552 results about "Isoquinoline" patented technology

The present invention relates to tetrahydrobenzo-isoquinoline sulfonamides derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FIERI receptor.

The present invention belongs to the technical field of drug synthesis, relating to the synthesis of drugs for the prevention or treatment of diseases such as Alzheimer's disease and Parkinson's disease. Specifically, it relates to pharmaceutical intermediates and synthesis methods and isoquinoline derivatives and synthesis methods therefor. The pharmaceutical intermediate has a chemical structure shown in Formula II, wherein X is a halogen, and R is an amino protecting group. The synthesis of the pharmaceutical intermediate is simple, operates under mild conditions, and results in a high yield. Additionally, the pharmaceutical intermediate can be used to prepare isoquinoline derivatives.

The present application relates to the technical field of small molecule drugs, in particular to a isoquinoline drug and its application in improving or treating digestive tract tumors, and aims to provide a compound, a pharmaceutical composition containing the compound and its application in treating colorectal cancer and gastric cancer, and provides a 3,13-position substituted berberine derivative, the drug itself has less toxicity and does not affect the growth of normal human cells, and has a good application prospect in the development of novel antitumor drugs, especially in the development of anti-digestive tract tumor drugs.

The invention belongs to the technical field of perfluoropolyether fluorosilicone oil preparation, and particularly relates to polyvinyl perfluoropolyether fluorosilicone oil and a preparation method thereof. The preparation method comprises the following steps: firstly, carrying out ring-opening reaction on tetramethyl tetravinyl cyclotetrasiloxane and cyclosiloxane to prepare polyvinyl polysiloxane, then carrying out reaction on the polyvinyl polysiloxane and perfluoropolyether trimethoxy silane to prepare polyvinyl perfluoropolyether fluorosilicone oil; the modified catalyst, which is prepared by carrying out a reaction on 1, 2, 5-g] isoquinoline and 2-iodopropane to prepare modified organic alkali and then carrying out a reaction on the modified organic alkali, tris (pentafluorophenyl) boron and mercaptan, has relatively high reaction activity, and avoids the difficulty in impurity removal by using a plurality of catalysts; the perfluoropolyether trimethoxy silane, which is prepared by reacting perfluoropolyether alcohol with allyl chloroformate and then carrying out addition with trimethoxy silane, has excellent mechanical properties. The preparation process is relatively simple, addition and use of a fluorine-containing solvent in the reaction process are reduced, and the prepared product contains more vinyl functional groups and has higher crosslinking degree and corrosion resistance.

The disclosure relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt % to 0.60 wt % of 1,3-bis(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6, 1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt % to 0.50 wt % of a biuret impurity of formula (A) relative to the total weight of ensifentrine. Further disclosed herein are liquid pharmaceutical compositions comprising the particulate composition, and a process 10 for producing the particulate composition are also described.

The present invention relates to compounds of formula (I), in particular their use as degradation agents for the human papilloma virus E7 protein: # imgabs0 #

Disclosed are a series of isoquinolone derivatives as ROCK protein kinase inhibitors and uses thereof in preparing medicaments for ROCK protein kinase inhibitor-related glaucoma or ocular hypertension diseases. Specially, disclosed are a compound of formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.

The invention discloses a fluorescent probe as well as a preparation method and application thereof. The invention provides a series of fluorescent probes with novel structures, and the fluorescent probes take 2-(isoquinoline-1-yl) pyrrole boron difluoride as fluorophores, so that the fluorescence quantum yield of the probes is improved, the detection resolution of nitric oxide is increased, and the detection sensitivity is improved. The fluorescent probe disclosed by the invention has the characteristics of large Stokes displacement, high fluorescence quantum yield, good selectivity and short response time.

The invention discloses a demethylase ODM gene for synthesizing benzylisoquinoline alkaloids and application thereof, the demethylase ODM gene is an ODM1 gene or an ODM2 gene, the nucleotide sequence of the CDS region of the ODM1 gene is shown as SEQ ID NO: 1, and the nucleotide sequence of the CDS region of the ODM2 gene is shown as SEQ ID NO: 2. Aiming at the current situation that the research basis of a key gene for synthesizing corydalmine in rhizoma corydalis is weak, the ODM1 gene for catalyzing tetrahydropalmatine demethylation to specifically generate corydalmine and tetrahydrojatrorrhizine and the ODM2 gene for specifically generating tetrahydrojatrorrhizine are cloned from rhizoma corydalis for the first time. An important theoretical basis is provided for producing the corydalmine by utilizing a synthetic biological method in the future, and the corydalmine mutant has a wide application prospect and a great economic value.

