29 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 present invention discloses a lubricating composition, which comprises an oil having lubricating viscosity and a benzazepine compound. A method of using such a lubricating composition is also disclosed.

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 the field of biomedicine technology, and more specifically to a benzazepine-2-one compound, its preparation method, and application. The benzazepine-2-one compound has high efficiency in inhibiting USP16 activity, providing a safe and efficient candidate drug molecule for the targeted treatment of prostate cancer. The benzazepine-2-one compound has a simple and easy preparation process and can be prepared in a single step via a click reaction. According to the experimental results in the examples of the present invention, the tumor inhibition rate of the tumor-bearing group of mice treated with the benzazepine-2-one compound was superior to that of the positive control group, indicating that the benzazepine-2-one compound can be used to treat prostate cancer and has good development prospects.

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 benzazaspiro derivatives represented by formula (I) and pharmaceutically acceptable salts thereof, as well as the compounds, can be used for diagnosing, preventing and / or treating diseases associated with vasopressin receptors.

The invention belongs to the field of organic synthesis, and discloses a sulfonylated benzoazepine [1, 2-a] indolone compound and a preparation method thereof. According to the preparation method, under the conditions of room temperature and visible light irradiation, 1-(2-(arylethynyl) benzoyl) indole, aryl thianthrene salt and 4-diazabicyclo [2.2. 2] octane-1, 4-dionium-1, 4-disulfinic acid are used as raw materials, tris (4-methoxyphenyl) amine is used as a catalyst, and the preparation of the sulfonylated benzazepine [1, 2-a] indolone compound is realized. The method has the advantages of mild reaction conditions, simplicity and convenience in operation, no photosensitizer, wide substrate application range and the like. The sulfonylated benzazepine [1, 2-a] indolone compound has potential application value in the research fields of organic synthesis and the like, a novel preparation method is provided for synthesis of the sulfonylated benzazepine [1, 2-a] indolone compound, and part of the synthesized compound has certain antitumor activity.

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.

The present invention provides benzodiazepine derivatives, radioactive probes and their applications, belonging to the field of biomedicine technology. The present invention modifies the benzodiazepine derivatives and introduces hydrophilic or lipophilic side chains. The prepared benzodiazepine derivatives can be used as precursors targeting V2R, which can achieve specific targeting of V2R and provide new molecular tools for the subsequent diagnosis and treatment of V2R-positive tumors. 68 The Ga-labeled radioactive probe of the present invention exhibits good tumor imaging effects and can achieve PET imaging of V2R-positive tumors, which helps to improve the accuracy of tumor diagnosis. It can also be used to evaluate treatment effects, has a high "target / non-target" ratio, and can better display the distribution of V2R receptors throughout the body. It has many applications in the diagnosis and treatment of cancer.

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 invention relates to the technical field of biological medicines, in particular to a benzazepine-2-ketone compound as well as a preparation method and application thereof. The benzazepine-2-one compound has the activity of efficiently inhibiting USP16, and provides a safe and efficient candidate drug molecule for targeted therapy of prostatic cancer; the preparation process of the benzoazepine-2-ketone compound is simple and easy to implement, and the benzoazepine-2-ketone compound can be prepared by Click reaction in one step. According to experimental results in the embodiment of the invention, the tumor inhibition rate of the benzazepine-2-one compound for treating a mouse tumor-bearing group is superior to that of a positive control group, so that the benzazepine-2-one compound can be used for treating prostatic cancer and has a good development prospect.

To provide a method for producing a benzazepine compound capable of easily removing impurities which are difficult to remove by purification by crystallization.SOLUTION: There is provided a method for producing a high-purity benzazepine compound by bringing a benzazepine compound into contact with activated carbon in a first solvent. The volume of pores having a diameter of 1.5 nm or more and 3.0 nm or less by a nitrogen gas adsorption method using activated carbon is preferably 0.1 mL / g or more and 0.5 mL / g or less.SELECTED DRAWING: None

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.

