Exelixis Patent Grants

P4HAS as modifiers of the IGFR pathway and methods of use

Granted: February 15, 2011
Patent Number: 7888048
Human P4HA 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 P4HA are provided.

Anaplastic lymphoma kinase modulators and methods of use

Granted: January 18, 2011
Patent Number: 7872014
The present invention comprises compounds and pharmaceutical compositions comprising the compounds that are inhibitors of ALK. The invention also comprises methods of using the compounds and compositions to treat diseases mediated by ALK, including diseases such as cancer, immunological disorders, cardiovascular diseases, and other degenerative disorders.

Bridged ring structures as pharmaceutical agents

Granted: January 4, 2011
Patent Number: 7863298
The present invention is directed to 1?,25-dihydroxyvitamin D3 mimics which modulate the vitamin D receptor (VDR). The invention is further directed to pharmaceutical compositions and methods for the treatment, prevention or amelioration of one or more symptoms of disease or disorder related to the activity of the vitamin D receptor using an effective amount of a compound of formula (I).

Raf modulators and methods of use

Granted: December 7, 2010
Patent Number: 7846959
The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X 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 Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat…

P70S6 kinase modulators and method of use

Granted: October 19, 2010
Patent Number: 7816353
Compounds of formula III: wherein R5a, R3, X, Y, Q, R1a and R1b are as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.

Azetidines as MEK inhibitors for the treatment of proliferative diseases

Granted: September 28, 2010
Patent Number: 7803839
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.

MAN2As as modifiers of the IGFR pathway and methods of use

Granted: August 31, 2010
Patent Number: 7785805
Human MAN2A 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 MAN2A are provided.

Tie-2 modulators and methods of use

Granted: July 27, 2010
Patent Number: 7763627
A compound according to Formula IV: or a pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof, wherein R1, R2, R3, R4, R5 and X are as defined in the specification.

Protein kinase modulators and methods of use

Granted: April 27, 2010
Patent Number: 7704995
This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of…

Azepinoindole derivatives as pharmaceutical agents

Granted: September 29, 2009
Patent Number: 7595311
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.

c-Met modulators and methods of use

Granted: August 25, 2009
Patent Number: 7579473
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,…

Human ADAM-10 inhibitors

Granted: March 3, 2009
Patent Number: 7498358
The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to…

Azepinoindole and pyridoindole derivatives as pharmaceutical agents

Granted: February 3, 2009
Patent Number: 7485634
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.

Multi-well apparatus

Granted: August 19, 2008
Patent Number: 7413910
A multi-well assembly (10) comprises a multi-well block (12) and a guide plate (14). The multi-well block (12) has a plurality of wells (18) each with a fluid-impermeable bottom surface (22). The guide plate (14) has a plurality of fluid passageways (34) corresponding to the wells (18) of the multi-well block (12). The guide plate (14) is configured to establish fluid communication between each well (18) and an associated fluid passageway (34) when the guide plate (14) is aligned with…

Identification and characterization of an Anthocyanin mutant () in tomato

Granted: December 4, 2007
Patent Number: 7304207
The present invention is directed to a novel plant phenotype, designated Anthocyanin 1 (ANT1), a nucleic acid sequence expressed in plants demonstrating the ANT1 phenotype and the corresponding amino acid sequence. Also provided are plant cells and plants that exhibit modified ANT1 expression.

Isoquinolinone derivatives and their use as therapeutic agents

Granted: September 4, 2007
Patent Number: 7265131
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.

System for functional gene discovery in plants

Granted: July 31, 2007
Patent Number: 7250553
The invention is directed to a method of multigenerational analysis of plants modified by insertional mutagenesis, and a method for associating plant mutant trait and genotype information. The invention is further directed to a method for managing data pertaining to plant mutant trait and genotype information in a database. The invention is further directed to a system for managing plant mutant trait and genotype information in a database, a system for allowing users to associate plant…

Seed-associated promoter sequences

Granted: February 20, 2007
Patent Number: 7179960
Plant promoters that exhibit seed-associated expression are described, including bi-directional promoters capable of directing seed-associated expression in either orientation.

Presenilin enhancers assays

Granted: October 24, 2006
Patent Number: 7125687
The invention provides methods and compositions relating to pen polypeptides having pen-specific structure and activity, related polynucleotides and modulators of pen function. The invention provides isolated pen hybridization probes and primers capable of specifically hybridizing with natural pen genes, pen-specific binding agents such as specific antibodies, and methods of making and using the subject compositions in diagnosis (e.g. genetic hybridization screens for pen transcripts),…

PRMTs as modifiers of the p53 pathway and methods of use

Granted: May 23, 2006
Patent Number: 7049088
Human PRMT 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 PRMT are provided.