Patents Assigned to ArQule, Inc.
  • Substituted Benzo-Pyrimido-Tetrazolo-Diazepine Compounds
    Publication number: 20110166127
    Abstract: The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-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: December 29, 2010
    Publication date: July 7, 2011
    Applicant: ArQule, Inc.
    Inventors: Rui-Yang Yang, Jeffrey S. Link
  • Substituted Pyrrolo-Aminopyrimidine Compounds
    Publication number: 20110160203
    Abstract: The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine 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: June 30, 2011
    Applicant: ArQule, Inc.
    Inventors: Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, Jianqiang Wang, Hui Wu
  • Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same
    Publication number: 20110160242
    Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 30, 2011
    Applicant: ArQule, Inc.
    Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
  • Substituted Triazolo-Pyrimidine Compounds
    Publication number: 20110160226
    Abstract: The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-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: June 30, 2011
    Applicant: ArQule, Inc.
    Inventor: Syed M. Ali
  • Substituted Heterocyclic Compounds
    Publication number: 20110160237
    Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic 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: June 30, 2011
    Applicant: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
  • Substituted Triazolo-Pyrazine Compounds
    Publication number: 20110160215
    Abstract: The present invention relates to substituted triazolo-pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrazine 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: June 30, 2011
    Applicant: ArQule, Inc.
    Inventor: Neil Westlund
  • Kinase inhibition models and their uses
    Patent number: 7960158
    Abstract: The present invention provides a c-Met inhibition model. The invention further provides a method to derive inhibition models for other kinases. The kinase inhibition models of the present invention can be used to design or screen for inhibitors for kinases.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: June 14, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Palma Rocio, Sudharshan Eathiraj
  • Kinase inhibition models and their uses
    Patent number: 7960134
    Abstract: The present invention provides a c-Met inhibition model. The invention further provides a method to derive inhibition models for other kinases. The kinase inhibition models of the present invention can be used to design or screen for inhibitors for kinases.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: June 14, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Rocio Palma, Sudharshan Eathiraj
  • Novel Lapachone Compounds And Methods of Use Thereof
    Publication number: 20110105470
    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: Application
    Filed: January 11, 2011
    Publication date: May 5, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, David Vensel, Chiang J. Li
  • Substituted tetrazole compounds and uses thereof
    Patent number: 7932279
    Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole 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 compound of the present invention.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: April 26, 2011
    Assignee: ArQule, Inc.
    Inventors: Rui-Yang Yang, Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Rocio Palma, Neil Westlund
  • Inhibitors of P38 and methods of using the same
    Patent number: 7902192
    Abstract: In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: March 8, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Syed Ali, Jifeng Liu, Yanbin Liu, Peter Lohse, Belew Mekonnen, Robert Selliah, Manish Tandon, Woj Wrona, Valery Antonenko
  • Lapachone compounds and methods of use thereof
    Patent number: 7902354
    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: August 21, 2007
    Date of Patent: March 8, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, David Vensel, Chiang J. Li
  • Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production
    Publication number: 20110034513
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
    Type: Application
    Filed: October 19, 2010
    Publication date: February 10, 2011
    Applicants: Wyeth LLC, ArQule, Inc.
    Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
  • 1,4-Disubstituted Naphthalenes as Inhibitors of P38 Map Kinase
    Publication number: 20100311754
    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: Application
    Filed: August 11, 2010
    Publication date: December 9, 2010
    Applicant: ARQULE, INC.
    Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
  • Heterocyclic sulfonamide inhibitors of beta amyloid production
    Patent number: 7842718
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: November 30, 2010
    Assignees: Wyeth LLC, ArQule, Inc.
    Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph Raymond Stock, George Diamantidis, Dennis Michael Kubrak, Kristina Martha Kutterer, William J. Moore, David S. Casebier
  • COMBINATIONAL COMPOSITIONS AND METHODS FOR TREATMENT OF CANCER
    Publication number: 20100297075
    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: February 11, 2010
    Publication date: November 25, 2010
    Applicants: ArQule, Inc., Kyowa Hakko Kirin Co., Ltd.
    Inventors: Thomas C.K. Chan, Dennis S. France, Kenichi Ishii, Paolo Pucci
  • 1,4-disubstituted naphthalenes as inhibitors of P38 MAP kinase
    Patent number: 7829560
    Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: November 9, 2010
    Assignee: Arqule, Inc.
    Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
  • HDAC Inhibitors
    Publication number: 20100261710
    Abstract: The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid 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 compound of the present invention.
    Type: Application
    Filed: August 21, 2008
    Publication date: October 14, 2010
    Applicant: ARQULE, INC.
    Inventors: Mark A. Ashwell, Manish Tandon, Nivedita D. Namdev, Jean-Marc Lapierre, Yanbin Liu, Hui Wu
  • Pharmaceutical compositions of ?-lapachone and ?-lapachone analogs with improved tumor targeting potential
    Patent number: 7812051
    Abstract: The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified ?-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. Polymer-modification of therapeutic agents, such as ?-lapachone compounds, provides effective transport of polymer-modified therapeutic agents to tumor cells or tumor tissues by exploiting the EPR effect in tumor tissues.
    Type: Grant
    Filed: August 11, 2005
    Date of Patent: October 12, 2010
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chiang J. Li, Manish Tandon, Yanbin Liu, Jean-Marc LaPierre, Zhiwei Jiang
  • SUBSTITUTED PYRAZOLO-PYRIMIDINE COMPOUNDS
    Publication number: 20100249110
    Abstract: The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine 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, 2010
    Publication date: September 30, 2010
    Applicant: ArQule, Inc.
    Inventors: Manish Tandon, Jianqiang Wang, Nivedita Namdev