121 results about "Dihydropyridine" patented technology

The invention relates to an application of a dihydropyridine compound or a salt thereof in preparation of a medicine for preventing and / or treating HPV infection, and belongs to the technical field of medicines and medicinal preparations. The invention provides application of a dihydropyridine compound or a salt thereof in preparation of a medicine for preventing and / or treating HPV (human papillomavirus) infection. The dihydropyridine compound is selected from one or more of nifedipine, amlodipine, lercanidipine, nimodipine, nitrendipine, nisoldipine, felodipine, benidipine, lacidipine and azelnidipine. According to the scheme, the application of the dihydropyridine compound or the salt thereof in prevention and / or treatment of HPV is reported for the first time, and an in-vitro cell experiment is carried out through azelnidipine in the dihydropyridine compound; furthermore, the inhibition effect on the HPV virus is verified through mouse intradermal vaccination virus model drug delivery and mouse vaginal vaccination virus model drug delivery.

The invention relates to a synthetic method of a finelrenone racemate, which comprises the following steps: carrying out Knoevenagel condensation, Hantzsch dihydropyridine synthesis, O-ethylation and deprotection four-step reaction, selecting a compound shown as a formula (2) and a compound shown as a formula (3) as initial raw materials, and carrying out Knoevenagel condensation reaction under the combined action of organic alkali and organic acid to synthesize a compound shown as a formula (4); carrying out Hantzsch reaction on the compound in the formula (4) and a compound in a formula (5) to synthesize a compound in a formula (6); carrying out O-ethylation reaction on the compound shown in the formula (6) and an ethylation reagent under the catalysis of acid to synthesize a compound shown in a formula (7); finally, 2, 4-dimethoxybenzyl is removed from the compound shown in the formula (7) under the promotion of acid to synthesize the finerenone racemate, the method is high in selectivity and simple in post-treatment, the yield and purity of the product are high, the HPLC purity can reach 99% or above, a new synthesis route and method are developed for synthesizing the finerenone racemate, and the method has good application potential and research value.

The invention provides a polyvinyl alcohol derivative as well as a preparation method and application thereof. The polyvinyl alcohol derivative comprises a structural unit of 1, 4-dihydropyridine, a structural unit of vinyl alcohol and a structural unit of vinyl acetate. The preparation method comprises the following steps: dissolving polyvinyl alcohol in an anhydrous organic solvent, adding an acetoacetic acid reagent for reaction to obtain a polyvinyl alcohol derivative containing beta-diketone, and in the presence of a catalyst, reacting an aldehyde compound containing an aggregation-induced emission structure, an ammonia source compound and 1, 2-diketone to obtain the beta-diketone-containing polyvinyl alcohol derivative. And adding a 1, 3-diketone compound into the obtained polyvinyl alcohol derivative containing beta-diketone, and carrying out Hantzsch reaction, so as to obtain the antioxidant aggregation-induced emission polyvinyl alcohol derivative containing the 1, 4-dihydropyridine structure. The polyvinyl alcohol derivative disclosed by the invention has excellent oxidation resistance and aggregation-induced emission performance, and can be applied to the fields of food packaging, biological medicine, health care and the like.

The application belongs to the field of organic synthesis, and particularly relates to a synthesis method of 2-(3,3-dimethylbutyl)pyridine. 2-vinylpyridine, brominated tertiary butane, a mixed solution of dimethyl ether and isopropyl ether as a reaction system solvent, nickel iodide as a nickel salt, bipyridine as a ligand, dicyclohexylmethylamine as a base in the system, 2,6-dimethyl-3,5-diethyl-1,4-dihydropyridine as a reducing agent, a photocatalyst 2,4,5,6-tetrakis(9 ‑ Carbazole) - m-phenylenedinitrile, under the condition of room temperature and nitrogen atmosphere, a reduction cross-coupling reaction is used to synthesize 2-(3,3-dimethylbutyl)pyridine. The application uses inexpensive nickel metal as a catalyst, constructs a cross-coupling reaction of carbon-carbon bond, and has the advantages of mild reaction condition, high economy and the like.

In one aspect, the use of compounds as active agents for the treatment and prevention of hearing impairment, and methods of using the compositions for the treatment and / or prevention of hearing impairment or disorder, are disclosed. In zebrafish and mice, the (E)-1-(3-(3, 4, 5-trimethoxyphenyl) acryloyl)-S, 6-dihydropyridine-2 (1H)-ketone and the derivative have an excellent protective effect on hearing loss induced by antibiotics, and the application of the (E)-1-(3-(3, 4, 5-trimethoxyphenyl) acryloyl)-S, 6-dihydropyridine-2 (1H)-ketone and the derivative has a good application prospect. In one aspect, (E)-1-(3-(3, 4, 5-trimethoxyphenyl) acryloyl)-S, 6-dihydropyridine-2 (1H)-one and derivatives are useful as therapies for the treatment and / or prevention of hearing loss. This abstract is intended as a scanning tool for purposes of retrieval in the particular art and is not intended to be limiting of the present invention.

The present invention relates to a pharmaceutical composition for treating myopia, preventing myopia and / or suppressing myopia progression, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a synthesis method of 1-(tert-butyl)-3-ethyl-4-(4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborane-2-yl)-5, 6-dihydropyridine-1, 3 (2H)-dicarboxylate. According to the invention, 1-(tert-butyl)-3-ethyl-4-oxopiperidine-1, 3-diformate, namely the compound A, is taken as a base material, two-step reaction is carried out, the reaction conditions are relatively mild, the product yield is high, and the operation is easy.

The application discloses a trifluoromethyl alkyl quinoline compound, a synthesis method and anti-tumor application in the field of organic synthesis and medicinal chemistry, which is synthesized from trifluoropropylene quinoline or N-benzoyl pyrrole (A) and redox active ester (B) as raw materials, dimethyl sulfoxide as a solvent, dihydropyridine as an electron donor, and under visible light irradiation, a trifluoromethyl alkyl quinoline and analogues (C) are synthesized at a high yield. The specific reaction formula is as follows: The compounds provided by the application all have excellent anti-tumor activity and low toxicity to normal cells, and therefore have application prospects for preparing anti-tumor drugs.

The invention relates to a synthesis method of 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, which comprises the following four steps: carrying out a Knoevenagel condensation reaction, carrying out a Hantzsch dihydropyridine synthesis method, carrying out an O-ethylation reaction and carrying out a deprotection reaction to synthesize the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, and carrying out a reaction to obtain the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide. The preparation method of the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide has the advantages that the selectivity is high, the post-treatment is simple, the yield and the purity of the product are high, a new synthesis route and method are developed for synthesizing the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, the amplified production is conveniently realized, and the method is suitable for industrial production. The method has good application potential and research value.

The present disclosure provides compounds of Formula I that are inhibitors of the histone methyltransferase polycomb repressive complex 2 (PRC2) and its subunits, including embryonic ectoderm development (EED) proteins, and are therefore useful for treating diseases treatable by inhibiting dysregulation of PRC2 and EED, such as cancer. Pharmaceutical compositions containing such compounds and methods for preparing such compounds are also provided. In certain embodiments, the subject matter described herein is directed to compounds of Formula I, including all of the subformulas of Formula I, or pharmaceutically acceptable salts or solvates thereof. JPEG2026504602000095.jpg5157

Provided herein is (R)-7-chloro-2-((1r,4R)-4-(3-methoxyaetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof for use in methods of treating certain cancers having at least one BAP1 mutation.

The present application provides a method for preparing a high-purity key intermediate M2 of dicardipine drugs, belonging to the technical field of drug intermediate preparation. A dehydrating agent is added during the preparation of the intermediate M2, and the dehydrating agent is an orthoester dehydrating agent. Using the method provided in the present application, the yield of the intermediate M2 is 84.3%, the HPLC purity is 99.63%, M2Z3: 0.17%; M2Z4: 0.15%; other impurities <0.10%, and the content of impurities P0Z4 (i.e., M2Z3) and P0Z5 in the further prepared nicardipine is determined to be: P0Z5 <0.02%, P0Z4 <0.02%.

