Exelixis Patent Applications

Combinations of Kinase Inhibitors for the Treatment of Cancer

Granted: September 18, 2014
Application Number: 20140271665
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.

Method for Treating Osteoporosis

Granted: August 14, 2014
Application Number: 20140228401
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.

Processes for Preparing Quinoline Compounds and Pharmaceutical Compositions Containing Such Compounds

Granted: July 17, 2014
Application Number: 20140200242
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.

C-Met Modulator Pharmaceutical Compositions

Granted: July 3, 2014
Application Number: 20140186407
Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.

Method of Treating Cancer and Bone Cancer Pain

Granted: June 26, 2014
Application Number: 20140179736
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.

LXR MODULATORS

Granted: June 12, 2014
Application Number: 20140163081
Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

c-Met Modulators and Method of Use

Granted: June 5, 2014
Application Number: 20140155378
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,…

METHOD OF TREATING LUNG ADENOCARCINOMA

Granted: May 1, 2014
Application Number: 20140121239
This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: or a pharmaceutically acceptable salt thereof.

Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture

Granted: April 17, 2014
Application Number: 20140107100
The invention is directed 10 Compound's of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.

Methods of Using PI3K and MEK Modulators

Granted: April 10, 2014
Application Number: 20140100215
The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.

Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture

Granted: March 20, 2014
Application Number: 20140080810
The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.

Method of Treating Cancer

Granted: March 6, 2014
Application Number: 20140066444
This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture

Granted: March 6, 2014
Application Number: 20140066431
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.

Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture

Granted: February 27, 2014
Application Number: 20140058103
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.

Method of Treating Cancer

Granted: February 27, 2014
Application Number: 20140057908
This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture

Granted: February 13, 2014
Application Number: 20140045825
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.

IMIDAZOLE BASED LXR MODULATORS

Granted: February 6, 2014
Application Number: 20140038964
Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.

BENZOXAZEPINES AS INHIBITORS OF mTOR AND METHODS OF THEIR USE AND MANUFACTURE

Granted: January 16, 2014
Application Number: 20140018347
The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein.

Pyrido [2, 3-D] pyrimidin-7-one compounds as inhibitors of P13K-Alpha for the treament of cancer

Granted: December 26, 2013
Application Number: 20130343988
The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer.

C-Met Modulator Pharmaceutical Compositions

Granted: December 12, 2013
Application Number: 20130330377
Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.