779 results about "Isoquinoline" patented technology

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a hydroxyl-substituted dihydroisoquinolinone compound. The compound has a good KRAS G12V mutant gene inhibition effect, and can be used for treating tumor diseases related to KRAS G12V gene mutation.

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 for producing the particulate composition are also described.

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 for producing the particulate composition are also described.

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 for producing the particulate composition are also described.

The invention 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. A liquid pharmaceutical composition comprising the particulate composition, and a process for producing the particulate composition are also described.

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 invention relates to the technical field of OLED (Organic Light Emitting Diode) luminescent materials, in particular to an anthracene azepine material as well as a preparation method and application thereof, and the structure of the anthracene azepine material is as shown in the following formula: # imgabs0 #, r is any one of a deuterated terphenyl group, an isoquinolyl group, a piryl group, a 9, 9-diphenyl fluorenyl group, a dibenzothienyl group and a deuterated N-phenyl carbazolyl group. The parent structure of the anthracene-azepine material has anthracene, deuterated carbazole, azepine structures and the like, and intramolecular large steric hindrance space distorted structures, so that the spin-orbit coupling effect between different excited states is remarkably improved, the molecules are greatly limited during relaxation, and finally, the device realizes dark blue light emission, and has wide application prospects. The introduced aryl heterocyclic structure can greatly improve the stability of the material, and meanwhile, the deuterated structure can obviously prolong the service life of the device and obviously improve the luminous efficiency of the device.

The invention discloses an isoquinolinone dihydropyridine-[1, 2-alpha] indole spiro compound as well as a preparation method and application thereof, and belongs to the technical field of synthesis of organic compounds. An N-indole connected o-alkynyl nitrone compound is used as a raw material, a two-step one-pot method is adopted, and the isoquinolinone dihydropyridine-[1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, the invention relates to a novel method for synthesizing a spiro [1, 2-alpha] indole. The method disclosed by the invention has the advantages of simplicity in operation, low catalyst loading capacity, wide reaction substrate range, single stereoselectivity, high yield and the like. The isoquinolinone dihydropyridine-[1, 2-alpha] indole spiro compound prepared by the invention has a certain inhibition effect on phytopathogen, and can be potentially applied to prevention and treatment of tomato gray mold, wheat scab and rhizoctonia solani.

The present invention refers to an antagonist of imidazoline-1 receptor (I1R) for use in the prevention and / or treatment of an autoinflammatory or autoimmune disease in a human subject, selected from the group consisting of (±)-2-endo-amino-3-exo- isopropylbicyclo[2.2.1]heptane (synonym: AGN192403), N-benzylguanidine, 2-(2- Fluoro-5-methylphenyl)-4,5-dihydro-1H-imidazole (synonym: S23757), 2-(2-chloro-4-iodo-phenylamino)-5-methyl-pyrroline (synonym: LNP911), 1-(4, 5-dihydro-1H-imidazol- 2-yl)isoquinoline (synonym: BU98008), 5-[2-bromophenoxy)methyl]-4,5-dihydro-1,3- oxazol-2-amine (synonym: S23515), 6-methylamino-2methylheptene (synonym: isometheptene), and 4-chloro-2,3-dihydro-2-oxo-1,3-benzothiazol-3-ylacetic acid (synonym: benazolin). Also, to the use of Imidazole propionate in the diagnosis of an autoinflammatory or autoimmune disease in a subject, and further to a method of diagnosis of atherosclerosis comprising assessing the level of ImP in a blood sample and determining whether said level is above or below a value of 41nM.

The present invention relates to novel isoquinoline derivatives. The derivative has the effect of promoting mitochondrial autophagy activity, so that mitochondria with damaged structure and / or function is reduced. Specifically, the novel isoquinoline derivative according to the present invention does not induce mitochondrial dysfunction and has been determined as a safe compound that is non-toxic to cells, and thus it can be used to prevent, ameliorate and / or treat various diseases that may be caused by mitochondrial abnormality.

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 invention discloses an application of a tetrahydroisoquinoline compound in preparation of an anti-leukemia drug. The compound has a remarkable inhibition effect on leukemia cells, has low toxicity to organisms, not only expands the variety of drugs for clinical treatment of leukemia, but also is suitable for large-scale production.

The invention relates to a synthetic method of an efficient polysubstituted pyrrolo [2, 1-a] isoquinoline compound, and discloses a method for synthesizing the polysubstituted pyrrolo [2, 1-a] isoquinoline compound by taking a 2-(3, 4-dihydroisoquinoline-2 (1H)-yl) malononitrile compound and 2, 3-dichloro-5, 6-dicyanobenzoquinone as oxidizing agents and substituted isocyano acetate under the action of a catalyst. The method has the advantages of cheap initial raw materials, mild reaction conditions and simple experimental operation, can save the investment of funds and labor force, and provides a simple and efficient preparation method for the polysubstituted pyrrole [2, 1-a] isoquinoline compound.

The invention provides a biisoquinoline-based iron complex which has a structure as shown in a formula (I), and also provides a preparation method of the biisoquinoline-based iron complex and an application of the biisoquinoline-based iron complex as a catalyst for an anisole hydroxylation reaction. The invention further provides a method for preparing p-hydroxyanisole and co-producing o-hydroxyanisole. When the biisoquinoline-based iron complex provided by the invention is used for catalyzing hydroxylation reaction of anisole, excellent reaction activity and selectivity to hydroxyl products can be obtained, a new process thought is provided for industrial production of p-hydroxyanisole, and the biisoquinoline-based iron complex has very important economic value and social value, # imgabs0 #

The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) a suspension of particles comprising 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554); and (ii) a diluent which is 1,1,1,2-tetrafluoroethane (HFA-134a), wherein the liquid pharmaceutical composition is substantially free of surfactant. The invention also relates to a pressurised metered dose inhaler comprising the liquid pharmaceutical composition.

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 preparation method of a pyridino-isoquinoline-2-ketone derivative, which comprises the following steps: under the protection of nitrogen, putting 1-aryl-3, 3-difluorocyclohexene, brominated N-(2-phenyl-2-oxo) ethyl isoquinolinium, alkali and a solvent into a reactor, reacting at 60 DEG C for a period of time, and then adding tert-butyl hydroperoxide to continue reacting; and after the reaction is finished, reducing pressure to remove the solvent, and carrying out column chromatography separation to obtain a pure product of the pyridino isoquinoline-2-ketone derivative. Initial raw materials are cheap, easy to obtain and wide in source, and products are complex and diversified in structure. The process flow is simple, and operation is simple and safe. Double bonds conjugated with two carbonyl groups in the target product can be further subjected to functionalization reaction, so that the target product can be conveniently subjected to diversified structural modification.

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.

The invention discloses a novel compound 2-fluoropyridino-isoquinoline derivative as well as a preparation method and application thereof. The structural formula of the novel compound 2-fluoropyridino-isoquinoline derivative is as follows: # imgabs0 #, wherein Ar1 is phenyl, Ar2 is 3-chlorphenyl or Ar1 is 4-fluorophenyl, and Ar2 is phenyl; the preparation method comprises the following steps: reacting 1-aryl-3, 3-difluorocyclohexene, brominated N-(2-aryl-2-oxo) ethyl isoquinolinium, alkali and a solvent under the protection of nitrogen at the temperature of 60 DEG C; and after the reaction is finished, reducing pressure to remove the solvent, and performing column chromatography separation to obtain a pure product of the 2-fluoropyridinoisoquinoline derivative. The 2-fluoropyridinoisoquinoline derivative disclosed by the invention has better activity of inhibiting the growth of tumor cells, and has important guiding significance and application prospects for finding novel and efficient antitumor drugs.

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 present invention provides an isoquinoline alkaloid compound selected from the compounds shown in the following structural formula, and a preparation method and application thereof. The present invention first confirms that the isoquinoline alkaloid compound is a K Inhibitors of potassium current and background potassium current, especially inhibitors of Kv2.1 channels and TRESK channels, can be used to treat diseases such as stroke, arrhythmia, atrial fibrillation, diabetes, pain, respiratory depression, depression, etc.