40 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.

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 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 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 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;

The present application relates to waste resource utilization technical field, especially disclose a kind of high azepine content tar waste residue generated in the production of p-phenylenediamine rubber antioxidant key intermediate-RT peiser high-efficiency resource utilization method and its application in the field of environmental remediation.The resource utilization method stably derives and prepares nano-porous carbon with high nitrogen doping amount with high yield to high-efficiency stabilization of azepine waste residue.The present application is simple, efficient, green and environmentally friendly, with no additional pollutant emissions, and the required raw materials can be recycled without wasting resources.The porous carbon prepared has excellent performance in adsorbing and removing various nitrophenol pollutants in water, achieving the goal of "waste treatment".

The invention provides immunoconjugates of Formula I comprising an anti-Claudin 18.2 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 belongs to the technical field of organic synthesis, and relates to an efficient synthesis method of an intermediate 6-methoxyl indole aza for synthesizing vindoline, 6-methoxyl tryptamine is used as an initial raw material, and the method comprises the following steps: (1) condensing 6-methoxyl tryptamine and 4-nitrobenzenesulfonyl chloride to obtain an N-sulfonylation product 2; (2) carrying out regioselective Michael addition reaction on the compound 3 and brominated methyl acrylate under an alkaline condition to obtain a compound 3; (3) carrying out an intramolecular free radical cyclization reaction under the action of a cuprous iodide / tris (2-picolyl) amine catalytic system to construct an indolo-aza skeleton, so as to obtain a compound 4; and (4) removing a sulfonyl protecting group through potassium phosphate / p-methoxythiophenol to obtain the vindoline intermediate. The synthetic route only needs four-step reaction, the total yield reaches 54.5%, compared with the prior art, the reaction steps are remarkably shortened, the yield is improved, the use of a toxic noble metal catalyst is avoided, the method has the advantages of being easy and convenient to operate, low in cost and the like, and an efficient way is provided for industrial preparation of vindoline.

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 a tricyclic thiazolo [5, 4-d] pyrimidone amine derivative and application thereof.The preparation method comprises the steps that ethyl cyanoacetate serves as a raw material, a hydroxylamine compound (A) is generated under the action of sodium nitrite and phosphoric acid, 2-amino ethyl cyanoacetate (B) is obtained through reduction, the 2-amino ethyl cyanoacetate (B) is subjected to a reaction with acetic anhydride and Lawson to obtain a 5-amino-4-formate thiazole compound (D), and the 5-amino-4-formate thiazole compound (D) is subjected to a reaction with acetic anhydride and Lawson to obtain the tricyclic thiazolo [5, 4-d] pyrimidone amine derivative. The preparation method comprises the following steps: under the action of phosphorus oxychloride, obtaining a 2-bromo-pyrroline [1, 2-a] thiazolo [5, 4-d] pyrimidinone compound (F), a 2-bromine-7, 8-dihydro-5H-pyridine [1, 2-a] thiazolo [5, 4-d] pyrimidine-10 (6H) ketone derivative (G) and a 2-bromine-6, 7, 8, 9-tetrahydrothiazolo [5 ', 4': 4, 5] pyrimidino [1, 2-a] azepine-11 (5H)-ketone (H); 36 different substituted tricyclic thiazolopyrimidinone amine compounds F1-F12, G1-G12 and H1-H12 are obtained under the action of alkali, and the inhibitory activity of the 36 compounds on cancer cells is investigated.

The present invention discloses a dihydropyrazole-azepine compound, a pharmaceutical composition containing the same, and its use in anti-tumor treatment. The structure of the dihydropyrazole-azepine compound is shown in Formula I. The inventors of the present invention have confirmed through multiple experiments that the compound of the present invention has a significant inhibitory effect on AKT1, exhibiting a potent anti-proliferative effect on tumor cell lines such as mouse neuroblastoma Neuro2a cells and a potent differentiation-inducing effect on Neuro2a cell lines. Therefore, the compound of the present invention can be used as a differentiation-inducing regulator and / or AKT inhibitor in drugs for treating solid tumors or blood cancers associated with cell proliferation and differentiation abnormalities in humans or animals.

The present invention discloses a tribenzo[b,f]azepine phosphoramidite ligand, a preparation method thereof, and an application thereof. The structural formula thereof is shown in formula (I): In the tribenzo[b,f]azepine phosphoramidite ligand of the present invention, the N-terminal structure is an asymmetric benzoiminostilbene. The benzoiminostilbene makes the fused ring system at the N-terminal of the ligand larger, and the conjugated system and the π electron cloud are expanded. This not only increases the coordination ability of the metal and the ligand, but also has a certain steric hindrance effect, which not only helps to promote the occurrence of asymmetric reactions, but also can expand the scope of application of the ligand, making the ligand suitable for catalyzing a variety of different asymmetric reactions.