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46 results about "Src family" patented technology
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Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
InactiveUS6949544B2Effective inhibitorAvoid cell deathBiocideSenses disorderDiseaseProtein kinase domain
The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Owner:VERTEX PHARMA INC
Bicyclic compounds and their uses as dual c-SRC / JAK inhibitors
Owner:AURIGENE DISCOVERY TECH +1
Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in lung cancer cells
InactiveUS20060019284A1Improved prognosisContinue treatmentMicrobiological testing/measurementTumor/cancer cellsDisease areaProtein-Tyrosine Kinases
The present invention describes polynucleotides that have been discovered to correlate to the relative intrinsic sensitivity or resistance of cells, e.g., lung cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Ephr. These polynucleotides have been shown, through a weighted voting cross validation program, to have utility in predicting the resistance and sensitivity of lung cell lines to the compounds. The expression level of some polynucleotides is regulated by treatment with a particular protein tyrosine kinase inhibitor compound, thus indicating that these polynucleotides are involved in the protein tyrosine kinase signal transduction pathway, e.g., Src tyrosine kinase. Such polynucleotides, whose expression levels correlate highly with drug sensitivity or resistance and which are modulated by treatment with the compounds, comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., lung cancer, in which signaling through the protein tyrosine kinase pathway, such as the Src tyrosine kinase pathway, is involved with the disease process.
Owner:BRISTOL MYERS SQUIBB CO
Small molecule thienopyrimidine-based protein tyrosine kinase inhibitors
InactiveUS20060004002A1BiocideOrganic active ingredientsProtein-Tyrosine KinasesAutoimmune condition
Various thienopyrimidine-based analog compounds are able to selectively inhibit the Src family of tyrosine kinases. These compounds are useful in the treatment of various diseases including hyperproliferative diseases, hematologic diseases, osteoporosis, neurological diseases, autoimmune diseases, allergic / immunological diseases, or viral infections.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
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
GRB2 SH3 binding peptides and methods of isolating and using same
InactiveUS6184205B1Increase ratingsPeptide/protein ingredientsAntibody mimetics/scaffoldsRandom Peptide LibraryADAMTS Proteins
Peptides having general and specific binding affinities for the Src homology region 3 (SH3) domains of proteins are disclosed in the present invention. In particular, SH3 binding peptides have been isolated from phage-displayed random peptide libraries which had been screened for isolates that bind to bacterial fusion proteins having an SH3 domain and glutathione S-transferase (GST). Preferred peptides are disclosed which comprise a core 7-mer sequence (preferably, a consensus motif) and two or more, preferably at least six, additional amino acid residues flanking the core sequence, for a total length of 9, preferably at least 13, amino acid residues and no more than about 45 amino acid residues. Such peptides manifest preferential binding affinities for certain SH3 domains. The preferred peptides exhibit specific binding affinities for the Src-family of proteins. In vitro and in vivo results are presented which demonstrate the biochemical activity of such peptides.
Owner:CYTOGEN CORP +1
Pyrazolyl-ureas as kinase inhibitors
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
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
Method to Treat and Prevent Posterior Capsule Opacification
ActiveUS20080193504A1Prevent proliferationInhibit migrationOrganic active ingredientsSenses disorderPosterior capsular opacificationMedicine
The invention provides a method to treat or prevent posterior capsular opacification. The method comprises administering a therapeutically or prophylactically effective amount of a pharmaceutical composition comprising at least one kinase inhibitor. The kinase inhibitor inhibits p38 kinases, ERK kinases, and / or Src family kinases. The invention also provides an ocular device coated with at least one kinase inhibitor.
Owner:THOMAS JEFFERSON UNIV
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
Inhibition of the Src kinase family pathway as a method of treating HBV infection and hepatocellular carcinoma
InactiveUS20030032596A1Highly specific and efficacious methodImprove efficacyBiocidePeptide/protein ingredientsDiseaseHepatocellular carcinoma
Owner:NEW YORK UNIV MEDICAL CENT
Anti-tumor compound preparation method
InactiveCN101597284AGood curative effectLittle side effectsOrganic chemistryAntineoplastic agentsSide effectTyrosine
The invention provides an anti-tumor compound preparation method, namely, a preparation method of a compound shown in general formula (I) or a salt of same which can be accepted in pharmacology; wherein, R is selected from H, optional substitutional alkyl, optional substitutional cycloalkyl, optional substitutional aryl, optional substitutional aralkyl or optional substitutional heterocyclic radical. The compound shown in the general formula (I) prepared by the invention can inhibit tyrosine kinase Bcr-Abl and other kinases (Lck, Fyn, SrC, Hck) of SRC family after decomposition in vivo so that the compound prepared by the invention shown in the general formula (I) or the salt can be accepted in pharmacology and can be used in the medical application of cancer treatment. Compared with the existing anti-tumor compounds, the compound of the invention has better curative effect and lower side effect.
