Patents Assigned to ArQule, Inc.
  • Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine
    Patent number: 11279679
    Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:
    Type: Grant
    Filed: October 3, 2019
    Date of Patent: March 22, 2022
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jianmin Mao, David P. Reed
  • Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
    Patent number: 11020400
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Grant
    Filed: November 4, 2019
    Date of Patent: June 1, 2021
    Assignee: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Sudharshan Eathiraj, Nivedita Namdev, Brian Schwartz, Yusuke Ota, Takayuki Momose, Tomoyuki Tsunemi, Hiroaki Inagaki, Kiyoshi Nakayama
  • Amino-pyrrolopyrimidinone compounds and methods of use thereof
    Patent number: 11020398
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of BTK, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: June 1, 2021
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Sudharshan Eathiraj, Hiroaki Inagaki, Jean-Marc Lapierre, Takayuki Momose, Kiyoshi Nakayama, Takashi Odagiri, Masahiro Ota, Yusuke Ota, Yoshihiro Shibata, Manish Tandon, Tomoyuki Tsunemi
  • TETRAHYDROPYRANYL AMINO-PYRROLOPYRIMIDINONE AND METHODS OF USE THEREOF
    Publication number: 20210145837
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Application
    Filed: January 27, 2021
    Publication date: May 20, 2021
    Applicant: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Sudharshan Eathiraj, Nivedita Namdev, Brian Schwartz, Yusuke Ota, Takayuki Momose, Tomoyuki Tsunemi, Hiroaki Inagaki, Kiyoshi Nakayama
  • Solid forms of tetrahydropyranyl amino-pyrrolopyrimidinone compounds
    Patent number: 10975087
    Abstract: The present application provides solid forms of (2-chloro-4-phenoxyphenyl)(4-(((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)methanone free base, and methods of preparing and using the same.
    Type: Grant
    Filed: August 13, 2019
    Date of Patent: April 13, 2021
    Assignee: ArQule Inc.
    Inventors: Craig Bates, Erika Volckova
  • Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
    Patent number: 10933065
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: March 2, 2021
    Assignee: ArQule Inc.
    Inventors: Jean-Marc Lapierre, Sudharshan Eathiraj, Nivedita Namdev, Brian Schwartz, Yusuke Ota, Takayuki Momose, Tomoyuki Tsunemi, Hiroaki Inagaki, Kiyoshi Nakayama
  • Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine
    Patent number: 10766868
    Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: September 8, 2020
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jianmin Mao, David P. Reed
  • Solid forms of substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds
    Patent number: 10717710
    Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: July 21, 2020
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, David P. Reed
  • Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
    Patent number: 10245263
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: April 2, 2019
    Assignee: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Sudharshan Eathiraj, Nivedita Namdev, Brian Schwartz, Yusuke Ota, Takayuki Momose, Tomoyuki Tsunemi, Hiroaki Inagaki, Kiyoshi Nakayama
  • Solid forms of substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds
    Patent number: 10227311
    Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: March 12, 2019
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, David P. Reed
  • Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine
    Patent number: 10093632
    Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: October 9, 2018
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jianmin Mao, David P. Reed
  • Solid forms of substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds
    Patent number: 9981921
    Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: May 29, 2018
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, David P. Reed
  • Compositions and methods for treating proliferation disorders
    Patent number: 9949981
    Abstract: The present invention relates to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-(3-morpholinophenyl)-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide. The methods of the present invention can also relate to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing the above compounds in combination with ((R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine).
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: April 24, 2018
    Assignee: ArQule, Inc.
    Inventors: Daniel T. Dransfield, Sudharshan Eathiraj, Jean-Marc Lapierre, Brian Schwartz, Yi Yu
  • Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine
    Patent number: 9834519
    Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: December 5, 2017
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jianmin Mao, David P. Reed
  • Process of preparing 3-(3-(4-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-YL)pyridin-2-amine
    Patent number: 9834556
    Abstract: The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: December 5, 2017
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jian-Xie Chen, Jianmin Mao, David P. Reed
  • Combinational compositions and methods for treatment of cancer
    Patent number: 9642847
    Abstract: The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: May 9, 2017
    Assignee: ArQule, Inc.
    Inventors: Thomas C. K. Chan, Dennis S. France, Kenichi Ishii, Paolo Pucci
  • Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
    Patent number: 9630968
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: April 25, 2017
    Assignee: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Sudharshan Eathiraj, Nivedita Namdev, Brian Schwartz, Yusuke Ota, Takayuki Momose, Tomoyuki Tsunemi, Hiroaki Inagaki, Kiyoshi Nakayama
  • Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same
    Patent number: 9499540
    Abstract: The present invention relates to a (±)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione dichloromethane.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: November 22, 2016
    Assignee: ArQule, Inc.
    Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
  • Process of preparing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-yl)pyridin-2-amine
    Patent number: 9464083
    Abstract: The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: October 11, 2016
    Assignee: ArQule Inc.
    Inventors: Craig Bates, Jian-Xie Chen, Jianmin Mao, David P. Reed
  • Compositions and methods for treatment of cancer
    Patent number: 9447088
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: September 20, 2016
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi