74results about How to "Inhibitor used" patented technology

The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1-R4 and Ar are as herein defined. Also disclosed in the present invention are methods of treating an HIV-1 infection with compounds defined herein and pharmaceutical compositions containing said compounds.

The invention relates to an ex vivo method for expanding monocytes, macrophages or dendritic cells, which method comprises inhibiting the expression or the activity of MafB and c-Maf in monocytes, macrophages or dendritic cells; and expanding the cells in the presence of at least one cytokine or an agonist of cytokine receptor signaling.

The present invention relates to a compound represented by the formula (I),wherein all symbols are as defined in the description,a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and / or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.

The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated by VEGFR-3 ligands VEGF-C and VEGF-D. More particularly, the present invention identifies novel methods and compositions for the inhibition of VEGF-C / D binding to VEGFR-3. The compositions of the present invention will be useful in the inhibition of angiogenesis and lymphangiogenesis.

The present invention relates to a compound represented by the formula (I),wherein all symbols are as defined in the description,a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and / or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.

The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.

The present invention relates to pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula III:wherein the variables are as defined herein.

The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.

The present invention relates to methods and pharmaceutical composition for the treatment of T-helper type 2 (Th2)-mediated diseases. More particularly, the present invention relates to an inhibitor of the Suv39h1-HP1a silencing pathway for use in the treatment of a T-helper type 2 (Th2)-mediated disease, in particular allergic asthma.

A novel polypeptide, a polynucleotide encoding the polypeptide, an expression vector comprising the polynucleotide, a cell transfected by the expression vector, a method for producing the polypeptide, and a convenient screening system for obtaining a substance useful in treating cell injuries due to postischemic reperfusion or an inflammatory disease, are disclosed.The polypeptide is a potassium-dependent sodium-calcium exchanger expressed in peripheral leukocytes.

The present invention relates to methods and compositions for the preservation of organs. The inventors showed that therapeutic intervention during cold ischemia could significantly alter outcome, suggesting active mechanisms taking place. More particularly, the inventors demonstrated that Unfolded Protein Response could be a critical pathway underlying the relationship between cold ischemia time and graft outcome, highlighting the potential for UPR-based therapeutics to improve transplantation efficiency. In particular, the present invention relates to an activator of PERK-ATF4 pathway, an inhibitor of the ATF6 pathway and an inhibitor of the RNase activity of IRE1α for use in the maintain of organ viability during cold ischemia.

The invention is in the field of therapy of gut inflammatory diseases such as Inflammatory Bowel Diseases (IBD) or Irritable Bowel Syndrome (IBS) including Gluten hypersensitivity. The inventors showed that ELA2A secreted by epithelial cells in the extracellular space is over-expressed in IBD conditions degrading tight junction proteins and controlling cytokines expression. Overexpression of ELA2A conferred a pro-inflammatory phenotype both in cell expression systems and in vivo in animal model of IBD. The inventors also showed that ELA2 over-expressing intestinal epithelial cells increase the release of CXCL8 protein compared to control cells. The increased CXCL-8 protein release observed in cells overexpressing ELA2A is inhibited by ELAFIN addition to the culture, in a dose-dependent manner. In particular, the invention relates to inhibitors of Elastase ELA2A, for use in the treatment of Inflammatory Bowel Diseases, such as Crohn's Disease, Ulcerative Colitis, Celiac disease, and Pouchitis.

The present invention relates to an inhibitor of Neutrophil Gelatinase-Associated Lipocalin (NGAL) activity or expression for use in a method for treating or preventing hypertension in a subject in need thereof.

The invention relates to an ex vivo method for expanding monocytes, macrophages or dendritic cells, which method comprises inhibiting the expression or the activity of MafB and c-Maf in monocytes, macrophages or dendritic cells; and expanding the cells in the presence of at least one cytokine or an agonist of cytokine receptor signaling.

The present invention relates to methods for the diagnosis and the treatment of cancer, in particular breast cancer. In particular, the present invention relates to a method of diagnosing cancer in a subject comprising the steps of i) determining the expression level of 11βHSD1 and / or 11βHSD2 in a sample obtained from the subject, ii) comparing the expression level determined at step i) with its predetermined reference value and ii) concluding that the subject suffers from a cancer when the expression level of 11βHSD1 is lower than its predetermined reference value or when the expression level of 11βHSD2 is higher than its predetermined reference value.

The present invention relates to methods and pharmaceutical compositions for the treatment of cardiovascular fibrosis. In particular, the present invention relates to an inhibitor of Neutrophil Gelatinase-Associated Lipocalin (NGAL) activity or expression for use in a method for treating or preventing cardiovascular fibrosis in a subject in need thereof.