The invention relates to a fluorescent probe for hypochlorous acid detection and a preparation method and application thereof, the chemical name of the fluorescent probe for hypochlorous acid detection is 5-butyl-10, 10-difluoro-9-(4-(methylthio) phenyl)-5-hydro-4H, 10H-9 lambda 4, 10 lambda 4-benzo [de] [1, 3, 2] oxazaboraza [6, 5-g] isoquinoline-4, 6-diketone, and the structural formula of the fluorescent probe for hypochlorous acid detection is as shown in the following formula I. The invention further discloses a preparation method of the fluorescent probe for hypochlorous acid detection. According to the fluorescent probe for hypochlorous acid detection, N-butyl-3-aldehyde-4-hydroxy-1, 8-naphthalimide and (E)-2-butyl-6-hydroxy-5-(((4-(methylthio) phenyl) imino) methyl)-1H-benzo [de] isoquinoline-1, 3 (2H)-diketone are used as raw materials, and the fluorescent probe can be used for detecting hypochlorous acid. Compared with the prior art, the fluorescent probe for hypochlorous acid detection is simple and convenient in synthesis method, simple and easily available in raw materials, good in hypochlorous acid selectivity, relatively high in sensitivity and large in Stokes shift, and has a very good application prospect in hypochlorous acid detection.

Provided in the present invention are a compound as represented by formula (I), or a pharmaceutically acceptable salt, a tautomer, a geometrical isomer, an optical isomer, a solvate or an isotopic derivative thereof, and the use thereof. The compound of the present invention has a significant inhibitory activity on PRMT5, has a significant inhibitory effect on tumor cells and in vivo tumor models, also has a good administration performance, and has clinical application potential for preventing and / or treating diseases which are at least partially mediated by PRMT5.

In certain embodiments, the present disclosure is directed to methods for treating disorders, including depressive disorders, seizure disorders, and anhedonia, in a pediatric subject, wherein the methods comprise orally administering a therapeutically effective amount of the voltage-gated potassium channel allosteric modulator, A-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6- dimethylphenyl]-3,3-dimethylbutanamide (azetukalner), or a pharmaceutically acceptable salt thereof, to the pediatric subject, for example, under fed conditions.

The invention discloses an organic-inorganic hybrid manganese-based halide crystal as well as a preparation method and application thereof, and belongs to the technical field of molecular materials. The molecular formula of the crystal is IQ2MnBr4, IQ is isoquinolyl, namely (C9H7N) 2MnBr4, and the crystal has a reversible crystal phase change characteristic, can be mutually converted between a centrosymmetric structure and a non-centrosymmetric structure, also has a photoluminescence characteristic and can emit green fluorescence under ultraviolet irradiation. Isoquinoline is used as an organic cation, manganese bromide tetrahydrate metal salt is used as a manganese metal ligand, and a room-temperature slow evaporation method is adopted to prepare the catalyst. The organic-inorganic hybrid manganese-based halide crystal disclosed by the invention is a novel monomolecular crystal which is flexible in structure, small in molecular weight and excellent in thermal stability, relatively stable in crystal growth and moderate in growth rate, emits green light under ultraviolet irradiation, and has application potential in photoluminescent devices.

The present invention provides a straightforward process for preparing pyrimido[6,1- a]isoquinoline-4-ones of formula (I), or a pharmaceutically acceptable acid addition salt thereof, preferably ensifentrine, involving the reaction of a precursor with an advanced alkylating agent.

The invention discloses a cephalotaxus hainanensis Ch2OGD1 gene and application thereof, and belongs to the technical field of gene engineering. The Ch2OGD1 gene is used for coding a 2-oxoglutaric acid dependent dioxygenase (2OGD) type Pictet-Spengler enzyme, and the Pictet-Spengler enzyme is used for coding a Pictet-Spengler enzyme. Through a tobacco transient expression system and in-vitro enzyme activity determination, the Ch2OGD1 is proved to be capable of specifically catalyzing the condensation of dopamine and 4-hydroxyphenylpropanal to generate 1-phenethyl isoquinoline. The invention provides a directional preparation method of 1-phenethyl isoquinoline based on the Ch2OGD1 gene, provides a key enzyme element for biosynthesis of a cephalotaxine alkaloid precursor compound, and provides a technical basis for expanding the application of the gene in plant genetic engineering. And a potential technical path is provided for relieving the problem of resource shortage of cephalotaxine alkaloids.

The present invention discloses the application of isoquinoline-3-carboxylic acid in preventing and controlling plant bacterial diseases. The isoquinoline-3-carboxylic acid provided by the present invention has an obvious inhibitory effect on plant bacterial diseases, and the plant bacterial diseases are Ralstonia solanacearum, Acidovorax avenae subsp. Citrulli, Pseudomonas syringae pv. actinidiae, Pectobacterium carotovorum subsp. carotovorum, Xanthomonas oryzae pv. oryzae, Xanthomonas oryzae pv. oryzicola, Alternaria brassicae, Xanthomonas citri subsp. citri, Pectobacterium carotovorum subsp. carotovorum, Xanthomonas fragariae, Pseudomonas syringae pv. lachrymans, Dickeya dadantii, Xanthomonas axonopodis pv. mangiferaeindicae. The isoquinoline-3-carboxylic acid of the present invention has protective and therapeutic effects on Acidovorax avenae subsp. Citrulli.

The invention discloses benzo [4, 5] imidazo [2, 1-a] isoquinoline compounds as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The benzo [4, 5] imidazo [2, 1-a] isoquinoline compound can be used for preparing anti-tumor (human breast cancer) drugs, the structure of the benzo [4, 5] imidazo [2, 1-a] isoquinoline compound is shown in the specification, in the formula, R1 is any one or two of hydrogen, halogen, alkyl, alkoxy, fused ring and aryl; r2 is any one of hydrogen, halogen, alkyl and alkoxy; and R3 is any one or two of hydrogen, halogen, alkyl and alkoxy. The preparation method of the compound comprises the following steps: by taking palladium acetate and norbornene as catalysts, tris (4-chlorphenyl) phosphine and the like as ligands, potassium carbonate and the like as alkali and 1, 4-dioxane as a solvent, carrying out one-pot synthesis on a 1-(2-bromo-1-phenyl vinyl) benzimidazole compound and an iodobenzene compound in an argon atmosphere. Structure of compound: # imgabs0 #

The invention relates to the technical field of pesticides, in particular to a hydrazide derivative containing a 3, 4-dihydroisoquinoline structure, a preparation method and application. The hydrazide derivative containing the 3, 4-dihydroisoquinoline structure is a compound as shown in a formula (I), or a stereoisomer, a tautomer, an isotope derivative and a pesticide acceptable salt thereof. The hydrazide derivative containing the 3, 4-dihydroisoquinoline structure has broad-spectrum inhibitory activity on phytopathogens such as plant pathogenic fungi, especially has excellent inhibitory activity on basidiomycota and ascomycomycota pathogenic fungi such as gaeumannomyces graminis, physalospora piricola, sclerotinia sclerotiorum, botrytis cinerea and rhizoctonia solani, and has broad-spectrum inhibitory activity. The bactericide is expected to be developed into a novel green bactericide which is efficient, safe, economical and environment-friendly.

Provided are an isoquinolinone compound as shown in formula (I), a pharmaceutically acceptable salt thereof, a prodrug molecule, and a mixture thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as an FABP4 / FABP5 dual-targeting inhibitor. Related aryl carboxylic acid compounds can be used for preparing drugs for treating metabolic diseases (such as diabetes, insulin resistance, hyperlipidemia, and atherosclerosis), autoimmune diseases and cancers.

The invention discloses a fused ring tin porphyrin photosensitizer with high singlet oxygen sensitization efficiency and photothermal effect, and relates to the technical field of biological medicine. The invention provides a structural general formula and a preparation method of a fused ring tin porphyrin photosensitizer. According to the invention, the photosensitizer is endowed with strong absorption capacity in an NIR region through an isoquinoline fused ring on the periphery of porphyrin, < 1 > O2 sensitization activity and photothermal effect of the photosensitizer under light excitation are promoted through metal tin coordination in a parent nucleus, and an efficient photodynamic / photothermal synergistic killing effect on 4T1 cells of a mouse breast cancer cell line under NIR light irradiation is realized; the problems of poor light stability, reduced photosensitive activity and the like in the prior art are effectively solved.

