191 results about "Isoquinoline" patented technology

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 provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (I), and sub-formulas thereof: Formula (I) or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment or prevention of diseases including heart (e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., lung inflammation, pneumonia, acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), respiratory (e.g.,respiratory infection, acute respiratory distress syndrome), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease, inflammatory bowel disease (IBD), ischemic reperfusion injury (e.g., stroke), retinopathy of prematurity (ROP), bronchopulmonary dysplasia (BPD), and white matter injury (WMI).

The invention discloses a preparation method of a covalent organic framework photocatalyst for photocatalytic reduction of CO2, which comprises the following steps: adding 4, 4 ', 4' '-(1, 3, 5-triazine-2, 4, 6-triyl) triphenylamine and 2, 5-dibromobenzene-1, 2, 4, 5-tetracarboxylic dianhydride into a reaction kettle, then adding 1-hydroxy-3-methylbenzene and isoquinoline, and uniformly mixing; and carrying out microwave heating on the reaction kettle, cooling to room temperature, filtering, collecting precipitate, washing, and then carrying out Soxhlet extraction and vacuum drying to obtain the covalent organic framework photocatalyst. A surface halogen atom modification strategy is designed and used for regulating and controlling electron distribution and light capture capacity of a donor-acceptor (D-A) in TzPm-COF, and results show that the strategy can effectively improve photocatalytic activity and selectivity of reduction of CO2 into CO, and can be applied to preparation of the TzPm-COF catalyst. A reasonable design strategy is provided for developing a functional modified COFs material for efficiently and selectively photocatalytic CO2 reduction.

The present disclosure provides methods, pharmaceutical compositions, and kits for treating cancer in patients in need thereof. The methods comprise administering to a patient in need a small ubiquitin-like modifier (SUMO) activating enzyme (SAE) inhibitor, such as [(1R,2S,4R)-4-{[5-({4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methyl-2-thienyl}carbonyl)pyrimidin-4-yl]amino}-2-hydroxy-cyclopentyl]methyl sulfamate (Compound I-263a) or a pharmaceutically acceptable salt, in combination with one or more anti-CD19 antibodies. Also provided are medicaments for use in treating cancer.

The application discloses a synthesis method of aromatic aldehyde, comprising the following steps: under inert atmosphere, a compound shown in formula I and a compound shown in formula II are reacted in an organic solvent containing a photocatalyst, a nickel catalyst, a ligand, a base and water under blue light irradiation to obtain aromatic aldehyde shown in formula III; formula I, formula II and formula III are structures as follows, ring A is selected from benzene, pyridine, thiophene, furan, pyridazine, indazole, indole, isoquinoline, quinoline, naphthalene, benzothiophene, dibenzofuran or dibenzothiophene; the application generates formyl radicals under the nickel synergistic photo-oxidation and reduction catalytic condition, and the formylation of bromobenzene and its derivatives is realized in a simple and efficient one-pot way, aromatic aldehyde is constructed, and the reaction has the characteristics of cheap and easily available raw materials, mild reaction conditions, controllable synthesis process, high separation yield / yield, green environmental protection, wide substrate applicability and the like.

The application belongs to the field of pharmaceutical chemistry and specifically relates to a preparation method of 1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline, which comprises the following steps: adding a reducing agent in an alkaline aqueous solution, adding a cosolvent under nitrogen protection, controlling the temperature at 10-30 DEG C, slowly adding an aqueous solution of compound 2, and stirring to react, thereby obtaining the product directly. In the application, after compound 2 is prepared, the post-reaction liquid is not concentrated, and the product is extracted with water, thereby solving the problem of unstable product concentration. In the reduction reaction from compound 2 to compound 3, the reducing agent is added in the aqueous solution of sodium hydroxide at one time, the solvent is added to assist dissolution, and then the aqueous solution of compound 2 is added to perform the reduction reaction, the process is mild, the cumbersome batch addition of the reducing agent is avoided, the reaction time is short, the energy consumption is low, the post-treatment is mild, and the obtained product has the advantages of high yield and high purity.

The present invention relates to isoquinolines as HPK1 inhibitors. Isoquinoline compounds and their use as HPK1 (hematopoietic kinase 1) inhibitors are described. The compounds are useful in treating HPK1 dependent disorders and in enhancing immune responses. Methods of inhibiting HPK1, methods of treating HPK1 dependent disorders, methods for enhancing immune responses, and methods for making the isoquinoline compounds are also described.

