333795-01-0

Upstream product

• 333794-97-1 4-{[1-(Trifluoroacetyl)-4-piperidinyl]methyl}benzenesulfonyl chloride 
• 157338-47-1 1-(trifluoroacetyl)-4-benzylpiperidine 
• 31252-42-3 4-benzylpyperidine 
• 333795-00-9 4-[(4-{[1-(Trifluoroacetyl)-4-piperidinyl]methyl)phenyl)-sulfonyl]morpholine 

Downstream Products

• 333796-43-3 N'-(4-chlorophenyl)-N-(3-{4-[4-(morpholin-4-ylsulfonyl)benzyl]piperidin-1-yl}propyl)-N-phenylurea hydrochloride 
• 711029-84-4 N-(3-{4-[4-(morpholin-4-ylsulfonyl)benzyl]piperidin-1-yl}propyl)aniline 

Relevant academic research and scientific papers

CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological evaluation of piperidine-4-carboxamide derivatives

Replacement of the 5-oxopyrrolidin-3-yl fragment in the previously reported lead structure with a 1-acetylpiperidin-4-yl group led to the discovery of a novel series of potent CCR5 antagonists. Introduction of small hydrophobic substituents on the central phenyl ring increased the binding affinity, providing low to sub-nanomolar CCR5 antagonists. The selected compound 11f showed excellent antiviral activity against CCR5-using HIV-1 replication in human peripheral blood mononuclear cells (EC50 = 0.59 nM) and an acceptable pharmacokinetic profile in dogs.

CCR5 antagonists as anti-HIV-1 agents. Part 2: Synthesis and biological evaluation of N-[3-(4-benzylpiperidin-1-yl)propyl]-N,N′- diphenylureas

We have previously reported the novel lead compound 1a as a CCR5 antagonist for treatment of HIV-1 infection. SAR studies on incorporating various acyl groups as a replacement for the 5-oxopyrrolidine-3-carbonyl group of the lead structure resulted in the

UREA COMPOUNDS, PROCESS FOR PRODUCING THE SAME AND USE THEREOF

A compound of the formula: [whereinR1 is a hydrocarbon group which may be substituted;R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted;R3 is halogen atoms, a carbam