315 results about "Drug compound" patented technology

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3, L4, L5, L6, M, m, and p are as defined herein. Methods associated with preparation and use of such compounds is also provided.

The invention provides a whole-process targeting polypeptide, a drug compound thereof, a drug delivery system and application of the whole-process targeting polypeptide. The whole-process targeting polypeptide comprises pHA and VAP which are covalently connected through a bridging structure; the VAP is LVAP, a reverse sequence polypeptide of the LVAP, DVAP or SVAP; wherein the amino acid sequence of the LVAP is as shown in SEQ ID NO: 1; the SVAP is a D-configuration polypeptide of the LVAP; the DVAP is a D-configuration polypeptide of the LVAP inverted sequence polypeptide; the bridging structure is amino-monoethylene glycol-carboxylic acid or a derivative thereof. The whole-process targeting polypeptide not only can cross a blood-brain barrier, target tumor neovascularization, cross a blood-tumor barrier, target tumor mimicry vessels, tumor cells and stem cells thereof, but also has better tumor cell affinity, anti-tumor treatment and in-vivo safety effects. Meanwhile, the drug compound or the drug delivery system has a synergistic effect after being combined with a chemotherapeutic drug, and the anti-tumor drug effect can be remarkably improved.

A method is disclosed for using an artificial intelligence engine to generate candidate drug compounds, wherein the method comprises: generating candidate drug compounds comprising sequences via a creator module of the artificial intelligence engine. The method includes generating, via a descriptor module, a respective description for each of the candidate drug compounds at nodes in a knowledge graph, wherein the knowledge graph comprises a multi-dimensional representation of the candidate drug compounds and the respective description comprises drug compound structural information, drug compound activity information, and drug compound semantic information. The method includes determining a shape of the multi-dimensional representation of the candidate drug compounds; determining, based on the shape, a slice configured to be obtained from the representation; determining, using a decoder, which dimensions are included in the slice; and based on the dimensions, determining an effectiveness of a biomedical feature of the slice.

The present invention provides a method and system for fabricating complex human tissues by integrating bio-electrospraying, cell electrospinning merged with 3D multi material microfluidic bioprinting, and future additions of magnetic and acoustic levitation technologies. The fabricated tissues serve as an alternative to animal testing in drug discovery processes, aiding in the prediction of human physiological responses to various drug compounds.

The present invention relates to antibodies or antibody fragments that bind to human and non-human primate transferrin receptors. The antibodies described herein can be used as agents to deliver pharmaceutical compounds into or through cells during receptor-mediated endocytosis and / or transendocytosis processes. As transferrin receptors are also present in the blood brain barrier endothelial cells, one aspect of the invention provides means and methods to increase delivery of pharmaceutical compounds to the central nervous system.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 5 kDa or more, the polymer matrix containing a hydrophobic polymer. The membrane polymer matrix includes from about 70 wt. % to about 99 wt. % of an ethylene vinyl acetate copolymer.

The present disclosure provides methods, pharmaceutical compositions, and kits for treating cancer in patients in need thereof. The methods comprise administering to a patient in need a STING (stimulator of interferon genes) agonist, such as Compound No. 14, or a pharmaceutically acceptable salt thereof, in combination with one or more checkpoint inhibitors. Suitable checkpoint inhibitors include anti-PD-1 antibodies, anti-PD-L1 antibodies and anti-CTLA-4 antibodies. Also provided are medicaments for use in treating cancer. Compound No. 14 has the structure:

A packaged, sealed container system for stable storage of a formulation of an oxygen-sensitive pharmaceutical compound, the packaged, sealed container system comprising a primary container including therein a formulation of an oxygen-sensitive pharmaceutical compound, a secondary outer container comprising a first flexible sheet layer, an opposing second flexible sheet layer, and a seal disposed along a common peripheral edge of the first and second flexible sheet layers, such that the primary container is disposed between and enclosed by the first and second flexible sheet layers of the secondary outer container. An oxygen scavenger is also disposed between and enclosed by the first and second flexible sheet layers of the secondary outer container. The oxygen scavenger is in fluid communication with the contents of the primary container.

The invention belongs to the technical field of computer biology, and relates to a lightweight drug-target interaction prediction method based on double pre-training language models. Downloading a protein information data set of required drug compounds and drug action targets from a public database; sending the protein sequence into an encoder to obtain a generated vector; the method comprises the following steps: labeling a compound sequence of a drug by using a tokenizer, pre-defining a corresponding relation between a compound sequence label and an integer, then converting into an integer value, and inputting the integer value into an encoder to generate a vector; splicing the class tokens to obtain a drug target pair, and feeding the drug target pair into an interaction head; and calculating an interaction probability between the two. According to the method, the drug pre-training language model and the protein pre-training language model are introduced at the same time, deep semantic coding is performed on the SMILES sequence and the amino acid sequence, molecular structure characteristics and protein sequence characteristics can be comprehensively captured, and the expression ability is remarkably enhanced.

The invention relates to the technical field of microorganisms, and particularly discloses bacillus deserticola for resisting tobacco target leaf spot, a bacterial drug compound and application of the bacillus deserticola and the bacterial drug compound. The bacillus deserticola is bacillus deserticola 127-2 and is preserved in the China General Microbiological Culture Collection Center on April 1, 2025, the address is Institute of Microbiology, Chinese Academy of Sciences, No.3, No.1 Yard, West Beichen Road, Chaoyang District, Beijing, the preservation number is CGMCC No.34058, and the bacillus deserticola is classified and named as Bacillus inaquorum; the in-vessel inhibition rate of the strain 127-2 to tobacco target leaf spot caused by rhizoctonia solani is 87.5%, the in-vivo inhibition activity also reaches 50% or above, the in-vivo inhibition activity of the strain 127-2 to tobacco target leaf spot caused by compounding of the strain 127-2 and pyraclostrobin reaches 98% or above, and the purposes of drug reduction, persistent effect and efficient prevention and control of rhizoctonia solani can be effectively achieved through the synergistic effect of bacteria and drugs.

The invention discloses a small molecular twin drug compound with a synergistic analgesic effect and a pharmaceutical composition, a preparation method and application thereof. The twin drug molecule is formed by connecting a drug A and a drug B through a covalent bond, the drug A is nefopam, and the drug B is gamma-aminobutyric acid (GABA) and analogues thereof and comprises gabapentin, pregabalin, GABA, melogabalin and crigabalin. The analgesic effect of the composition is superior to that of combined administration and single administration, and the composition can obviously improve various acute and chronic inflammation pains and can relieve paclitaxel-induced peripheral neuralgia; the anti-inflammatory activity is higher than that of combined use and single drug, so that the compound has the potential of treating pain, inflammation and inflammatory pain related diseases; the interaction among the medicines can be effectively reduced, and the medication compliance of a patient is improved.

The invention provides a complex comprising Zn2+ and a compound of formula (I): or a deuterated analog thereof, or an ion or poly-ion thereof, or a salt thereof that is useful for treating cancer, as well as compositions and kits comprising such complexes.

The invention relates to an RGD (arginine-glycine-aspartic acid) peptide modified mercaptododeborane derivative and a synthesis method, the derivative utilizes RGD peptide to perform chemical coupling modification on mercaptododeborane anion salt (BSH), and the BSH and the RGD peptide are connected through a hydrophilic intermediate connector with a double bond at one end and carboxyl at the other end. A hydrophilic chain is selectively introduced to serve as an intermediate connector, a series of compounds are synthesized through a convenient and efficient sulfydryl-alkene click reaction and an amino-carboxyl amidation condensation reaction and are purified, various cationic BSH salts and RGD peptide are connected, and targeted modification of the RGD peptide on an existing boron carrying agent BSH is achieved. The derivative obtained by the invention is not reported before, has the potential to improve the tumor targeting ability of the existing boron carrying agent, and is expected to be used as a drug compound for BNCT treatment.

The invention relates to the technical field of biological medicines, and discloses hyaluronic acid modified metal coordination albumin nanoparticles as well as a preparation method and application thereof. The hyaluronic acid modified metal coordination albumin nanoparticle comprises a core and a hyaluronic acid shell layer, wherein the core is formed by self-assembly of an albumin-drug compound, poly-L-aspartic acid and ferric ions through coordination, and the hyaluronic acid shell layer is connected to the surface of the core through coordination or adsorption. According to the hyaluronic acid modified metal coordination albumin nanoparticles as well as the preparation method and the application thereof, the preparation method is simple, convenient and rapid, does not need complex covalent modification, is mild in condition and is easy for large-scale production, and the prepared nanoparticles are uniform in particle size, good in stability and high in stability. In addition, due to the fact that the hyaluronic acid is modified on the surface, the active targeting capacity on CD44 receptor high-expression tumor cells is achieved, the enrichment and treatment effects of the medicine on the tumor site are remarkably improved, and the application prospect in preparation of the anti-tumor medicine is wide.

The invention relates to the technical field of cytobiology and biomedicine detection, and discloses a time sequence fluorescence tracing system based on a coupling detection lipid probe. Comprising an imaging detection module which is used for adding FM lipophilic styrene fluorescent dye in a culture environment, forming a membrane probe to observe the morphological change of a membrane and detect the formation of vesicles, and completing the complete time sequence tracing of the cell endocytosis process by adopting a content dyeing method; the deep learning module is used for carrying out deep learning on the obtained time sequence image, establishing a living cell imaging screening and image analysis system, and identifying protein molecules related to the target external vesicles; carrying out image description on the generation, transportation and fusion processes of the vesicles generated by the proteins in different stages before fusion of the outer vesicles and the cell membranes and after fusion and shearing; and the knock-down operation module is used for exploring the generation mode of the vesicle contents in the early endosome in combination with knockout and knock-down operations of the specific drug compound.

The present invention relates to pharmaceutical compounds of Formula (I):as further described herein, and pharmaceutical compositions containing such compounds, as well as methods of using these compounds to modulate the activity of aryl hydrocarbon receptor (AhR) and to treat conditions comprising inflammation inside the intestinal tract and certain disorders of the central nervous system affected by the gut-brain axis, including IBD, ulcerative colitis, Crohn's disease, Huntington's disease, and multiple sclerosis.

Provided herein are pharmaceutical formulations and pharmaceutical compound salts which utilize complexing agents as counterions. Such formulations and salts are useful for treating a variety of disease and disorders.

The present invention provides engineered sucrose phosphorylase (SP) enzymes, polypeptides having SP activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. Methods for producing SP enzymes are also provided. The present invention further provides compositions comprising the SP enzymes and methods of using the engineered SP enzymes. The present invention finds particular use in the production of pharmaceutical compounds.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 0.5 kDa or more, the polymer matrix containing a hydrophobic polymer. Further, the membrane layer comprises a plurality of water-soluble particles distributed within a membrane polymer matrix containing an ethylene vinyl acetate copolymer, wherein the water-soluble particles have a D50 particle size of about 150 micrometers or less and contain a non-polymeric, hydroxy-functional compound.

The application provides, among others, antibody-drug conjugates formed from a bispecific antibody and an auristatin drug unit, or a pharmaceutically acceptable salt or solvate thereof, and methods of making and using thereof. The application further provides linker-drug compounds, their isomers, endo-, racemates, enantiomers, or mixtures thereof, or pharmaceutically acceptable salts or solvates thereof, and methods of making and using thereof.

The present invention relates to pharmaceutical compounds, compositions, and methods, particularly as they relate to compositions and methods for treating and / or preventing proliferative disorders associated with TGFβR1 activity, such as cancer or fibrosis. The present invention provides compounds of Formula (I) and Formula (II) as further described herein, which have an acidic moiety that enhances tissue specificity to target tissues and organs. The present invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of using these compounds to treat disorders including cancer or fibrosis.

