Abstract: The present invention relates to the use of CBP/EP300 inhibitors and BET inhibitors for the treatment of cancer. In some embodiments, the use is to treat cancer that is resistant to BET inhibitors.
Type:
Application
Filed:
March 20, 2017
Publication date:
July 13, 2017
Applicants:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Richard C. Centore, Andrew R. Conery, Karen Gascoigne, Robert J. Sims, III
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
June 6, 2013
Date of Patent:
April 18, 2017
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Victor S. Gehling, Alexander M. Taylor, Rishi G. Vaswani
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
June 24, 2014
Date of Patent:
December 20, 2016
Assignee:
CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, James Edmund Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael Charles Hewitt, Yves Leblanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
September 4, 2014
Date of Patent:
November 29, 2016
Assignees:
Genentech, Inc., Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange, Yves LeBlanc, Jun Liang, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Birong Zhang
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Application
Filed:
May 16, 2016
Publication date:
November 17, 2016
Applicant:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Andrew Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
June 6, 2013
Date of Patent:
November 15, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Michael Charles Hewitt, Victor S. Gehling, Rishi G. Vaswani
Abstract: The present invention relates to use of CBP/EP300 bromodomain inhibitors for the treatment of cancer.
Type:
Application
Filed:
April 11, 2016
Publication date:
November 3, 2016
Applicants:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, James Edmund Audia, Steven Bellon, Andrea Cochran, Alexandre Cote, Terry Crawford, Benjamin Fauber, Srimoyee Ghosh, Jean-Christophe Harmange, Georgia Hatzivassiliou, Hariharan Jayaram, Jeong Kim, Jose M. Lora, Steven Magnuson, Ira Mellman, Anthony F. Romero, Alexander M. Taylor, Vickie Tsui
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Grant
Filed:
August 28, 2015
Date of Patent:
October 18, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
May 4, 2012
Date of Patent:
August 23, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Victor S. Gehling, Michael Charles Hewitt, Alexander M. Taylor, Jean-Christophe Harmange
Abstract: Agents of formulas (I)/(II)/(III) for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Application
Filed:
August 15, 2014
Publication date:
June 30, 2016
Applicant:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Grant
Filed:
March 18, 2015
Date of Patent:
June 21, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Type:
Application
Filed:
November 25, 2015
Publication date:
June 9, 2016
Applicants:
Genentech, Inc., Constellation Pharmaceuticals, Inc.
Inventors:
Marc Adler, Brian K. Albrecht, Sarah Bronner, Kevin X. Chen, Alexandre Côté, Terry Crawford, Patrick Cyr, Jackson Egen, Steven Kauder, Kwong Wah Lai, Jiangpeng Liao, Steven Magnuson, Jeremy Murray, Richard Pastor, F. Anthony Romero, Alexander M. Taylor, Vickie Hsiao-Wei Tsui, Fei Wang, Bing-Yan Zhu
Abstract: Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of KDM5.
Type:
Application
Filed:
March 14, 2014
Publication date:
May 26, 2016
Applicants:
CONSTELLATION PHARMACEUTICALS, INC., GENENTECH, INC.
Inventors:
Shilpi Arora, Michael Robert Costa, Ted Lau, Patrick Trojer, Brian K. Albrecht, Shane Buker, Marie Classon, Victor S. Gehling, Jean-Christophe Harmange, Erica L. Jackson, Jun Liang, Heidi Phillips, Peter Sandy, Jeffrey Settleman, Jean-Philippe Stephan
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
June 15, 2012
Date of Patent:
May 3, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Jean-Christophe Harmange, Alexandre Cote, Alexander M. Taylor
Abstract: Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
Type:
Application
Filed:
March 13, 2014
Publication date:
March 3, 2016
Applicants:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange, Kwong Wah Lai, Jun Liang, Peter Dragovich, Dan Ortwine, Sharada Labadie, Birong Zhang, Jim Kiefer
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
December 2, 2011
Date of Patent:
February 2, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael Charles Hewitt, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
Abstract: The invention provides methods for treating Th2 cytokine-mediated diseases by inhibiting bromodomain function.
Type:
Application
Filed:
March 14, 2014
Publication date:
January 28, 2016
Applicants:
CONSTELLATION PHARMACEUTICALS, INC., GENENTECH, INC.
Inventors:
Brian K. Albrecht, Alexandre Cote, Terry Crawford, Benjamin Fauber, Hon-Ren Huang, Jose M. Lora, Steven Magnuson, Christopher G. Nasveschuk, Andres Salmeron, Robert J. Sims, III, Alexander M. Taylor
Abstract: The present invention relates to fusion proteins comprising at least one chromatin binding module and at least one reporter module, wherein a plurality of fusion proteins are capable of forming foci, and associated methods for identifying bromodomain inhibiting compounds.
Type:
Application
Filed:
March 14, 2014
Publication date:
January 7, 2016
Applicant:
CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Hon-Ren Huang, Robert J. Sims, III, Steven Frank Bellon
Abstract: Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.
Type:
Application
Filed:
February 11, 2014
Publication date:
December 31, 2015
Applicant:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani