57 results about "Azepine" patented technology

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

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 relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

The invention provides a benzene azepine derivative, a radioactive probe and application thereof, and belongs to the technical field of biological medicine. According to the present invention, the benzazepine derivative is modified, and the hydrophilic or lipophilic side chain is introduced, such that the prepared benzazepine derivative can be used as the V2R targeting precursor for application, the specific V2R targeting can be achieved, and the new molecular tool is provided for the subsequent V2R positive tumor diagnosis and treatment. The radioactive probe combined with the 68Ga marker shows a good tumor imaging effect, can realize PET imaging of V2R positive tumors, is helpful for improving the accuracy of tumor diagnosis, can also be used for evaluating the treatment effect, has a relatively high target / non-target ratio, can better display the distribution of whole body V2R receptors, and has a good application prospect. The invention has various applications in cancer diagnosis and treatment.

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

The invention belongs to the field of pharmacy, and particularly relates to application of a nitrogen-containing heterocyclic compound in preparation of antibacterial drugs. The compound provided by the invention is prepared by electrochemical driving under the condition of no metal and no oxidant, is a yellow solid, and gives a quasi-molecular ion peak [M + Na] +: 632.1. 1101 through a high-resolution mass spectrum. The invention relates to application of (E)-8-chloro-6-(2-fluorophenyl)-1-p-methyl-4-(p-methyl)-1, 2, 3, 4-tetrahydrobenzo [b] azepine in preparation of antibacterial drugs, in particular to application of (E)-8-chloro-6-(2-fluorophenyl)-1-p-methyl-4-(p-methyl)-1, 2, 3, 4-tetrahydrobenzo [b] azepine in preparation of antibacterial drugs.

Disclosed are an epinastine hydrochloride oral dissolving film composition, a preparation method therefor, and use thereof. The present invention provides an epinastine hydrochloride oral dissolving film composition comprising an active drug, a film-forming material, and a flavoring agent. The active drug is one or more of 3-amino-9,13-dihydro-1H-dibenzo[c,f]-imidazo[1,5-a]azepine hydrochloride, which is represented by formula I, and a solvate thereof. The epinastine hydrochloride oral dissolving film composition of the present invention has the advantages of a small thickness, rapid disintegration, stable properties, good mechanical properties, a pleasant taste, instant oral dissolution without the need for water, and quick oral absorption. Moreover, the composition is uniform in appearance and good in flexibility, and the process is simple; no sedimentation occurs in the process of preparing a film solution; the content uniformity meets the requirement, and the drug loading capacity is high.

The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more toll-like receptor (TLR), amino-azepine derivatives. The invention also provides TLR agonist amino-azepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more toll-like receptor (TLR), amino-azepine derivatives. The invention also provides TLR agonist amino-azepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

The present invention relates to a compound, of the formula:Wherein variables are as defined in the specification and pharmaceutical composition comprising thereof, more specifically compound of the present invention is thiophenyl and pyrrolyl azepine compound; The compound is serotonin receptor (5-HT2c) ligand, useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).

The present invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators with apical sodium-dependent bile acid transporter (ASBT) and / or hepatic bile acid transport (LBAT) inhibitory activity. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases, and liver diseases.

The present disclosure provides a compound of formula (I), a pharmaceutical composition thereof, and a use thereof in treating and / or preventing diseases or conditions related to the activity of RIPK1 kinase.

The invention relates to 1,5-benzothiadiazepine and 1,2,5- benzothiadiazepine derivatives of formula (1). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases, liver diseases and renal diseases.

The application belongs to the technical field of detection and analysis, and discloses a normal phase detection method for imine reaction control. The method is detected by normal phase liquid chromatography, and the detection conditions include: a polysaccharide derivative normal phase coated type chiral chromatographic column is used, and a mixed solution of n-hexane, ethanol, ethylenediamine and trifluoroacetic acid is used as the mobile phase, wherein the volume ratio of n-hexane, ethanol, ethylenediamine and trifluoroacetic acid is (75-85):(15-25):(0.05-0.15):(0.05-0.15). The method can realize effective separation, detect the content of 1,2,3,4,10,14B-hexahydrodibenzo[C,F]pyrazino[1,2-A]azepine in the reaction solution, and has the advantages of simplicity, accuracy, rapidness and reliability.

The present invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transporter (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the treatment of cardiovascular diseases, disorders of fatty acid metabolism and glucose utilization, gastrointestinal diseases and liver diseases.

