24783 results about "Combinatorial chemistry" patented technology

The present invention relates to a compound of formula (I), or a stereoisomer, a tautomer, a deuterated compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof as a drug for treating and / or preventing KRAS-mediated diseases.

The present application relates to the technical field of medicines, and relates to a macrocyclic compound containing amide substitution, in particular to a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof in the treatment of disease.

The invention discloses an oxygen-containing heterocyclic compound salt, and a crystal form and application thereof. The oxygen-containing heterocyclic compound salt disclosed by the invention has a structure as shown in a formula II. The oxygen-containing heterocyclic compound salt and the crystal form thereof provided by the invention have one or more improved characteristics, which are represented by extremely high water solubility, and high dissolution rate and high solubility in physiological related medium simulated gastrointestinal fluid, so that the stability of the oxygen-containing heterocyclic compound under an oxidation condition is remarkably improved, and the stability of the oxygen-containing heterocyclic compound is improved. Low hygroscopicity and good crystal form stability are achieved, and oral absorption and long-term storage of the medicine are facilitated; and the preparation method is simple and suitable for industrial production. # imgabs0 #

The present disclosure relates to compositions and methods for reversible fixation of biological samples using fixation reagents that form bis-carbamate crosslinks between amine-bearing moieties in biomolecules.

Provided are a pyrimidine polycyclic derivative inhibitor, a preparation method therefor and the use thereof. In particular, provided are a compound as shown in the general formula, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the treatment of cancers and other related diseases.

The invention relates to a fused ring compound, a preparation method thereof and application of the fused ring compound in medicine. Specifically, the invention relates to a fused ring compound as shown in a general formula (IN), a preparation method thereof, a pharmaceutical composition containing the compound and application of the fused ring compound as a therapeutic agent, in particular to application of the fused ring compound in preparation of drugs for inhibiting KRAS G12D. Wherein each group in the general formula (IN) is as defined in the specification. # imgabs0 #

The invention relates to the technical field of oil exploitation, and discloses a compound containing an amide group as well as a preparation method and application thereof. The compound containing the amide group has a structure as shown in a formula (1). The polymer obtained by polymerizing the compound can improve the water-drive recovery efficiency of conventional oil reservoirs and common heavy oil reservoirs. # imgabs0 #

Provided are a crystal form of a pyridopyrimidine derivative, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a crystal form of a compound of formula (I), a preparation method therefor, a pharmaceutical composition thereof and the use thereof.

A tricyclic compound as a VHL ligand, a preparation method therefor, and a use of the compound or a pharmaceutical composition thereof for preventing and / or treating a series of diseases, disorders, and conditions.

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic protein.

A spiro compound, and a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite, or prodrug thereof, a pharmaceutical composition comprising the compound, a preparation method therefor, and a use thereof in preparation of a drug for preventing or treating KRAS-mediated related diseases.

The invention discloses a novel synthetic method for 5-phenyl tetrazole, which includes the following steps: firstly performing acid neutralization to hydrazine hydrate; then adding mixing solution formed by cyanobenzene, water and ethyl alcohol to generate phenyl aminoguanidine salt; adopting sodium nitrite for diazotization to obtain nitrine amidine under the acidic condition; obtaining 5-phenyl tetrazole crude product through closed loop under the alkaline condition; obtaining 5-phenyl tetrazole acceptable product through adopting ethyl alcohol for refining. The method has the advantages of simple technology, simplicity in operation and high product yield.

The application provides a process method for preparing (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid, and particularly relates to the technical field of organic synthesis. The process method is that, under alkaline conditions, a halogenated phosphonate compound is added into a 3,6-dimethoxy-9H-carbazole solution to perform a reaction, hydrochloric acid aqueous solution is added after the reaction to perform acidolysis degreasing, and finally (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid is obtained through extraction, reflux adsorption and beating purification. The process method uses 3,6-dimethoxy-9H-carbazole as a starting material, realizes the synthesis of the target product through one-pot reaction, has mild reaction conditions, uses non-toxic raw materials which are easy to obtain, has simple synthesis process, is convenient to operate, and has high separation yield.

The invention relates to a dialkyl imidazole bionic lipid compound and a preparation method and application thereof.The structure of the dialkyl imidazole bionic lipid compound imitates natural phospholipid design, alkyl with no less than 10 carbon atoms is modified on the fourth site and the fifth site of imidazole, and primary amines with different alkyl chain lengths are modified on the second site; the dialkyl imidazole bionic lipid compound is mixed with a therapeutic drug and other auxiliary materials to prepare lipid nanoparticles loaded with the therapeutic drug, and the lipid nanoparticles can be used as a drug delivery system for preparation of brain-targeted drugs. The dialkyl imidazole bionic lipid has the function of dynamically regulating and controlling the blood-brain barrier, and can realize reversible opening of the blood-brain barrier; the formed drug-loaded lipid composition can pass through a blood brain barrier and well realize brain-targeted delivery of loaded therapeutic drugs; the drug-loaded lipid composition composed of the dialkyl imidazole bionic lipid belongs to a new generation of bionic nano-drug carriers, and provides a new strategy for realizing brain-targeted delivery of different types of drugs.

Disclosed in the present invention are a polycyclic derivative, and a preparation method therefor and the use thereof. In particular, the present invention relates to a compound represented by general formula (I) or a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the preparation of a drug for treating diseases. The compound has a structure as represented by formula (I).

The invention discloses a tetranuclear ladder type organic tin carboxylate complex as well as a preparation method and application thereof, and belongs to the technical field of metal complexes, the tetranuclear ladder type organic tin carboxylate complex is prepared by taking para-position or ortho-position substituted benzoic acid as a ligand and taking organic tin dimethyl tin oxide as a substrate. The preparation method is simple to operate and mild in condition. The tetranuclear ladder type organic tin carboxylate complex can be used as a photocatalyst for photocatalytic production of H2O2, and the photocatalytic H2O2 production rate is as high as 5.12 * 10 < 3 > [mu] mol.g <-1 >. H <-1 > and is higher than the H2O2 production rate of a photocatalyst reported in the existing literature.

The invention discloses a nano-enzyme as well as a preparation method and application thereof, and relates to the technical field of nano-enzymes. According to the preparation method, natural polyphenol, a cerium source and polyethylene glycol are mixed to prepare the novel polyphenol nano-enzyme, the preparation method is simple and easy to implement, the preparation cost is low, the prepared nano-enzyme has good biocompatibility, and a new way is provided for effective treatment of inflammatory diseases.

Embodiments of the present invention provide methods and intermediates for the large scale preparation of 2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide hemisuccinate, as well as formulations and product forms prepared by these methods. Embodiments of the present invention further provide for the preparation of lamidetan acetate (2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide acetate) and / or a pharmaceutical composition thereof, and / or the use of lamidetan acetate and formulations thereof in subcutaneous drug delivery.

The invention belongs to the technical field of anion exchange membranes, and relates to a cross-linked polyaromatic piperidine anion exchange membrane and a preparation method thereof. The exchange membrane structure comprises a copolymer structure of the following repetitive structural units, the selected rigid main chain polyaromatic hydrocarbon can ensure the mechanical strength of the anion exchange membrane, meanwhile, the toughness of the anion exchange membrane is further enhanced by adopting a cross-linked structure, and a formed cross-linked network can reduce swelling of the anion exchange membrane, so that the anion exchange membrane is more stable in performance. The mechanical performance is improved; according to the invention, ether-free skeleton polyaromatic hydrocarbon is selected as a main chain and has the characteristic of strong alkali-resistant stability, six-membered nitrogen heterocyclic ions are adopted as functional groups, and a large steric hindrance structure can hinder nucleophilic substitution and elimination reaction, so that the alkali-resistant stability of the anion exchange membrane is improved, and the service life of the anion exchange membrane is prolonged. And in the # imgabs0 #, X is equal to 0.05 to 0.15.

Provided in the present invention are a tetrahydropyridopyrazole derivative and use thereof in medicine. Specifically provided is a compound as shown in general formula (I) or a racemate, stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, a preparation method therefor, and use thereof in the preparation of a related drug for treating diabetes or obesity.

The invention discloses a polyimidazolone compound as well as a preparation method and application thereof. The preparation method comprises the following steps: dissolving a bilateral alkyne ester compound, amidine hydrochloride, a catalyst and a desalting agent in an organic solvent, and carrying out polymerization reaction to obtain the polyimidazolone compound. The polyimidazolone compound with the five-membered ring is selectively generated, and the method has the advantages that monomers are easy to obtain, operation is easy, and by-products are low in toxicity. The polyimidazolone compound prepared by the invention has better machinability and has potential application value in the aspects of metal ion detection and biogenic amine detection.

The invention relates to a tricyclic derivative inhibitor as well as a preparation method and application thereof. In particular, the invention relates to a tricyclic derivative compound, a preparation method thereof, a pharmaceutical composition containing the compound, and an application of the compound in treating cancers.

Monoorgano tin compounds having chemical formula R′SnX3 and high purity are described. R′ is an optionally substituted hydrocarbyl group, X is selected from NR2 and OR, and each R is independently a linear or branched alkyl group having about 1 to about 10 carbon atoms. Methods for synthesizing and purifying these compounds are also provided. The monoorgano tin compounds may be used for the formation of high-resolution EUV lithography patterning precursors and are attractive due to their high purity and minimal concentration of diorgano tin impurities.

Compounds are provided having the following structure:or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein a, b, c, d, G1, G2, L1, L2, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8 and X are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, nanoparticles comprising the compounds and methods for their use and preparation are also provided.

The present invention relates to a stable pharmaceutical composition of therapeutically active agent, wherein the amount of nitrosamine impurity is below the FDA acceptable intake limit for shelf life of the pharmaceutical composition and a process for preparing the same.

The invention discloses a preparation method and application of amino-modified single-benzene-ring copper-based MOFs (metal organic frameworks), and the method comprises the following steps: dropwise adding a copper nitrate monohydrate solution into a diamino terephthalic acid solution, fully stirring to react, and centrifugally washing and drying the product to obtain the amino-modified single-benzene-ring copper-based MOFs. The amino-modified single-benzene-ring copper-based MOFs are used for electrocatalytic reduction of carbon dioxide. The prepared amino-modified single-benzene-ring copper-based MOFs have unique morphology, active sites can be exposed on the inner surface and the outer surface, the accessibility of the active sites is improved, and meanwhile the reaction mass transfer capacity is enhanced.

The invention provides methods for the preparation of particles including one or more agents, e.g., therapeutic or diagnostic agents. The particles can be formed by creating droplets of a first liquid, e.g., including an agent, and removing the first liquid, e.g., through its dispersal in a second liquid and / or evaporation, to solidify the droplets. Advantageously, the process of forming the particles does not significantly alter the structure or activity of the agents and may enhance the stability of the agents. For example, the particles may be stored for long periods of time without significant loss of activity, and in some embodiments, without the need for refrigeration. These particles may be used to generate stabilized pharmaceutical compositions for storage or other logistical purposes, pharmaceutical suspensions, pharmaceutical powder formulations (e.g., inhalable powders, injectable powders), creams or other topical pastes, nutraceuticals, or cosmetics.