Exelixis Patent Applications

Methods of Using PI3K and MEK Modulators

Granted: March 25, 2010
Application Number: 20100075947
The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.

IMIDAZOLE BASED LXR MODULATORS

Granted: March 25, 2010
Application Number: 20100075964
Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3 and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

LXR and FXR Modulators

Granted: March 18, 2010
Application Number: 20100069367
Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Azepinoindole and Pyridoindole Derivatives as Pharmaceutical Agents

Granted: December 31, 2009
Application Number: 20090326218
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.

4-Aryl-2-Amino-Pyrimidnes or 4-Aryl-2-Aminoalkyl-Pyrimidines as Jak-2 Modulators and Methods of Use

Granted: December 3, 2009
Application Number: 20090298830
This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.

11 Beta-HSD1 Modulators

Granted: October 1, 2009
Application Number: 20090247515
A compound according to Formula A: or a pharmaceutically acceptable salt thereof, wherein R11, G1 and G2 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

Benzofuropyrimidinones

Granted: October 1, 2009
Application Number: 20090247559
A compound according to formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3a, R3b, R3c and R3d are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

Methods of Using IGFIR and ABL Kinase Modulators

Granted: September 17, 2009
Application Number: 20090232828
The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s).

C20ORF23 as modifier of the IGFR pathway and methods of use

Granted: August 13, 2009
Application Number: 20090202563
Human C20ORF23 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 C20ORF23 are provided.

Azepinoindole Derivatives As Pharmaceutical Agents

Granted: August 13, 2009
Application Number: 20090203577
The present invention relates to compounds of formula I, which exhibit affinity for the farnesoid X receptor.

Pharmaceutical Compositions

Granted: August 6, 2009
Application Number: 20090197870
Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists, or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as…

ANAPLASTIC LYMPHOMA KINASE MODULATORS AND METHODS OF USE

Granted: July 23, 2009
Application Number: 20090186905
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…

c-Met modulators and methods of use

Granted: July 2, 2009
Application Number: 20090170896
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,…

Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases

Granted: June 18, 2009
Application Number: 20090156576
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.

RORS as Modifiers of the p21 Pathway and Methods of Use

Granted: June 11, 2009
Application Number: 20090149413
Human ROR genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of ROR are provided.

Pfks as modifiers of the igfr pathway and methods of use

Granted: June 4, 2009
Application Number: 20090142272
Human PFK 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 PFK are provided.

INHIBITORS OF HEDGEHOG PATHWAY

Granted: April 23, 2009
Application Number: 20090105211
The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

c-MET MODULATORS AND METHODS OF USE

Granted: April 23, 2009
Application Number: 20090105299
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,…

MAP3Ks as modifiers of the p53 pathway and methods of use

Granted: March 12, 2009
Application Number: 20090068186
Human MAP3K 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 MAP3K are provided.

Pyridopyrimidinone inhibitors of pi3kalpha

Granted: March 5, 2009
Application Number: 20090062274
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.