Abstract: The present invention provides methods of treating cancer by administering a compound of formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with an inhibitor that targets HER2 and/or HER3.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
April 21, 2015
Assignee:
Exelixis, Inc.
Inventors:
Dana T. Aftab, Carlos L. Arteaga, Veronique Blanc, Anindita Chakrabarty, Marielle Chiron-Blonde, Celine Nicolazzi, Ariella Hanker, Loic Vincent
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Abstract: The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.
Type:
Grant
Filed:
February 9, 2011
Date of Patent:
December 2, 2014
Assignee:
Exelixis, Inc.
Inventors:
Dana T. Aftab, Wolfgang M. Korn, Olga K. Mirzoeva
Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
Type:
Grant
Filed:
April 28, 2011
Date of Patent:
November 18, 2014
Assignee:
Exelixis, Inc.
Inventors:
William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane -1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-ffuorophenyl)cyclopropane-1,1-dicarboxamide.
Type:
Grant
Filed:
January 15, 2010
Date of Patent:
November 4, 2014
Assignee:
Exelixis, Inc.
Inventors:
Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Abstract: The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of Formula (I): in combination with one or both of bendamustine and rituximab.
Type:
Application
Filed:
June 15, 2012
Publication date:
October 9, 2014
Applicants:
Sanofi, Exelixis, Inc.
Inventors:
Arthur DeCillis, Joanne Lager, Tal Zaks
Abstract: Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein.
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Type:
Application
Filed:
June 27, 2013
Publication date:
September 18, 2014
Applicant:
Exelixis, Inc.
Inventors:
Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
Abstract: The present invention provides methods of treating cancer by administering a compound of formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with an inhibitor that targets HER2 and/or HER3.
Type:
Application
Filed:
July 8, 2011
Publication date:
September 18, 2014
Applicants:
Exelixis, Inc., Sanofi, Vanderbilt University
Inventors:
Dana T. Aftab, Carlos L. Arteaga, Veronique Blanc, Anindita Chakrabarty, Marielle Chiron-Blonde, Celine Nicolazzi, Ariella Hanker, Loic Vincent
Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
Abstract: This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent.
Type:
Grant
Filed:
October 16, 2009
Date of Patent:
August 12, 2014
Assignee:
Exelixis, Inc.
Inventors:
Geetha Shankar, Frauke Bentzien, Peter Lamb, David Matthews
Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
Type:
Grant
Filed:
October 16, 2009
Date of Patent:
July 29, 2014
Assignee:
Exelixis, Inc.
Inventors:
Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
Abstract: Human SCD genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SCD are provided.
Type:
Grant
Filed:
February 26, 2010
Date of Patent:
July 8, 2014
Assignee:
Exelixis, Inc.
Inventors:
Marcia Belvin, Helen Francis-Lang, Lori Friedman, Gregory D. Plowman, Timothy S. Heuer
Abstract: This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.
Abstract: Human CDK9 genes are identified as modulators of the IGF pathway, and thus are therapeutic targets for disorders associated with defective IGF function. Methods for identifying modulators of IGF, comprising screening for agents that modulate the activity of CDK9 are provided.
Type:
Grant
Filed:
June 20, 2005
Date of Patent:
June 24, 2014
Assignee:
Exelixis, Inc.
Inventors:
Mark E. Maxwell, Michael Martin Ollmann, Timothy S. Heuer, Lynn Margaret Bjerke
Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.
Type:
Grant
Filed:
September 28, 2011
Date of Patent:
June 10, 2014
Assignee:
Exelixis, Inc.
Inventors:
Richard Martin, Jeffrey D Kahl, Brenton T Flatt, Ronald Griffith