The present invention relates to agents useful in the treatment and / or prophylaxis in mammals, pharmaceutical compositions comprising such compounds, and their use as menin / MLL protein / protein interaction inhibitors useful in the treatment of diseases such as cancer, including but not limited to leukemia.

The present application provides a kind of preparation of doravirine intermediate 3-chloro-5-[[2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl]oxy]benzonitrile synthesis method, the method includes from formula D compound and 3-chloro-5-hydroxybenzonitrile in the presence of base, catalyst coupling to obtain formula E compound, formula E compound is cyclized to obtain 3-chloro-5-[[2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl]oxy]benzonitrile in the presence of acid.The method uses cheap starting material, avoids the use of noble metal catalyst and expensive material fragment, process operation and post-processing are simple, suitable for industrial scale production.

Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

Disclosed herein is a method of treating breast cancer by administering 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile, alone or in combination with a second agent such as aromatase inhibitor or a selective estrogen receptor degrader. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and second agent such as aromatase inhibitor or a selective estrogen receptor degrader.

The invention relates to a polymorphic form of hydrobromide or hydrochloride of 5-(6-(4-(cyclopropylmethyl) piperazine-1-yl)-2-methylpyridine-3-yl)-N-((4, 6-dimethyl-2-oxo-1, 2-dihydropyridine-3-yl) methyl)-3-(N-ethylcyclopropanecarboxamide)-2-methylbenzamide, a pharmaceutical composition of the polymorphic form and application of the polymorphic form and the pharmaceutical composition of the hydrobromide or hydrochloride of the 5-(6-(4-(cyclopropylmethyl) piperazine-1-yl)-2-methylpyridine-3-yl)-N-(4, 6-dimethyl-2-oxo-1, 2-dihydropyridine-3-yl)-3-(N-ethylcyclopropanecarboxamide.

The invention provides an application of a pyridine ring compound A in the aspect of inhibiting phenylalanyl-tRNA (transfer ribonucleic acid) synthetase. Specifically, the invention provides a compound as shown in a formula A, or a pharmaceutically acceptable salt or ester thereof, or an optical isomer and raceme thereof, or a hydrate or solvate thereof, or a deuterated compound thereof as a phenylalanyl-tRNA synthetase inhibitor. The invention also relates to application of the phenylalanyl-tRNA synthetase in preparation of drugs for treating diseases or symptoms related to activity or expression quantity of the phenylalanyl-tRNA synthetase.

Cosmetic preparation containing a) 4-dicyanomethylene-2,6-dimethyl-1,4-dihydropyridine-N-(ethyloxysulfate ester salt), b) 2,4,6-Tris-(biphenyl)-1,3,5-triazine.

The present disclosure provides compounds of Formula I that are inhibitors of histone methyltransferase multi-comb inhibition complex 2 (PRC2), including embryonic ectoderm development (EED) protein, and its subunits, and are thus useful in the treatment of diseases that can be treated by inhibition of disorders of PRC2 and EED, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

The present invention relates to a process for the synthesis of Pirfenidone (1) from 5-Methyl-3,4-dihydro-2-pyridone and halobenzene (chlorobenzene, bromobenzene, or iodobenzene) in the presence of a catalytic system consisting of a copper salt and an organic ligand, in the presence of a base.

The application relates to a dihydropyridine small-molecule compound and a preparation method and application thereof in preparing a drug for treating neuroblastoma, and belongs to the technical field of drug preparation. The application discloses a dihydropyridine small-molecule compound, a structural formula of which is as shown in the description, which can be used for preparing a drug for treating neuroblastoma with high ALDH18A1 expression, can effectively solve the problems of poor water solubility of YG1702, low inhibition rate of neuroblastoma and other drug application problems, and has a good application prospect.

