16 results about "Benzazepine" patented technology

A benzazepine fused ring derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and the use of a compound in the diagnosis, prevention and / or treatment of diseases related to vasopressin receptors.

The invention relates to a composition comprising a piperazine-benzazepine, a buffer and a surfactant, and uses of such compositions such as treating, preventing, and / or suppressing symptoms of schizophrenia, schizoaffective disorders, and / or Parkinson's disease. The compositions have improved parameters such as a lower variance in pH, improved stability during storage, and lower solubility of piperazine-benzazepines, resulting in piperazine-benzazepine particle formation with improved particle size and particle size distribution. The compositions are useful as therapeutic agent, for instance through parenteral administration to a subject.

The invention belongs to the technical field of medicinal chemistry, and relates to a benzazepine compound or pharmaceutically acceptable salt thereof as well as a preparation method and application of the benzazepine compound, in particular to a compound with a structural general formula as shown in a formula (I). The benzoazepine compound disclosed by the invention has a remarkable curative effect on treating brain organic lesion diseases, including vascular lesion and degenerative lesion, especially vascular dementia, Alzheimer's disease and cholinergic deficiency related diseases. Formula (I).

The application relates to a method for preparing an eight-membered selenium-containing benzazepine compound, which comprises the following steps: taking an N-(but-3-en-1-yl)-4-methyl-N-(2-(1-phenylvinyl)phenyl)benzenesulfonamide compound as a substrate, generating a selenyl radical through anodic oxidation of a selenide under electrochemical driving, and obtaining the eight-membered selenium-containing benzazepine compound through radical coupling-cyclization of the selenyl radical and the substrate. The method steps have the advantages of green simple operation, use of traceless electrons instead of an external oxidizing and reducing agent, avoidance of use of a metal catalyst and an external oxidizing and reducing agent, economy, simple and easy-to-prepare raw materials, wide substrate range and the like.

The present invention relates to a salt type and crystal form of a benzazepine fused ring compound and use thereof, and in particular to a maleate of a compound represented by formula (I), the structure of the maleate being represented by formula (II).

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 benzo-aza compound as well as a preparation method and application thereof. The benzazepine compound and the pharmaceutically acceptable salt of the benzazepine compound prepared by the invention have relatively high sensitivity and very strong cytotoxic activity to human colon cancer cells HCT116 tumor cells. The triethylene diamine catalyst is adopted in the process of preparing the benzo-aza compound, the reaction conditions are relatively conventional, the reaction process is mild, simple and convenient, the operation is easy, the cost is low, and the method is suitable for industrial large-scale production; according to the method, various substrates are used as reactants, products with various and complex structures are obtained, the yield is high, and the application range of the method is widened. The compound prepared by the preparation method disclosed by the invention has relatively high cytotoxic activity on human colon cancer cells HCT116. Therefore, the preparation method provided by the invention can provide a basis for screening the benzazepine compound with good activity on tumor cells, and is beneficial to further screening out compounds with more excellent biological activity.

Benzazepine compounds, methods of making and medical uses thereof. In particular, compounds of Formula II-1 or Formula VIII-1 and pharmaceutical compositions containing the same, and medical uses thereof. The benzazepine compounds can be used for treating diseases associated with vasopressin receptors, in particular hypertension, heart disease, etc.

The application relates to the technical field of pharmaceutical chemistry, and discloses a benzazepine bridged ring derivative and a preparation method thereof. The preparation method comprises the following steps: adding a substrate (1.0 eq), a sulfur-substituted benzylpropyl aldehyde (1.5 eq), a base DABCO (0.2 eq) and dry acetonitrile (2.0 mL) into a reaction test tube, mixing the mixture at normal temperature for 24 hours, concentrating and purifying after the reaction is completed to obtain a hemiacetal product 3. Then the hemiacetal product, chloroform (0.5 mL) and H2O (100 muL) are added into the reaction test tube, and stirring is carried out at 60 DEG C for 72 hours. The reaction is monitored to be completed through thin layer chromatography, then the reaction mixture is directly purified through column chromatography to obtain a corresponding target product. The preparation method has the advantages of simple operation, mild reaction and high yield. The derivative provided by the application has good antibacterial activity, and has a wide market application prospect.

