89 results about "Dihydropyridine" patented technology

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 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.

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.

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 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 application belongs to the field of organic synthesis, and particularly relates to a method for synergistically synthesizing 1,1-diaryl-2-alkyl compounds by using nickel and light. The method comprises the following steps: using styrene derivatives, p-bromoacetophenone and tert-butyl bromide as raw materials, and mixing a metal nickel catalyst (nickel bis(acetylacetone)), a photocatalyst (1,2,3,5-tetrakis(carbazole-9-yl)-4,6-dicyano benzene), a nitrogen ligand ((4S,4'S)-1,1'-bis(3-tert-butylphenyl)-4,4',5,5'-tetrahydro-4,4'-bis[(1S)-1-methylpropyl]-2,2'-bis-4H-imidazole), a Bronsted base (N,N-dicyclohexylmethylamine), a reducing agent (1,4-dihydropyridine derivatives) and an organic solvent (glycol dimethyl ether, isopropyl ether) to generate a three-component cross-coupling reaction and synthesize 1,1-diaryl-2-alkyl compounds with one chiral center. The three-component cross-coupling reaction is realized by using nickel and light, so that the use of a metal reducing agent is avoided, and the preparation raw materials are not needed. The method has the advantages of high reaction yield, high enantiomeric selectivity, fast reaction speed, easy-to-obtain raw materials and simple process.

This invention discloses an isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound, its preparation method, and its applications, belonging to the field of organic compound synthesis technology. Using N-indole-linked o-alkynyl nitrone compounds as raw materials, this invention employs a two-step, one-pot method to provide a novel synthesis of isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compounds that are difficult to prepare using conventional methods. This method is based on a rhodium-catalyzed internal redox / dearomatization [3+2] cycloaddition reaction and a cerium ammonium nitrate-promoted oxidative debenzylation / spirocyclic tandem reaction strategy. The method of this invention has advantages such as simple operation, low catalyst loading, broad substrate range, single stereoselectivity, and high yield. The isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound prepared by this invention has a certain inhibitory effect on plant pathogens and can be potentially applied to the control of tomato gray mold, wheat scab, and rice sheath blight.

The present disclosure relates to a variant polypeptide having attenuated dihydrodipicolinate reductase activity and a method of producing L-threonine using the same.

Disclosed herein are novel 2,3-dihydro-lH-pyrido[2,3-b][l,4]oxazepine or 1,2,3,4-tetrahydropyrido[2,3-b][l,4]oxazepine derivatives that act as antagonists of IAP (inhibitor of apoptosis proteins), also known as Smac mimetics. Disclosed herein are uses of these antagonists for inducing or sensitizing cells to induce apoptotic cell death, as well as uses of such compounds for treating proliferative diseases, such as cancer.

A method for synthesizing 6-substituted 5,6-dihydropyridinebisindole compounds includes the following steps: 1) mixing a bisindole derivative with DMF, stirring at a certain temperature to dissolve the bisindole derivative, and then adding an organic amine; 2) dissolving a catalyst CuCl2·2H2O in DMF, adding the CuCl2·2H2O DMF solution to the mixed solution from step 1), and reacting; 3) repeatedly extracting with ethyl acetate and ultrapure water, collecting the organic layer, removing water and ethyl acetate, eluting the collected solution, removing the solvent, and obtaining the product. This method efficiently synthesizes 6-substituted 5,6-dihydropyridinebisindole compounds through a one-step reaction of a bisindole derivative with an organic amine, providing a synthetic basis for the study of the biological functions of these compounds.

This invention provides a method for detecting actual radiation dose, comprising: A) mixing medical-grade polymer raw materials and dihydropyridine 3,5-dicarboxylic acid derivatives to prepare a standard plate; B) placing a dosing strip on the standard plate, irradiating it, and measuring the actual radiation dose received by the standard plate using the dosing strip; irradiating the standard plate under the same conditions, and measuring the fluorescence intensity using fluorescence spectroscopy; C) constructing a standard curve with the actual radiation dose as the abscissa and the fluorescence intensity as the ordinate; D) measuring the fluorescence intensity of the plate to be tested using fluorescence spectroscopy, and calculating the actual radiation dose using the standard curve. The method provided by this invention involves adding a radiation-resistant additive with fluorescence response to the medical polymer raw material, and calculating the actual radiation dose using a standard curve. This invention provides a method for monitoring radiation dose distribution, which has the advantages of high biosafety and accurate detection.

Provided herein are pharmaceutical compositions comprising a class of calcium channel blockers and at least one chelating agent. More specifically, the pharmaceutical compositions comprise at least one 1,4-dihydropyridine (DHP) compound and at least one chelating agent. The chelating agents used in this disclosure can decrease the degradation of the constituent DHPs of the DHP compositions. The DHP compositions can be used to treat cardiovascular disorders and are more stable for prolonged periods of time.

The application relates to 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 pharmaceutical preparations. The application provides application of the dihydropyridine compound or the salt thereof in preparation of the medicine for preventing and / or treating HPV infection, wherein the dihydropyridine compound is selected from one or more of nifedipine, amlodipine, lercanidipine, nimodipine, nitrendipine, nisoldipine, felodipine, benidipine, lacidipine and azelnidipine. The application scheme first reports the application of the dihydropyridine compound or the salt thereof in prevention and / or treatment of HPV, and in-vitro cell experiments are carried out through azelnidipine in the dihydropyridine compound, and further, the inhibiting effect of the dihydropyridine compound on HPV virus is verified through medicine administration of a mouse intradermal virus inoculation model and medicine administration of a mouse vaginal virus inoculation model.

The invention discloses application of dihydropyridine in preparation of a medicine for treating choroidal neovascularization, and belongs to the technical field of biological medicines.The proliferation, migration and lumen formation of human choroidal endothelial cells under the hypoxia condition are inhibited through dihydropyridine, and blood vessel leakage, area and volume of laser-induced choroidal neovascularization of mice are reduced; the formation of laser-induced choroidal neovascularization of mice is relieved through dihydropyridine, and the proliferation, migration and lumen formation of hypoxia-induced human choroidal endothelial cells can be down-regulated, so that the PHD has a treatment effect on CNV.