Exelixis Patent Grants

LXR modulators

Granted: September 5, 2017
Patent Number: 9751869
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.

C-met modulator pharmaceutical compositions

Granted: August 8, 2017
Patent Number: 9724342
Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.

Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds

Granted: August 1, 2017
Patent Number: 9717720
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.

Inhibitors of PI3K-delta and methods of their use and manufacture

Granted: June 6, 2017
Patent Number: 9670212
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.

Process for preparing quinoline derivatives

Granted: June 14, 2016
Patent Number: 9365516
A process for preparing a compound of Formula I is disclosed: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with…

Inhibitors of PI3K-delta and methods of their use and manufacture

Granted: May 24, 2016
Patent Number: 9346807
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.

Combinations of kinase inhibitors for the treatment of cancer

Granted: April 21, 2015
Patent Number: 9011863
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.

Imidazole based LXR modulators

Granted: April 7, 2015
Patent Number: 9000022
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.

Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K and mTOR in combination with autophagy inhibitors

Granted: December 2, 2014
Patent Number: 8901137
The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.

Phosphatidylinositol 3-kinase inhibitors and methods of their use

Granted: November 18, 2014
Patent Number: 8889664
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.

(L)-malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Granted: November 4, 2014
Patent Number: 8877776
Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane -1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of…

TGR5 agonists

Granted: September 30, 2014
Patent Number: 8846739
TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.

Synergistic effects between sphingosine-1-phosphate receptor antagonists and antimicrotubule agents

Granted: August 12, 2014
Patent Number: 8802692
This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL┬« from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE┬« from Sanofi-aventis,…

Inhibitors of the hedgehog pathway

Granted: August 5, 2014
Patent Number: 8796294
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.

Acetanilide sphingosine-1-phosphate receptor antagonists

Granted: July 29, 2014
Patent Number: 8791102
This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor…

Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity

Granted: July 22, 2014
Patent Number: 8785488
The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises…

SCDs as modifiers of the p53 pathway and methods of use

Granted: July 8, 2014
Patent Number: 8771942
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: June 24, 2014
Patent Number: 8758994
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.

Inhibitors of the hedgehog pathway

Granted: June 17, 2014
Patent Number: 8754092
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.

Quinazolinone modulators of nuclear receptors

Granted: June 10, 2014
Patent Number: 8748440
Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.