552 results about "Amine derivatives" patented technology

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

A heteroaryl amine derivative is provided that contributes to a substantial improvement in the lifespan of an organic electroluminescent device by effectively absorbing high-energy external light in the UV region to minimizes damages to organic materials inside the organic electroluminescent device. An organic electroluminescent device according to the present invention comprises: a first electrode; a second electrode; at least one organic material layer disposed between the first electrode and the second electrode; and a capping layer, wherein the capping layer contains a heteroaryl amine derivative represented by chemical formula 1 according to the present invention.

The invention belongs to the field of medicinal chemistry, and particularly discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. According to the benzimidazole amine derivative disclosed by the invention, R1 is a hydrogen atom or a bromine atom; r2 is substituted benzoyl, substituted benzyl and the like. Pharmacological results show that the benzimidazole amine derivative disclosed by the invention has relatively good antagonistic activity on beta2AR, and the functional activity of isoprenaline (ISO) can be subjected to negative allosteric regulation.

The invention discloses 4-(pyridine-4-yl)-1H-imidazole-2-amine derivatives and compositions of a machine for assembling key proteins on an outer membrane of targeted gram-negative bacteria, and belongs to the technical field of chemical medicines. The invention provides a small molecule compound as shown in a formula (I): # imgabs0 #, the small molecule compound can be used as a brand new targeting gram-negative bacterium inner membrane lipoprotein positioning machine (LolCDE) and has bacteriostatic activity, and a new way is provided for specific antibacterial treatment of gram-negative bacteria.

The present disclosure provides engineered transaminase polypeptides for the production of amines, polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to prepare compounds useful in the production of active pharmaceutical agents.

The invention provides a flame-retardant polycarbonate composite material and a preparation method thereof, the flame-retardant polycarbonate composite material comprises the following raw materials in parts by weight: 100 parts of polycarbonate, 3-5 parts of an organic boron flame retardant, 2-3 parts of a phosphate flame retardant and 0.1-0.5 part of an antioxidant, and the structural formula of the organic boron flame retardant is as shown in the following formula I. According to the invention, the triazine aniline derivative and the formylphenylboronic acid acetate derivative react to prepare the organic boron flame retardant, and the organic boron flame retardant not only significantly improves the flame retardant property of the composite material, but also has a high light transmittance retention value after high-temperature aging, so that good balance between flame retardance and transmission performance is realized.

The nanofiltration membrane comprises a base membrane and a functional layer, the functional layer comprises a polymer, polymerization unit monomers of the polymer comprise amine monomers and cyanuric chloride, the amine monomers comprise aliphatic amine and aromatic amine derivatives, the aliphatic amine comprises at least two primary amine or secondary amine groups, and the aromatic amine derivatives comprise at least two aromatic amine derivatives. The aromatic amine derivative comprises at least two reaction functional groups and at least one hydrophilic group, the reaction functional groups comprise at least one of amino groups and hydroxyl groups, and the hydrophilic group comprises at least one of sulfonic acid groups, amino groups, hydroxyl groups, carboxyl groups and phosphate groups. Therefore, the nanofiltration membrane provided by the invention has relatively high desalination rate and stable alkali resistance.

The invention provides a preparation method of a polyphenylene sulfide-based thermoplastic composite prepreg and a corresponding prepreg, and the preparation method specifically comprises the following steps: (1) preparing a suspension dispersion system containing polyphenylene sulfide, polyamide acid and ammonia water, and (2) preparing the prepreg containing polyimide, and adding a dopamine derivative in the step (2) for dispersion. The polyamic acid and the dopamine jointly improve the dispersity of the polyphenylene sulfide, the mechanical property of the composite material is improved, and the polyphenylene sulfide thermoplastic composite material has a good application prospect and can be used as a polyphenylene sulfide thermoplastic composite material.

The present invention relates to compounds that include a thiazolopyridylamide structure, methods for their synthesis, and the use of such compounds to inhibit DNA polymerase theta (Pol theta) and in the treatment of various diseases, including cancer.

The invention relates to a pyrrolo [2, 3-d] pyrimidine-4-amine derivative and application thereof in medicine, in particular to a compound shown in a formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, and application of the compound in preparation of medicines for treating sGC-related diseases.

The present invention relates to isoxazoline compounds of formula I, wherein the variables have the meanings as defined in the description; to a composition comprising the same; to active compound combinations comprising the same; and to the use thereof for protecting growing plants and animals from infestation or infestation by invertebrate pests; furthermore, to seeds comprising such compounds. Preferred compounds are, for example, N-(3-(aminomethyl)-4-fluorophenyl)-5-(4-fluorophenyl)-5-(trifluoromethyl)-4, 5-dihydroisoxazole-3-amine derivatives. # imgabs0 #

Provided herein are novel drug-linker conjugates and antibody-drug conjugates of imidazoquinoline amine derivatives, which have agonistic activities towards Toll-like receptors (TLRs), in particular TLR7 and / or TLR8, as well as pharmaceutical compositions and methods of treatment thereof for certain diseases or conditions mediated by or associated with TLR7 and / or TLR8 (e.g., graft rejection, autoimmunity, inflammation allergy, asthma, infection, sepsis, cancer and immunodeficiency).

The invention discloses a chiral alpha-hydroxyamide derivative as well as a synthesis method and application thereof. The synthesis method comprises the following steps: in the presence of a chiral thiourea catalyst, aromatic amine and alpha-carbonyl acyl silane are subjected to a catalytic asymmetric nucleophilic addition reaction in a solvent under illumination, and the chiral alpha-hydroxyamide derivative is generated. The reaction takes illumination as driving force, so that green synthesis is realized; and secondly, due to the introduction of the chiral thiourea catalyst, the enantioselectivity is remarkably improved, the use of a metal catalyst is avoided, and the concept of green chemistry is met. In addition, the reaction substrates alpha-carbonyl acyl silane and aromatic amine are cheap and easily available chemicals, so that the synthesis cost is reduced, and the feasibility and practicability of the method are improved.

The invention discloses a ketoazine-based polymer, an anion exchange membrane and a preparation method and application of the ketoazine-based polymer and the anion exchange membrane. A first linking group and a second linking group are mixed and then mixed with an aryl monomer A in an aprotic solvent of halogen atoms; slowly adding a super acid mixture; performing polymerization reaction in an environment of-5 to 3 DEG C to obtain a reaction solution; pouring the reaction liquid into a first mixed solvent to obtain PAAz; carrying out primary quaternization reaction on PAAz through carbonate, bicarbonate or hydroxide salt of alkali metal, and adding an organic base catalyst to assist the primary quaternization reaction; in the first quaternization reaction, a quaternization reagent is added; and pouring into a second mixed solvent, and precipitating to obtain purified PAAz. Under the condition of super acid catalysis, two or more alicyclic amine derivatives containing ketone groups react with one or more aromatic fused rings to generate a polymer containing secondary or tertiary amine. And carrying out quaternization treatment to finally form the cationic polymer.

The present disclosure relates to an OLED that includes a first electrode; a second electrode facing the first electrode; a first emitting material layer including a first host being an anthracene derivative and a first dopant being a pyrene derivative and positioned between the first and second electrodes; and a first electron blocking layer including an electron blocking material of a heteroaryl-substituted amine derivative and positioned between the first electrode and the first emitting material layer, wherein at least one of hydrogen atoms in the anthracene derivative and the pyrene derivative is deuterated.

The invention belongs to the technical field of friction power generation, and particularly relates to a microcrystalline cellulose triboelectric composite film, a preparation method thereof and a triboelectric nano-generator. Comprising the following steps: adding soluble trivalent iron salt into microcrystalline cellulose dispersion liquid, uniformly dispersing, and adding polyethyleneimine in a stirring state to form a dispersion system; adjusting the pH value of the dispersion system, adding a cross-linking agent for activation to obtain a mixture, carrying out a cross-linking reaction to cross-link microcrystalline cellulose and a liquid amine derivative, complexing with ferric ions to obtain a composite film precursor, and drying the composite film precursor to obtain the microcrystalline cellulose triboelectric composite film. According to the invention, microcrystalline cellulose is taken as a matrix, polyethyleneimine and microcrystalline cellulose are crosslinked and complexed with Fe < 3 + >, and a recyclable, biodegradable and biocompatible composite film is constructed, so that the triboelectricity output and humidity adaptability of the cellulose-based triboelectricity material are improved, and the energy efficiency of the material in a self-powered process in a high-humidity environment is enhanced.

The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.

The invention relates to the field of medicinal chemistry, and discloses application of cyclobutene amide compounds in antiviral drugs. The structural characteristics of the compounds are as shown in a general formula (I), wherein EWG is an electron withdrawing group and is selected from aryl-substituted sulfonyl; r1 is selected from alkyl or aryl; r2 is selected from alkyl or aryl; and n represents the number of carbon atoms and may be 1 or 2. In-vitro pharmacodynamic studies show that the series of compounds have a remarkable inhibition effect on influenza A virus (H1N1 subtype), and the antiviral efficacy of the compounds is obviously superior to that of a clinical common antiviral drug ribavirin. In addition, toxicological evaluation proves that the compounds have ideal safety characteristics. The cyclobuteneamide derivative can be used as an effective component for developing an anti-influenza A virus drug, and a new candidate drug molecule is provided for clinical treatment of influenza virus infection. # imgabs0 #

The use of certain alkanolamines in hair treatment compositions as an alternative to some or all ammonium hydroxide is disclosed. These compositions are useful in curling and straightening applications. Benefits include similar or reduced hair damage; relatively mild alkalinity; the curling or straightening efficiency and the shape retentivity are very good; heating is not needed; and useful results have been obtained using different hair races.

The invention discloses an amide derivative and its application. The amide derivative is 5-chloro-N-(2-fluoro-3-(2-iodo-4-(perfluoropropane-2-yl)-6-(trifluoromethyl)phenyl)carbamoyl)phenyl)thiophene-2-carboxamide. The amide derivative of the invention has excellent persistence and rapidity in killing and controlling agricultural and forestry pests, especially chewing mouthparts pests such as diamondback moth, beet armyworm, cotton bollworm, etc., and is not easy to produce cross-resistance with existing diamide compounds. Moreover, the safety to mammals is very excellent, and the safety to beneficial insects such as bees is excellent. The product has huge market potential in the field of agricultural and forestry pest control in the future and has very good prospects for promotion and application.

The invention discloses a cycloalkane substituted amine derivative as well as a preparation method and application thereof. Specifically disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The cycloalkane substituted amine derivative provided by the invention has good 5-HT2A receptor agonistic activity and a wide application prospect. # imgabs0 #

The invention belongs to the technical field of synthesis of organic compounds, and particularly relates to a synthesis method of a thiophene naphthenic amine derivative. The method comprises the following steps: reacting with benzylamine to generate a halogenated thiophene imine derivative, carrying out cyclization reaction in the presence of alkali to generate a thiophene naphthenic imine derivative, and reacting with organic acid to generate the product thiophene naphthenic amine derivative, so that the reaction conditions are mild, the yield is high, and the method is more suitable for industrial production.

The present invention provides a method for producing a compound represented by formula (I) suitable for mass synthesis as API. Provided according to one aspect of the present invention is a method for producing a compound represented by formula (I) or a salt thereof, the method including deprotecting a protecting group represented by R1 in formula (II) under basic conditions to thereby form a compound represented by formula (I) or a salt thereof.

The invention relates to the technical field of microbial probiotic preparations, in particular to a sodium alginate multifunctional composite microsphere as well as a preparation method and application thereof. The sodium alginate multifunctional composite microspheres are obtained by dissolving the carbohydrate vesicles, the traditional Chinese medicine nanoparticles and the probiotics in a sodium alginate solution and then dropwise adding the solution into a calcium chloride solution through an ionic cross-linking effect. According to the invention, the amphiphilic xylooligosaccharide-cystamine derivative with H2S response is synthesized through a click reaction on the basis of prebiotic xylooligosaccharide. And the amphipathic saccharide vesicles are obtained through self-assembly by virtue of hydrophilic and hydrophobic effects. Sanguinarine iodide prepared by purification, separation and reflux and baicalin are self-assembled in an aqueous solution through a non-covalent bond, and the traditional Chinese medicine nanoparticles are prepared through ultrasonic treatment. An in-vitro simulated release experiment proves that the sodium alginate multifunctional composite microsphere is relatively low in release rate under an acidic condition, so that substances are favorably delivered to intestinal tracts; and the release of encapsulated substances can be better realized in neutral and alkaline environments.

The present invention is directed to (phthalazin-3-yl)amine derivatives of formula (I) as BFL-1 inhibitors for use in methods of treatment of leukemias, lymphomas and other cancers.

The invention provides an aldehyde insect pheromone derivative, which takes a compound containing at least one primary amine group as a carrier, and aldehyde insect pheromone forms an imine derivative with the compound through chemical reaction. The invention also provides a preparation method, application and a release method of the aldehyde insect pheromone derivative. According to the aldehyde insect pheromone derivative provided by the invention, aldehyde insect pheromones are treated in a chemical reaction manner, the stability of the aldehyde insect pheromones can be remarkably improved, slow release and controlled release of the pheromones can also be realized, the carrier material is wide in source, more in selectivity, convenient and economical, and in addition, the aldehyde insect pheromone derivative has good application prospects. The aldehyde insect pheromone derivative provided by the invention can also realize combined fixation and release of various pheromones, so that trapping, prevention and control of various insects can be realized.