Abstract: The present disclosure relates to a novel crystalline form of a proteasome inhibitor, and to the processes for the preparation thereof. The novel crystalline form according to the disclosure may be used in the preparation of pharmaceutical compositions for the treatment of cancer.
Type:
Grant
Filed:
February 10, 2016
Date of Patent:
September 11, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Marianne Langston, Debra Mazaik, Eric Elliott, Anton Peterson, Patricia Andres, Jing Teng
Abstract: Provided is a formulation containing an immunoconjugate comprising an anti-GCC antibody molecule and a therapeutic agent, which is superior in stability and useful as a prophylactic or therapeutic agent for gastrointestinal cancer and the like. A formulation comprising (i) an immunoconjugate of the following formula (I): wherein Ab is an anti-GCC antibody molecule, X is a linker component, Z is a therapeutic agent, and m is an integer from 1-15, or a pharmaceutically acceptable salt thereof, (ii) polysorbate 20, and (iii) histidine or a salt thereof.
Abstract: Antibody formulations are described comprising a mixture of an anti-?4?7 antibody, an antioxidant or chelator, and at least one free amino acid. The disclosed formulations may have improved stability, reduced aggregate formation, or both. The present invention further provides a safe dosing regimen of these antibody formulations that is easy to follow, and which results in a therapeutically effective amount of the anti-?4?7 antibody in vivo.
Type:
Grant
Filed:
May 2, 2012
Date of Patent:
August 7, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Willow Diluzio, Phoung M. Nguyen, Csanad M. Varga, Vaithianathan Palaniappan, Jason Brown
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: The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.
Type:
Grant
Filed:
October 13, 2016
Date of Patent:
July 10, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Ian Armitage, Martin I. Cooper, Mark D. Eddleston, Neil C. Faiber, Quentin J. McCubbin, Stephen W. Watt
Abstract: Methods for inducing clinical remission of ulcerative colitis in a human patient are described comprising administration of an antibody that has binding specificity for human ?4?7 integrin using a safe dosing regimen of these antibody formulations that is easy to follow, and which results in a therapeutically effective amount of the anti-?4?7 antibody in vivo.
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.
Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
Type:
Grant
Filed:
August 25, 2011
Date of Patent:
June 5, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
Type:
Grant
Filed:
April 17, 2017
Date of Patent:
May 8, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Matthew O. Duffey, Dylan England, Brian Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
Abstract: The present invention is directed to the identification of predictive markers that can be used to determine whether patients with cancer are clinically responsive or non-responsive to a therapeutic regimen prior to treatment. In particular, the present invention is directed to the use of certain individual and/or combinations of predictive markers, wherein the expression of the predictive markers correlates with responsiveness or non-responsiveness to a therapeutic regimen. Thus, by examining the expression levels of individual predictive markers and/or predictive markers comprising a marker set, it is possible to determine whether a therapeutic agent, or combination of agents, will be most likely to reduce the growth rate of tumors in a clinical setting.
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
May 8, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Barbara M. Bryant, Andrew I. Damokosh, George J. Mulligan
Abstract: Antibodies and antigen-binding fragments of antibodies that bind OV064 are disclosed. The antibodies bind an extracellular domain of OV064. Some of the antibodies and antigen-binding fragments bind an epitope on OV064 sufficient to induce internalization. In some embodiments, the antibodies are humanized, chimeric or human. Nucleic acids and vectors encoding the antibodies or portions thereof, recombinant cells that contain the nucleic acids, and compositions comprising the antibodies or antigen-binding fragments are also disclosed. The invention also provides therapeutic and diagnostic methods utilizing the antibodies and antigen-binding fragments provided herein.
Abstract: Disclosed are markers associated with sensitivity to treatment with proteasome inhibitors. Sensitivity is observed when RAS gene is wild type in tumor cells. Compositions and methods are further provided to assess markers of marker genes to predict outcome of treatment using proteasome inhibitors to patients having a solid tumor, such as a lung tumor or a colon tumor.
Type:
Grant
Filed:
November 9, 2012
Date of Patent:
March 20, 2018
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Allison Berger, Nibedita Chattopadhyay, Erik M. Koenig
Abstract: The present invention provides methods of inhibiting Raf kinase activity in a patient, the method comprising administering to the patient a compound having formula I: or a pharmaceutically acceptable salt thereof, wherein Rx, Ry, R1, L1, L2, Cy1, and Cy2 are as defined as set forth in the specification.
Type:
Grant
Filed:
December 15, 2016
Date of Patent:
March 20, 2018
Assignees:
Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
Inventors:
Weirong Chen, Jennifer Cossrow, Lloyd Franklin, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Benjamin Lane, Adam Littke, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
Abstract: Disclosed is a method for treating a subject having primary sclerosing cholangitis, comprising administering to said subject an effective amount of a humanized antibody or antigen-binding fragment thereof having binding specificity for alpha 4 beta 7 integrin.
Type:
Application
Filed:
March 4, 2016
Publication date:
February 22, 2018
Applicants:
Takeda Development Centre Europe Ltd., Takeda Pharmaceutical Company Limited, Millennium Pharmaceuticals, Inc.
Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
Type:
Grant
Filed:
July 10, 2014
Date of Patent:
January 23, 2018
Assignees:
Sunesis Pharmaceuticals, Inc., Millennium Pharmaceuticals, Inc.
Inventors:
Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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.
Abstract: Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(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 and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
Type:
Grant
Filed:
July 8, 2014
Date of Patent:
December 26, 2017
Assignee:
MILLENNIUM PHARMACEUTICALS, INC.
Inventors:
Ashley Sue McCarron, Todd B. Sells, Matthew Stirling, Stephen G. Stroud
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 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:
Grant
Filed:
October 26, 2012
Date of Patent:
November 28, 2017
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Stephen J. Blakemore, Bin Li, George J. Mulligan, Matthew C. Schu, Peter G. Smith
Abstract: A method for treating a human patient suffering from fistulizing Crohn's disease, comprising administering to a patient suffering from fistulizing Crohn's disease, a humanized antibody having binding specificity for human ?4?7 integrin, wherein the human patient has a seton that was surgically placed prior to administration of the antibody, and wherein the dosing regimen induces fistula(e) healing.