The present invention discloses a benzazepine derivative, a conjugate containing the same, and applications thereof. The present invention provides an antibody-immunostimulatory conjugate represented by Formula I or a pharmaceutically acceptable salt thereof. The benzazepine derivative has a good regulatory effect on TLR8 and can effectively treat, alleviate, and / or prevent various related diseases caused by immunosuppression, such as cancer. [Formula 1] JPEG2025537044000630.jpg13169

The invention relates to a novel use of benzazepine, benzoxazepine, benzothiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having both neutral endopeptidase (NEP) and / or human soluble endopeptidase (hSEP), and endothelin convertase (ECE), inhibitory activity. The compounds of this invention are useful for the preparation of pharmaceutical compositions to reduce harmful effects of symptomless progressive disseminated perfusion deficiency of organs, or parts thereof, that may be suggestive of systemic diseases.

The present invention provides immunoconjugates of Formula I, which immunoconjugates comprise an antibody linked by conjugation to one or more aza-benzaza derivatives. The present invention also provides an aza-benzaza derivative intermediate composition comprising a reactive functional group. Such intermediate compositions are suitable substrates for forming the immunoconjugates via linkers or linking moieties. The invention further provides methods of treating cancer with the immunoconjugates. Ab-[L-D] pI

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 discloses a method for synthesizing benzazepine compounds; in a nitrogen atmosphere, a sulfonium salt in-situ generated from methyl trifluoromethanesulfonate and dimethyl sulfide is used as an activator, and undergoes a cyclization reaction with N,N-dibenzyl-3-phenylpropylamide compounds at 80 °C to generate benzazepine compounds; wherein methyl trifluoromethanesulfonate and dimethyl sulfide are activator precursors; the amide compounds include aryl amides, alkyl amides, heterocyclic amides, and amides with asymmetric functional groups connected to N; this method is a new method for synthesizing benzazepine compounds, without the participation of catalysts and additives, and the raw materials required are simple and easily available, the reaction conditions are mild, the operation is simple, the reaction yield is high, the substrate functional group compatibility is excellent, and it has high application value.

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.

Benzaza # imgabs0 # derivatives of formula (I), compositions comprising therapeutically effective amounts of these benzaza # imgabs1 # derivatives, and methods of using these derivatives or compositions in the treatment of cognitive impairment associated with central nervous system (CNS) disorders or associated with cognitive impairment risk factors. In particular, the present invention relates to the use of an alpha5-containing GABAA R agonist (e.g., an alpha5-containing GABAA R positive allosteric modulator) in the treatment of cognitive impairment associated with central nervous system (CNS) disorder or having a risk factor associated with cognitive impairment in a subject in need or at risk, the subjects include, but are not limited to, subjects having or at risk of age-related cognitive impairment, mild cognitive impairment (MCI), amnetic MCI (aMCI), age-related memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), proactive AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), or the like. Cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X disorder, Rett syndrome, compulsive behavior and substance addiction associated with cancer treatment. The present invention also relates to the use of [alpha] 5-containing GABAA R agonists (e.g., [alpha] 5-containing GABAA R positive allosteric modulators), as described herein, in the treatment of brain cancer, including brain tumors, e.g., myeloblastoma, and cognitive impairment associated therewith. # imgabs2 #

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.

The invention relates to the field of medical chemistry, and discloses a benzaza # imgabs0 # dipeptide ester compound as well as a preparation method, a pharmaceutical composition and application of the benzaza # imgabs0 # dipeptide ester compound. The structural general formula of the benzaza # imgabs 1 # dipeptide ester compound is as shown in formula (I): # imgabs 2 # R2 is selected from-CH (CH3) 2 or-CH (CH2) 2, R6 is selected from-CH (CH3) 2 or-CH (CH2) 2, and R8 is selected from-H or-OH. According to the benzaza # imgabs 3 # dipeptide ester compound provided by the invention, the problem of poor lipid solubility of benzaza # imgabs 4 # seven-membered ring is solved, and the problem that the benzaza # imgabs 4 # seven-membered ring permeates a blood brain barrier is solved by covalent coupling of propofol (the Log P value is increased from-0.44 to 3.96); moreover, a benzaza # imgabs5 # dipeptide ester compound with a dual hybrid molecular structure is constructed, and benzaza # imgabs6 # and propofol pharmacophores simultaneously play an anti-inflammatory function by different targets after penetrating through BBB (Benzoyl Boron Boron) at the same time, so that a synergistic multi-target effect is achieved.

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.