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48 results about "Syk kinase" patented technology
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Syk is a nonreceptor protein tyrosine kinase that is involved in signal transduction in immune cells bearing Fcγ-activating receptors, including macrophages, mast cells, B cells, neutrophils and synoviocytes.
Kinase inhibitors
InactiveUS20140057915A1Weak affinityImproved profileBiocideOrganic active ingredientsTyrosineP38 Mitogen Activated Protein Kinase
There are provided compounds of formula I,wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:RESPIVERT +1
Pyrazole derivatives as p38 MAP inhibitors
InactiveUS9249125B2Weak affinityImproved profileSenses disorderOrganic chemistryUveitisUlcerative colitis
Compounds of formula (I):wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
Owner:RESPIVERT +1
1,6 naphthridines useful as inhibitors of syk kinase
Disclosed are compounds of formula (I):wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Owner:BOEHRINGER INGELHEIM PHARMA INC
Pyrazine kinase inhibitors
Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARM INC
Kinase inhibitors
InactiveUS20150166483A1Maintain good propertiesSenses disorderOrganic chemistryMedicineP38 Mitogen Activated Protein Kinase
There is provided a compound of formula I,which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:RESPIVERT +1
Pyrazole derivatives as p38 map inhibitors
InactiveUS20150203475A1Weak affinityImproved profileBiocideOrganic active ingredientsUveitisUlcerative colitis
Compounds of formula (I):wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
Owner:RESPIVERT +1
Kinase inhibitors
ActiveUS20160340375A1Good anti-inflammatory propertyMaintain good propertiesGroup 4/14 element organic compoundsAntipyreticMedicineTyrosine
There are provided compounds of formula I.wherein R1 to R5, X1, X2, Ar, L, A, A1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
Kinase inhibitors
ActiveUS20160340343A1Maintain good propertiesOrganic active ingredientsGroup 4/14 element organic compoundsDiseaseTyrosine
There are provided compounds of formula I,wherein R1 to R5, X1, X2, Ar, L, E, A, A1, G and G1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
Kinase inhibitors
ActiveUS20160318909A1Weak affinityImproved profileOrganic active ingredientsAntipyreticTyrosineP38 Mitogen Activated Protein Kinase
There are provided compounds of formula I,wherein:Y represents NR2R3;one of R2 and R3 represents —[C2-4 alkylene-O]1-12—[C2-4 alkylene]-R2a and the other of R2 andR3 has a meaning given in the description; andR, R1, R2a, Ra, Rb, Q, X and Y have meanings given in the description,which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
2, 6-diamino- pyrimidin- 5-yl-carboxamides as SYK or JAK kinases inhibitors
The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods ofinhibilion the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as cardiovascular disease, inflammatory disease and autoimmune disease and cell proliferative disorder. Formula (I) Y1 is selected from the group consisting of: (a) and (b); Z is O or S; D1 is selected from the group consisting of: (a) phenyl substituted with a group, R5 (b) naphthyl (c) C3-8cycloalkyl (d) heteroaryl (e) heterocyclyl.
Owner:PORTOLA PHARMA INC
Combination therapy with syk kinase inhibitor
The invention encompasses methods of increasing platelet levels in a patient having or at risk for immune thrombocytopenia comprising co-administering a Syk kinase inhibitor and a thrombopoietin receptor agonist, and methods of treating thrombocytopenia comprising co-administering a Syk kinase inhibitor and a thrombopoietin receptor agonist to a patient in need thereof, as well as pharmaceutical compositions for use in these methods.
Owner:RIGEL PHARMA
Kinase inhibitor
There is provided a compound of formula I,which compound has anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
Inhibitors of syk and JAK protein kinases
The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
Owner:ALEXION PHARMA INC
Pyrazolyl-ureas as kinase inhibitors
ActiveUS9701670B2Weak affinityImproved profileSenses disorderOrganic active ingredientsDiseaseTyrosine
There are provided compounds of formula I,wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
Selective kinase inhibitors
Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARMA INC
Substituted pyrazine-2-carboxamide kinase inhibitors
Provided are substituted pyrazine-2-carboxamide compounds of Formula I:useful for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARMA INC
Urea derivatives useful as kinase inhibitors
ActiveUS9890185B2Good anti-inflammatory propertyMaintain good propertiesSenses disorderAntipyreticUrea derivativesMedicine
There are provided compounds of formula I, wherein R1, R1A, R1C to R1E, Ra, Rb, X1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
Kinase inhibitor
There is provided a compound of formula VIIa,wherein Qx represents —C(O)O—C1-4 alkyl, or a salt or protected derivative thereof, and other compounds that are useful in the preparation of compounds that have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:OXULAR ACQUISITIONS LTD
1,2,4-triazine-6-carboxamide kinase inhibitors
Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARMA INC
Pyrazine Kinase Inhibitors
Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARMA INC
New Signaling Molecule Involved in Ultraviolet Damage to Skin
The present invention includes a method of detecting ultraviolet radiation (UVR)-induced skin damage in a mammal. The present invention also includes a method of identifying a mammal at risk of developing U VR-induced skin damage, photoaging, or photocarcinogenesis. The present invention further includes a method of inhibiting UVR-induced skin damage in a mammal at risk of developing U VR-induced skin damage. The present invention also includes a method of reducing the level of Syk kinase in the skin of a mammal. The present invention further includes methods of treating or diagnosing a disease associated with a change of Syk kinase expression in the skin in a mammal.
Owner:DREXEL UNIV
Benzamides and nicotinamides as Syk modulators
The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
Owner:ALEXION PHARMA INC
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and / or prevent diseases associated with inappropriate kinase activity. The compounds of the present invention are according to structural formula (I):or a salt or N-oxide thereof, whereinB is selected from
Owner:RIGEL PHARMA
Benzamides and nicotinamides as syk modulators
The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
Owner:ALEXION PHARMA INC
1,6 naphthyridines useful as inhibitors of SYK kinase
Disclosed are compounds of formula (I):wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Owner:BOEHRINGER INGELHEIM PHARMA INC
Method for sustaining enos activity
The present invention is directed to methods for sustaining eNOS activity to inhibit platelet aggregation, clot retraction, and enhance fibrinolysis. One embodiment of the invention provides methods of treating thrombosis by inhibiting the activity of the syk kinase. Another embodiment provides assays for the discovery of improved compounds to treat thrombosis, by screening for compounds which sustain eNOS activity. Yet another embodiment provides assays for the discovery of improved compounds to treat thrombosis, by identifying inhibitors of calpain and IIbIIIa by screening for compounds which act through calpain or IIbIIIa to sustain eNOS activity. Yet another embodiment provides for enhancing fibrinolysis, by inhibiting the activity of the syk kinase or calpain.
Owner:SARKAR SIBAJI
Syk kinase inhibitors as treatment for malaria
The disclosure relates to methods, compositions, and kits for treatment of parasite-mediated disease. In one embodiment, the disclosure relates to compounds, compositions, methods and kits for the treatment of malaria. In still another embodiment, the disclosure relates to a method for treating malaria comprising the use of a Syk kinase inhibitor.
Owner:PURDUE RES FOUND INC
Substituted pyrimidinyl kinase inhibitors
Owner:ALEXION PHARMA INC
Substituted picolinamide kinase inhibitors
Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Owner:ALEXION PHARMA INC
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