115 results about "Drug candidate" patented technology

A device may include a data acquisition layer comprising a patient information collector and a drug information collector, each operable to ingest patient-specific clinical data and drug-specific data, respectively. A device may include an analysis engine comprising a multi-criteria ranking engine configured to compute composite suitability score for candidate medications by weighting one or more of medication efficacy, medication safety, medication resistance, medication cost, or patient-specific coverage factors. A device may include a presentation layer comprising a summary dashboard configured to display a ranked medication recommendation set produced by the analysis engine.

The application discloses medical use of gelated cells loaded with sulfonated chitosan in treatment of atherosclerosis, and belongs to the technical field of biological medicine. The gelated cells loaded with sulfonated chitosan take macrophages as host cells, and intracellular cross-linking forms a photocrosslinking hydrogel network composed of methacrylated hyaluronic acid and sulfonated chitosan. The gelated cells completely retain cell membrane structure and membrane surface protein expression, lose the proliferation ability, and have excellent blood lipid selective adsorption capacity and foam cell lipid metabolism regulation capacity. In-vivo and in-vitro experiments prove that the gelated cells can significantly reduce blood lipid levels of atherosclerosis model animals, reduce aortic plaque area, and have good biological safety, thereby providing a new strategy and candidate drug for prevention and treatment of atherosclerosis, and having a good clinical application prospect.

The application discloses a dehydrocostus lactone derivative, a preparation method and medical application thereof, and belongs to the technical field of chemical synthesis. The dehydrocostus lactone derivative is shown as a general formula I. The compound has certain inhibiting effect on HBsAg and HBeAg, can be used for preparing anti-HBV drugs, and provides more efficient and safe candidate drug molecules for clinical anti-HBV treatment.

The application relates to kaempferol cerium nanoparticles and a preparation method and application thereof, and belongs to the technical field of biological medicines. The kaempferol cerium nanoparticles are prepared by performing coordination co-assembly on kaempferol and cerium ions in the presence of polyethylene glycol at a specific molar ratio, and the nanoparticles have uniform particle sizes and good dispersity. The nanoparticles have the anti-inflammatory activity of kaempferol and the ROS scavenging capacity of cerium ions, and show a significant synergistic effect in in-vivo and in-vitro experiments, can effectively reduce lung inflammation, inhibit oxidative stress, improve lung function, and have good biological safety, thereby providing a new drug candidate scheme for the treatment of ARDS.

This invention relates to a taraxasterol nitrobenzoate derivative in the field of medicinal chemistry, with the following structural formula: Compound B is obtained by reacting taraxasterol 1 with 4-nitrophthalic anhydride in a suitable alkaline catalyst and organic solvent. This synthetic route offers high yield and is easy to implement. Activity tests demonstrate that the taraxasterol nitrobenzoate derivative shown as B, designed and synthesized in this invention, is a suitable antitumor drug candidate, particularly as a candidate drug for lung cancer.

The application provides a method for constructing a spontaneous esophageal precancerous lesion or esophageal cancer non-human animal model and application thereof. The non-human animal model of spontaneous esophageal precancerous lesion or esophageal cancer is obtained by deleting the expression of Trp53 and Cdkn2a in the non-human animal. The non-human animal model prepared by the application can be used as an ideal animal model for screening drug candidates, evaluating the therapeutic effect of drugs, evaluating the toxicological effect of drugs and researching the pathogenesis of esophageal precancerous lesion or esophageal cancer.

This invention discloses the application of platelet-reactive protein-4 (THBS4) in the diagnosis and treatment of endometriosis. Through bioinformatics integration analysis, clinical sample validation, and in vitro and in vivo experiments, this invention confirms that THBS4 is significantly highly expressed in both ectopic lesions and peripheral blood of patients with endometriosis, and its expression level is positively correlated with disease severity. The area under the receiver operating characteristic (AUC) curve for THBS4 alone in diagnosing endometriosis is 0.930, significantly superior to cancer antigen 125 (CA125); the AUC for the combined diagnosis of THBS4 and CA125 reaches 0.968. Simultaneously, silencing the THBS4 gene effectively inhibits the proliferation, migration, and invasion of human endometrial stromal cells, and significantly reduces the volume and fibrosis area of ​​ectopic lesions in a mouse model of endometriosis. This invention provides a highly sensitive and specific new biomarker for the non-invasive or minimally invasive early diagnosis of endometriosis, and provides new targets and candidate drugs for non-hormone-dependent targeted therapy.