The application discloses a preparation method of enciferstat bulk drug and belongs to the field of drug synthesis. 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (SM) is used as a raw material, and the raw material is reacted with cyclohexylamine under alkaline conditions, and the reaction is washed with water, dried, and concentrated to obtain an intermediate I; the intermediate I is reacted with urea under pressurized heating conditions to prepare an enciferstat drug molecule, the two-step yield is more than 67%, and the purity is more than 99%, the method has a simple operation process, the product is easy to purify, the yield is high, the product purity is high, and a new method for preparing enciferstat bulk drug is provided.

The invention provides a purification method of a naphthalimide high-purity electronic-grade photoacid generator. The method solves the problem that photo-acid cannot be purified by traditional recrystallization or directly through ion exchange columns and other methods. The method comprises the following steps: firstly synthesizing and preparing 1, 3-diketone-2-hydroxy-6-(1-hexyne) benzisoquinoline, then reacting with triethylamine and trifluoromethylsulfonyl chloride to generate a crude product 1, 3-diketone-2-(1, 1, 1-trifluoromethyl) methanesulfonic ester-6-(1-hexyne) benzisoquinoline, removing impurities from normal hexane to obtain a pure product, sublimating the material into a gas phase by using a quartz vacuum sublimation instrument, and purifying to obtain the 1, 3-diketone-2-(1, 1, 1-trifluoromethyl) methanesulfonic ester-6-(1-hexyne) benzisoquinoline. And then passing through Pure MTS9500 amino phosphonic acid type chelating resin, and finally cooling in a quartz tube to obtain the high-purity electronic-grade photoacid generator. According to the invention, the stability is high, the metal ion content is low, the purification process is convenient to process, the product is used as a photoresist-level core main material, the product is widely applied in the fields of semiconductor photoresist, other imaging systems, photocureable coatings and the like, the market scale is continuously expanded, and the product is an indispensable key material in semiconductor manufacturing and other related fields.

The present invention belongs to the field of organic synthesis, and particularly relates to indolizino[2,1-a]isoquinoline derivatives, a preparation method and applications thereof. The indolizino[2,1-a]isoquinoline derivative has the structural formula: wherein, R 1 includes an alkyl group, an alkoxy group, hydrogen, fluorine, chlorine, bromine, trifluoromethyl or cyano; R 2 includes an aryl group, an alkoxy group, hydrogen, chlorine or bromine; R 3 includes an aryl group, an alkoxy group, hydrogen, chlorine or bromine; R 4 includes an electron-withdrawing group; R 1 is located at the C8, C9, C10 or C11 position of the indolizino[2,1-a]isoquinoline derivative; R 2 or R 3 is located at the C2 or C3 position of the corresponding indolizino[2,1-a]isoquinoline derivative, and the said R 2 or R 3 can be the same or different. The product of the present invention is a novel product. The preparation method is green and efficient, the preparation conditions are mild, the requirements for equipment are low, the operation is simple, the substrate scope of application is wide, the raw materials are low in price, the production cost is low, the yield is relatively high, and it can be mass-produced industrially, thus having broad application prospects.

This invention provides an aminoisoquinoline derivative and its application in the preparation of antiviral drugs. The invention reveals that the aminoisoquinoline derivative exhibits significant inhibitory effects against various RNA and DNA viruses, demonstrating broad-spectrum activity. This small-molecule inhibitor has low toxicity and does not affect the normal growth of host cells. It shows good antiviral efficacy even at low concentrations. The results of this invention indicate that the compound has the potential to be used in the preparation of antiviral drugs and has promising clinical application prospects.

