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74results about How to "Inhibitor used" patented technology
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Compounds useful as inhibitors of atr kinase
InactiveUS20120027874A1Surprising synergyInhibitor usedOrganic active ingredientsHeavy metal active ingredientsDiseasePyrazine
The present invention relates to pyrazine and 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 I:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC
Compounds useful as inhibitors of atr kinase
ActiveUS20130034616A1Surprising synergyInhibitor usedBiocideHeavy metal active ingredientsPyrroleComparative evaluation
The present invention relates to pyrrolopyrazines 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.
Owner:VERTEX PHARMA INC
Compounds useful as inhibitors of atr kinase
InactiveUS20120178756A1Surprising synergyInhibitor usedOrganic active ingredientsOrganic chemistryDiseasePyrazine
Owner:VERTEX PHARMA INC
Non-nucleoside reverse transcriptase inhibitors
InactiveUS20070088053A1Reduction in susceptibilityInhibitor usedBiocideOrganic chemistryCompound (substance)Human immunodeficiency virus (HIV)
Owner:ROCHE PALO ALTO LLC
Method for Expanding Monocytes
ActiveUS20100003272A1Extended half-lifeImprove stabilityAntibacterial agentsPeptide/protein ingredientsDendritic cellAgonist
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Thienopyrimidines useful as modulators of ion channels
The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Owner:VERTEX PHARMA INC
Indole compound and use thereof
InactiveUS7728023B2Increased airway hyperreactivityImprove respiratory functionBiocideSenses disorderClinical trialObstructive Pulmonary Diseases
Owner:ONO PHARMA CO LTD
VEGFR-3 inhibitor materials and methods
InactiveUS7611711B2Extended shelf lifeImprove stabilityImmunoglobulinsCyclic peptide ingredientsDiseaseLymphatic vessel
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.
Owner:VEGENICS PTY LTD
Indole Compound and Use Thereof
InactiveUS20080188532A1Increased airway hyperreactivityImprove respiratory functionBiocideSenses disorderDiseaseBronchial epithelium
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.
Owner:ONO PHARMA CO LTD
Benzimidazoles useful as modulators of ion channels
InactiveUS20050209282A1Inhibitor usedReduce severityAntibacterial agentsBiocideMedicinal chemistryIon channel
Owner:VERTEX PHARMA INC
Aminopyrazines as ATR kinase inhibitors
InactiveUS8877759B2Surprising synergyInhibitor usedHeavy metal active ingredientsOrganic chemistryDiseaseKinase inhibition
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.
Owner:VERTEX PHARMA INC
Compounds useful as inhibitors of ATR kinase
ActiveUS9096584B2Surprising synergyInhibitor usedBiocideHeavy metal active ingredientsDiseasePyridine
Owner:VERTEX PHARMA INC
Ion channel modulators and methods of use
ActiveUS20060160817A1Inhibitor usedReduce severityBiocideOrganic active ingredientsIon channel modulationCombinatorial chemistry
Owner:VERTEX PHARMA INC
Compounds useful as inhibitors of atr kinase
ActiveUS20150031661A1Surprising synergyInhibitor usedBiocideGroup 5/15 element organic compoundsDiseasePyrazine
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.
Owner:VERTEX PHARMA INC
Methods and pharmaceutical compositions for the treatment of th2 mediated diseases
InactiveUS20150038496A1Extended half-lifeImprove stabilityCompound screeningSenses disorderDiseaseAllergic asthma
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2
Condensed ring compound and use thereof
InactiveUS20060194797A1Increased airway hyperreactivityImprove respiratory functionBiocideOrganic chemistryNasal inflammationARDs - Acute respiratory distress syndrome
The present invention relates to a compound of formula (I) (wherein all symbols have the same meanings as described hereinbefore). The compound antagonizes cysLT2 and therefore, it is useful as an agent for the prevention and / or treatment of respiratory diseases such as bronchial asthma, bronchial asthma, chronic obstructive pulmonary disease, pneumonectasia, chronic bronchitis, pneumonia (e.g. interstitial pneumonitis etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), and the like, or as an expectorant or antitussives.
Owner:ONO PHARMA
Methods for preparing accessory cells and uses thereof for preparing activated nk cells
InactiveUS20140050710A1Improve efficiencyReduce expressionBiocideGenetically modified cellsBiologyCancer treatment
The present invention relates to a method for preparing accessory cells, said accessory cells may themselves be used for preparing activated NK cells that may be used in various therapeutic protocols (e.g. cancer treatment). More particularly, the present invention relates to a method for preparing an accessory cell comprising the steps consisting of i) providing a cell and ii) inhibiting in said cell the expression of a gene encoding for a Killer-Cell Immunoglobulin-like Receptor(s) (KIR) ligand.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2
Selective inhibitors of cb2 receptor expression and/or activity for the treatment of obesity and obesity-related disorders
InactiveUS20100056758A1Decrease constitutive levelBiological activity is prevented and reducedBiocideNervous disorderDiseaseObesity
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Methods and pharmaceutical compositions (ctps 1 inhibitors, e.g. norleucine) for inhibiting t cell proliferation in a subject in need thereof
InactiveUS20160051674A1Prevent proliferationReducing and inhibiting cell proliferationLibrary screeningAntibody ingredientsDrugT cell
The present invention relates to methods and pharmaceutical compositions for inhibiting lymphocyte proliferationin a subject in need thereof. In particular, the invention relates to a CTP synthase 1 (CTPS1) inhibitor for use in a method for inhibiting lymphocyte proliferationin a subject in need thereof. The invention also relates to a method for screening a plurality of test substances useful for inhibiting lymphocyte proliferationin a subject in need thereof comprising the steps consisting of i) testing each of the test substances for its ability to inhibit CTPS1 activity or expression and ii) identifying the test substance which inhibits CTPS1 activity or expression thereby to identify a test substance useful for inhibiting lymphocyte proliferationin a subject in need thereof.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +4
Non human animal models for increased retinal vascular permeability
InactiveUS20120142609A1Increased retinal vascular permeabilityIncrease vascular permeabilitySenses disorderPeptide/protein ingredientsRetinaBlood vessel
The present invention relates to a non human animal model for increased retinal vascular permeability wherein said increased retinal vascular permeability is induced by inhibiting in Müller cells of said animal the expression of a gene encoding for Dp71 or a dystrophin associated protein (DAP). Furthermore, the present invention relates to methods and compositions for the treatment of a disease associated with an increased retinal vascular permeability in a subject in need thereof.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Methods and Pharmaceutical Composition for Modulation Polarization and Activation of Macrophages
InactiveUS20180125876A1Suitable for treatmentReduces and abolishes and activityOrganic active ingredientsPeptide/protein ingredientsM2 polarizationP2Y2 Receptors
The present invention relates to methods and pharmaceutical composition for modulation polarization and activation of macrophages. In particular, the present invention relates to methods for modulating macrophage M1 / M2 polarization in a subject in need thereof comprising administering to the subject a therapeutically effective amount of P2Y2 receptor agonists or antagonists.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +3
Method and composition for treating osteoporosis
This invention relates to a novel class of acidic amino acid / dicarboxylic acid derivatives (sulfonic acid / sulfate derivatives of naturally occurring amino acids and their amides) useful as inhibitors of osteoclastogenesis. The invention also provides methods of using the novel class of acidic amino acid / dicarboxylic acid derivatives of the general formula ZOC—(CRR)m—COOH, wherein: m=2, 3 or 4; Z is OH or NH2; one R in the compound is from the group consisting of SO3H, OSO3H, CH2—SO3H, CH2—OSO3H, and NHSO3H, and the remaining Rs are H or NH2, for inhibition of osteoclastogenesis.
Owner:COUNCIL OF SCI & IND RES
Potassium-dependent sodium-calcium exchanger
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.
Owner:ASTELLAS PHARMA INC
Methods and compositions for the preservationof organs
InactiveUS20190183114A1Extended half-lifeImprove stabilityDead animal preservationDNA/RNA fragmentationOrgan ViabilityRNase activity
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2
Method of treatment of gut inflammatory diseases such as inflammatory bowel diseases (IBD) or irritable bowel syndrome (IBS)
ActiveUS20190177433A1Reduced activityImproved prognosisCompound screeningApoptosis detectionControl cellTreatment field
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2
Methods and pharmaceutical compostions for treating rhabdomyolysis
ActiveUS20180325890A1High affinityStrong specificityOrganic active ingredientsMuscular disorderSkeletal muscle damageRhabdomyolysis
Owner:UNIVERSITÉ PARIS CITÉ +4
Methods and pharmaceutical compositions for the treatment of hypertension
ActiveUS9212361B2Avoid difficult choicesHigh affinityOrganic active ingredientsGenetic material ingredientsGelatinaseNGAL Protein
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.
Owner:UNIVERSITÉ PARIS CITÉ +1
Method for Expanding Monocytes
ActiveUS20120122207A1Extended half-lifeImprove stabilityAntibacterial agentsPeptide/protein ingredientsDendritic cellAgonist
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Methods of diagnosing and treating cancer
InactiveUS20180231556A1Keep for a long timeShort survival timeMicrobiological testing/measurementBiological material analysisOncologyBreast cancer
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +1
Method for the treatment of cardiovascular fibrosis
InactiveUS9594083B2Avoid difficult choicesHigh affinityCompound screeningOrganic active ingredientsVascular fibrosisGelatinase
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.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +4
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