198 results about "Amine derivatives" patented technology

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 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 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 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.

The invention belongs to the technical field of organic dyes, and particularly relates to an anti-ultraviolet dye taking tannic acid as a coupling component as well as a preparation method and application of the anti-ultraviolet dye. Under a stirring condition, adding a diazonium salt solution of an arylamine derivative into the mixed solution for reaction, and continuously stirring for reaction after the diazonium salt solution is added, so as to obtain a reaction solution; adjusting the pH value of the reaction liquid, evaporating, filtering and drying to obtain the anti-ultraviolet dye taking tannic acid as the coupling component. The uvioresistant dye taking tannic acid as a coupling component can endow real silk with color and uvioresistant function during dyeing; the dyeing process is simple and short in time, damage to real silk is small, dye liquor composition is simple, follow-up wastewater is easy to treat, and the whole dyeing process is low-carbon and environment-friendly.

The present invention provides novel drug-linker conjugates and antibody-drug conjugates of imidazo quinoline amine derivatives, which have agonistic activity against Toll-like receptors (TLRs), in particular TLR7 and / or TLR8, also provided are pharmaceutical compositions and methods of treatment against 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 provides compounds of formula (IA) and compounds of formula (IB) and pharmaceutically acceptable salts thereof; wherein A is selected from group (A1) and group (A2): wherein #1 is attached to the carbon atom forming the oxime moiety and wherein group (A1) is optionally substituted by one or two R10 and group (A2) is optionally substituted by one R10, and wherein R1, X, R2 and R10 are as defined in the claims, as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.

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.

The application belongs to the field of pharmaceutical chemistry, and specifically discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. In the benzimidazole amine derivative, R1 is a hydrogen atom or a bromine atom; and R2 is a substituted benzoyl group or a substituted benzyl group. Pharmacological results show that the benzimidazole amine derivative has good antagonistic activity on beta2AR and can negatively allosterically regulate the functional activity of isoprenaline (ISO).

Provided in the present invention are a solid form of a cyclic amine derivative, a preparation method therefor, and a pharmaceutical composition, specifically relating to a solid form of a compound of formula I or a salt thereof, a preparation method therefor, and a pharmaceutical composition. The compound of formula I or the salt thereof provided by the present invention has strong binding ability to apo(a) and high stability, and can be better used in clinical practice.

The invention belongs to the technical field of medicines, and relates to a compound as shown in a formula I, a stereoisomer, a prodrug and a pharmaceutically active metabolite thereof, pharmaceutically acceptable salt, a solvate and a hydrate thereof, a pharmaceutical composition containing the compound, and application of the compound in preparation of medicines for preventing and / or treating diseases or symptoms related to virus infection.

The present invention relates to a 5-cyclopropylpicolinamide derivative represented by chemical formula I or II, and the like. The compound and the like according to the present invention have an inhibitory ability against HPK1, and thus can be effectively used in the prevention, amelioration, and / or treatment of diseases related thereto.

The present invention aims to provide a novel compound having SF-1 antagonist activity and a polyfunctional molecule containing a moiety corresponding to the compound, particularly an SF-1 degrader. The present invention relates to a 3-phenylpropylamine derivative compound represented by the formula (1) and the like, and a polyfunctional molecule containing a moiety corresponding to the compound represented by the formula (1) and the like.

The preparation of high-value-added aromatic carboxylic acids via CO2 carboxylation coupling through activation of the benzyl C-H bond in alcohols / amines is a green and sustainable pathway to achieve CO2 resource utilization and contribute to carbon neutrality. However, this field currently faces challenges such as poor catalyst selectivity, low CO2 activation efficiency, and a narrow substrate applicability range, making it difficult to meet practical application needs. To address this issue, this patent discovers that in a heterogeneous electrocatalytic system, cuprous selenide (V2), rich in selenium vacancies, can be used... Se -Cu 2‑x Using Se as the core catalyst, it can not only efficiently promote the synergistic activation of benzyl C-H bonds and CO2 carboxylation, significantly improving the overall catalytic activity of the reaction, but also achieve precise chemoselective carboxylation control for different types of substrates. Specifically, this V Se -Cu 2‑x Se electrocatalysts can efficiently and selectively activate the benzyl C-H bond in alcohols and subsequently induce CO2 carboxylation, exhibiting excellent chemoselectivity in the conversion of benzyl alcohol to mandelic acid and its derivatives. Simultaneously, they also demonstrate excellent catalytic performance for amines, selectively catalyzing the carboxylation of amine substrates such as benzylamine with CO2 to directionally generate phenylglycine and aromatic amine-derived carboxylates. Crucially, in addition to typical benzyl alcohol and benzylamine, the substrate applicability of this catalytic system can be extended to various alcohols and amine derivatives, realizing the carboxylation transformation from simple model substrates to diverse functional molecules, providing a new approach for the large-scale preparation of high-value-added aromatic carboxylates.

The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of a pyrrolopyrimidine-4-amine derivative, which selects methanol, ammonium formate and formic acid as a reaction system to carry out directional reaction, avoids the use of high-pressure hydrogen and a high-pressure kettle, avoids the safety risk caused by high-pressure operation, and improves the yield of the pyrrolopyrimidine-4-amine derivative. And the alcoholic solution solves the problems of low solubility and obvious amplification effect of a starting material when water is used as a solvent in the prior art, and realizes homogeneous reaction. By adopting the fixed bed reaction unit, the problem of pipeline blockage caused by sublimation of ammonium formate is solved, the potential safety hazard in large-scale production is eliminated, the fixed bed reaction unit is used for continuous catalytic reaction to replace the traditional staged reaction, the production period is remarkably shortened, the production efficiency is improved, and the method is suitable for large-scale industrial production.

This invention discloses a method for preparing a bis(trifluoromethyl)quinazolinone amide derivative, comprising the following steps: under nitrogen protection, intermediate A is activated using an alkaline reagent, and then an acylation reagent is added to react and obtain the target compound. By innovatively utilizing a precise ratio system of bis(trimethyl)silylamine lithium (LiHMDS) and acetic anhydride, and conducting the reaction under low-temperature conditions, the acylation step can be completed in only 1-5 minutes, significantly shortening the overall process cycle compared to traditional methods and greatly improving production efficiency.

The invention provides anti-alopecia hair-strengthening scalp care essence and a preparation method thereof. The anti-alopecia hair-strengthening scalp care essence is prepared from the following raw materials in parts by mass: 50 parts of water; 8-12 parts of a humectant; 1-3 parts of a cosolvent; 0.3 to 0.6 part of organic acid; 0.5-1 part of a preservative; 2-5 parts of a plant extract; 3.5 to 4.5 parts of a nicotinamide-citryl flavone bisamide derivative; 15 to 20 parts of a signal peptide-zinc gluconate complex; 25 to 35 parts of a citryl amino acid amide derivative; 0.3 to 0.6 part of caffeine; 1-2 parts of a yeast extract; and 0.1-0.3 part of costus oil. The anti-alopecia hair-strengthening scalp care essence can prevent alopecia and improve the hair density.

An imidazo [2,1-f] [1,2,4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof which are used as a TLR7 agonist in the treatment of cancer are provided. Pharmaceutical compositions comprising the imidazo [2,1-f] [1,2,4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof are also provided.

The invention relates to a composition containing a glucosamine derivative, which comprises the following components based on the total weight of the composition: 55-70 wt%, preferably 55-65 wt%, more preferably 60-65 wt% of a compound as shown in a formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutically acceptable auxiliary materials. The invention also relates to application of the compound in preparation of a medicine for preventing or treating bone or joint diseases of a subject in need of the compound.

The invention provides an arylamine derivative and an organic electroluminescent device thereof, and relates to the technical field of organic electroluminescent materials. The invention aims to solve the technical problems of low luminous efficiency and short service life of an organic electroluminescent device caused by low mobility of a current hole transport material and low refractive index of a covering layer material. The compound provided by the invention has high hole mobility and refractive index, good thermal stability and good film-forming property, and can significantly improve the luminous efficiency and service life of a device, optimize the light extraction effect and block impurities. The organic light-emitting device can be widely applied to the fields of panel display, illumination light sources, flexible OLEDs, electronic paper, organic solar cells, organic photoreceptors or organic thin film transistors, indication boards, signal lamps and the like.