26 results about "Benzazepines" 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 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 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 relates to the technical field of the synthesis of benzodiazepine compounds, and specifically discloses a magnetic nano-bifunctional acid catalyst, a preparation method thereof, and a catalytic application. In the present invention, Fe3O4@SiO2 core-shell nanoparticles modified with a chlorosilane coupling agent are selected as the carrier, and an aminophosphonic acid compound is used as the grafting substance. Through the dehydrochlorination reaction between the Cl in the silane coupling agent and the NH2 in the aminophosphonic acid compound, the grafting of the aminophosphonic acid compound on the surface of the magnetic nanoparticles is realized. Then, with the aminophosphonic acid compound as the loading medium, the metal atom in the Lewis acid is coordinated with the N in the amino group and the O in the phosphoric acid group of the aminophosphonic acid compound respectively, forming a stable polycyclic structure, and the purpose of stably loading the transition metal Lewis acid and phosphonic acid on the surface of the magnetic nanoparticles is achieved. It has broad application prospects in the field of synthesizing 1,5-benzodiazepine compounds containing a spiro ring structure.

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.

To provide a pharmaceutical composition capable of reducing side effects of tolvaptan.SOLUTION: A pharmaceutical composition comprising a compound represented by Formula (1) or a metal salt thereof is provided, wherein it is used such that 4 to 20 mg of the compound represented by Formula (1) or a metal salt thereof is transvascularly administered over a period of 10 minutes or more.SELECTED DRAWING: None

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 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 current invention provides a novel electrochemical synthetic method for producing a novel dihydrobenzo[b,e] pyrroloazepines hybrides containing maleimide and tetrahydroquinoline heterocycles using specially designed olefin known as 2-amino substituted benzylidene derivatives as starting material. Seven-membered N-containing heterocycles, in particular 1-benzazepines are the integral structure of many bioactive compounds such as antidepressant drugs, anti-convulsants, anti-HIV etc. This present method provides an oxidant-free and metal-free process for the synthesis of a new class of Dihydrobenzo[b,e] pyrroloazepines hybrid containing maleimide / succinamide, benzoazepine and tetrahydroisoquinoline as well as other cyclic / acyclic amines via electrochemical C(sp3)- H functionalizing followed by cascade cyclization using easily available reagents. unique, efficient, eco-friendly, cost-effective, and safe technology has been developed to expedite the novel synthetic process. This method comprises the simple electrochemical synthesis of dihydrobenzo[b,e] pyrroloazepines derivatives using a suitable electrode and electrolyte under ambient temperature. The synthesis employs an environmentally friendly electrochemical method that doesn't rsequire transition metals and external oxidants. This method is highly effective and scalable, contributing to both atom and step economy in the process. As a result, this methodology holds substantial significance. It presents a novel avenue for synthesizing new scaffolds that are useful as potential bioactive heterocyclic scaffolds photophysically relevant, including and chemo sensors to detect picric acid and other nitro compounds.

The present disclosure relates to compositions and methods, including prodrugs of (S)-3-(3-(((3,4- dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)methyl)(methyl)amino)propyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-2H- benzo[d]azepin-2-one that find use in the treatment of diseases and disorders, such as therapies for cardiovascular disease, including cardiac arrhythmias, including, without limitations, sinus tach (e.g. inappropriate sinus tachycardia (IST)), postural orthostatic tachycardia syndrome (POTS), coronavirus (COVID-19) (e.g. long COVID) and COVID-associated cardiovascular abnormalities, supraventricular tachycardia (SVT), tachycardia (e.g. rapid heart rate, atrial tachycardia), heart failure (e.g. congestive heart failure (CHF), systolic heart failure, pediatric heart failure, chronic heart failure), myocardial ischaemia, angina (e.g. angina pectoris), myocardial infarct, rhythm disturbances (e.g. supraventricular rhythm disturbances), chest pain, cardiomyopathy, coronary artery disease, and left ventricular dysfunction (LVD).

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 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.

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 is based on the system Xc - Compounds of formula (I) or pharmaceutically acceptable salts thereof are useful in the treatment of diseases and / or disorders in which [Formula 1] JPEG2026505789001043.jpg5648 Regarding.

The current invention provides a novel electrochemical synthetic method for producing a novel dihydrobenzo[b,e] pyrroloazepines hybrides containing maleimide and tetrahydroquinoline heterocycles using specially designed olefin known as 2-amino substituted benzylidene derivatives as starting material. Seven-membered N-containing heterocycles, in particular 1-benzazepines are the integral structure of many bioactive compounds such as antidepressant drugs, anti-convulsants, anti-HIV etc. This present method provides an oxidant-free and metal-free process for the synthesis of a new class of Dihydrobenzo[b,e] pyrroloazepines hybrid containing maleimide / succinamide, benzoazepine and tetrahydroisoquinoline as well as other cyclic / acyclic amines via electrochemical C(sp3)- H functionalizing followed by cascade cyclization using easily available reagents. unique, efficient, eco-friendly, cost-effective, and safe technology has been developed to expedite the novel synthetic process. This method comprises the simple electrochemical synthesis of dihydrobenzo[b,e] pyrroloazepines derivatives using a suitable electrode and electrolyte under ambient temperature. The synthesis employs an environmentally friendly electrochemical method that doesn't rsequire transition metals and external oxidants. This method is highly effective and scalable, contributing to both atom and step economy in the process. As a result, this methodology holds substantial significance. It presents a novel avenue for synthesizing new scaffolds that are useful as potential bioactive heterocyclic scaffolds photophysically relevant, including and chemo sensors to detect picric acid and other nitro compounds.

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 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 application belongs to the technical field of pharmacy, and particularly relates to a preparation method and application of 3,3-difluoro-1,7-dimethyl-5-phenyl-1,3-dihydro-2H-benzo[b]azepin-2-one. The compound is prepared under the conditions of no metal and no oxidant by photochemical driving, and the compound has antitumor activity.

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 Alzheimer's disease prevention and treatment medicine containing a benzaza # imgabs0 # ligand and application thereof.The adopted benzazepine ligand is a compound SOMCL-668, the compound SOMCL-668 is adopted for activating an ERK1 / 2 signal channel in the brain of an Alzheimer's disease transgenic model 3 * Tg-AD mouse, apoptosis of nerve cells is reduced, and the Alzheimer's disease is prevented and treated. The deposition of amyloid plaques, the entanglement of nerve fibers and the loss of neurons are reduced, and the learning and memory ability of 3 * Tg-AD mice is improved. Therefore, the benzaza # imgabs 1 # ligand can be used as a pharmaceutical active ingredient for preparing a medicine for preventing or treating the Alzheimer's disease.

The application relates to a method for synthesizing triphenobenzo[b, d, f] azepine from a cyclic diaryliodonium salt, and belongs to the field of chemical synthesis. Under proper reaction conditions, triphenobenzo[b, d, f] azepine is obtained in one step by taking isatin anhydride derivatives and a cyclic diaryliodonium salt as substrates. The application provides a more economical and simple synthesis method for the synthesis of triphenobenzo[b, d, f] azepine, has the advantages of simple steps, high atom economy and excellent yield, and is expected to realize industrialized scale production.

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.