Synergistic Effects Between Sphingosine-1-Phosphate Receptor Antagonists and Antimicrotubule Agents
Granted: December 8, 2011
Application Number:
20110301188
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,…
Pyrrole Derivatives As Pharmaceutical Agents
Granted: December 8, 2011
Application Number:
20110301128
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.
Sphingosine-1-Phosphate Receptor Antagonists
Granted: November 24, 2011
Application Number:
20110288076
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 particularly, 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…
1-Phenylpyrrole Derivatives
Granted: October 27, 2011
Application Number:
20110263544
The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; 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 sulfamoyl group or a…
Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases
Granted: October 27, 2011
Application Number:
20110263558
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.
Atropisomers of (Hydroxyalkyl) Pyrrole Derivatives
Granted: October 27, 2011
Application Number:
20110263673
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…
Pyridopyrimidinone Inhibitors of PI3Kalpha
Granted: September 29, 2011
Application Number:
20110237608
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.
Phosphatidylinositol 3-Kinase Inhibitors And Methods Of Their Use
Granted: August 25, 2011
Application Number:
20110207712
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.
CDK Modulators
Granted: August 18, 2011
Application Number:
20110201599
A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.
GFATS As Modifiers of the AXIN Pathway and Methods of Use
Granted: July 7, 2011
Application Number:
20110167505
Human GFAT genes are identified as modulators of the Axin pathway, and thus are therapeutic targets for disorders associated with defective Axin function. Methods for identifying modulators of Axin, comprising screening for agents that modulate the activity of GFAT are provided.
GFATS as Modifiers of the P53 Pathway and Methods of Use
Granted: June 30, 2011
Application Number:
20110159508
Human GFAT 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 GFAT are provided.
Heterocyclic Carboxamide Compounds as Steroid Nuclear Receptors Ligands
Granted: June 16, 2011
Application Number:
20110144128
Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described.
EYA2S As Modifiers of the PTEN/AKT Pathway and Methods of Use
Granted: June 9, 2011
Application Number:
20110135629
Human MPTENAKT genes are identified as modulators of the PTEN/AKT pathway, and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT, comprising screening for agents that modulate the activity of MPTENAKT are provided.
COMBINATION THERAPIES COMPRISING QUINOXALINE INHIBITORS OF P13K-ALPHA FOR USE IN THE TREATMENT OF CANCER
Granted: May 26, 2011
Application Number:
20110123434
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.
KIFS as Modifiers of the RHO Pathway and Methods of Use
Granted: May 12, 2011
Application Number:
20110111402
Human KIF23 genes are identified as modulators of the RHO pathway, and thus are therapeutic targets for disorders associated with defective RHO function. Methods for identifying modulators of RHO, comprising screening for agents that modulate the activity of KIF23 are provided.
C-Met Modulators and Method of Use
Granted: March 31, 2011
Application Number:
20110077233
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,…
Raf Modulators And Methods Of Use
Granted: March 24, 2011
Application Number:
20110071145
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…
PAKs as Modifiers of the CHK Pathway and Methods of Use
Granted: March 10, 2011
Application Number:
20110059066
Human PAK genes are identified as modulators of the CHK pathway, and thus are therapeutic targets for disorders associated with defective CHK function. Methods for identifying modulators of CHK, comprising screening for agents that modulate the activity of PAK are provided.
CSNKS As Modifiers of the RAC Pathway and Methods of Use
Granted: February 10, 2011
Application Number:
20110033853
Human CSNK 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 CSNK are provided.
P70S6 Kinase Modulators and Method of Use
Granted: January 27, 2011
Application Number:
20110021525
The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 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 pathways related to the changes in cellular activities as mentioned…
