279 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 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.

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.

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.

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 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 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.

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.

The present application relates to the field of biological medicine and modernization of traditional Chinese medicine, and particularly relates to a therapeutic target, an inhibitor and a traditional Chinese medicine composition for treating ovarian hypofunction caused by oxidative stress and application thereof. The present application first determines SRC tyrosine kinase as a key drug target for preventing and treating the disease. The application of the SRC tyrosine kinase inhibitor (such as secaitinib) in preparing related drugs is provided, which can alleviate the damage of ovarian granulosa cells by inhibiting the SRC activity, down-regulating the expression of antioxidant enzyme related genes and reducing the level of active oxygen. Meanwhile, the present application provides a traditional Chinese medicine composition composed of mulberry, kudzu root, tuckahoe and medlar. The composition can improve the hormone level, enhance the antioxidant capacity, improve the ovarian function and fertility by inhibiting the SRC tyrosine kinase activity and the SRC-RAF1-MEK-ERK signal pathway. The present application provides a new solution for the targeted treatment of ovarian hypofunction and the modernization of traditional Chinese medicine.

Two major treatment strategies employed in fighting non-small cell lung cancer (NSCLC) are tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors (ICIs). The choice of strategy is based on heterogeneous biomarkers expressed by the lung tumor tissue. A major challenge for molecular testing of these biomarkers is the insufficiency of biopsy specimens from patients with advanced NSCLC. Disclosed herein is a method for predicting a response to immune-checkpoint blockade immunotherapy. The method generally involves imaging the subject with positron emission tomography with 2-deoxy-2-[fluorine-18] fluoro-D-glucose integrated with computed tomography to produce 18F-FDG PET / CT images of the tumor, analyzing the images using PET, CT, and Kulbek Leibler Divergence statistical (KLD) features or, alternatively using deep leaning such as Neural Networks; generating a radiomic signature from the identified features or Network characteristics; and computing a radiomic score based on the radiomic signature that is predictive of responsiveness to ICIs or TKIs.

The present application provides a method of treating cancer in an individual, the method comprising administering to the individual a tyrosine kinase inhibitor and an inflammatory agent (such as a TLR agonist, a STING activator, radiation therapy, or an immune checkpoint inhibitor). In some cases, the method involves administering the tyrosine kinase inhibitor when the individual is under inflammatory conditions. In one aspect, the present application provides a method of treating cancer in an individual, the method comprising administering to the individual a) a tyrosine kinase inhibitor and b) an inflammatory agent, optionally comprising intermittently administering the tyrosine kinase inhibitor to the individual.

Provided herein are compositions, methods, and uses involving bispecific binding molecules that specifically bind to HER2, a receptor tyrosine kinase, and to CD3, a T cell receptor, and mediate T cell cytotoxicity for managing and treating disorders, such as cancer. Also provided herein are uses and methods for managing and treating HER2-related cancers.

Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

The present invention discloses an aromatic amine compound and its application. The aromatic amine compound can effectively inhibit the tyrosine kinase activity of Abelson protein (ABL1), Abelson-associated protein (ABL2) and related chimeric proteins, especially BCR-ABL1. The aromatic amine compound can be used to prepare inhibitors of Abelson protein (ABL1), Abelson-associated protein (ABL2) and related chimeric proteins, and can be used as a drug for treating diseases related to abnormal activity of BCR-ABL1 fusion protein.

In one aspect, a novel method that allows for evaluation of an RTK activity is provided. Provided is a method for evaluating an RTK activity, the method including: a step (A1) for determining diffusion dynamics A1 of the RTK by contacting a target substance with a cell that expresses a labeled RTK on a cell membrane, a step (B1) for determining diffusion dynamics B1 of the RTK by contacting the target substance and a ligand that activates the RTK with the cell that expresses the labeled RTK on a cell membrane, a step (C1) for calculating a ratio of the diffusion dynamics A1 of the RTK obtained at the step (A1) and the diffusion dynamics B1 of the RTK obtained at the step (B1), and a step (D1) for evaluating an effect of the target substance on an RTK activity by comparing the ratio of the diffusion dynamics obtained at the step (C1) with a threshold; and at the step (D1), when the ratio of the diffusion dynamics obtained at the step (C1) is equal to or greater than the threshold, it can indicate that the target substance has an effect on a molecular function of the RTK.

The present invention provides novel human fms related tyrosine kinase 3 (FLT3) antigen binding proteins, such as antibodies, having improved FLT3 binding affinity, and / or anti-tumor activity. The FLT3 antibodies of the invention were generated by mutation of a parent FLT3 antibody and tested in in vitro in binding assays as well as in vivo in a mouse tumor model and in human patient tumor samples. The antibodies of the invention are provided as monospecific constructs or in a bispecific FLT3xCD3 antibody format and show excellent target affinity and / or tumor cell killing. The present invention also relates methods for producing the antigen binding proteins of the invention as well as nucleic acids encoding them, vectors for and host cells for their expression. The invention further relates to methods of treating or diagnosing a disease such as leukemia using an FLT3 antigen binding protein (ABP) of the invention.

The present disclosure relates to compounds and compositions for inhibiting Bcr-Abl tyrosine kinase, methods for preparing the compounds and compositions, and the use of the compounds and compositions in treating various cancers such as chronic myeloid leukemia (CML).

The present application relates to a kind of polymorphs of FGFR4 protein kinase inhibitor and its preparation method.N-(2-(4-cyclopropylpiperazine-1-yl)-5-(4-(2,6-dichloro-3,5-dimethoxyphenyl)imidazo [1,2-a][1,6] naphthyridin-8-yl)-4-methoxyphenyl) acrylamide is a kind of FGFR4 protein kinase inhibitor, it can high selectivity inhibit FGFR4 tyrosine kinase, and the inhibitory effect of FGFR1-3 is weak, so it can safely, effectively treat the liver cancer patient of FGFR4 high expression.

The invention relates to the field of radiotherapy and, more particularly, to the use of a compound based on FMS-like tyrosine kinase 3 ligand (FLT3L) and adoptive cell therapy using dendritic cells in the prevention of cognitive damage associated with radiotherapy.