Exelixis Patent Applications

Isoquinolinone Derivatives and Their Use As Therapeutic Agents

Granted: June 5, 2008
Application Number: 20080132521
Compounds of formula (I): wherein n, R1, R2, R3 and R7 are disclosed herein, are useful in treating disease-states associated with nuclear receptor activity. Pharmaceutical compositions comprising and methods of using said compounds are also disclosed herein.

Heterocyclic Compounds As Pharmaceutical Agents

Granted: June 5, 2008
Application Number: 20080132519
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 the disease or disorder directly or indirectly related to the activity of the receptors.

Modulators Of Nuclear Receptors

Granted: May 22, 2008
Application Number: 20080119488
Compounds of the invention, such as compounds of formula (I), where n, m, A, 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.

SCDs As Modifiers of the p53 Pathway and Methods of Use

Granted: May 1, 2008
Application Number: 20080102070
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.

Cdk9 as Modifier of the Igf Pathway and Methods of Use

Granted: April 24, 2008
Application Number: 20080095763
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.

C-Kit Modulators And Methods Of Use

Granted: April 24, 2008
Application Number: 20080096892
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellu-lar activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.

Kinase Modulators and Methods of Use

Granted: March 27, 2008
Application Number: 20080076774
The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical…

Sulfs as Modifiers of the Beta-Catenin Pathway and Methods of Use

Granted: February 28, 2008
Application Number: 20080050313
Human SULF 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 SULF are provided.

Raf Modulators and Methods of Use

Granted: January 10, 2008
Application Number: 20080009488
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 Raf. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.

Pyrazole Kinase Modulators And Methods Of Use

Granted: December 20, 2007
Application Number: 20070293507
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. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.

Itpks as Modifiers of the Igfr Pathway and Methods of Use

Granted: December 20, 2007
Application Number: 20070292349
Human MIGFR genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of MIGFR are provided.

Sppls as Modifiers of the P53 Pathway and Methods of Use

Granted: December 13, 2007
Application Number: 20070286852
Human SPPL 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 SPPL are provided.

Tie-2 Modulators and Methods of Use

Granted: November 29, 2007
Application Number: 20070275952
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.

Nadks as Modifiers of Branching Morphogenesis and Methods of Use

Granted: November 22, 2007
Application Number: 20070269378
Human NADK genes are identified as modulators of branching morphogenesis, and thus are therapeutic targets for disorders associated with defective branching morphogenesis function. Methods for identifying modulators of branching morpho-genesis, comprising screening for agents that modulate the activity of NADK are provided.

Ranbp2 as Modifiers of the Pten/Igf Pathway and Methods of Use

Granted: November 22, 2007
Application Number: 20070269802
Human RANBP2 genes are identified as modulators of the PTEN/IGF pathway, and thus are therapeutic targets for disorders associated with defective PTEN/IGF function. Methods for identifying modulators of FEN/IGF, comprising screening for agents that modulate the activity of RANBP2 are provided.

Man2as as Modifiers of the Igfr Pathway and Methods of Use

Granted: November 15, 2007
Application Number: 20070264268
Human MIGFR genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of MIGFR are provided.

c-MET MODULATORS AND METHOD OF USE

Granted: October 18, 2007
Application Number: 20070244116
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. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above,…

C-MET MODULATORS AND METHOD OF USE

Granted: September 27, 2007
Application Number: 20070225307
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. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above,…

Tao Kinase Modulators And Method Of Use

Granted: September 6, 2007
Application Number: 20070208166
The invention provides compounds and methods for inhibition of kinases, such as those of the TAO family, more specifically KIAA1361, TAO, and JIK 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…

HPRP4s Modifiers of the p53 Pathway and Methods of Use

Granted: July 12, 2007
Application Number: 20070160539
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.