Patents Assigned to Exelixis, Inc.
  • Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases
    Publication number: 20110263558
    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: March 15, 2011
    Publication date: October 27, 2011
    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
  • Atropisomers of (Hydroxyalkyl) Pyrrole Derivatives
    Publication number: 20110263673
    Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy-C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.
    Type: Application
    Filed: October 7, 2009
    Publication date: October 27, 2011
    Applicants: DAIICHI SANKYO COMPANY, LIMITED, EXELIXIS, INC.
    Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Kazumasa Aoki, Hiroyuki Tsuruoka, Noriyuki Hayashi, Tsuyoshi Homma
  • 1-Phenylpyrrole Derivatives
    Publication number: 20110263544
    Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.
    Type: Application
    Filed: October 7, 2009
    Publication date: October 27, 2011
    Applicants: DAIICHI SANKYO COMPANY, LIMITED, EXELIXIS, INC.
    Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Hiroyuki Tsuruoka, Kazumasa Aoki, Masatoshi Honzumi, Yusuke Asoh, Keiji Saito, Tsuyoshi Homma
  • Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
    Patent number: 8044062
    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.
    Type: Grant
    Filed: October 9, 2006
    Date of Patent: October 25, 2011
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K. S. Yeung
  • Pyridopyrimidinone Inhibitors of PI3Kalpha
    Publication number: 20110237608
    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.
    Type: Application
    Filed: June 2, 2011
    Publication date: September 29, 2011
    Applicant: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K.S. Yeung
  • Pyrrole derivatives as pharmaceutical agents
    Patent number: 8026237
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: July 30, 2005
    Date of Patent: September 27, 2011
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B Mac, Larry W Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C Stevens, Tie-Lin Wang, Yong Wang, Jason H Wu
  • Modulators of LXR
    Patent number: 8013001
    Abstract: Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Christopher D. Bayne, Alan T. Johnson, Shao Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Jr., Haixia Wang, Yinong Xie
  • Tie-2 modulators and methods of use
    Patent number: 8013156
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
    Type: Grant
    Filed: March 19, 2004
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, S. David Brown, Wei Cheng, Vasu Jammalamadaka, John M. Nuss, Morrison B. Mac, Jason Jevious Parks, Matthew A. Williams, Wei Xu, Atwood Kim Cheung, Lisa Esther Dalrymple, Sergey Epshteyn, Mohamed Abdulkader Ibrahim, James William Leahy, Gary Lee Lewis, Robin Tammie Noguchi, Larry Wayne Mann, Brian Hugh Ridgway, Joan C. Sangalang, Kevin Luke Schnepp, Xian Shi, Richard George Khoury
  • Tropane compounds
    Patent number: 8012956
    Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Kenneth D. Rice, Naing Aay, Neel Kumar Anand, Arlyn Arcalas, Tae-Gon Baik, Charles M. Blazey, Owen Joseph Bowles, Chris A. Buhr, Joerg Bussenius, Simona Costanzo, Jeffrey Kimo Curtis, Steven Charles Defina, Larisa Dubenko, Abigail R. Kennedy, Angie Inyoung Kim, Katherine Lara, Sunghoon Ma, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Longcheng Wang
  • Phosphatidylinositol 3-Kinase Inhibitors And Methods Of Their Use
    Publication number: 20110207712
    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: Application
    Filed: April 28, 2011
    Publication date: August 25, 2011
    Applicant: 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
  • TAOJIKs as modifiers of the beta-catenin pathway and methods of use
    Patent number: 8003315
    Abstract: Human TAOJIK genes are identified as modulators of the beta-catenin pathway, and thus are therapeutic targets for disorders associated with defective beta-catenin function. Methods for identifying modulators of beta-catenin, comprising screening for agents that modulate the activity of TAOJIK are provided.
    Type: Grant
    Filed: December 12, 2002
    Date of Patent: August 23, 2011
    Assignee: Exelixis, Inc.
    Inventors: Michael A. Costa, Steven Brian Gendreau, Emery G. Dora, III, Monique Nicoll, Lenore Urbani, Jeffrey S. Larson
  • CDK Modulators
    Publication number: 20110201599
    Abstract: A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: July 2, 2009
    Publication date: August 18, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Suleyman Bahceci, Bryan Chan, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Maurizio Franzini, Vasu Jammalamadaka, Joon Won Jeong, Lisa Renee Jones, Ryan Michael Kelley, Moon Hwan Kim, James W. Leahy, Morrison B. Mac, Robin Tammie Noguchi, Pallavi Rao, Brian Hugh Ridgway, Wei Xu, Yong Wang
  • Methods of using MEK inhibitors
    Patent number: 7999006
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: August 16, 2011
    Assignee: Exelixis, Inc.
    Inventor: Peter Lamb
  • [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
    Patent number: 7994172
    Abstract: The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
    Type: Grant
    Filed: December 27, 2005
    Date of Patent: August 9, 2011
    Assignee: Exelixis, Inc.
    Inventors: Ken Rice, Erick Wang Co, Moon Hwan Kim, Lynn Canne Bannen, Joerg Bussenius, Donna Tra Le, Amy Lew Tsuhako, John Nuss, Yong Wang, Wei Xu, Rhett Ronald Klein
  • HPRP4s modifiers of the p53 pathway and methods of use
    Patent number: 7993829
    Abstract: Human hPRP4 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 hPRP4 are provided.
    Type: Grant
    Filed: January 26, 2007
    Date of Patent: August 9, 2011
    Assignee: Exelixis Inc.
    Inventors: Lori Friedman, Gregory D. Plowman, Tak Hung, Helen Francis-Lang, Danix Li, Roel P. Funke, Michael Costa
  • Phosphatidylinositol 3-kinase inhibitors and methods of their use
    Patent number: 7989622
    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: October 9, 2006
    Date of Patent: August 2, 2011
    Assignee: Exelixis, Inc.
    Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison B. Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
  • c-MET modulators and method of use
    Patent number: 7977345
    Abstract: A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification, compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: July 12, 2011
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Lisa Esther Dalrymple, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Yong Wang, Wie Xu
  • Benzylthiazolone inhibitors of estrogen-related receptors (ERR)
    Patent number: 7977489
    Abstract: Compounds of the following general structure for use in compositions and methods for modulating the activity of nuclear receptors are provided: The compounds are useable in compositions and methods for modulating the estrogen related receptors and are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: July 12, 2011
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Raju Mohan, Brett B. Busch, Michael Charles Nyman, William C. Stevens, Jr.
  • GFATS As Modifiers of the AXIN Pathway and Methods of Use
    Publication number: 20110167505
    Abstract: Human GFAT genes are identified as modulators of the Axin pathway, and thus are therapeutic targets for disorders associated with defective Axin function. Methods for identifying modulators of Axin, comprising screening for agents that modulate the activity of GFAT are provided.
    Type: Application
    Filed: June 20, 2006
    Publication date: July 7, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Steven Brian Gendreau, Emery G. Dora, III, Kim Lickteig
  • Anaplastic lymphoma kinase modulators and methods of use
    Patent number: 7973061
    Abstract: The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions; (Formula I).
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: July 5, 2011
    Assignee: Exelixis, Inc.
    Inventors: James William Leahy, Gary Lee Lewis, John M. Nuss, Brain Hugh Ridgway, Joan C. Sangalang