CONNECTICUT, INC., GENENTECH INC.
    Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
  • PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
    Publication number: 20180179229
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 26, 2018
    Publication date: June 28, 2018
    Applicants: GILEAD CONNECTICUT, INC., GENENTECH INC.
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • Formulation of syk inhibitors
    Patent number: 9949932
    Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: April 24, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
  • Formulation of Syk inhibitors
    Patent number: 9918939
    Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: March 20, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
  • 6-(benzo[d]thiazol-5-yl)-n-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
    Patent number: 9796718
    Abstract: Provided are imidazopyrazine compounds, particularly including 6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions:
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: October 24, 2017
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford, James P. Harding, Antonio J. M. Barbosa, Jr., Zhongdong Zhao, David M. Armistead, Soumya Mitra
  • Polymorph of Syk inhibitors
    Patent number: 9657023
    Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: May 23, 2017
    Assignee: Gilead Connecticut, Inc.
    Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
  • PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
    Publication number: 20170073356
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in intro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 30, 2016
    Publication date: March 16, 2017
    Applicants: GILEAD CONNECTICUT, INC., GENENTCH INC.
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • Substituted pyrazolo[1,5-a]pyrimidines as Syk inhibitors
    Patent number: 9567348
    Abstract: Certain pyrazolo[1,5-a]pyrimidines: or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: February 14, 2017
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Imidazopyridines Syk inhibitors
    Patent number: 9562056
    Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: February 7, 2017
    Assignee: GILEAD CONNECTICUT, INC.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
  • Pyridone and aza-pyridone compounds and methods of use
    Patent number: 9505785
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: November 29, 2016
    Assignees: Gilead Connecticut, Inc., Genentech, Inc.
    Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
  • Formulation of Syk inhibitors
    Patent number: 9382256
    Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: July 5, 2016
    Assignee: Gilead Connecticut, Inc.
    Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
  • Pyridinones/pyrazinones, method of making, and method of use thereof
    Patent number: 9249123
    Abstract: Pyridone and pyrazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: February 2, 2016
    Assignees: Genentech, Inc., Gilead Connecticut, Inc.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
  • 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a] pyrazin-8-amine as a spleen tyrosine kinase inhibitor
    Patent number: 9212191
    Abstract: Provided are imidazopyrazine compounds, particularly including 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazine-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions:
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: December 15, 2015
    Assignee: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. Mitchell, Kevin S. Currie
  • 6-(1-indazol-6-YL)--(4-morpholinophenyl)imidazo[1,4-A]pyrazin-8-amine for treating leukemia or lymphoma
    Patent number: 9120811
    Abstract: Provided are imidazopyrazine compounds, including 6-(1H-indazol-6-yl)-N-(4 -moirpholinophenyl)imidazo-[1,2-a]pyrazine-8-amine: and methods for using the imidazopyrazine compounds for treating diseases and disorders responsive to the inhibition of Syk activity, including leukemia and lymphoma.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: September 1, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie
  • Pyridazinones, method of making, and method of use thereof
    Patent number: 8975260
    Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: March 10, 2015
    Assignees: Genetech, Inc, Gilead Connecticut, Inc.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
  • Imidazopyrazine Syk inhibitors
    Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford