539 results about "Drug development" patented technology

The invention discloses a computer-aided drug screening method, system or device based on FBXO2 and PKM2. The invention provides a brand-new method, system or equipment for screening oral squamous cell carcinoma treatment drugs based on FBXO2 and PKM2, provides a tool for new drug development and clinical application for treatment of oral squamous cell carcinoma, and has a wide application prospect.

The invention relates to the technical field of drug safety evaluation, in particular to a multi-center combined evaluation method and system for drug safety based on a graph neural network and federated learning. Known and unknown drug interaction is systematically predicted based on a drug multi-relation knowledge graph and a graph neural network, a key path of DDI is identified through a graph attention mechanism, a molecular mechanism of the interaction is revealed, and natural language interpretation is generated. And meanwhile, through privacy protection and multi-center cooperation, a federal learning architecture is utilized to break data islands and improve the external effectiveness of an evaluation conclusion on the premise of protecting patient privacy and meeting data compliance requirements. The heterogeneity of data of different mechanisms is effectively evaluated through distribution deviation detection, deviation caused by blind extrapolation is avoided, a real-world evidence methodology report and a data traceability auditing clue are automatically generated, the requirement of a supervision mechanism for real-world evidence quality is met, medicine supervision decision is supported, and medicine research, development and review are accelerated.

The invention discloses bifidobacterium longum B14 with efficient lactose degradation capability and low gas production characteristic and application of the bifidobacterium longum B14, and belongs to the technical field of microorganisms. The preservation number of the bifidobacterium longum B14 is GDMCC No: 67276. The bifidobacterium longum B14 strain provided by the invention can effectively decompose lactose in intestinal tracts, meanwhile, uncomfortable symptoms such as abdominal distension caused by gas production are reduced to the maximum extent, and the technical problem that in the prior art, an efficient lactose degradation strain and the low gas production characteristic are difficult to consider at the same time is successfully solved. The invention provides a core strain resource for developing probiotic products capable of relieving main symptoms of lactose intolerance and remarkably reducing side effects. The strain has a definite application prospect and a remarkable industrial value in development of health care products and medicines.

The present invention discloses a method for preparing a peptide compound with CCK receptor agonistic and / or antagonistic activity. The method uses a sequence of solution-phase reactions to generate high-purity and scalable product without chromatographic purification, suitable for industrial production and pharmaceutical development.

The invention relates to the technical field of gene therapy and drug development, and provides application of a UCH37 inhibitor in preparation of a drug for treating osteoporosis. The expression level of UCH37 in blood of osteoporosis patients is obviously higher than that of UCH37 in blood of healthy people, and the UCH37 is in positive correlation with osteoclast active markers such as NFATC1 and MMP9. The UCH37 inhibitor is applied to preparation of the medicine for treating osteoporosis and directly targets UCH37, the curative effect does not depend on the expression change of ADRM1, no matter the ADRM1 of osteoporosis patients is in a low or high expression state, an osteoclast activation pathway can be stably blocked, the consistency of treatment effects of different individuals is ensured, the range of applicable people of the medicine is expanded, and the application prospect is broad. The compound has the characteristics of clear action mechanism and wide application range, and provides important theoretical basis and conversion prospect for developing novel and efficient medicines for treating osteoporosis.

The invention discloses a 2-amino-4-(5-cyano-1-isopropyl-1H-indole-3-yl) pyrimidine compound and application thereof, the compound has the following structural general formula: in the formula, substituent R is substituted phenyl, the number of substituent groups on the benzene ring of the substituted phenyl is 1-2, and the substituent groups on the benzene ring of the substituted phenyl are 1-2. Substituent groups are respectively and independently selected from nitro, cyano, halogen, carbamoyl, furyl or pyridyl. The 2-amino-4-(5-cyano-1-isopropyl-1H-indole-3-yl) pyrimidine compound designed and synthesized by the invention is a novel efficient NF-kappa B induced kinase (NIK) inhibitor, and is suitable for drug development taking NF-kappa B induced kinase (NIK) as a target spot, and the obtained drug can be used for treating malignant tumors such as leukemia, multiple myeloma and the like.

The application discloses a covalent polypeptide inhibitor targeting protein kinase A, a conjugate, a kit, a pharmaceutical composition and application. The general formula of the covalent polypeptide inhibitor is Z1-Seq-Z2; wherein Seq is an amino acid sequence; the C-terminal of Seq comprises a pseudo-substrate recognition motif recognized by protein kinase A, a non-natural amino acid with a covalent reaction group, and can be covalently crosslinked with a Cys200 residue on a catalytic subunit of protein kinase A; Z1 is selected from hydrogen, an acyl group, a fluorescent group, biotin, an isotopic tag or a biological ortho-reaction group; and Z2 is selected from a hydroxyl group, an amino group, a cell-penetrating peptide or a stabilization modification group. The covalent polypeptide inhibitor can strongly and irreversibly inhibit PKA activity, and can be used as an active probe to specifically label active PKA in a complex biological sample, and is used for biological research and drug development.

This invention relates to the application of β-sitosterol glycoside in the preparation of products for treating lung cancer. This invention creatively provides a new use for the active monomer β-sitosterol glycoside, demonstrating that β-sitosterol glycoside can significantly inhibit the migration ability of lung cancer cells at doses without cell proliferation inhibitors, clarifying the specificity of its anti-metastatic effect, and laying the foundation for further new drug development of this monomer component. Through an in vivo mouse lung metastasis model, this invention demonstrates that β-sitosterol glycoside effectively inhibits the formation of lung metastases while exhibiting no significant toxic side effects in experimental animals, demonstrating high safety, and providing a new candidate molecule for the development of low-toxicity, highly effective anti-lung cancer metastasis drugs.

The application discloses a marine source penicillium and a fermentation method and application thereof. The marine source penicillium is named Penicillium sp. DSF059, and the preservation number is CCTCC NO: M 20232310. Penicilliu The application optimizes the culture condition of the strain, selects a culture medium and culture condition with high yield of antibacterial active compounds to carry out fermentation, so that more target products can be obtained, the operation is simple, the cost is low, and meanwhile, the marine source penicillium Penicilliu Penicillium sp. DSF059 can provide an excellent strain for new drug development of resisting plant pathogenic fungi such as coffee leaf blight, coffee brown spot disease, grape gray mold disease, Chinese cinnamon brown spot disease, citrus black rot disease, pepper late blight, hickory leaf blight, coffee black spot disease and four pathogenic fungi separated from coffee leaf diseases and Staphylococcus aureus, and has a good application prospect for preventing and treating the plant pathogenic fungi and Staphylococcus aureus.

Provided are small-fragment RNA derived from a circular RNA and the use thereof in the treatment of diabetic vascular diseases. The nucleotide sequence of the small-fragment RNA is CUAGCCGAAUGUUAAAAAAU. The provided small-fragment RNA has the effects of well protecting and maintaining the biological functions of vascular endothelial cells, has good structural stability, has a long half-life in vivo, and has the advantages of low effective concentration, high biological safety, etc. The provided small-fragment RNA has good application potentials in the field of clinical nucleic acid drug development, and provides a new idea for the treatment of chronic progressive vascular lesions caused by diabetes.

This invention provides a non-cytotoxic, in vivo compatible proximity labeling method for peroxidases, Hi-APEX, and its applications, belonging to the field of biotechnology. This invention provides a method for labeling interacting proteins, neighboring proteins, and / or neighboring RNA. By introducing TP probes, it completely overcomes the core limitation of peroxidase dependence on H2O2 without sacrificing the original high spatiotemporal resolution. The method provided by this invention exhibits significantly superior technical effects compared to existing technologies in terms of reduced toxicity, enabling in vivo application, precise analysis of redox-sensitive processes, dynamic tracking of protein transport, and simultaneous spatial multi-omics analysis. It provides a powerful tool for life science research and drug development, possessing significant scientific value and broad application prospects.

The application provides an islet-vascular co-culture system based on a microfluidic chip, a building method and application, and the building method of the islet-vascular co-culture system comprises the following steps: S1, preparing microfibers loaded with islets; S2, preparing an assembled chip, the assembled chip comprises a containing cavity, first microchannel networks and second microchannel networks are symmetrically arranged on two sides of the containing cavity, and the first microchannel networks and the second microchannel networks are respectively communicated with a liquid inlet and a liquid outlet at an end away from the containing cavity; S3, controlling the flow of the liquid inlet to be 6-8 muL / min to carry out dynamic culture. The application can simulate the key structure and characteristics of islet tissue, can evaluate a diabetes treatment drug in vitro, can bridge the gap between in vitro and in vivo models, and can provide new tools and methods for the fields of drug development, disease model construction and personalized medical treatment.

The invention belongs to the technical field of crystal form drug molecules, and particularly relates to a baricitinib-trimesic acid eutectic crystal and a preparation method thereof. The baricitinib-trimesic acid eutectic crystal provided by the invention is good in stability and high in solubility, and has improved pharmacokinetics, so that subsequent development requirements of drugs are met; the preparation method is simple to operate, easy to control the crystallization process, good in reproducibility and suitable for industrial production.

The application belongs to the field of chemical medicines, and particularly relates to a quinoline compound, a preparation method and use thereof and a pharmaceutical composition thereof. The application provides a quinoline compound shown in formula I, which has excellent DNA methyltransferase 1 (DNMT1) inhibitory activity and good selectivity, can be used as a novel DNMT1 inhibitor, and provides a new option for drug development and application of diseases driven by DNMT1. Formula I.

The application discloses a kind of miraculin compounds and its extraction method and application, belong to the field of traditional Chinese medicine extraction, specifically related to a kind of miraculin compounds as shown in general formula (I) and (II) isolated from Rhododendron dauricum and the extraction method of the compound, and the compound or the isomer of the compound, or the inhibitory effect of the compound on inflammation in pharmaceutically acceptable salt or pharmaceutical composition comprising the compound can be used for preparing anti-inflammatory drugs.The application further enriches the structural diversity of active substances of Rhododendron dauricum, which lays a foundation for subsequent related biological activity tests of monomeric compounds, provides active lead compounds for new drug development, and also provides a theoretical basis for in-depth research and development of Rhododendron dauricum medicinal materials.

This invention discloses a chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups, with the following structural formula: The preparation includes the following steps: 1. Sequentially adding a metal catalyst, a chiral ligand, a base, indigo-derived trifluoromethylimine ylide, and 3-methylene β-lactam, followed by the addition of an organic solvent to obtain a mixture. The mixture is stirred at a reaction temperature of 0℃ to 50℃. 2. After the reaction is complete, the chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups is obtained through post-processing. The chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups prepared in this application lays a material foundation for in-depth drug activity research based on new drug development.

The invention discloses a photo-induced phase change protein and application thereof. The protein with the phase change function is provided for the first time, and the amino acid sequence of the protein is shown as SEQ ID NO.7; the invention further provides the IDR polypeptide with the phase change function, and the amino acid sequence of the IDR polypeptide is shown as SEQ ID NO.5. The invention also provides an application of the PE1 protein in photo-induced phase transition. The tool has the advantages of being high in space-time precision, good in biocompatibility, capable of integrating physiological signals and the like, can be used for controllable phase separation research, local enrichment, material construction and the like, and has wide prospects in the fields of life science research, drug development and synthetic biology.

The invention discloses application of a TREX1 protein non-substrate DNA binding interface as a target spot in preparation of an immunoregulation medicine, and relates to the technical field of biological medicines. Wherein the TREX1 protein is a human source TREX1 protein, and the non-substrate DNA binding interface comprises threonine at the 49th site of the TREX1 protein, arginine at the 211th site of the TREX1 protein, glutamine at the 213th site of the TREX1 protein and arginine at the 217th site of the TREX1 protein. The non-substrate DNA binding interface in the TREX1 is found for the first time, the key function of the non-substrate DNA binding interface in maintaining immune homeostasis and tumor immune escape is defined through mutation verification and functional analysis, and a new anti-tumor immune strategy with the non-substrate DNA binding interface as a target spot is provided. The discovery not only makes up the blank of TREX1 structure research, but also provides a new theoretical basis and a drug development direction for immune regulation molecule design.

The invention relates to an acid salt of a compound shown as a formula (I), in particular to a hydrochloride of the compound shown as a crystalline form (I) and a preparation method and application of the hydrochloride, and the compound is a PD-1 / PD-L1 inhibitor with the structure of the compound shown as the formula (I). The acid salt of the compound as shown in the formula (I) has improved dissolving capacity in a biological medium, and particularly, the crystalline compound hydrochloride has moderate hygroscopicity, good crystallinity, good solubility and stable physicochemical properties, which all meet the industrial production requirements and meet the development requirements of clinical pharmaceutical preparations. The acid salt or crystalline compound hydrochloride of the compound shown in the formula (I) can be widely applied to preparation of drugs for treating PD-1 / PD-L1 signal channel mediated tumors, immune related diseases and disorders, infectious diseases, infectious diseases or metabolic diseases.

The present application relates to the field of medicine, and particularly to the application of schisantherin B in the preparation of a medicine for preventing or treating radiation damage of the intestinal tract. The present application finds that schisantherin B has a protective effect on the intestinal tract after irradiation, and experiments prove that schisantherin B can reduce the pathological damage degree of the intestinal tract after irradiation, including increasing the length of intestinal villi and the number of crypts, maintaining the stability of the intestinal mucosal barrier, reducing the content of inflammatory factors in the intestinal tissue, restoring the activity of the intestinal epithelial cells after irradiation, and inhibiting the apoptosis. Meanwhile, schisantherin B can reduce the iron death caused by irradiation. Therefore, schisantherin B has a wide application prospect as a potential radiation protection agent in the treatment of radiation-induced intestinal injury and drug development.

The application discloses a NbP2 single-domain antibody, a TAT-NbP2 fusion single-domain antibody and application thereof, and belongs to the technical field of biological medicines. The NbP2 single-domain antibody is composed of a framework region FR and three complementarity determining regions CDR1, CDR2 and CDR3, the amino acid sequence of the CDR1 is shown as SEQ ID NO. 1, the amino acid sequence of the CDR2 is shown as SEQ ID NO. 2, and the amino acid sequence of the CDR3 is shown as SEQ ID NO. 3. The TAT-NbP2 fusion single-domain antibody is a fusion protein of the NbP2 single-domain antibody and a TAT peptide segment of HIV-1 virus. The NbP2 single-domain antibody and the TAT-NbP2 fusion single-domain antibody provided by the application have dual activities of anti-virus and anti-inflammation, are safe, and provide a new idea for treating SARS-CoV-2 infection and developing anti-SARS-CoV-2 drugs.

Among other things, the present disclosure provides technologies for efficient and effective identification of ETaGs, for example, from fungi genomes. In some embodiments, provided technologies are particularly useful for identifying mammalian targets of biosynthetic products of fungi. In some embodiments, provided technologies are particularly useful for identifying and / or prioritizing human targets for drug development. In some embodiments, provided technologies are particularly useful for developing modulators for human targets based on biosynthetic products of fungi.

The invention provides a medicine for treating sepsis-related acute kidney injury, belongs to the technical field of small molecule medicines, and particularly provides a medicine for treating sepsis-related acute kidney injury, which comprises a NOX4 inhibitor. And the NOX4 inhibitor comprises GLX351322 (GLX351322). According to the application, it is clear that the NOX4 level in serum of an S-AKI patient is remarkably increased and is in positive correlation with kidney injury, it is proved that GLX351322 has remarkable treatment and renal function protection effects on acute kidney injury caused by bacterial infection or acute kidney injury caused by lipopolysaccharide exposure, and a new treatment target and a new drug development direction are provided for sepsis-related acute kidney injury.

The invention belongs to the technical field of biological medicine, and discloses a natural product QS-C derived from marine microorganisms and a preparation method and application thereof. The structure of the natural product QS-C is shown as a formula (1), and the natural product QS-C has remarkable anti-hepatic fibrosis activity, improves the pathological morphology of hepatic tissues in a dose-dependent manner, reduces collagen deposition and inhibits expression of key fibrosis markers, and has very excellent application prospects in preparation of anti-hepatic fibrosis drugs and / or health care products. Moreover, the natural product QS-C is separated from metabolites of the marine microorganism talaromyces stipes, industrial production can be realized through large-scale fermentation culture, and the natural product QS-C has a very excellent drug development prospect.

The invention provides a construction method and application of a humanized MECP2 gene mouse model, and relates to the field of gene engineering. The model animal with the humanized hMECP2 gene is successfully prepared, the humanized hMECP2 protein can be normally expressed in the body of the model, and the model can be used for MECP2 gene function research and screening and evaluation of human MECP2 targeted drugs and therapies. The animal model prepared by the invention can be used for rapidly establishing more different MECP2 mutation humanized disease mouse models, and is applied to drug screening, drug effect research, related nervous system disease and tumor treatment and the like aiming at human MECP2 target sites, so that the research and development process of new drugs is accelerated, the time and the cost are saved, and the drug development risk is reduced. And a powerful tool is provided for researching the functions of the MECP2 protein and screening drugs.

The application belongs to the technical field of organic chemical synthesis, and particularly relates to a nitrogen center chiral base derivative, a preparation method and application thereof. The preparation method of the nitrogen center chiral base derivative provided by the application can effectively synthesize a base with only a nitrogen chiral center by using a tetrahydrodibenzo-diazocine compound as a raw material and through chiral phosphoric acid catalyzed amination reaction. Moreover, the synthesis method provided by the application has the advantages of high efficiency, simple steps and strong enantioselectivity, is suitable for industrialized production of chiral bases and derivatives thereof, and provides a new approach for research and application of chiral compounds. Meanwhile, the base derivative prepared by the application is a base molecule with a nitrogen center chirality, and has wide application prospects in the fields of molecular recognition, DNA binding, supramolecular chemistry, material science, asymmetric catalysis and drug development.

This invention relates to the field of animal model construction technology, and more particularly to a method for constructing an SMDT1 gene knockout animal model. The method utilizes gene editing technology to enable the animal model to... SMDT1 The sequence shown in SEQ ID No. 1 is missing from the locus. Stable and reliable results can be obtained using the construction method of this invention. SMDT1 Gene knockout animal models do not exhibit recombination repair and can be stably inherited, making them suitable for research. SMDT1 The biological functions of genes and MCU complexes, and their potential applications in... SMDT1 Gene-targeted drug development and guidance for livestock breeding have broad application prospects.

The invention discloses application of coronavirus SL5 as a target spot in preparation of a medicine for preventing and treating coronavirus infection. The drug target coronavirus SL5 is a No.5 stem loop of a 5 'UTR region of the coronavirus and participates in regulation and control of virus mRNA translation. The invention further discloses seven inhibitors capable of infecting human coronavirus SL5, namely the antisense oligonucleotides specifically targeting SL5 are used for inhibiting coronavirus infection. Experiments prove that the translation level of coronavirus mRNA can be remarkably inhibited by applying the antisense oligonucleotide specifically targeting the coronavirus SL5 in vitro. The coronavirus SL5 provided by the invention can be used as a drug target for screening candidate drugs for inhibiting the translation of coronavirus mRNA, and is of great significance to the development, prevention and treatment of anti-coronavirus drugs in the future.

The invention belongs to the field of traditional Chinese medicine extraction and separation, and particularly relates to a heterocyclic alkaloid compound in purslane as well as an extraction and separation method and application thereof. The molecular formula of the compound is C9H12N4O5, and the chemical name of the compound is 5-(4-hydroxy-3-((hydroxymethyl) amine) isoxazolidin-5-yl)-5H-pyrrolo [3, 4-d] isoxazolidin-4-ol. The structural formula of the compound is shown in the specification, and the structural formula of the compound is shown in the specification. The invention also provides an extraction and separation method of the compound. Ethanol extraction, ODS column chromatography separation, sephadex gel chromatographic column separation and ultra-high performance liquid chromatography are adopted for separation, purification and preparation. The structure of the compound is determined as a new compound by mass spectrum, hydrogen spectrum, carbon spectrum and two-dimensional nuclear magnetic spectrum analysis methods, and the compound has anti-inflammatory, anti-cholinesterase and antioxidant activity. The heterocyclic alkaloid compound and the salt or derivative thereof can be used as raw materials for drug development and pharmacological activity research.

The invention relates to the technical field of traditional Chinese medicine extraction and separation, in particular to two alkaloid compounds in portulaca oleracea and an extraction and separation method and application thereof. The molecular formulas of the two kinds of alkaloid compounds are both C27H33NO15, and the two kinds of alkaloid compounds are respectively named as oleraclamie K and oleraclamie L. The invention further discloses a preparation method of the oleraclamie. According to the method, water extraction, ODS column chromatography, Sephadex LH-20, a high performance liquid chromatograph and the like are adopted for separation, purification and preparation, the compounds oleraclamie K and oleraclamie L are successfully extracted and separated out, the method is simple, convenient and rapid, the extraction and separation process mainly adopts a water extraction process, the method is environmentally friendly, the purity of the compounds separated through the method is high and larger than 90%, and the method is suitable for industrial production. In addition, researches show that the two compounds have anti-inflammatory effects, so that the alkaloid compound and the salt and the derivative thereof can be used as synthesis primers of other compounds and raw materials for new drug development and pharmacological activity research, and can also be used for preparing anti-inflammatory drugs.