Owner:BEIJING LABSOLUTIONS PHARMA
NA+K+-ATPase-Specific Peptide Inhibitors/Activators of SRC and SRC Family Kinases
ActiveUS20100056446A1Reduce expressionSilencing expressionPeptide/protein ingredientsHydrolasesATPaseCardiotonic steroid
A method for regulating Src and its downstream signaling pathway which includes binding between Src and Na+ / K+-ATPase is disclosed. The Na+ / K+-ATPase / Src complex is a functional receptor for cardiotonic steroids such as ouabain. Also disclosed are Src inhibitors or activators which include either Na+ / K+-ATPase or Src that interfere with the interaction between the Na / K-ATPase and Src, act via a different mechanism from ATP analogues, and is pathway (Na+ / K+-ATPase) specific.
Owner:UNIVERSITY OF TOLEDO
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
Na+K+-ATPase-specific peptide inhibitors/activators of SRC and SRC family kinases
ActiveUS8283441B2Reduce expressionSilencing expressionPeptide/protein ingredientsHydrolasesATPaseSrc inhibitor
A method for regulating Src and its downstream signaling pathway which includes binding between Src and Na+ / K+-ATPase is disclosed. The Na+ / K+-ATPase / Src complex is a functional receptor for cardiotonic steroids such as ouabain. Also disclosed are Src inhibitors or activators which include either Na+ / K+-ATPase or Src that interfere with the interaction between the Na / K-ATPase and Src, act via a different mechanism from ATP analogues, and is pathway (Na+ / K+-ATPase) specific.
Owner:UNIVERSITY OF TOLEDO
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
Methods of treatment and diagnosis using modulators of virus-induced cellular gene sequences
InactiveUS20070087982A1Reduce expressionReducing and preventing expression of mRNABiocideGenetic material ingredientsDiseaseImmunodeficiency virus
Applicants have used microarrays, gene expression profiling, and gene silencing methods to identify and provide a plurality of ‘validated’ virus-induced cellular gene sequences (e.g., HMG20B, HRH1, NP and c-YES (src family kinases)) and pathways useful as therapeutic targets for modulation of viral-mediated cellular effects. Particular embodiments provide therapeutic compositions, and methods for modulation of viral infection, replication, maturation, progression, or other virally-related conditions or diseases, comprising inhibition of virally-induced gene sequences and gene products. Additional embodiments provide screening assays for compounds useful to modulate viral infection, replication, maturation or progression, or viral-related conditions or diseases. Further embodiments provide diagnostic and / or prognostic assays for viral infection, replication, maturation or progression. Preferably, the viruses all selected from the group consisting of retroviruses (e.g., human immunodeficiency virus (HIV), and viruses of the family Flaviviridae that includes the flaviviruses (e.g., West Nile virus (WNV), Japanese encephalitis virus (JEV), yellow fever virus (YFV) and Dengue fever virus (DEN)), and hepatitis C virus (HCV).
Owner:OREGON HEALTH & SCI UNIV
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
Nck SH3 binding peptides
InactiveUS6432920B1Increase ratingsPeptide/protein ingredientsAntibody mimetics/scaffoldsRandom Peptide LibraryBinding peptide
Peptides having general and specific binding affinities for the Src homology region 3 (SH3) domains of proteins are disclosed in the present invention. In particular, SH3 binding peptides have been isolated from phage-displayed random peptide libraries which had been screened for isolates that bind to bacterial fusion proteins having an SH3 domain and glutathione S-transferase (GST). Preferred peptides are disclosed which comprise a core 7-mer sequence (preferably, a consensus motif) and two or more, preferably at least six, additional amino acid residues flanking the core sequence, for a total length of 9, preferably at least 13, amino acid residues and no more than about 45 amino acid residues. Such peptides manifest preferential binding affinities for certain SH3 domains. The preferred peptides exhibit specific binding affinities for the Src-family of proteins. In vitro and in vivo results are presented which demonstrate the biochemical activity of such peptides.