An anti-inflammatory drug compound, and a preparation method therefor and the use thereof. The structural formula of the compound is A-Y—B, wherein A is a group after dehydrogenation of an amine compound having JAK inhibitory activity, Y is a direct connection or —(CH2)-O— or, and B is a group formed by means of dehydroxylation of a carboxy-containing carboxylic acid compound B1, or a group formed by means of dehydrogenation of a hydroxy-containing compound B2. The compound has the special effects of having a strong transdermal property, controlled drug release, high efficacy, etc.

The invention discloses a benzofuran glycoside compound as well as a separation and extraction method, a pharmaceutical composition and application thereof. The compound 1 is separated from an eupatorium chinense extract. And separating and purifying chemical components of the n-butyl alcohol part of the eupatorium chinense root to obtain the benzofuran compound. The inhibition activity of target cyclooxygenase-2 of inflammatory related diseases of all the separated compounds 1 is tested, and the compounds 1 have good inhibition activity on COX-2 enzyme and have good binding energy with target protein. In addition, the compound also has a good NLRP3-related inhibition effect, can be independently used or combined with other medicines to regulate NLRP3-related proteins, and is used for treating NLRP3-related mediated diseases and / or diseases and preparing medicines for preventing or treating the diseases or diseases. The compound 1 also has a good inhibition effect on acetylcholin esterase, and can be used for treating Alzheimer's disease, myasthenia gravis, Parkinson's disease and other diseases.

The present invention relates to pharmaceutical compounds and formulations comprising said compounds, wherein said compounds have the structure according to Formula I or II. The compounds and formulations are suitable for use as medicaments for the prevention or treatment of diseases or conditions characterized by percutaneous cell dysfunction, detachment and / or loss, for medical treatment for vascular stabilization, for treatment for promoting, restoring or maintaining attachment of percutaneous cells to blood vessels, and / or for the treatment of vascular-related diseases in patients. (I) (II)

The invention relates to the technical field of biochemistry, and provides a pesticide nano-composite and a preparation method and application thereof, the pesticide nano-composite comprises a dendritic polymer (SSP) and a drug molecule connected with the dendritic polymer through a hydrogen bond and / or Van der Waals force; the drug molecules are selected from at least one of benomyl, carbendazim and thiophanate-methyl; according to the drug compound, aggregation of drug molecules can be avoided, the drug effect of the drug molecules can be improved, the lasting period of the drug molecules can be prolonged, and the usage amount of the drug molecules is reduced; a solution containing the medicine compound is sprayed in the plant growth process and used for inhibiting growth of the aureocystis aureocystis and / or verticillium dahliae; the method is simple and convenient in process and wide in applicability.

The application relates to, among others, self-stabilizing bridged ring connecting units and their application in antibody-drug conjugates, linker-drug compounds prepared by incorporating said linkers, and ligand-drug conjugates with stable quality and excellent homogeneity. The application also discloses methods for the preparation the linkers, linker-drug compounds, and ligand-drug conjugates, as well as the application of the linker -drug compounds, and ligand-drug conjugates in the treatment of tumors, infections, and immune diseases.

The present invention relates to the field of microbial technology, and specifically discloses a new broad-spectrum disease-resistant Bacillus species, a fungicide compound, and applications thereof. The new broad-spectrum disease-resistant Bacillus species is Bacillus species 129-52, which was deposited on April 1, 2025, at the General Microbiology Center of the China Culture Collection Administration, located at the Institute of Microbiology, Chinese Academy of Sciences, No. 3, Yard 1, Beichen West Road, Chaoyang District, Beijing, with a deposit number of CGMCC No. 34059, and is classified as Bacillus sp.; the strain 129-52 of the present invention has a living inhibition rate of 66.82% on branches with apple rot disease. After using fungicide-drug synergistic treatment, it was found that the inhibition rate of two tested drugs, carbendazim and pyraclostrobin, on apple rot disease reached more than 80% after the dosage of the two tested drugs, carbendazim and pyraclostrobin, was reduced by half. The fungicide-drug synergistic treatment can effectively achieve the purpose of reducing the dosage, maintaining the effect, and efficiently preventing and controlling apple rot disease.