Exelixis Patent Applications

Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use

Granted: February 16, 2017
Application Number: 20170044106
The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly…

LXR MODULATORS

Granted: October 20, 2016
Application Number: 20160304499
The present invention provides compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXR), compositions comprising any of such novel compounds, methods of using these compounds or compositions as medicaments for prevention or treatment of diseases or disorders related to liver X receptor (LXR), as well as methods of preparing these LXR modulators and using them in the manufacture of medicaments.

LXR MODULATORS

Granted: October 6, 2016
Application Number: 20160289222
The present invention provides compounds of Formula I and Formula II: or pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXRs), and compositions comprising any of such novel compounds and methods of use thereof. These compounds are useful as medicaments for treatment and/or prophylaxis for diseases or conditions related to activity of LXRs.

LXR MODULATORS

Granted: September 29, 2016
Application Number: 20160280661
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.

Cabozantinib Dosage Form and Use in the Treatment of Cancer

Granted: January 28, 2016
Application Number: 20160022662
This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.

LXR MODULATORS

Granted: October 22, 2015
Application Number: 20150299136
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.

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

Granted: December 25, 2014
Application Number: 20140378436
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.

Combination Therapies for Treating Hematologic Malignancies Using Pyridopyrimidinone Inhibitors of PI3K/mTOR with Bendamustine and/or Rituximab

Granted: October 9, 2014
Application Number: 20140302012
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.

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

Granted: October 9, 2014
Application Number: 20140303151
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.

Phosphatidylinositol 3-Kinase Inhibitors for the Treatment of Lymphoproliferative Malignancies

Granted: October 9, 2014
Application Number: 20140303172
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.

Method of Treating Lymphoma Using Pyridopyrimidinone Inhibitors of PI3K/mTOR

Granted: October 2, 2014
Application Number: 20140296265
The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I:

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.

Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases

Granted: September 18, 2014
Application Number: 20140275527
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.

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.