24 results about "Azepine" patented technology

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 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 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.

Provided are organic electroluminescent materials based on azepine and its analogues, such as compounds of Formula (I) in which two of ring A, ring B, and ring C independently each represent a structure of Formula (II). Also provided are formulations comprising these compounds. Further provided are OLEDs and related consumer products that utilize these compounds.

This invention belongs to the field of synthesis of benzo[b]azapyrrolizidine derivatives, specifically disclosing an antitumor active molecule, a benzo[b]azapyrrolizidine derivative, its synthesis method, and its application. This invention uses a transition metal Pd catalyst to generate a benzo[b]azapyrrolizidine derivative active molecule, as shown in general formula (2), from an acetylacetamide of general formula (1) in the presence of a ligand, a basic substance, and a solvent, under a nitrogen atmosphere and irradiation with light at a wavelength of 420–500 nm. This invention achieves the synthesis of structures containing benzo[b]azapyrrolizidine molecular fragments through a free radical relay tandem cyclization reaction from aryl to alkyl to vinyl groups catalyzed by transition metal Pd, realizing the synthesis of such molecules. Furthermore, a series of synthesized benzo[b]azapyrrolizidine molecules and their derivative active molecules have been tested and found to possess antitumor activity.

The invention discloses an aza-fused ring compound as well as a pharmaceutical composition and application thereof. The structure of the compound is shown in a formula I, the compound can effectively inhibit ASM activity, the optimal enzyme inhibition rate of the micromolar concentration level reaches 100%, and the optimal enzyme inhibition IC50 value is lower than 5 nM; the medicine effect can be achieved at the molecular level, the cell level and the animal level, and the treatment effect is excellent; the compound has application prospects in treating ASM-related diseases such as depression, senile dementia, cognitive impairment, cerebral apoplexy, myocardial ischemia, pulmonary fibrosis, chronic obstructive pulmonary disease, lung injury, pulmonary arterial hypertension, respiratory distress syndrome, respiratory cystic fibrosis, fatty liver, hepatic fibrosis, autoimmune diseases, tumors, diabetes and the like.

This invention discloses a benzo[a]oxo(carbon / sulfur)nitrogen compound and its applications. The general structural formulas of the benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention are shown in formulas (I) and (II): wherein: A is selected from methyl (racemic, R configuration, S configuration), ethyl (racemic, R configuration, S configuration), or cyclopropyl; X1 is selected from oxygen, ammonia, or sulfur; X2 is selected from methylene, oxygen, or sulfur; R1 is selected from hydrogen, fluorine, chlorine, bromine, or methyl; R2 is selected from hydrogen, fluorine, chlorine, bromine, or methyl. The benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention exhibit good monoamine oxidase B inhibitory activity and show extremely high selectivity within the monoamine oxidase family; in a mouse Parkinson's disease model, the benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention show good therapeutic effects.