146396-02-3

Upstream product

• 146395-96-2 2-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanenitrile 
• 146395-97-3 4-Cyano-4-(3,4-dichloro-phenyl)-7-(tetrahydro-pyran-2-yloxy)-heptanoic acid ethyl ester 
• 146395-98-4 5-tetrahydropyranyloxypropyl-5-(3,4-dichlorophenyl)piperidone 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 33821-94-2 3-(tetrahydro-2H-pyran-2-yloxy)propyl bromide 
• 98-88-4 benzoyl chloride 
• 146395-99-5 3-(3,4-Dichloro-phenyl)-3-[3-(tetrahydro-pyran-2-yloxy)-propyl]-piperidine 

Downstream Products

• 146396-03-4 1-benzoyl-3-(3,4-dichlorophenyl)-3-(3-methane-sulphonyloxypropyl)piperidine 
• 172734-75-7 [3-(3,4-Dichlorophenyl)-3-(3-hydroxy-propyl)-piperidin-1-yl]-phenyl-methanone 

Relevant academic research and scientific papers

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1

We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template

High affinity, selective hNK2 or hNK3 ligands can be prepared from the common template 1 in a few simple chemical operations. The hNK3 ligands 3 antagonise the calcium mobilisation caused by activation of hNK3 receptors expressed in CHO cells as measured using fura-2 microspectrofluorimetry.