397277-96-2

Upstream product

• 350-46-9 4-Fluoronitrobenzene 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 138227-62-0 tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate 
• 162402-39-3 4-(4-nitrophenoxy)piperidine 
• 916344-70-2 1-isopropyl-4-(4-nitrophenoxy)piperidine 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 5570-78-5 1-isopropylpiperidin-4-ol 

Relevant academic research and scientific papers

Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer's disease

Based on our previous work, a series of N-phenyl-3-methoxy-4-pyridinone derivatives were designed as orally bioavailable dual functional agents for therapy of Alzheimer's disease, through introducing alkyloxy moiety into 4-pyridinone ring to avoid the pos

Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H3 Receptor Inverse Agonist with Robust Wake-Promoting Activity

A series of chemical optimizations guided by in vitro affinity at a histamine H3 receptor (H3R), physicochemical properties, and pharmacokinetics in rats resulted in identification of N-[4-(1-cyclobutyl-piperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide dihydrochloride (17v, SUVN-G3031) as a clinical candidate. Compound 17v is a potent (hH3R Ki = 8.73 nM) inverse agonist at H3R with selectivity over other 70 targets, Compound 17v has adequate oral exposures and favorable elimination half-lives both in rats and dogs. It demonstrated high receptor occupancy and marked wake-promoting effects with decreased rapid-eye-movement sleep in orexin-B saporin lesioned rats supporting its potential therapeutic utility in treating human sleep disorders. It had no effect on the locomotor activity at doses several fold higher than its efficacious dose. It is devoid of hERG and phospholipidosis issues. Phase-1 evaluation for safety, tolerability, and pharmacokinetics, and long-term safety studies in animals have been successfully completed without any concern for further development.

N-substituted phenylpyridin-4-one derivatives and its preparation and use

The invention provides N-substituted phenyl-4-one derivatives and salts thereof. The N-substituted phenyl-4-one derivatives are synthesized through condensation of o-hydroxypyrone derivatives and aminophenol, alkylation, amine condensation and hydrogenation deprotection. A series of the N-substituted phenyl-4-one derivatives are designed and synthesized in the invention, and pharmacological activity screening tests show that like compounds have a substantial histamine H3 acceptor antagonist activity and an anti-Abeta-aggregation activity. The invention also provides an application of the N-substituted phenyl-4-one derivatives, salts thereof, and intermediates generated in the preparation process in the preparation of Alzheimer-related treatment medicines, especially a use of the derivatives, the salts thereof and the intermediates in the preparation of medicines for treating histamine H3 acceptor and Abeta-aggregation related diseases as a histamine H3 acceptor antagonist and a amyloid peptide (Abeta) aggregation inhibitor. A synthesis method of the compounds has the advantages of easily-available required raw materials, reasonable route design, mild reaction conditions, high yield of each step, simple operation and low production cost. A structural general formula of the derivatives is shown in the specification.

NOVEL PIPERIDINE DERIVATIVE

Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmac