c-Met modulators and methods of use
Granted: November 29, 2011
Patent Number:
8067436
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,…
MELKS as modifiers of the Rac pathway and methods of use
Granted: November 29, 2011
Patent Number:
8067181
Human MELK 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 MELK are provided.
Pyridopyrimidinone inhibitors of PIM-1 and/or PIM-3
Granted: November 8, 2011
Patent Number:
8053454
Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.
Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
Granted: October 25, 2011
Patent Number:
8044062
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.
Pyrrole derivatives as pharmaceutical agents
Granted: September 27, 2011
Patent Number:
8026237
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.
Tropane compounds
Granted: September 6, 2011
Patent Number:
8012956
A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Modulators of LXR
Granted: September 6, 2011
Patent Number:
8013001
Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Tie-2 modulators and methods of use
Granted: September 6, 2011
Patent Number:
8013156
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. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
TAOJIKs as modifiers of the beta-catenin pathway and methods of use
Granted: August 23, 2011
Patent Number:
8003315
Human TAOJIK genes are identified as modulators of the beta-catenin pathway, and thus are therapeutic targets for disorders associated with defective beta-catenin function. Methods for identifying modulators of beta-catenin, comprising screening for agents that modulate the activity of TAOJIK are provided.
LXR and FXR modulators
Granted: August 16, 2011
Patent Number:
7998995
Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Methods of using MEK inhibitors
Granted: August 16, 2011
Patent Number:
7999006
The present invention provides methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.
Modulators of LXR
Granted: August 16, 2011
Patent Number:
7998986
Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.
HPRP4s modifiers of the p53 pathway and methods of use
Granted: August 9, 2011
Patent Number:
7993829
Human hPRP4 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 hPRP4 are provided.
[1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
Granted: August 9, 2011
Patent Number:
7994172
The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction…
Phosphatidylinositol 3-kinase inhibitors and methods of their use
Granted: August 2, 2011
Patent Number:
7989622
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.
c-MET modulators and method of use
Granted: July 12, 2011
Patent Number:
7977345
A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification, compositions thereof, and methods of use thereof.
Benzylthiazolone inhibitors of estrogen-related receptors (ERR)
Granted: July 12, 2011
Patent Number:
7977489
Compounds of the following general structure for use in compositions and methods for modulating the activity of nuclear receptors are provided: The compounds are useable in compositions and methods for modulating the estrogen related receptors and are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?.
Anaplastic lymphoma kinase modulators and methods of use
Granted: July 5, 2011
Patent Number:
7973061
The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate…
Human adam-10 inhibitors
Granted: May 31, 2011
Patent Number:
7951972
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…
C20ORF23 as modifier of the IGFR pathway and methods of use
Granted: May 17, 2011
Patent Number:
7943302
Human C20ORF23 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 C20ORF23 are provided.
