59 results about "Dihydropyridine" patented technology

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 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 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.

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 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.

This invention discloses a 2-oxo-1,2-dihydropyridine-3-amide compound, its preparation method, and its uses, belonging to the field of pharmaceutical technology. In the 2-oxo-1,2-dihydropyridine-3-amide compound structure disclosed in this invention, the pyrimidine ring structure can theoretically form hydrogen bond interactions with the receptor, making it more suitable for binding to Mer and c-Met kinases. Furthermore, the novel structural type of compound of this invention exhibits strong enzyme inhibitory activity while also showing specificity and selectivity against tumor cells and normal cells. Simultaneously, the novel structural compound has high safety and fewer toxic side effects, making it easier to use as an anti-tumor drug.

This invention belongs to the field of analytical chemistry, specifically relating to an analytical detection method for related substances in dihydropyridine compounds. Specifically, it includes adding ninhydrin to a test solution containing dihydropyridine compounds to prepare a test solution, and then using liquid chromatography-mass spectrometry (LC-MS) to detect the content of compound I in the dihydropyridine compounds. The analytical detection method provided by this invention has good precision, high accuracy, high sensitivity, good linearity, good stability of the test solution, low detection limit, and accurate detection results.

Disclosed are spray-dried formulations of 4-chloro-5-(4-(4-fluoro-2-(trifluoromethyl)phenoxy)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)pyridazin-3(2H)-one, methods and compositions for making the same, and solid dosage forms comprising the same. The dosage forms described herein are useful in methods of treating kidney diseases or neuropathies associated with diseases or conditions, and in methods of treating pain, anxiety, or depression.

The invention discloses injectable dextran hydrogel with antibacterial and self-healing properties and a preparation method of the injectable dextran hydrogel. According to the hydrogel, beta-keto ester grafted glucan, oxidized glucan, polylysine carbon dots and ammonium acetate are used as raw materials, dual covalent crosslinking is performed through a Hantzsch reaction and an aldehyde-amine Schiff base reaction, and the hydrogel has a dual-network structure. Wherein the beta-keto ester is grafted with the glucan, the oxidized glucan and the ammonium acetate are subjected to Hantzsch reaction to form a 1, 4-dihydropyridine cross-linking point; meanwhile, the oxidized dextran and the polylysine carbon dots are subjected to aldehyde-amine Schiff base reaction to form dynamic imine bond crosslinking points. The double-crosslinking strategy endows the hydrogel with good self-healing performance and injectable performance. In addition, due to the introduction of the polylysine carbon dots, the glucan hydrogel shows broad-spectrum antibacterial activity. The preparation method disclosed by the invention is mild in condition, simple and efficient, and the prepared hydrogel has a wide application prospect in the biomedical fields such as antibacterial dressings and the like.

The present disclosure relates to a crystalline form of a fumarate salt of a diaminocyclopentyl-substituted heteroaryl derivative and uses thereof. In particular, the present disclosure provides a crystalline form A of a fumarate salt of 1-(6-{[(1S,3S)-3-(6,7-dihydro[1,4]dioxino[3,2-d]pyrimidin-2-ylamino)cyclopentyl]amino}pyridin-3-yl)-1,2-dihydropyridin-2-one and a preparation method thereof, which has good stability and can be better used for clinical treatment.

The purpose of the present invention is to provide: a cured product which is included in an electronic component and which has excellent mechanical properties and excellent migration resistance, while achieving both residue suppression in a pattern hem and excellent halftone characteristics; and an electronic component having excellent migration resistance. The present invention is a photosensitive composition containing (A) a binder resin and (C1-C1) an oxime ester compound, and further containing (B) a radical polymerizable compound and / or (F) a cross-linking agent, the (C1-C1) oxime ester compound having a structure (Ia): a condensed polycyclic heterocyclic structure comprising two rings; or a condensed polycyclic heterocyclic structure which comprises a naphthalene structure, a piperidine structure, a tetrahydropyridine structure, a dihydropyridine structure, a pyrrolidine structure or a pyrroline structure and is composed of three rings; the structure (Ib) is an oxime ester carbonyl structure; and structure (Ic): aromatic structure.

Spray-dried formulations of 4-chloro-5-(4-(4-fluoro-2-(trifluoromethyl)phenoxy)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)pyridazin-3(2H)-one, methods and compositions for their preparation, and solid dosage forms containing them are described. The described dosage forms are useful for the treatment of kidney disease or neuropathies associated with illnesses or conditions, as well as for the treatment of pain, anxiety, or depression.

The application belongs to the field of medicine, and particularly relates to a 4-phenoxy quinoline compound containing dihydropyridine amide and dihydropyridazine amide and application thereof. The 4-phenoxy quinoline compound containing dihydropyridine amide and dihydropyridazine amide and pharmaceutically acceptable salts thereof have the structure of general formula (I). The application also relates to the compounds of general formula (I) having a strong inhibitory effect on c-Met kinase, and further relates to the application of the compounds in the preparation of drugs for treating and / or preventing diseases caused by abnormally high expression of c-Met kinase, particularly in the preparation of drugs for treating and / or preventing cancer. The compounds of the application are particularly suitable for the preparation of drugs for treating and / or preventing gastric cancer and breast cancer.

The application provides an antioxidant polyvinyl alcohol derivative containing a 1,4-dihydropyridine structure and a preparation method and application thereof. The antioxidant polyvinyl alcohol derivative contains a 1,4-dihydropyridine structural unit, a vinyl alcohol structural unit and a vinyl acetate structural unit. The preparation method is as follows: polyvinyl alcohol is dissolved in anhydrous organic solvent, divinyl ketone is added for reaction to obtain a polyvinyl alcohol derivative containing a beta-diketone, in the presence of a catalyst, an aldehyde compound, an ammonia source compound and a 1,3-diketone compound are added into the obtained polyvinyl alcohol derivative containing a beta-diketone for Hantzsch reaction to obtain the antioxidant polyvinyl alcohol derivative containing the 1,4-dihydropyridine structure. The prepared polyvinyl alcohol derivative has excellent antioxidant performance and can be applied to the fields of food packaging, biological medicine, health care and the like.

This invention belongs to the field of compound synthesis technology, specifically relating to a diarylguanidine derivative with anti-lymphoma function, its preparation method, and its application. The chemical name of this diarylguanidine derivative is 3-ethyl-5-methyl-(E)-4-(2-chlorophenyl)-6-methyl-2-((2-(2-(3-phenoxyphenyl)-3-phenylguanidinyl)ethoxy)methyl)-1,4-dihydropyridine-3,5-dicarboxylic acid ester. The preparation method includes step 1: reacting phenol and 4-bromonitrobenzene in DMF solution to obtain 4-nitrodiphenyl ether compounds; step 2: placing the 4-nitrodiphenyl ether compounds in an iron-containing ethanol solution to obtain 4-aminodiphenyl ether compounds; step 3: placing the 4-aminodiphenyl ether compounds and phenyl thioisocyanate in tetrahydrofuran solution to react and obtain 1-(4-phenoxyphenyl)-3-phenylurea compounds; and step 4: reacting the 1-(4-phenoxyphenyl)-3-phenylurea compounds with amlodipine under light irradiation to obtain the target compound. The product of this invention is intended for use in the preparation of anti-lymphoma drugs.

The present invention relates to novel forms of Compound I, preparation thereof, pharmaceutical composition containing the same and use thereof, wherein, the compound is (S)-5-((1-(3-(5-methyl-3-(trifluoromethyl)-8,9-dihydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazin-7(6H)-yl)-3-oxopropoxy)propan-2-yl)oxy)-4-(trifluoromethyl)pyridazin-3(2H)-one.

The application discloses a preparation method of a monoamine oxidase B inhibitor, and comprises the following steps: 6-fluoroindole and 1-(dimethylamino)-2-nitroethylene are subjected to trifluoroacetic acid catalysis to generate 6-fluoro-3-[(E)-2-nitrovinyl]-1H-indole, and then subjected to sodium borohydride and iron powder / hydrochloric acid reduction to generate 6-fluoro-tryptamine; under an acidic condition, Pictet-Spengler reaction is carried out between 6-fluoro-tryptamine and ethyl glyoxylate to generate ethyl 7-fluoro-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-1-carboxylate and 7-fluoro-4,9-dihydro-3H-pyrido[3,4-b]indole-1-carboxylate, and then subjected to oxidative dehydrogenation aromatization reaction to generate ethyl 7-fluoro-9H-pyrido[3,4-b]indole-1-carboxylate; under the catalysis of aluminum trichloride, amine ester exchange reaction is carried out between ethyl 7-fluoro-9H-pyrido[3,4-b]indole-1-carboxylate and 3-fluorobenzylamine to generate a target compound. The method has high overall yield.

The application discloses industry scalable methods of using bifunctional bidentate pyridone-carboxylic acid ligands, such as 2-methyl-2-(6-oxo-1,6-dihydropyridin-2-yl)propanoic acid, that enable room-temperature Pd-catalyzed C—H hydroxylation of a broad range of benzoic and phenylacetic acids with an industry-compatible oxidant, aqueous hydrogen peroxide, at room temperature. Further disclosed are methods of derivatization of the resulting hydroxylation products, synthesis of polyfluorinated natural products coumestan or pterocarpene from phenol building blocks, and hydroxylation of ibuprofen using this methodology,