This invention relates to the fields of organic light-emitting materials and tumor drugs, and particularly to a benzozaindolone compound, its preparation method, and its application. The structural formula of the benzozaindolone compound is shown in formula (3). This invention adopts a one-step synthesis strategy, which is simple, mild, has inexpensive and widely available substrates, and has a high conversion yield. It provides a simple and green synthetic approach for the synthesis of benzozaindolone compounds. Furthermore, the target compound (benzozaindolone compound) has excellent fluorescence luminescence properties and biocompatibility, and can be directly applied to fluorescence imaging of cancer cells and type I photodynamic therapy.

Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. Specifically, disclosed is a class of benzazepine fused ring derivatives as V2 receptor antagonists.

The present invention relates to the field of compound synthesis, and in particular to a method for aryl debromination and acylation of a brominated benzazepine compound. The method comprises the following steps: mixing a solution containing a brominated benzazepine compound with a solution containing a dehydrogenation reagent to implement a first reaction to remove active hydrogen from an azacyclic ring, so as to obtain a first material; mixing the first material with a solution containing a debromination reagent to implement a second reaction to obtain a second material; subjecting the second material and a solution containing an amide compound to a third reaction, so that a nucleophilic substitution occurs in a substitution position of original bromine on the aryl of the brominated benzazepine compound to obtain an acylated substituent; and after the reaction is complete, quenching the resulting material and performing work-up to obtain an acyl-substituted benzazepine compound, wherein the brominated benzazepine compound is selected from one of a brominated indole compound, a brominated benzimidazole compound, a brominated indazole compound, a brominated indoline compound, and a brominated carbazole compound. The method of the present invention employs mild conditions and provides a product yield of 80% or more.

The invention discloses a medicine containing a small molecule compound with a 2-aryl formyl benzo-aza structure and application of the medicine. The small molecule compound with the 2-arylformyl benzo-aza structure and pharmaceutically acceptable salt or eutectic, deuterated compound, solvate and enantiomer thereof can be used for preparing medicines for preventing and / or treating inflammatory lung diseases, or preparing medicines for inhibiting alveolar macrophages from generating inflammatory factors; the medicine is a medicine which contains a small molecule compound with a 2-aryl formyl benzo-aza structure and is used for preventing and / or treating inflammatory lung diseases. The compound provided by the invention can provide a new treatment strategy for preventing or treating inflammatory lung diseases, and has a wide application prospect.

The application discloses a medicine containing a small-molecule compound with a 2-aromatic benzoyl benzazepine structure and an application thereof. The small-molecule compound with the 2-aromatic benzoyl benzazepine structure and a pharmaceutically acceptable salt or co-crystal, deuterated compound, solvate or enantiomer thereof can be used for preparing a medicine for preventing and / or treating an inflammatory lung disease or for preparing a medicine for inhibiting alveolar macrophages from producing inflammatory factors; the medicine is a medicine for preventing and / or treating an inflammatory lung disease and contains the small-molecule compound with the 2-aromatic benzoyl benzazepine structure. The compound provided by the application can provide a new treatment strategy for the prevention or treatment of an inflammatory lung disease and has a wide application prospect.

The invention belongs to the technical field of chemical medicine raw material medicine and preparation manufacturing, and particularly relates to a preparation method of a varenicline tartrate intermediate. According to the present invention, 2, 3, 4, 5-tetrahydro-7, 8-dinitro-3-(trifluoroacetyl)-1, 5-methylene-1H-3-benzaza is adopted as a raw material, and the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5-methylene-1H-3-benzaza is prepared through the reduction of disulfurous acid or a salt thereof, such that the method does not need to use hydrogen pressurization, can be used for preparing the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5-methylene-1H-3-benzaza, and can be used for preparing the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5- meanwhile, the use of heavy metal palladium is avoided, the reaction condition is mild, the cost is low, the target product yield is high (greater than 75%), the purity is excellent (greater than 97%), and the industrial production of varenicline tartrate is facilitated.

A tetrahydro-1H-benzazepine compound as a potassium channel modulator, a preparation method, and a medicament containing the compound are provided. Specifically, the compound has the structure shown by formula A, in which the definitions of each group and substituent are described in the description. A preparation method for the compound and its use as potassium channel modulator are also described.