The application discloses application of long-chain non-coding RNA LncZFHX2 in preparation of a drug for treating osteoarthritis. LncZFHX2 is specifically combined with KLF4 protein through a specific structure and a base sequence of LncZFHX2, and promotes transcriptional regulation of the KLF4 protein on RIF1 protein. LncZFHX2 indirectly regulates RIF1 protein to improve a cell state. Overexpression of LncZFHX2 inhibits osteoarthritis in vitro. In the results of the examples of the application, it is verified that overexpression of LncZFHX2 inhibits development of osteoarthritis, and a new intervention approach and a candidate drug are provided for clinical prevention and treatment of osteoarthritis. LncZFHX2 has a short sequence, does not need to be translated into a protein to play a role, has the characteristics of quick effect, high efficiency and low cost, and has high cost performance in synthesis and application.

The application discloses radix sophorae tonkinensis polysaccharide STGP-1, a preparation method thereof and pharmaceutical use for treating lung squamous carcinoma, and relates to the technical field of medicines. The monosaccharide composition of STGP-1 includes fucose Fuc, arabinose Ara, galactose Gal, glucose Glc, xylose Xyl and mannose Man, and the molar ratio is 0.34:12.15:25.76:57.07:1.06:3.62. The STGP-1 is obtained by extraction, separation and purification from dried roots and rhizomes of radix sophorae tonkinensis, and the preparation method comprises the steps of pretreatment and crude extraction, impurity removal treatment, anion exchange column chromatography separation, gel column chromatography purification and the like. The STGP-1 can be used alone or in combination with anti-PD-1 monoclonal antibody for preparing a medicine for treating lung squamous carcinoma. The preparation process is stable, the source is natural, and the STGP-1 can provide a new high-efficiency and low-toxicity candidate medicine for immune combined treatment of lung squamous carcinoma.

The application of raspberry ketone in the immunotherapy of pancreatic cancer belongs to the technical field of biological medicine, and provides the application of raspberry ketone in the immunotherapy of pancreatic cancer. The application discloses that raspberry ketone can specifically and widely up-regulate the expression of MHC-I molecules on the surface of pancreatic cancer cells, and significantly enhances the infiltration and function of anti-tumor effector T cells in the tumor immune microenvironment. In-vivo and in-vitro experiments prove that raspberry ketone can reverse tumor immune escape by up-regulating MHC-I, and after being combined with a PD-1 immune checkpoint inhibitor, the raspberry ketone can produce a significant synergistic anti-tumor effect, significantly inhibit the growth of pancreatic cancer and prolong the survival period of tumor-bearing mice. The application provides a new strategy of combining a natural small molecule immunomodulator with an existing immunotherapy, and provides an innovative solution and a drug candidate for overcoming the difficulty of pancreatic cancer tolerance to immunotherapy.

This invention discloses a micropeptide, its encoding nucleic acid, and its application in regulating inflammatory activation of microglia. The amino acid sequence of the micropeptide is shown in SEQ ID NO:3. Simultaneously, this invention discloses the nucleic acid encoding the micropeptide, which contains either the nucleotide sequence shown in SEQ ID NO:1 or the nucleotide sequence shown in SEQ ID NO:2, wherein SEQ ID NO:2 is a small open reading frame located within the sequence of SEQ ID NO:1. This invention validated the translational expression of the micropeptide in microglia by constructing an EGFP reporter gene fusion vector and a SUMO tag fusion expression vector. Functional experiments showed that under oxygen-glucose deprivation / reperfusion injury conditions, the micropeptide significantly inhibited inflammatory activation of microglia. This invention provides a new potential target and candidate drug for the treatment of neuroinflammatory diseases such as stroke.

This invention provides an application of tartary buckwheat antioxidant peptide as a PPARα agonist. The tartary buckwheat antioxidant peptide (SEQ ID NO:1) is used to prepare a PPARα agonist, and this tartary buckwheat antioxidant peptide is used to prepare a drug for improving metabolic dysfunction-related fatty liver disease (MASLD). The tartary buckwheat antioxidant peptide of this invention provides a new drug candidate for improving MASLD and has broad clinical application prospects.

This invention relates to the application of Gen-miR-1 as a KARS inhibitor in the preparation of antitumor and antifibrotic drugs. Specifically, it discloses the application of Gen-miR-1 in the prevention and / or treatment of cell proliferation and migration diseases, particularly suitable for the preparation of drugs for the prevention and / or treatment of tumors and myocardial fibrosis associated with high KARS protein expression. This invention clarifies the specific inhibitory effect of Gen-miR-1 on KARS, providing a novel therapeutic target and drug candidate molecule derived from traditional Chinese medicine for cell proliferation and migration diseases (tumors, fibrosis) targeting the KARS pathway, thus broadening the application scenarios of active ingredients in traditional Chinese medicine in the treatment of related diseases.

Methods and systems for generating drug repurposing predictions for a disease caused by a pathogen, such as a novel pathogen, are provided. A multi-modal system includes a protein-protein interaction network (PPI), a graph neural network (GNN), a diffusion module, a proximity module, and an aggregation module. The GNN is configured to predict new edges between candidate drug nodes and disease nodes in an embedded representation of the PPI to produce a decoded embedding space. The diffusion module is configured to determine a proximity distance for pairs of nodes in the PPI, and the proximity module is configured to determine a proximity distance for pairs of nodes in the PPI, each pair comprising a pathogen-protein node and a drug-protein node. A ranked list of candidate drugs predicted to be effective in treatment of the disease based on candidate drug lists generated by the other modules is generated by the aggregation module.

The application relates to the technical field of medical artificial intelligence, and discloses a drug recommendation system and method based on multi-agent cooperation. The system comprises the following steps: a retrieval agent performs structured processing and retrieval enhancement generation on extracted multi-source heterogeneous data to obtain a first drug candidate set related to a target disease; a pharmacological agent performs hierarchical quantitative scoring and reflection-driven rearrangement on the first drug candidate set to obtain a second drug candidate set; a clinical agent performs clinical quantitative scoring and diagnosis and treatment adaptation rearrangement on the first drug candidate set to obtain a third drug candidate set; a coordination agent performs dynamic weighted fusion on the first drug candidate set, the second drug candidate set and the third drug candidate set to obtain a drug comprehensive evaluation score matrix, and performs conflict resolution and precision rearrangement output on the drug comprehensive evaluation score matrix to obtain a drug recommendation result related to the target disease. The application significantly improves the accuracy, explainability and reliability of drug recommendation.

The application discloses application of an inhibitor targeting CCL28 in treatment of visceral pain. The application firstly proves that CCL28 is significantly up-regulated in spinal cord dorsal horn neurons of a mouse model of visceral pain, and establishes CCL28 as a new target for treatment of visceral pain. On this basis, the application designs and screens a high-efficiency and specific siRNA sequence targeting CCL28, the siRNA can be delivered to the spinal cord locally through intrathecal injection, specifically silences CCL28 gene expression, inhibits activation of a downstream ERK signal pathway, thereby significantly alleviating visceral pain, and has no obvious off-target effect. The application provides a complete technical scheme from target discovery to drug intervention, provides a new strategy and a drug candidate molecule for treatment of visceral pain, and has a good clinical application prospect.

This invention relates to the field of pharmaceutical technology, and discloses an atrasentan derivative, its preparation method, and its applications. The atrasentan derivative is a tetrasubstituted pyrrole derivative designed using atrasentan as a lead, significantly reducing the difficulty and cost of synthesis by decreasing three chiral centers. This atrasentan derivative exhibits high safety in HK-2 cells and can significantly improve the pathological state of fibrosis induced by TGF-β in HK-2 cells. It has the potential to be used in the preparation of drugs for the prevention and treatment of renal fibrosis-related diseases, breaking through the synthetic bottleneck of atrasentan and providing a novel candidate drug for the treatment of renal fibrosis.

This invention belongs to the field of novel pharmaceutical uses, and more specifically, relates to the application of ethyl acetate extract of turmeric in the preparation of drugs for treating colorectal cancer. The preparation method of the extract is as follows: turmeric slices are soaked overnight in 15 times their weight of a 70% (v / v) ethanol solution, refluxed at 85°C three times, 2 hours each time. The extracts are combined and concentrated until no alcohol odor remains. The extract is then dried to constant weight to obtain the total extract. The total extract is reconstituted with water and extracted three times with ethyl acetate at an equal volume ratio. The extracts are combined and dried to constant weight to obtain the final product. Experimental results show that this extract is particularly effective in improving disease activity index, restoring colon length, reducing tumor number, and alleviating histopathological damage, and has no significant toxicity to major organs. This extract can be formulated into oral or injectable preparations, providing a new natural drug candidate for the treatment of colorectal cancer.

