Patents Assigned to Millennium Pharmaceuticals, Inc.
  • Heteroaryls and uses thereof
    Patent number: 9802960
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: October 31, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Sulfamoylating reagents
    Patent number: 9802938
    Abstract: The present invention provides sulfamoylating reagents of formula RuN?—S(O)2X+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and Ru is an amine protecting group or hydrogen.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: October 31, 2017
    Assignee: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Ian Armitage, Eric L. Elliott, Marianne Langston, Steven P. Langston, Quentin J. McCubbin, Hiro Mizutani, Matthew Stirling, Lei Zhu
  • Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
    Patent number: 9796725
    Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: October 24, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Mario Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
  • Derivatives of 1-amino-2-cyclobutylethylboronic acid
    Patent number: 9771381
    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.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: September 26, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Jing Li
  • Compounds and methods for inhibiting mitotic progression
    Patent number: 9765078
    Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: September 19, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Lloyd J. Payne, Richard J. Boyce, Todd B. Sells, Stephen G. Stroud, Stuart Travers, Tricia J. Vos, Gabriel S. Weatherhead
  • Formulation for anti-?4?7 antibody
    Patent number: 9764033
    Abstract: Antibody formulations are described comprising a mixture of a non-reducing sugar, an anti-?4?7 antibody and at least one amino acid. The disclosed formulations have improved stability, reduced aggregate formation, and may retard degradation of the anti-?4?7 antibody therein or exhibit any combinations thereof. 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: September 19, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Willow Diluzio, Nobel T. Truong, Csanad M. Varga, Vaithianathan Palaniappan, Jason Brown, Catherine Scholz
  • Heteroaryls and uses thereof
    Patent number: 9751854
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: September 5, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Combination of catalytic mTORC1/2 inhibitors and selective inhibitors of Aurora A kinase
    Patent number: 9724354
    Abstract: Disclosed are methods for the treatment of proliferative disorders. Disclosed in particular, are methods for treatment of proliferative disorders such as cancer, by administering an mTORC1/2 inhibitor in combination with a selective inhibitor of Aurora A kinase. Preferred MTORC1/2 inhibitors include MLN0128 and the preferred Aurora A kinase inhibitor of the combination is MLN8237.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: August 8, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Rachael L. Brake, Huifeng Niu
  • HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
    Publication number: 20170216290
    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: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. DUFFEY, Dylan England, Brian Scott Freeze, Zhigen Hu, Steven Langston, Charles Mclntyre, Hirotake Mizutani, Koji Ono, He Xu
  • Heteroaryl compounds useful as inhibitors of E1 activating enzymes
    Patent number: 9718788
    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: Grant
    Filed: August 29, 2016
    Date of Patent: August 1, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil
  • Heteroaryl inhibitors of sumo activating enzyme
    Patent number: 9695154
    Abstract: Disclosed are compounds of formula (I); or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra?, Rc, Rf, X2, Rd, Rd?, Re, Re?, m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, 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: July 1, 2014
    Date of Patent: July 4, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan B. England, Zhigen Hu, Mitsuhiro Ito, Steven P. Langston, Charles McIntyre, Hirotake Mizutani, He Xu
  • Inhibitor of breast cancer resistance protein (BCRP)
    Patent number: 9695174
    Abstract: Disclosed are compounds that inhibit breast cancer resistance protein (BCRP), of which compound (I-1), ((3S,6S,12aS)-6-isobutyl-9-methoxy-3-methyl-2,3,6,7,12,12a-hexahydropyrazino[1?,2?:1,6]pyrido[3,4-b]indole-1,4-dione) or a pharmaceutically acceptable salt thereof, and the compound 12, ((3S,6S,12aS)-6-isobutyl-9-methoxy-3,10-dimethyl-2,3,6,7,12,12a-hexahydropyrazino[1?,2?:1,6]pyrido[3,4-b]indole-1,4-dione) or a pharmaceutically acceptable salt thereof. Also disclosed are methods of inhibiting BCRP or decreasing BCRP activity and methods of determining potential BCRP substrates.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: July 4, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Yuexian Li, Shimoga R. Prakash, Cindy Qi Xia, Mingxiang M. Liao
  • QUINOXALINE COMPOUNDS AND USES THEREOF
    Publication number: 20170174704
    Abstract: This invention provides compounds of formula I and subsets thereof: wherein T, J, R, R4, Rq, o, RA, and RB and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, or T-cell mediated autoimmune disease.
    Type: Application
    Filed: April 17, 2015
    Publication date: June 22, 2017
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth M. Gigstad, David P. Cardin, Takaharu Hirayama, Masaaki Hirose, Yongbo Hu, Hiroyuki Kakei, Hong Myung Lee, Takashi Motoyaji, Noriyuki Nii, Zhan Shi, Stepan Vyskocil, Hiroyuki Watanabe
  • Heteroaryl compounds useful as inhibitors of SUMO activating enzyme
    Patent number: 9683003
    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: June 30, 2015
    Date of Patent: June 20, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan England, Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
  • Compounds Useful as Raf Kinase Inhibitors
    Publication number: 20170158686
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Application
    Filed: December 15, 2016
    Publication date: June 8, 2017
    Applicants: 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
  • Chemokine receptor antagonists and methods of use
    Patent number: 9663537
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: May 30, 2017
    Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kirin Co., Ltd.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Formulation for anti-?4?7 antibody
    Patent number: 9663579
    Abstract: Methods for achieving clinical response of Crohn's disease 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.
    Type: Grant
    Filed: July 20, 2016
    Date of Patent: May 30, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Irving H. Fox, Catherine Scholz
  • Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
    Patent number: 9663525
    Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: May 30, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Marlo Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
  • Solid pharmaceutical compositions and processes for their production
    Patent number: 9655856
    Abstract: This invention provides novel solid pharmaceutical compositions and processes for the bulk production of said compositions. This invention also provides methods of using the pharmaceutical compositions in the treatment of cancer.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: May 23, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventor: Bhavishya Mittal
  • Combination of MEK inhibitors and selective inhibitors of Aurora A kinase
    Patent number: 9629850
    Abstract: The present invention relates to methods for the treatment of proliferative disorders. In particular, the invention provides methods for treatment of proliferative disorders by administering a MEK inhibitor in combination with a selective inhibitor of Aurora A kinase.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: April 25, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Arijit Chakravarty, Patrick Vincent