The present invention belongs to the field of pharmaceutical technology, and relates to an azepine alkaloid compound isolated from the plant Polygonum tinctorium Ait. of the genus Polygonum in the Polygonaceae family, which has a heptacyclic azepine-fused pyrrolidine mother nucleus. The present invention also relates to a preparation method of the compound and its use in the preparation of a drug for treating neurodegenerative diseases. The preparation method of the present invention is simple and easy to operate, has good reproducibility, and has a high purity. The obtained compound has a good neuroprotective effect. #imgabs0#

The invention discloses an epinastine hydrochloride oral soluble film composition as well as a preparation method and application thereof. The invention provides an epinastine hydrochloride oral soluble film composition. The epinastine hydrochloride oral soluble film composition comprises an active medicine, a film forming material and a taste masking agent, the active drug is one or more of 3-amino-9, 13-dihydro-1H-dibenzo [c, f]-imidazo [1, 5-a] azepine hydrochloride as shown in a formula I and a solvate of the 3-amino-9, 13-dihydro-1H-dibenzo [c, f]-imidazo [1, 5-a] azepine hydrochloride. The epinastine hydrochloride oral soluble film composition has the advantages of being thin in thickness, rapid in disintegration, stable in property, good in mechanical property, good in taste, capable of being instantly dissolved in the oral cavity without drinking water and high in oral absorption speed, and is uniform in appearance, good in flexibility, simple in process, free of sedimentation in the preparation process of film liquid and suitable for large-scale production. The content uniformity meets the requirements, and the drug loading capacity is high.

The invention belongs to the technical field of organic synthesis, and particularly relates to a method for catalytically synthesizing a dibenzo [b, d] azepine compound by using an N-heterocyclic carbene oxazoline cyclic palladium compound. The invention aims to provide a novel synthesis method of a dibenzo [b, d] azepine compound, and particularly relates to a method for synthesizing the dibenzo [b, d] azepine compound by using a high-catalytic-activity N-heterocyclic carbene oxazoline cyclic palladium compound as a catalyst through a carbon-nitrogen / carbon-carbon bond cascade reaction. The 2, 2 '-dihalogenated biphenyl compound and an N-alkyl substituted allylamine compound are directly synthesized into the dibenzo [b, d] azepine compound in one step. The catalyst used in the invention has high catalytic activity, and the reaction has good compatibility of products and functional groups; the catalyst is easy to synthesize, and the raw materials of the 2, 2 '-dihalogenated biphenyl compound used in the synthesis route are cheap and easy to obtain.

The invention discloses antibacterial application of an indole azepine-spiro-benzothiophene ketone compound, and belongs to the technical field of medicinal chemistry. The indole azepine-spiro-benzothiophene ketone compound provided by the invention has excellent inhibitory activity on four common pathogenic bacteria: peanut root rot bacteria, strawberry botrytis cinerea, valsa mali and cucumber fusarium wilt bacteria, so that the indole azepine-spiro-benzothiophene ketone compound has important application value in the field of agricultural germ control.

The invention belongs to the technical field of organic synthetic chemistry, and discloses an efficient synthesis method of an indoline and azepine ketone derivative. The derivative has a structure as shown in a formula (I), and is prepared according to the following steps: reacting 1 equivalent of carboxylic acid, 1 equivalent of o-alkynylaniline, 1 equivalent of pyridine-2-formaldehyde and 1 equivalent of isocyanide as reaction raw materials at room temperature for 5 hours under the condition that methanol is used as a solvent to obtain an intermediate Ugi compound. Then, spin-drying a reaction solvent, adding n-butyl alcohol (1.5 mL), XPhosAuCl (0.01 mmol, 0.05 equivalent) and silver acetate (0.01 mmol, 0.05 equivalent), and transferring a reaction system to a microwave condition of 110 DEG C to react for 1 hour, so as to finally obtain the indoline and azepine ketone derivative as shown in the formula (I). The indoline azepine ketone derivative is efficiently prepared through a one-pot method, the compound is a quasi-natural product compound with a novel structure, and the developed organic synthesis method has the advantages of being high in atom economy, simple in step and the like. Meanwhile, the compound also shows good anti-tumor cell proliferation activity. # imgabs0 #

The invention relates to the field of organic electroluminescent materials (OLEDs), in particular to a novel host material structure based on a seven-membered ring triphenyl [b, d, f] azepine unit and application of the material in an organic electroluminescent display device. The novel host material based on the seven-membered ring triphenyl [b, d, f] azepine unit has a structure as shown in a formula (1): # imgabs0 #. The invention provides a preparation method of the organic electroluminescent host material based on the seven-membered ring triphenyl [b, d, f] azepine unit and application of the organic electroluminescent host material as the host material to manufacture an organic electroluminescent device.