The present invention belongs to the field of novel photocatalytic materials, and particularly relates to a photocatalyst for the efficient catalytic synthesis of halogenated aromatic hydrocarbons, as well as a preparation method and application thereof. The photocatalyst prepared by the present invention comprises titanium dioxide and a 1,4-dihydropyridine compound supported on the surface of the titanium dioxide; wherein the mass ratio of the 1,4-dihydropyridine compound to the titanium dioxide is 1:1 to 100; the present invention generates halogenated aromatic hydrocarbons by inducing a photocatalytic reaction using a visible light source. The scheme used is green, safe, and has high atomic utilization efficiency, avoids the use of toxic solvents, reduces energy consumption by reacting at room temperature, and the catalyst can be recycled and reused multiple times, reducing costs.

This invention discloses a rhodium-catalyzed asymmetric dearomatization cyclization method for synthesizing chiral dihydropyridine spirocyclic compounds, belonging to the field of asymmetric catalytic synthesis technology. The method uses a rhodium chiral bisphosphine complex and a base as the catalytic system, and alkynylpyridine salts and arylboronic acids as substrates to synthesize chiral dihydropyridine spirocyclic compounds through asymmetric dearomatization cyclization. The synthesis process of this invention is simple to operate, uses inexpensive and readily available reactants, operates under mild reaction conditions (not exceeding 60°C), exhibits high reactivity and enantioselectivity, complete reaction, specific products, and convenient separation, and can obtain pure products with high enantiomeric excess (up to 98%), showing excellent application prospects.

The present disclosure relates to solid forms and salts of 7-chloro-2- (4- (3-methoxyazetidin-1-yl) cyclohexyl) -2, 4-dimethyl-N- ((6-methyl-4- (methylthio) -2-oxo-1, 2-dihydropyridin-3-yl) methyl) benzo [d] [1, 3] dioxole-5-carboxamide, which is useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.

A method of inducing expression of a calcium channel and / or a calcium pump in a cell includes: irradiating the cell with light in a wavelength range of 315-325 nm. The calcium channel and / or the calcium pump is / are at least one selected from the group consisting of dihydropyridine receptor (DHPR), voltage-gated calcium channel (VGCC), ryanodine receptor (RYR), and sarcoendoplasmic reticulum Ca2+-ATPase (SERCA).

A method for preparing a meta-(chiral allyl)-substituted pyridine compound includes: S1, in a glove box filled with nitrogen, adding a boron catalyst, a solvent, pinacol borane, and pyridine to a reaction flask and reacting the mixture under stirring at room temperature to 120° C. for 1-12 hours to obtain dihydropyridine; S2, adding a metal catalyst and a chiral ligand to the reaction flask, stirring the mixture, then adding an alkali and allyl ester, and reacting the mixture at −10° C. to 60° C. for 12-24 hours to obtain a meta-(chiral allyl)-substituted dihydropyridine; and S3, placing the reaction flask in air, reacting the mixture under stirring at room temperature for 1 minute to 12 hours, then performing distillation under reduced pressure to remove the solvent and separation by column chromatography to obtain the meta-(chiral allyl)-substituted pyridine compound.

The invention provides antioxidant functional polyolefin containing a 1, 4-dihydropyridine structure as well as a preparation method and application of the antioxidant functional polyolefin. The polyolefin with the antioxidant function comprises a single polyolefin unit and a 1, 4-dihydropyridine substituted polyolefin unit. Wherein the 1, 4-dihydropyridine antioxidant monomer containing double bonds is prepared through a Hantzsch reaction, then polyolefin and the antioxidant monomer react under the conditions of illumination (390 nm), 120 DEG C and no water and oxygen under the catalysis of an iron-based catalyst TBAFeCl4, precipitation washing is conducted with ethyl alcohol, and the antioxidant functional polyolefin material containing the 1, 4-dihydropyridine structure is obtained after filtering and drying are conducted. The prepared polyolefin with the antioxidant function has excellent antioxidant performance and can be applied to the fields of food packaging, biological medicine, health care and the like.