The invention provides a tetrahydroisoquinoline derivative and application thereof. Specifically, the invention relates to a compound as shown in a formula (I), or an isotope variant, a tautomer, a stereoisomer, a prodrug, a polymorphic form, a hydrate or a solvate thereof, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition containing the compound, and an effect of the compound in prevention and treatment of diseases related to the central nervous system.

The present invention relates to compositions comprising 4-({(4-cyclopropylisoquinolin-3-yl)[4- (trifluoromethoxy)benzyl] amino }sulfonyl)benzoic acid (elismetrep; MT-8554), or a pharmaceutically acceptable salt thereof, for treating or preventing pain, particularly migraine or a trigeminal pain disease or condition such as medication overuse headache, cluster headache, general headache, trigeminal neuralgia, trigeminal neuropathy, trigeminal autonomic cephalalgia, orofacial pain, and dental pain.

The application provides novel N-heterocyclic compounds, such as quinoline or isoquinoline compounds, preferably quinazoline compounds, as calcineurin inhibitors (CNIs,) that provide improved safety profiles, and the pharmaceutical composition and formulation thereof, as well as a method of using the N-heterocyclic compounds for the treatment of, inter alia, an inflammatory-related disease or disorder.

The present invention relates to novel compounds that are photo-crosslinked by visible light and spatiotemporal proximity photo-crosslinking by visible light activation (spotlight) using the same. When a target nucleic acid or target protein is bound to the novel compounds by the property of being photo-crosslinked to the proximal protein or peptide by irradiation with visible light and it is irradiated with visible light, the novel compounds according to the present invention can be photo-crosslinked with a protein or peptide that physically interacts with the target protein or target nucleic acid, and thus, there are advantages in that it is possible to overcome diffusive labeling, which is a limitation of the conventional proximity labeling technology, by photo-crosslinking by visible light irradiation, which is a safe method for a living body, and to improve the accuracy of protein interactome identification.

Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions / disorders / diseases due to mutations or dysregulation of the Wnt pathway and / or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

The isoquinolin-1(2H)-one derivative of formula (I), or its stereoisomer, tautomer, or pharmaceutically acceptable salt is disclosed herein, and the variables (e.g., L 2A , R 1 , R 2A , R 3 , R 4A , R 4B , R 4C , R 4D , Q 2 , Q 3 , Q 4 ) have the values as described herein. Also disclosed are pharmaceutical compositions containing such derivatives, and methods for treating or preventing disorders or diseases responsive to inhibition of PI3Kα activity in a subject using such derivatives. TIFF2026516333000335.tif53165

The invention discloses a polyimide dielectric film containing carboxyl betaine and a preparation method thereof. The carboxyl betaine-containing polyimide dielectric film is prepared from carboxyl betaine-containing polyimide, and the carboxyl betaine-containing polyimide is prepared by the following steps: firstly, taking a precursor of carboxyl betaine, m-phenylenediamine and bisphenol a type diether dianhydride as monomers, and carrying out condensation polymerization to obtain polyamide acid; carrying out complete imidization on the polyamide acid under the action of a catalyst isoquinoline to obtain polyimide containing a precursor; and reacting the polyimide containing the precursor with sodium bromoacetate to obtain polyimide containing carboxyl betaine. The zwitterions are introduced into the polyimide structure to improve the dielectric and energy storage performance of the polyimide dielectric film, and meanwhile, the preparation method has the advantages of being low in cost, simple in process, controllable and adjustable in performance, suitable for large-scale application and the like.

This invention provides an imine reductase mutant, its preparation method, and its application in the catalytic preparation of dextromethorphan intermediates. The imine reductase mutant is an imine reductase with an amino acid mutation, comprising the amino acid sequence shown in SEQ ID NO:1. The amino acid mutation type includes any one or a combination of at least two of I122T, D212A, or G228R. By introducing a mutation into the imine reductase, this invention significantly improves the enzyme's activity and stereoselectivity, enabling the high-yield synthesis of the dextromethorphan intermediate (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline under mild conditions, greatly reducing production costs and making it suitable for industrial production.

