Patents Assigned to ArQule, Inc.
  • Substituted imidazolyl-5,6-dihydrobenzo[N]isoquinoline compounds
    Patent number: 8263610
    Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: December 30, 2009
    Date of Patent: September 11, 2012
    Assignee: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Chris Brassard, Audra Dalton, Anton Filikov, Jason Hill, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Jianqiang Wang, Neil Westlund
  • Quinazolinone compounds and methods of use thereof
    Patent number: 8232285
    Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. 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 quinazolinone compound of the present invention.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: July 31, 2012
    Assignee: ArQule, Inc.
    Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
  • Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same
    Publication number: 20120165278
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Darin Kizer, Takahiro Murai, Daisuke Nakai, Takanori Yasukochi
  • Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
    Patent number: 8178672
    Abstract: An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: May 15, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre
  • Substituted naphthalenyl-pyrimidine compounds
    Patent number: 8173808
    Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: May 8, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
  • Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds
    Publication number: 20120108574
    Abstract: The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 3, 2012
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
  • Methods for Treatment of Non-Small Cell Lung Cancer
    Publication number: 20120052062
    Abstract: The present invention provides methods of treating non-small cell lung cancer by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound in combination with a therapeutically effective amount of an epidermal growth factor tyrosine kinase inhibitor
    Type: Application
    Filed: August 31, 2011
    Publication date: March 1, 2012
    Applicant: ArQule, Inc.
    Inventors: Yinpu Chen, Edward G. Garmey, Brian Schwartz
  • 1,4-disubstituted naphthalenes as inhibitors of p38 map kinase
    Patent number: 8114873
    Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 14, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Yanbin Liu, Syed M. Ali, Jason Hill, Woj Wrona
  • Phosphorylated NF45 Biomarkers, Antibodies And Methods Of Using Same
    Publication number: 20120021432
    Abstract: The present invention relates to isolated phosphorylated NF45 peptides and isolated phosphorylation site-specific antibody or antigen-binding portion thereof that specifically binds a phosphorylated NF45 protein. The present invention also relates to methods of utilizing these antibodies to determine the therapeutic efficacy of a candidate compound and methods for screening for candidate compounds that increase the phosphorylation of NF45 protein in a cell.
    Type: Application
    Filed: April 15, 2011
    Publication date: January 26, 2012
    Applicant: ArQule, Inc.
    Inventors: Yi Yu, Xiubin Gu, Xiaolan Zhao, Carol Waghorne, Thomas C.K. Chan, Taiping Chen
  • Substituted Tetrahydropyrazolo-Pyrido-Azepine Compounds
    Publication number: 20120015935
    Abstract: The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Applicant: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Rui-Yang Yang, Nivedita Namdev, Jeffrey S. Link
  • Combinational Compositions And Methods For Treatment Of Cancer
    Publication number: 20120004191
    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: Application
    Filed: July 1, 2011
    Publication date: January 5, 2012
    Applicant: ArQule, Inc.
    Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C.K. Chan
  • Inhibitors of P38 and Methods of Using the Same
    Publication number: 20110301160
    Abstract: In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.
    Type: Application
    Filed: December 3, 2010
    Publication date: December 8, 2011
    Applicant: ARQULE, INC.
    Inventors: Mark A. ASHWELL, Syed ALI, Jifeng LIU, Yanbin LIU, Peter LOHSE, Belew MEKONNEN, Robert SELLIAH, Manish TANDON, Woj WRONA, Valery ANTONENKO
  • Method for Determining Treatment Efficacy
    Publication number: 20110301194
    Abstract: The present invention provides a method for determining the efficacy of a c-Met inhibitor in treating a cell proliferative disorder, comprising: a) administering to a subject in need thereof a therapeutically effective amount of the c-Met inhibitor, or a pharmaceutically acceptable salt, prodrug or metabolite thereof, either alone or in combination with a therapeutically effective amount of a second anti-proliferative agent; and b) measuring the concentration of hepatocyte growth factor (HGF) in the serum from the subject, wherein if the concentration of serum HGF does not decrease, or if the concentration of serum HGF increases, the c-Met inhibitor is efficacious in treating the cell proliferative disorder.
    Type: Application
    Filed: June 1, 2011
    Publication date: December 8, 2011
    Applicant: ArQule, Inc.
    Inventors: Thomas C.K. Chan, Carol Waghorne, Giovanni Abbadessa
  • Lapachone compounds and methods of use thereof
    Patent number: 8067459
    Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: November 29, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, Yanbin Liu, Chiang J. Li
  • Substituted tetrahydropyrazolo-pyrido-azepine compounds
    Patent number: 8049005
    Abstract: The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: November 1, 2011
    Assignee: ArQule, Inc.
    Inventors: Jean-Marc Lapierre, Rui-Yang Yang, Nivedita Namdev, Jeffrey S. Link
  • Lapachone compounds and methods of use thereof
    Patent number: 8039503
    Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: October 18, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed M. Ali, David Vensel, Chiang J. Li
  • Substituted Benzo-Pyrido-Triazolo-Diazepine Compounds
    Publication number: 20110245236
    Abstract: The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: March 31, 2011
    Publication date: October 6, 2011
    Applicant: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Steffi Koerner, Jean-Marc Lapierre, Jeffrey S. Link, Yanbin Liu, Magdi Moussa, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
  • Quinazolinone Compounds and Methods of Use Thereof
    Publication number: 20110217300
    Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds.
    Type: Application
    Filed: April 6, 2011
    Publication date: September 8, 2011
    Applicant: ARQULE, INC.
    Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20110172203
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 29, 2010
    Publication date: July 14, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto
  • Substituted Naphthalenyl-Pyrimidine Compounds
    Publication number: 20110166137
    Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 29, 2010
    Publication date: July 7, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel