19786-58-4

Usage

General Description

1H-Azepine-1,4-dicarboxylic acid, hexahydro-5-oxo-, 1,4-diethyl ester is a chemical compound with the molecular formula C14H23NO4. It is an ester of a hexahydro-5-oxo-1H-azepine-1,4-dicarboxylic acid. 1H-Azepine-1,4-dicarboxylic acid, hexahydro-5-oxo-, 1,4-diethyl ester is commonly used as a pharmaceutical intermediate and can be found in various drugs and medications. It is known for its potential therapeutic properties, including its use as an anticonvulsant and anxiolytic. Furthermore, studies have also shown its potential as a treatment for various neurological disorders. However, the compound is known to be toxic if ingested or inhaled, and proper safety precautions should be followed when handling it.

Upstream product

• 623-73-4 diazoacetic acid ethyl ester 
• 29976-53-2 N-ethoxycarbonyl-4-piperidone 
• 1972-28-7 diethylazodicarboxylate 

Relevant academic research and scientific papers

Discovery of β-Arrestin Biased Ligands of 5-HT7R

Though many studies have been published about therapeutic potentials of selective 5-HT7R ligands, there have been few biased ligands of 5-HT7R. The development of potent and selective biased ligands of 5-HT7R would be of great help in understanding the relationship between pharmacological effects and G protein/β-arrestin signaling pathways of 5-HT7R. In order to identify 5-HT7R ligands with biased agonism, we designed and synthesized a series of tetrahydroazepine derivatives 1 and 2 with arylpyrazolo moiety or arylisoxazolo moiety. Through several biological evaluations such as binding affinity, selectivity profile, and functions in G protein and β-arrestin signaling pathways, 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine 1g was discovered as the β-arrestin biased ligand of 5-HT7R. In an electroencephalogram (EEG) test, 1g increased total non-rapid eye movement (NREM) sleep time and decreased total rapid eye movement (REM) sleep time.

SUBSTITUTED AZEPINE- AND DIAZEPINE-SULFONAMIDES USEFUL TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1

In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11BETA-hydroxysteroid dehydrogenase type-1, pharmaceutical compositions containing the compounds, and met

The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors

Discovery of a series of azepine sulfonamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has

Pentacyclic kinase inhibitors

The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.

TETRACYCLIC KINASE INHIBITORS

The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R1, R2, R3, Ra,

Substituted azepine derivatives as serotonin receptor modulators

The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Design, Synthesis, and Evaluation of Metabolism-Based Analogues of Haloperidol Incapable of Forming MPP+-like Species

The long-term, irreversible, Parkinsonism-like side effects of haloperidol have been speculated to involve several mechanisms. More recently, it has been speculated that the metabolic transformation to MPP+-like species may contribute to the Parkinsonism-like side effects. Because BCPP+ and its reduced analogue have been shown to possess the potential to destroy dopamine receptors in the nigrostriatum, we have designed new analogues of haloperidol lacking the structural features necessary to form neurotoxic quaternary species but retaining their dopamine-binding capacity. The most potent agent at the D2 receptor, the homopiperidine analogue 11, was found to be equipotent to haloperidol. It was also of interest to identify analogues with DA binding profiles similar to that of clozapine at the dopamine receptor subtypes. Evaluation of the proposed agents shows that the ratio of D2 to D4 (2) binding of clozapine was mimicked by 7 [Ki(D2) = 33, Ki(D3) = 200, Ki(D4) = 11 nM; Ki(D2)/Ki(D4) = 3] and 9 [Ki(D2) = 44, Ki(D3) = 170, Ki(D4) = 24 nM; Ki(D2)/Ki(D4) = 2]. A preliminary in-vivo testing of compound 7 shows that its behavioral profile is similar to that of clozapine. This profile suggests that there is a need for further evaluation of these two synthetic agents and their enantiomers for efficacy and lack of catalepsy in animal models.

4-Anilidopiperidine Analgesics. 3. 1-Substituted 4-(Propananilido)perhydroazepines as Ring-Expanded Analogues

A study of ring-expanded analogues of the 4-(propananilido)piperidine analgesics has been undertaken in order to evaluate the influence of this structural modification on both analgesic activity and physical-dependence capacity.Thus, a series of 1-substit