Pyridopyrimidinone inhibitors of PI3K? for the treatment of cancer
Granted: August 21, 2012
Patent Number:
8247408
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.
6-phenylpyrimidinones as PIM modulators
Granted: August 14, 2012
Patent Number:
8242129
A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
Methods of using IGFIR and ABL kinase modulators
Granted: July 17, 2012
Patent Number:
8222256
The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s).
Inhibitors of hedgehog pathway
Granted: July 17, 2012
Patent Number:
8222263
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.
Pyrimidine derivatives as kinase modulators and method of use
Granted: July 3, 2012
Patent Number:
8211929
The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. 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 and/or modulate kinase receptor signal…
c-Met modulators and method of use
Granted: May 15, 2012
Patent Number:
8178532
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,…
Tie-2 modulators and methods of use
Granted: May 15, 2012
Patent Number:
8178570
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.
11 ?-HSD1 modulators
Granted: April 24, 2012
Patent Number:
8163771
A compound according to Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R11, L1 and X are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Marks as modifiers of the p53 pathway and methods of use
Granted: April 10, 2012
Patent Number:
8153384
Human MARK 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 MARK are provided.
Azepinoindole and pyridoindole derivatives as pharmaceutical agents
Granted: March 13, 2012
Patent Number:
8133992
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.
Mylks as modifiers of branching morphogenesis and methods of use
Granted: January 31, 2012
Patent Number:
8105785
Human MYLK genes are identified as modulators of branching morphogenesis, and thus are therapeutic targets for disorders associated with defective branching morphogenesis function. Methods for identifying modulators of branching morphogenesis, comprising screening for agents that modulate the activity of MYLK are provided.
Pyridopyrimidinone inhibitors of PI3K? and mTOR
Granted: January 24, 2012
Patent Number:
8101622
The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.
Pyrimidinones as Casein Kinase II (CK2) modulators
Granted: January 24, 2012
Patent Number:
8101625
A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
JAK-2 modulators and methods of use
Granted: January 3, 2012
Patent Number:
8088767
This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that…
Kinase modulators and methods of use
Granted: December 13, 2011
Patent Number:
8076338
The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 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 p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical…
MAPKs as modifiers of the rac, axin, and beta-catenin pathways and methods of use
Granted: November 29, 2011
Patent Number:
8067180
Human MAPK genes are identified as modulators of the Rac, axin, and beta-catenin pathways, and thus are therapeutic targets for disorders associated with defective Rac, axin, and beta-catenin function. Methods for identifying modulators of Rac, axin, and beta-catenin, comprising screening for agents that modulate the activity of MAPK are provided.
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.
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,…
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.