This invention relates to a method for disease therapeutic target discovery and drug prediction based on multi-omics networks and deep learning models, belonging to the interdisciplinary field of bioinformatics and artificial intelligence drug discovery. The method includes: integrating genomic expression profiles and common molecular interaction data from disease and control groups to construct a candidate whole-genome network; refining the network based on expression profile data through systematic modeling and the AIC criterion to obtain the real molecular interaction network; extracting the core network using the master network projection method and identifying key targets through pathway analysis; predicting candidate drugs interacting with the targets using a pre-trained deep neural network model; and finally screening potential therapeutic drugs based on multi-dimensional criteria such as regulatory ability, sensitivity, and toxicity. This invention achieves a complete integration from disease mechanism analysis to drug prediction, and is particularly suitable for complex diseases such as atopic dermatitis. It can systematically discover precise targets and efficiently predict repositionable drugs, significantly improving R&D efficiency.

This invention belongs to the field of biomedicine, specifically relating to the development and application of oligonucleotide drugs targeting the key assembly proteins G3BP1 / 2 of stress granules. The oligonucleotides in these drugs are all composed of 20 bases, with 5 bases at each end modified with 2'-O-methoxyethyl, and 10 consecutive ordinary bases in the middle to ensure targeting specificity. Simultaneously, the entire nucleic acid chain is modified with thiophosphorylation. The oligonucleotide molecules disclosed in this invention possess targeting specificity, high molecular activity, and in vivo metabolic stability, providing research directions and candidate drugs for clinical targeting of stress granules and improvement of neurodegenerative diseases such as ALS.

This invention belongs to the field of biomedical technology and discloses the application of Rab30 as a target and its activator in the preparation of drugs for the prevention or treatment of metabolic dysfunction-related fatty liver disease (MASLD). This invention reveals for the first time that Rab30 plays a crucial role in lipid clearance and protection in the pathological process of MASLD by mediating lipophage and fatty acid oxidation pathways. It also confirms that the small molecule compound curculigoside A can serve as a targeted activator of Rab30. In vitro and in vivo experiments show that curculigoside A can directly bind to the Rab30 protein and significantly enhance its stability, thereby specifically and dependently targeting Rab30 to effectively improve lipid overload in the liver under pathological stress and inhibit the associated inflammation and fibrosis. This invention provides a clear therapeutic target and targeted drug candidate for the prevention and treatment of MASLD, and has significant clinical translational value.

This invention discloses an antimicrobial peptide, its pharmaceutical composition, and its applications. The invention optimizes the structure of the antimicrobial peptide through deuteration modification technology, significantly enhancing its targeted binding ability to β-1,3-D-glucan synthase. The affinity of this antimicrobial peptide for the aforementioned target is 9-27 times that of the control peptide. In vitro assays show that its minimum inhibitory concentration (MIC) against nine standard Candida strains is consistently 0.002 μg / mL, exhibiting significantly superior activity compared to fluconazole, anidoxurine, and the control peptide. It also exhibits extremely low cytotoxicity against L02 human normal hepatocytes. In in vivo experiments, in a neutropenic mouse model of Candida albicans infection, the antimicrobial peptide at all doses showed superior reduction in renal fungal load compared to anidoxurine and the control peptide. The antimicrobial peptide of this invention combines highly efficient anti-Candida activity, low cytotoxicity, and excellent in vivo efficacy, providing a safe and effective candidate drug for the treatment of drug-resistant candidiasis and possessing good clinical translational value.

This invention provides the application of ginsenoside Rh1 in the treatment of inflammatory skin diseases, belonging to the field of biomedical technology. It is the first to demonstrate that ginsenoside Rh1 inhibits AQP3 expression by activating the oxidative phosphorylation pathway and regulating cellular homeostasis, thereby inhibiting AQP3 gene transcription and / or expression. As a novel AQP3 inhibitor, it downregulates AQP3 protein expression levels in an animal model of rosacea. This provides a novel strategy and drug candidate for targeted therapy of rosacea and other AQP3-related inflammatory skin diseases.

