kinase (Total 28237 Patents Found)

The present invention relates to uses of the compounds of Formula I as well as pharmaceutically acceptable salts and stereoisomers thereof in methods to treat a variety of tumors in mammals involving abnormal tyrosine kinase signalling, the compounds represented as: wherein R 1 and R...
Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:...
There is provided compounds of formula I, wherein R1, R 2a , R 2b , R 2c , X, Y, Z, R 3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinas...
The present invention relates to chemical compounds having a general formula I wherein A 1 , A 2 , C 1 , C 2 , D, L 1 , L 2 , Z and R 3 , R 4 , R 6 , R 7 and R 8 are defined herein, which are capable of modulating Auro...
The present invention provides new tyrphostin derivatives acting as protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, and/or which directly or indirectly affect proteins in the PTK-mediated signal transduction pathway, methods of their preparation, pharmaceutical compositions inclu...
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G 1 , R 2 , R 3 , R 4 , R 5 , n, p, q, Ar 1 , and Ar 2 are defined in the description. The presen...
Methods of inhibiting phosphotidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating disease, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not ...
The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer....
Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concent...
PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity....
Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4 H - thieno[3,2- c ]pyrrole-2-(substituted benzyl)pyridazin-3(2 H )-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1 H -quinolin-2-one of formula (II...
The present invention provides a compound of the formula: (Formula I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, par...
The present invention provides novel substituted 2-amino pyrimidine derivatives kinase enzyme inhibitor compounds of formula (1), which may be therapeutically useful kinase inhibitor, more particularly PI3K inhibitors. Formula (1) in which A, R 1 , R 2 R 3 . R 4 , Q and 'n' have the same meanings given in the ...
Described herein are Chk2 -inhibitor compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof....
Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the c...
The present invention relates to a method for determining whether therapy with a p38 MAP kinase inhibitor is potentially beneficial or potentially contraindicated for a subject suffering from a p38-mediated condition comprising measuring in a sample obtained from the subject the presence of at least one chromatin remod...
The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-IR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-IR kinase inhibitor, comprising assessing whether the tumor...
The present invention relates to a method for determining if an individual suffering from chronic myeloid leukemia (CML) is at risk of developing resistance to treatment by a tyrosine kinase inhibitor targeting the BCR-ABL fusion protein or if the individual is likely to respond to treatment by a tyrosine kinase inhibi...
The present invention is directed to a method for preventing or decreasing the incidence of or treating aneurysm or cardiac hypertrophy, comprising administering an effective amount of a rhokinase inhibitor, such as fasudil, to a subject in need thereof....
La présente invention concerne des composés inhibant l'association du facteur de croissance dérivé des plaquettes sanguines et phosphatidylinositol 3-kinase. Cette composition concerne également des compositions pharmaceutiques contenant un composé qui inhibe l'association du facteur de croissance dériv...
L'invention concerne une composition destinée à être utilisée pour gérer le sevrage d'une substance engendrant une dépendance. La composition comprend un ou plusieurs peptides possédant une activité spécifique pour isozyme ε et/ou ? de protéine kinase C (PKC). Le ou les peptide(s) peuvent être admi...
Disclosed are methods and compositions for stimulating cellular nitric oxide (NO) synthesis, cyclic guanosine monophosphate levels (cGMP), and protein kinase G (PKG) activity for purposes of treating diseases mediated by deficiencies in the NO/cGMP/PKG signal transduction pathway, by administration of various compounds...
Efficient sequence specific gene silencing is possible through the use of siRNA technology. By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design...
In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or ...
A transgenic plant transformed by a Lectin-like Protein Kinase Stress-Related Polypeptide (LPKSRP) coding nucleic acid, wherein expression of the nucleic acid sequence in the plant results in increased plant growth and/or increased tolerance to an environmental stress as compared to a wild type variety of the plant. Al...
Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protei...
Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein....
The present invention provides nucleic acid and amino acid sequences that identify and encode a novel human map kinase homolog (SMAP) expressed in cells of the human stomach. The present invention also provides for PCR oligomers or hybridization probes for the detection of nucleotide sequences encoding SMAP or SMAP-lik...
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R 1 , R 2 , Ar 1 and HetAr 2 are as described in the specification....
Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the...
Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from ...