Abstract: This invention provides compounds of formula (I) wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
Type:
Grant
Filed:
June 21, 2010
Date of Patent:
August 4, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
Abstract: Novel CARD-9, CARD-10, or CARD-11 polypeptides, proteins, and nucleic acid molecules are disclosed. In addition to isolated CARD-9, CARD-10, or CARD-11 proteins, the invention further provides CARD-9, CARD-10, or CARD-11, fusion proteins, antigenic peptides and anti-CARD-9, CARD-10, or CARD-11 antibodies. The invention also provides CARD-9, CARD-10, or CARD-11 nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which a CARD-9, CARD-10, or CARD-11 gene has been introduced or disrupted. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided.
Abstract: Disclosed herein are markers associated with sensitivity to treatment with proteasome inhibitors. Sensitivity is observed when RAS gene is wild type in tumor cells.
Type:
Application
Filed:
November 9, 2012
Publication date:
July 2, 2015
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Allison Berger, Hughes Bernard, Nibedita Chattopadhyay, Erik M. Koenig, George J. Mulligan, Matthew J. Schu
Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
Type:
Application
Filed:
September 8, 2014
Publication date:
July 2, 2015
Applicant:
MILLENNIUM PHARMACEUTICALS, INC.
Inventors:
Christopher F. Claiborne, Stephen Critchley, Courtney Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, G1, W, n, and A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
Type:
Grant
Filed:
February 17, 2014
Date of Patent:
June 23, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Craig Grant, James P. Kanter, Graeme Langlands
Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
Type:
Grant
Filed:
October 9, 2013
Date of Patent:
May 19, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
Abstract: This invention provides thiophene compounds of formula I: wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
Type:
Grant
Filed:
January 26, 2009
Date of Patent:
May 12, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christelle C. Renou, Tricia J. Vos, Matthew O. Duffey, Robert Downham
Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Abstract: Disclosed herein are markers whose mutational status is associated with sensitivity to treatment with NAE inhibitors. Mutational status is determined by measurement of characteristics of markers associated with the marker genes. Compositions and methods are provided to assess markers of marker genes to predict response to NAE inhibition treatment.
Type:
Application
Filed:
October 26, 2012
Publication date:
April 30, 2015
Applicants:
Millennium Pharmaceuticals, Inc, Massachusetts General Hospital
Inventors:
Cyril H. Benes, Stephen J. Blakemore, Jonathan L. Blank, Eric S. Llightcap, George J. Mulligan, Matthew C. Schu, Peter G. Smith, Jeffrey E. Settleman
Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.
Type:
Application
Filed:
May 29, 2014
Publication date:
April 23, 2015
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
Abstract: Disclosed herein are markers whose mutational status is associated with sensitivity to treatment with NAE inhibitors. Mutational status is determined by measurement of characteristics of markers associated with the marker genes. Compositions and methods are provided to assess markers of marker genes to predict response to NAE inhibition treatment.
Type:
Application
Filed:
October 26, 2012
Publication date:
April 16, 2015
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Stephen J. Blakemore, Bin Li, George J. Mulligan, Matthew C. Schu, Peter G. Smith
Abstract: Antibodies and antigen-binding fragments of antibodies that bind GCC are disclosed. The invention also provides therapeutic and diagnostic methods utilizing the antibodies and antigen-binding fragments provided herein.
Type:
Grant
Filed:
April 27, 2013
Date of Patent:
April 7, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Helen Alison Frank, Alice A. McDonald, Theresa L. O'Keefe
Abstract: Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.
Type:
Grant
Filed:
February 1, 2013
Date of Patent:
March 24, 2015
Assignees:
Millennium Pharmaceuticals, Inc., Portola Pharmaceuticals, Inc.
Inventors:
Anjali Pandey, Emilia P. T. Leitao, Jose Rato, Zhiguo Jake Song
Abstract: The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1S,2S,4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.
Type:
Application
Filed:
November 25, 2014
Publication date:
March 19, 2015
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Ian Armitage, Eric L. Elliott, Marianne Langston, Steven P. Langston, Quentin J. McCubbin, Hiro Mizutani, Matthew Stirling, Lei Zhu
Abstract: The present disclosure relates to methods for the treatment of cancer in patients in recognized need of such treatment. The methods comprise administering to such a patient an NAE inhibitor or a pharmaceutically acceptable salt thereof, such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216), and a hypomethylating agent or a pharmaceutically acceptable salt thereof, such as azacitidine or decitabine. Also disclosed are medicaments for use in the treatment of cancer.
Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
Type:
Application
Filed:
April 8, 2014
Publication date:
March 12, 2015
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
Type:
Grant
Filed:
May 30, 2013
Date of Patent:
February 10, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher Blackburn, Kenneth M. Gigstad, He Xu
Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.