516 results about "Tyrosine kinase" patented technology

The invention relates to talaromyces purpurogenus D2 and application thereof, and belongs to the technical field of microorganisms. The talaromyces purpurogenus D2 disclosed by the invention has the preservation number of GDMCC (Graphics Decific Microorganism Center) NO.66320 The strain is obtained by being separated from soil and domesticated, the zinc tolerance concentration of the strain can reach 2g / L, and the strain can efficiently convert inorganic zinc into organic active zinc which can be easily absorbed and utilized by a human body. The organic zinc prepared from the strain has a remarkable ABTS free radical scavenging capability, and also has tyrosine kinase and 5-alpha reductase inhibition capability; the organic zinc prepared from the talaromyces purpurogenum D2 can be used for preparing zinc-supplementing health-care products, can also be used as cosmetic active matter raw materials with free radical scavenging and whitening effects, and has a wide market application prospect.

The present invention relates to a bispecific antibody comprising a first variable domain that can bind to an extracellular portion of human epidermal growth factor receptor (EGFR) and a second variable domain that can bind to an extracellular portion of human MET prooncogene receptor tyrosine kinase (cMET) for use in a method of treatment of cancer in an individual, the subject has received a previous treatment with i) a third generation EGFR tyrosine kinase inhibitor, or ii) chemotherapy and tyrosine kinase inhibitor, or iii) a cMET tyrosine kinase inhibitor.

The invention relates to a substituted heterocyclic derivative and application thereof. Particularly, the invention relates to a compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition thereof and application of the compound as shown in the general formula (I) or the pharmaceutical composition thereof in preparation of drugs for preventing and / or treating FGFR tyrosine kinase mediated diseases, and substituents in the general formula (I) are as defined in the specification. # imgabs0 #

The present disclosure provides compounds that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Provided herein are combinations for inhibiting tyrosine kinase activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and / or symptomology of the disease.

This disclosure relates to the field of therapeutic tyrosine kinase inhibitors, in particular, Bruton tyrosine kinase (“BTK”) inhibitors, for treatment of patients with MG or MS.

Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The compound and composition above can inhibit wild-type KIT and / or mutant KIT tyrosine kinase activity and treat, prevent, or alleviate diseases, disorders, or conditions associated with wild-type KIT and / or mutant KIT kinase activity.

The invention provides a cyclic compound with a structure as shown in a formula (I) or a pharmaceutically acceptable salt or a stereoisomer or a prodrug molecule of the cyclic compound, and a pharmaceutical composition and application of the cyclic compound or the pharmaceutically acceptable salt or the stereoisomer or the prodrug molecule of the cyclic compound. The compound can be used as a protein kinase inhibitor, has very strong inhibitory activity on FLT3 mutant kinase, has very strong proliferation inhibitory activity on Ba / F3-FLT3-ITD and stable strain cells containing drug-resistant point mutation, can inhibit proliferation, migration and invasion of various tumor cells, and especially can overcome the drug resistance of existing clinical drugs. The cyclic compound provided by the invention can be used for preparing medicines for preventing or treating FLT3 tyrosine kinase mediated diseases (such as hematological malignancies), and can be used for treating various hematological malignancies of human beings and other mammals. # imgabs0 #

A construction and use of an environmentally adaptive co-regulated mRNA nanodelivery system. By incorporating EACR molecules into mRNA nanoparticles, the microenvironment is remodeled to be suitable for robust and sustained mRNA expression, while tissue damage associated with the self-immunogenicity of mRNA drugs is avoided. The nanodelivery system is compatible with ionizable lipid nanoparticles, cationic liposomes, cationic nanoemulsions, and polymeric nanoparticles. The EACR molecules include: anti-inflammatory drugs, tyrosine kinases / adaptors, JAK / STAT and MAPK pathway inhibitors, nutrients and metabolites, membrane transporters / ion channels, phosphodiesterase and cellular stress inhibitors, and natural viral proteins. The therapeutic mRNAs may encode tumor, viral, or bacterial antigens, immunomodulatory factors, therapeutic antibodies, or functional proteins / enzymes, and can play a role in the fields of regenerative medicine, protein supplementation / replacement therapy, targeted gene editing, and immunotherapy.

Disclosed herein are kits and methods for treating pulmonary arterial hypertension (PAH), the method comprising administering to a subject in need thereof: * a therapeutically effective amount of a tyrosine kinase inhibitor or a pharmaceutically acceptable salt thereof; and * a therapeutically effective amount of a dimeric fusion protein comprising: * an extracellular domain of activin type 2A (ACTR IIA) or activin type 2B receptor (ACTR IIB); and an Fc domain of human immunoglobulin G1 (IgG1). In some embodiments, the tyrosine kinase inhibitor is cellatinib or a pharmaceutically acceptable salt thereof, and the fusion protein is sotasercept.

The present invention relates to a substituted heterocyclic derivative and a use thereof. In particular, the present invention relates to a compound as shown in general formula (IA), a preparation method therefor, a pharmaceutical composition thereof, and a use of the compound as shown in general formula (IA) or the pharmaceutical composition thereof in the preparation of prevention and / or treatment of FGFR tyrosine kinase-mediated diseases, each substituent in general formula (IA) being the same as defined in the description.

Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and / or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.

The disclosure provides compositions of a bispecific binding molecule-based degrader that degrades a target protein, such as a protein other than a receptor tyrosine kinase (a non-RTK protein) on a cancer cell, via a lysosomal pathway. The bispecific binding molecule specifically binds to the target protein of interest and to a neuropilin-1 (NRP1). The disclosure also provides methods of using the bispecific binding molecule-based degrader, such as to enhance the therapeutic efficacy of cancer treatment.

The invention relates to a medicinal salt used as a tyrosine kinase inhibitor, a crystal, a preparation method and application thereof, in particular to a medicinal salt of (E)-4-(dimethylamino)-N-(7-(2-ethoxyethoxy ether)-4-((3-ethynyl phenyl) amino)-6-quinazoline)-2-buteneamide, a crystal form and a preparation method thereof. The invention also relates to a pharmaceutical composition containing a therapeutically effective amount of the crystal form and application of the crystal form in cancer treatment.

This disclosure relates to the field of therapeutic tyrosine kinase inhibitors, in particular, Bruton tyrosine kinase (“BTK”) inhibitors, for treatment of patients with multiple sclerosis (MS).

The present invention relates to four-membered fused cyclic compounds and preparation methods and uses thereof, and specifically relates to four-membered fused cyclic compounds, preparation methods thereof and pharmaceutical compositions containing a therapeutically effective amount of the compound, as well as uses thereof as tyrosine kinase inhibitors, especially in the preparation of drugs that inhibit the tyrosine kinase activity of a protein selected from the group consisting of ABL1 protein, ABL2-related proteins and chimeric protein BCR-ABL1.

This disclosure relates to the field of therapeutic tyrosine kinase inhibitors, in particular, Bruton tyrosine kinase ("BTK") inhibitors, for treatment of patients with multiple sclerosis (MS).

This disclosure relates to the field of therapeutic tyrosine kinase inhibitors, in particular, Bruton tyrosine kinase (“BTK”) inhibitors, for treatment of subjects with myelin oligodendrocyte glycoprotein antibody disease (MOGAD).

The present invention discloses a tyrosine kinase inhibitor and its pharmaceutical application. The tyrosine kinase inhibitor of the present invention is a quinazoline derivative with the following structural formula: #imgabs0# The present invention introduces a functional group containing XCH2(CH2)nC=O on the basis of the quinazoline structure, which can easily combine with the cysteine ​​thiol group through a nucleophilic reaction to form a covalent bond, thereby irreversibly inhibiting the activity of tyrosine kinase.

The invention relates to the technical field of molecular probes, and particularly discloses a molecular probe of a targeted tyrosine kinase receptor as well as a preparation method and application of the molecular probe, the molecular probe comprises radioisotope, targeted polypeptide and a chelating group, the targeted polypeptide specifically targets the tyrosine kinase receptor, the chelating group is connected with the targeted polypeptide to form a targeted precursor, and the chelating group is connected with the targeted polypeptide to form the targeted precursor. The radioactive isotope labeled precursor forms a molecular probe, and the sequence of the targeted polypeptide is shown as any one of SEQ ID No.1-8. The targeting polypeptide has good targeting property on a tyrosine kinase receptor coded by an RET gene, can realize specific high uptake in a cell line of NEPC, has relatively good biological safety, can realize accurate imaging aiming at NEPC, and clearly and durably visualizes NEPC tumors in PET imaging; meanwhile, the molecular probe can effectively delay the growth capacity of NEPC, can provide a new treatment choice for NEPC patients, and has good clinical transformation potential.

To provide 5- and 6-azaindole compounds for inhibition of BCR-ABL tyrosine kinases.SOLUTION: The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing the compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML). Provided herein are compounds and compositions that selectively inhibit Bcr-Abl tyrosine kinases and that are useful for treating disorders mediated by Bcr-Abl tyrosine kinases.SELECTED DRAWING: None

A method for treating a subject to reduce the risk of early onset preeclampsia in a pregnant subject determining a level of soluble fms-like tyrosine kinase-1 (sFlt-1) or fragment(s) thereof in a sample that has been isolated from said pregnant subject. The the sample is isolated from a subject before the end of the 12th week of gestation, where the level of sFlt-1 or fragment(s) thereof is indicative of early onset preeclampsia occurring before the end of the 33rd week of gestation. The subject is then treated to decrease the risk of developing, delay the time point of the onset and / or reduce the severity of preeclampsia.

The invention relates to a response type DNA tetrahedral lysosome targeting chimera as well as a construction method and application thereof, and belongs to the technical field of biology. The response type DNA tetrahedron lysosome targeting chimera is obtained by self-assembling a tetrahedron I and a tetrahedron II; a sticky tail end H1 is arranged on the tetrahedron I, and a sticky tail end H2 is arranged on the tetrahedron II; three tyrosine kinase receptor aptamers are anchored on the first tetrahedron, three lysosome shuttle receptor aptamers are anchored on the second tetrahedron, stimuli-responsive factor aptamers are hybridized on the cohesive end H2, and the binding capacity with cells is obviously enhanced based on a trivalent aptamer modification strategy of a tetrahedral framework. According to the present invention, the VEGF is adopted as the stimulation response factor to construct the responsive DNA tetrahedral lysosome targeting chimera, and the responsive DNA tetrahedral lysosome targeting chimera carries the HER2 protein to the lysosome under the mediation of the lysosome shuttle receptor IGF2R so as to degrade, such that the HER2 protein expression on the cell membrane is reduced, and the degradation specificity and the degradation effect are enhanced.

Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

A novel fused pyrimidine based sulfonamide derivative represented by Formula I, a solvate thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition including the same as an active ingredient, and the uses thereof are disclosed. The novel fused pyrimidine based sulfonamide derivative can effectively suppress the growth of cancer cells and resistance to drugs, which are induced by mutations in the tyrosine kinase domain of epidermal growth factor receptors, or the growth of cancer cells having such resistance.

Provided herein are compounds, preferably (R)-N-(4-(chlorodifluoromethoxy) phenyl)-2-(difluoromethyl)-1-(1-hydroxypropan-2-yl)-7-(pyrimidin-5-yl)-1H-benzo[d]imidazole-5-carboxamide having the Formula Ior a pharmaceutically acceptable salt or tautomer thereof, that inhibits tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and / or symptomology of the disease.

The purpose of the present invention is to provide a composition for suppressing muscle atrophy. The present invention relates to a composition for suppressing muscle atrophy, characterized by containing ergothioneine or a salt thereof as an active ingredient.

The invention relates to a sustained release biodegradable ocular implant containing axitinib dispersed in a hydrogel for the treatment of a retinal disease for an extended period of time.