The present invention provides an acid salt of a Sigma-1 receptor agonist or a crystal form thereof, and a preparation method and application thereof. Specifically, it relates to an acid salt of 5-((2-(cyclopropylmethyl)-1,2,3,4-tetrahydroisoquinolin-7-yl)(isopropyl)amino)-1-methylpyridin-2(1H)-one having high affinity for the sigma-1 receptor and a crystal form thereof. The present invention relates to a preparation method of the acid salt and the crystal form and its application in the pharmaceutical field. The acid salt of the compound 5-((2-(cyclopropylmethyl)-1,2,3,4-tetrahydroisoquinolin-7-yl)(isopropyl)amino)-1-methylpyridin-2(1H)-one and the crystal form thereof provided by the present invention have improved physical and chemical properties, such as appearance, hygroscopicity and chemical stability.

The present invention discloses a method and kit for analyzing endotoxins in complex matrix samples based on liquid chromatography-mass spectrometry. 3-hydroxydecanoic acid, 3-hydroxydodecanoic acid, 3-hydroxytetradecanoic acid, 3-hydroxyhexadecanoic acid or 3-hydroxyoctadecanoic acid characteristic of endotoxins are released by KOH methanol solution for quantitative analysis of various types of endotoxin content; the hydrolyzate is derivatized with isoquinoline-1-carboxylic acid hydrazine to significantly improve the ionization efficiency of the hydrolyzate; using optimized liquid chromatography and mass spectrometry parameters, high stability, high sensitivity and broad spectrum detection of endotoxins from different bacterial sources are achieved. The method has strong anti-interference ability, is applicable to complex matrices, and solves the problem of high false negative rate caused by matrix interference in the prior art.

The invention discloses purslane isoquinoline alkaloid as well as a preparation method and application thereof. The purslane isoquinoline alkaloid is shown as a formula 1 or a formula 2, has GLP-1 receptor agonistic activity and can be used for preparing medicines and health-care foods for preventing and treating diabetes mellitus.

Disclosed herein is an isoquinoline-1 (2H)-one derivative of formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof wherein the values of the variables (e.g., L2A, R1, R2A, R3, R4A, R4B, R4C, R4D, Q2, Q3, Q4) are as described herein. Also disclosed is a pharmaceutical composition comprising such derivatives, and a method of using such derivatives to treat or prevent a condition or disease responsive to inhibition of PI3K [alpha] activity in a subject.

The invention discloses an organic-inorganic hybrid copper-based monomolecular crystal and a preparation method and application thereof, the molecular formula of the monomolecular crystal is (C9H7N) 2CuBr2, and the preparation method comprises the following steps: dissolving an organic cation source in a medium solvent to obtain an organic solution; dissolving a copper metal ligand in hydroiodic acid to obtain an acid solution; mixing the organic solution and the acid solution, putting the mixed solution into a sealed bottle filled with a diffusion solvent, sealing by a sealing cover to form a sealed system, keeping out of the light, standing after the diffusion solvent in the bottle is completely volatilized, and observing a light green needle-like crystal to obtain a finished product. Isoquinoline is selected as an organic cation source, copper bromide metal salt is selected as a metal ligand, the monomolecular crystal which is flexible in structure, small in molecular weight, high in stability and excellent in performance is prepared through an anti-solvent diffusion single crystal method, the synthesis process is simple, the preparation period is short, the yield is high, and environment friendliness is achieved; and the application of the monomolecular crystal in the field of multifunctional miniaturized circuits is widened.

The present application relates to the technical field of organic synthesis, and particularly relates to a method for preparing (+)-crispine A by means of biological enzyme resolution. First, 6,7-dimethoxy-3,4-dihydroisoquinoline-2-oxide is subjected to 1,3-dipolar cycloaddition with allyl alcohol to obtain a first compound; then the first compound is added into a sulfonylation reagent and zinc powder to obtain a racemate second compound through a three-step continuous series reaction of primary alcohol sulfonylation, nitrogen-oxygen bond cleavage and ring formation; then the second compound is mixed with vinyl acetate and biological enzyme, and chiral resolution is carried out under the action of the biological enzyme to obtain a third compound with right-handed optical rotation and a fourth compound with left-handed optical rotation; finally, the third compound is mixed with an alkaline reagent and a sulfonylation reagent, and then secondary alcohol sulfonylation is carried out to obtain a fifth compound with right-handed optical rotation; the fifth compound is mixed with a deoxidizing reagent to carry out deoxidation reaction, and (+)-crispine A is prepared. The method is simple, green and environmentally friendly, and can be produced in large quantities.