This invention discloses an iron complex with a triazacyclic nonane macrocyclic skeleton, its preparation method, and its applications, belonging to the field of coordination chemistry. The iron complex has a triazacyclic nonane macrocyclic skeleton with two acetate side groups and one pyridine-N derivative side group. The iron complex exhibits excellent catalytic activity in the aerobic oxidation of N-aryltetrahydroisoquinoline, while also possessing good stability. The solvents for the catalytic reaction are water and acetonitrile, resulting in low pollution. This invention features mild reaction conditions, simple synthesis operations, and straightforward post-processing, meeting the requirements of environmental friendliness and clean production.

The invention discloses a copper-catalyzed aryl aldehyde ortho-position direct C-H etherification method, which comprises the following steps: by taking aryl aldehyde as a raw material, adding alcohol or phenol as shown in a formula (II), a copper catalyst, a guiding group, alkali and a solvent into a reactor, and reacting in an argon gas atmosphere to prepare an aryl ether compound as shown in a formula (III), a substituent group R1 is hydrogen, methyl, trifluoromethyl, methoxyl, phenyl, iodo, isopropyl, trimethylsilyl, dimethylamino, fluoro, chlorine, ester, tourmaline, naphthyl, isoquinolyl, benzothienyl or phenanthryl; a substituent group R2 is hydrogen, methyl, trifluoromethyl, methoxyl, phenyl, iodo, isopropyl, trimethylsilyl, dimethylamino, fluoro, chlorine, ester, tourmaline, naphthyl, isoquinolyl, benzothienyl or phenanthryl; and a substituent group R2 is methyl, 4-fluorophenyl, cyclobutane methyl, 4-tert-butyl phenyl, pentafluorophenyl, 4-cyanophenyl, 4-methyl ester phenyl, 3-nitrophenyl, adamantane methyl, cyclohexyl or an oestrone analogue. The copper catalyst and amino acid which are low in cost and easy to obtain are used as guiding groups, the operation process is simple and efficient, and the corresponding aryl ether compound can be obtained with the good yield.

Suppresses discoloration of halogenated isoquinoline derivative-containing aqueous compositions during high-temperature storage. To provide technology. [Solution] The following general formula (1) TIFF2026116450000013.tif45170 [In the formula, X represents a halogen atom.] An aqueous composition containing a compound represented by or a salt thereof, or a solvate thereof, is polio A pharmaceutical preparation housed in a container made of refin resin.

The invention discloses a tetrahydroisoquinoline hydroximic acid collecting agent and a preparation method thereof. According to the collecting agent, tetrahydroisoquinoline serves as a basic framework, and various special functional groups such as a chelating group, an ether bond and a hydrogen bond donor are contained. The preparation method comprises the steps that tyrosine methyl ester and formaldehyde react in a solvent concentrated hydrochloric acid to generate a tetrahydroisoquinoline ring skeleton, then the tetrahydroisoquinoline ring skeleton and brominated hydrocarbon react in an alkaline environment to generate ether, and finally a hydroximation reaction is conducted to obtain the corresponding hydroximic acid collecting agent. The collecting agent of the type has very high chelating capacity, shows good collecting performance and selectivity in ilmenite flotation, and can effectively improve the grade and the recovery rate of ilmenite concentrate.

This disclosure relates to a salt form of a tricyclic tetrahydroisoquinoline derivative. Specifically, this disclosure relates to different salt forms of the compound shown in formula (I) and methods for their preparation. The salt forms of the compound of formula (I) provided in this disclosure have good stability and can be better used in clinical treatment.

To provide a new compound useful for treatment, prevention and / or diagnosis of seizure or the like in diseases accompanied by epileptic seizure or convulsive seizure (including multidrug-resistant seizure, intractable seizure, acute symptomatic seizure, febrile seizure and status epilepticus).SOLUTION: There are provided a compound represented by formula [I] and a salt thereof. Ring C is selected from pyridazine, pyrimidine, indole, pyrrolopyridine, indazole, pyrazolopyridine, imidazopyridine, imidazopyrazine, imidazopyridazine, triazolopyridine, pyrazolopyrimidine, imidazopyrimidine, triazolopyrimidine, isoquinoline, naphthyridine, quinazoline, quinoxaline, benzodioxole, oxazine, oxazepine, benzothiazole, and triazolopyridazine, with the proviso that pyrimidine-2, 4-dione and dihydropyrimidine-2, 4-dione are excluded.SELECTED DRAWING: None

The present invention relates to a particulate composition comprising ensafetine wherein the particulate composition further comprises: from more than 0.00% to 0.60% by weight of 1, 3-bis (2-(2-(mesitylene imino)-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 ensafetine, and a particulate composition comprising: from more than 0.00% to 0.60% by weight of 1, 3-bis (2-(2-(mesitylene imino)-9, 10-dimethoxy-4-oxo-6, 7-dihydro-2H-pyrimido [6, 1-a] isoquinolin-3 (4H)-yl) ethyl) urea And 0.00% to 0.50% by weight of a biuret impurity of formula (A) with respect to the total weight of ensefin. Also described are liquid pharmaceutical compositions comprising the particulate compositions, as well as methods for producing the particulate compositions.

The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, compositions thereof, and methods of using the same in methods of treating diseases, disorders, and conditions such as myotonic dystrophy type 1 (DM1).

The invention discloses an iron complex with a triazacyclononane macrocyclic skeleton as well as a preparation method and application of the iron complex, and belongs to the technical field of coordination chemistry. The iron complex has a triazacyclononane macrocyclic skeleton, and is attached with two acetate side groups and one pyridine-N derivative side group; the iron complex shows excellent catalytic activity in the aerobic oxidation reaction of N-aryl tetrahydroisoquinoline and has good stability, solvents for the catalytic reaction are water and acetonitrile, and pollution is small. The method is mild in reaction condition, simple in synthesis operation and simple in post-treatment, and meets the requirements of environment friendliness and clean production.

The invention provides an isoquinoline derivative with a novel structure, a pharmaceutically acceptable salt thereof, a preparation method of the isoquinoline derivative, a pharmaceutical composition containing the isoquinoline derivative and pharmaceutical application of the isoquinoline derivative, and belongs to the technical field of medicines. In-vitro experiments show that the isoquinoline derivative has significant inhibitory activity on arachidonic acid-induced platelet aggregation, and the antiplatelet activity of part of compounds is superior to that of aspirin. In a rat carotid artery thrombosis model induced by FeCl3, the isoquinoline derivative remarkably prolongs thrombosis time and reduces thrombus weight, and the in-vivo antithrombotic curative effect of the isoquinoline derivative is equivalent to that of aspirin and ticagrelor. A mouse tail bleeding model shows that the side effects of bleeding amount and bleeding time of the isoquinoline derivative are obviously lower than those of aspirin and ticagrelor. Therefore, the series of isoquinoline derivatives have the advantages of efficient antithrombotic effect and low bleeding risk, and have good application prospects in preparation of drugs for preventing and treating thrombotic diseases. In addition, the preparation method provided by the invention has the advantages of easily available raw materials, simple steps and strong operability, and the obtained target product has high quality and good efficiency.

To provide a bee repellent in order to prevent damage to honeybees, which are not the intended target of pesticides applied to crops or pesticides used to control carnivorous bees such as hornets and paper wasps. [Solution] A bee repellent comprising one or more components selected from tetradecane, furfuryl alcohol, cinnamyl alcohol, cinnamaldehyde, 3-methyl-2-butenal, methyl cinnamate, geranyl formate, allyl cyclohexanepropionate, isoquinoline, borneol, carvacrol, δ-dodecalactone, β-ionone, quinoline, butylamine, and citronella oil as active ingredients.

This invention belongs to the technical field of organometallic luminescent materials and photosensitizers, specifically relating to a triphenylamine-containing heteropolymer luminescent iridium(III) complex capable of generating reactive oxygen species, its preparation method, and its applications. The iridium(III) complex has the structure shown in formula (I), [Ir(L1)2(L2)]PF6, where L1 is 1-(4-(diphenylamino)phenyl)isoquinoline and L2 is 2-[3-methyl-1-(4-(diphenylamino)phenyl)-1H-1,2,4-triazol-5-yl]pyridine. The complex can be prepared by first preparing a chlorobridged iridium dimer intermediate, then coordinating it with an auxiliary ligand and followed by anion exchange. This complex exhibits luminescent properties in both dilute solutions and solid states, and displays certain solvent-dependent luminescence behavior. Under LED white light irradiation, the complex can effectively generate reactive oxygen species (ROS). Detection using DCFH-DA, HPF, and DHR123 probes indicates that it possesses the ability to generate total ROS, hydroxyl radicals, and superoxide anion radicals. The complex can be used to prepare luminescent materials, ROS-generating materials, and photodynamic photosensitive materials.