Owner:CYTOGEN CORP +1
Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells
InactiveUS7537891B2Improved prognosisContinue treatmentSugar derivativesPeptide/protein ingredientsDisease areaProtein-Tyrosine Kinases
The present invention describes polynucleotides that have been discovered to correlate to the relative sensitivity or resistance of cells, e.g., breast cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Eph receptors. These polynucleotides have been shown to have utility in predicting the resistance and sensitivity of breast cell lines to the compounds. Such polynucleotides comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., breast cancer, in which signaling through one or more of the aforementioned Src tyrosine and protein tyrosine kinases is involved with the disease process.
Owner:BRISTOL MYERS SQUIBB CO
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
Method for treating diseases associated with abnormal kinase activity
InactiveUS20060140947A1Effective treatmentReestablishment of transcriptional activityBiocidePeptide/protein ingredientsTyrosineThreonine
Owner:SUPERGEN
Thienopyrimidine-based inhibitors of the src family
Various thienopyrimidine-based analog compounds are able to selectively inhibit the Src family of tyrosine kinases. Compounds of the present invention, capable of such selective inhibition, are of the basic structure seen in formulae (I), (II) or (III):These compounds are useful in the treatment of a wide variety of diseases including hyperproliferative diseases, hematologic allergic / immunological diseases, or viral infections. Methods of synthesis of these compounds and their methods of inhibiting the Src family of tyrosine kinases are presented.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
Construction method for streptomycete expression plasmids and production method for keratinase
InactiveCN102533833AIncrease productionHydrolasesVector-based foreign material introductionAmylaseSrc family kinase
The invention relates to a construction method for streptomycete expression plasmids and a production method for keratinase. The construction method for streptomycete expression plasmids includes the following steps: a promoter Xi of actinoplanes missouriensis xylose isomerase and a terminator of streptomycete avermitilis amylase are sleeved, and the promoter-shine-dalgarno (SD) sequence comes from 90 to 269bp of an actinoplanes missouriensis xylose isomerase gene; a cloned src family kinases (sfks) gene is inserted in a construction expression frame structure of a synthetic Xi promoter-SD-amyA2 terminator fragment, and then a conventional method is used for constructing the streptomycete expression plasmids. The production method for keratinase includes: leading the streptomycete expression plasmids into an expression host of streptomycete lividans TK24 through conjugal transfer, performing recombinant expression and generating the keratinase. Specific activity of a crude enzyme solution is 1700 U / mg after expression of the expression plasmids in the streptomycete lividans TK24 and is improved by 50 times compared with specific activity of starting strain streptomycete fradiae varieties S-221, and yield of the keratinase is much higher than starting strains after the expression.
Owner:SHANGHAI JIAO TONG UNIV
Methods of using EPHA2 for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells
InactiveUS7504211B2Modulate effectImproved prognosisPeptide/protein ingredientsMicrobiological testing/measurementDisease areaProtein-Tyrosine Kinases
The present invention describes polynucleotides that have been discovered to correlate to the relative sensitivity or resistance of cells, e.g., breast cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Eph receptors. These polynucleotides have been shown to have utility in predicting the resistance and sensitivity of breast cell lines to the compounds. Such polynucleotides comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., breast cancer, in which signaling through one or more of the aforementioned Src tyrosine and protein tyrosine kinases is involved with the disease process.
Owner:BRISTOL MYERS SQUIBB CO
Thiazolyl-containing compounds for treating proliferative diseases
ActiveUS20170233411A1Convenient treatmentReduces and avoids symptomOrganic chemistryAntineoplastic agentsBruton's tyrosine kinaseSrc family kinase
The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g., Src family kinases (e.g., hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and / or preventing proliferative diseases (e.g., myelodysplasia, leukemia, lymphoma (e.g., Waldenstrom's macroglobulinemia)) and in inducing apoptosis in a cell (e.g., malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
Owner:DANA FARBER CANCER INST INC
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