The present disclosure provides a compound of formula (I), a pharmaceutical composition thereof, and a use thereof in treating and / or preventing diseases or conditions related to the activity of RIPK1 kinase.

The invention discloses an indeno [1, 2-d] pyrrolo [1, 2-a] aza derivative as well as a preparation method and application thereof. The compound has a structural formula as shown in a formula I, wherein R1 is selected from H, alkyl of C1-6, phenyl or phenyl substituted by alkyl of C1-6, alkoxy of C1-6 and halogen; r2 is selected from alkyl of C1-6, phenyl or phenyl substituted by alkyl of C1-6, alkoxy of C1-6 and halogen; and R3 is one or more substitutions and is independently selected from H, halogen, alkyl of C1-6 and alkoxy of C1-6. The invention provides a series of indeno [1, 2-d] pyrrolo [1, 2-a] aza derivatives with novel structures, and the derivatives have a fluorescent effect and can be used for luminescent materials and fluorescence detection.

The application discloses a benzazepine nine-membered ring lactone compound and a preparation method and application thereof, and adopts a palladium and azepine carbene catalyst synergistic catalysis reaction, so that reaction steps are simplified, reaction conditions are more moderate, an ideal yield can be obtained, a feasible reaction path is provided for preparation of the benzazepine nine-membered ring lactone compound and industrial production thereof, meanwhile, the prepared benzazepine nine-membered ring lactone compound can effectively inhibit MRSE and MSSE, has good antibacterial activity, and is expected to be applied to preparation or screening of drugs for inhibiting MRSE or MSSE.

The invention relates to a synthesis method of 5H-dibenzo [b, e] azepine-6, 11-diketone. According to the method, a brand new intermediate is provided, 5H-dibenzo [b, e] azepine-6, 11-diketone is synthesized from the intermediate, raw materials in the method are cheap and easy to obtain, sodium azide in traditional synthesis is avoided, the reaction is green and safe, the product is unique, aftertreatment is simple and convenient, and the method is suitable for industrial large-scale production.

The invention discloses a preparation method of an azepam injection, the azepam injection comprises an azepam nanocrystal, a nonionic surfactant and purified water, the weight ratio of the azepam nanocrystal to the nonionic surfactant is 1: (0.05-0.2), and the weight ratio of the azepam nanocrystal to the nonionic surfactant is 1: (0.05-0.2). The azepine nanocrystal is prepared by the following process: taking a raw material medicine azepine, a surfactant and an organic solvent as solvents, and the preparation method comprises the following specific steps: a, dissolving azepine in the organic solvent to form a medicine solution; b, dissolving a surfactant in water to form a water phase solution; c, slowly dropwise adding the medicine solution into the water-phase solution at normal temperature and normal pressure, and stirring to form an oil / water type emulsion; d, crystallizing: heating the emulsion to 53-60 DEG C, increasing the pressure to 2.38 atm, evaporating for 30 minutes to remove the organic solvent, and precipitating the azepine to form nanocrystals; and e, filtering and washing. According to the invention, the problem of poor water solubility of the azepam is solved, and the prepared azepam injection is safe, stable and small in side effect.

The present invention provides a preparation method for a dihalogen-substituted dibenzo[b,f]azepine-5-carbonyl chloride compound that is prepared from compound II by means of a dihalogen substitution reaction. The method of the present invention has a reasonable process and a high reaction yield, and is suitable for large-scale industrial production. The reaction formula is as follows: wherein, R1 may be a halogen substituent such as bromine, chlorine, or iodine, and R2 may be H, C1-C6 alkoxy, etc.

The invention relates to the technical field of chemical synthesis, in particular to a method for oxidative synthesis of benzoxazepine or azepine compounds, which specifically comprises the following steps: taking biphenyl derivatives and sodium benzenesulfinate compounds as reaction raw materials, and electrifying and reacting in an electrolytic tank to obtain dibenzoxazepine derivatives. According to the method, firstly, an additional chemical oxidizing agent is not needed, a traditional chemical oxidation mode is replaced with electrode oxidation, impurities introduced by the chemical oxidizing agent and generated waste salt pollutants are reduced, the method better conforms to the green, economical and environment-friendly concepts, and the environment-friendly treatment cost is reduced;