This invention discloses the application of a drug in the prevention or treatment of hydrocephalus, belonging to the field of pharmaceutical formulation technology. The drug comprises a pharmaceutically acceptable formulation of one or more of the following active ingredients: compound A, compound B, or compound C, and their pharmaceutically acceptable salts, solvates, or crystal forms; compound A is carbaspirin calcium, compound B is aspirin, and compound C is salicylic acid. This invention utilizes the above-mentioned drug in the prevention or treatment of hydrocephalus. Carbaspirin calcium and its metabolites can significantly reduce ventricular enlargement in a hydrocephalus model rat, and carbaspirin calcium and its metabolites show promise in the preparation of drugs for treating hydrocephalus, providing an effective candidate drug to alleviate the suffering of hydrocephalus patients, reduce treatment risks and costs; it broadens the scope of action of carbaspirin calcium and optimizes the stability formulation of carbaspirin calcium.

1. Name of the product in this design: Operation display unit of a cascaded graphical user interface for microbial antibiotic susceptibility testing of an electronic device. 2. Purpose of this design: An electronic device. 3. The key design features of this product are: the content that the graphical user interface requires protection for. 4. The picture or photo that best illustrates the key design points: Design 1 front view. 5. Design 1 is designated as the basic design. 6. Uses of the graphical user interface: Overall use of the interface: For microorganisms in patient samples, clinicians use the interface to identify drugs that the microorganisms are susceptible to, build cascades for candidate drug families, and create multiple tiers if the microorganisms show resistance to drugs in the previous tier. The part of the interface is the operation display section of the cascaded graphical user interface. The buttons on the left side of the interface allow users to add new cascades and view existing cascades; the two buttons in the upper right corner allow users to delete and save cascades; users can enter the cascade name in the first rectangle from the left at the top, select the biological interpretation group by clicking the second rectangle, and select the style type by clicking the third rectangle; users can select a specific drug by clicking the "Select drug" rectangle in the interface, add a new drug family by clicking the rectangle with the "+" symbol on the right; and add a new cascade by clicking the "+" rectangle at the bottom. After a user clicks the "Select drug" rectangle in the main view of Design 1 to select a drug, the interface changes to Design 1's modified state diagram 1. The user can then click the delete icon to the right of the name to delete the drug. After the user clicks the "Select drug" rectangle below Drug Family 1 in Design 1's modified state diagram 1, the interface changes to Design 1's modified state diagram 2. After the user clicks the rectangle with a "+" symbol in the middle right of Design 1's modified state diagram 2, the interface changes to Design 1's modified state diagram 3. After the user clicks the "Select drug" rectangle below Drug Family 2 in Design 1's modified state diagram 3, the interface changes to Design 1's modified state diagram 4. After the user clicks the rectangle with a "+" symbol in the middle right of Design 1's modified state diagram 4, the interface changes to Design 1's modified state diagram 5. After the user clicks the rectangle with a "+" symbol at the bottom of Design 1's modified state diagram 5 to add a new cascade, the interface changes to Design 1's modified state diagram 6. After the user clicks the "Select" rectangle in the second cascade of Design 1's modified state diagram 6... After selecting a drug using the "drug" rectangle, the interface changes to Design 1, state diagram 7. When the user clicks the rectangle with the "+" symbol at the bottom of Design 1, state diagram 7, to add a new cascade, the interface changes to Design 1, state diagram 8. The change process of Design 2 is the same as Design 1. 7. Other matters to be noted: The dotted line part of the figure is not claimed.

The application belongs to the technical field of biological medicine, and particularly relates to application of a GCN2 kinase inhibitor in preparation of a drug for treating heart failure with preserved ejection fraction. 18 H 12 ClF2N5O3S, the inhibitor can inhibit the activity of GCN2 kinase, and exhibits significant therapeutic effect in a disease model: can obviously improve ventricular diastolic function (E / E' ratio is reduced), reduce the level of heart failure markers, reduce cardiomyocyte hypertrophy and interstitial fibrosis, inhibit the expression of oxidative stress level and inflammatory factors, reduce the accumulation of triglyceride and total cholesterol in myocardium and serum, and improve obesity-related insulin resistance and metabolic disorder. The application provides a novel targeted treatment strategy and candidate drug for heart failure with preserved ejection fraction.