Imidazole based LXR modulators
Granted: October 29, 2013
Patent Number:
8569352
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.
Azepinoindole derivatives as pharmaceutical agents
Granted: September 3, 2013
Patent Number:
8524704
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.
Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K alpha
Granted: August 20, 2013
Patent Number:
8513266
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 other cancer treatments. (Formula I)
C-met modulators and method of use
Granted: July 30, 2013
Patent Number:
8497284
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,…
Atropisomers of (hydroxyalkyl) pyrrole derivatives
Granted: July 16, 2013
Patent Number:
8487117
The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy-C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen…
PIK4CA as modifier of the Rac pathway and methods of use
Granted: July 9, 2013
Patent Number:
8481269
Human PIK4CA genes are identified as modulators of the RAC pathway, and thus are therapeutic targets for disorders associated with defective RAC function. Methods for identifying modulators of RAC, comprising screening for agents that modulate the activity of PIK4CA are provided.
Combination therapies comprising quinoxaline inhibitors of P13K-alpha for use in the treatment of cancer
Granted: July 9, 2013
Patent Number:
8481001
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 other cancer treatments.
c-Met modulators and method of use
Granted: July 2, 2013
Patent Number:
8476298
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,…
Azepine derivatives as pharmaceutical agents
Granted: June 18, 2013
Patent Number:
8466143
Compounds, compositions and methods are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the receptors.
Substituted pyrimidine compositions and methods of use
Granted: June 4, 2013
Patent Number:
8455489
Novel compositions and methods of using substituted pyrimidines which have the general formula: (I).
4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use
Granted: May 14, 2013
Patent Number:
8440663
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.
RORS as modifiers of the p21 pathway and methods of use
Granted: April 23, 2013
Patent Number:
8426147
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.
Pyrazolo pyrimidines as casein kinase II (CK2) modulators
Granted: February 12, 2013
Patent Number:
8372851
A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
Pyrrole derivatives as pharmaceutical agents
Granted: February 5, 2013
Patent Number:
8367667
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-kit modulators and methods of use
Granted: January 29, 2013
Patent Number:
8362017
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. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.
Azetidines as MEK inhibitors for the treatment of proliferative diseases
Granted: January 29, 2013
Patent Number:
8362002
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.
Pyrimidinones as casein kinase II (CK2) modulators
Granted: December 4, 2012
Patent Number:
8324231
A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.
PGDS as modifiers of the PTEN pathway and methods of use
Granted: October 16, 2012
Patent Number:
8288119
Human PGD genes are identified as modulators of the PTEN pathway, and thus are therapeutic targets for disorders associated with defective PTEN function. Methods for identifying modulators of PTEN, comprising screening for agents that modulate the activity of PGD are provided.
Marks as modifers of the PTEN pathway and methods of use
Granted: September 25, 2012
Patent Number:
8273536
Human MARK genes are identified as modulators of the PTEN pathway, and thus are therapeutic targets for disorders associated with defective PTEN function. Methods for identifying modulators of PTEN, comprising screening for agents that modulate the activity of MARK are provided.
MAP3Ks as modifiers of the p53 pathway and methods of use
Granted: September 18, 2012
Patent Number:
8268548
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.
