83674-75-3

Upstream product

• 3612-20-2 1-phenylmethyl-4-piperidone 
• 95-46-5 2-methylphenyl bromide 

Downstream Products

• 821768-11-0 1,2,3,6-tetrahydro-4-(2-methylphenyl)-1-(phenylmethyl)-pyridine 
• 630116-52-8 4-(2'-methylphenyl)piperidine 
• 82212-02-0 4-(2-methylphenyl)piperidine hydrogen chloride salt 
• 1370256-34-0 1-benzyl-4-(2-methylphenyl)-1,2,3,6-tetrahydropyridinium chloride 
• 1623467-77-5 3,3-diethyl-5-(4-o-tolyl-piperazin-1-ylmethyl)-dihydrofuran-2-one 
• 864830-75-1 (7RS)-7-(4-o-tolylpiperidin-1-ylmethyl)-5,6,7,9-tetrahydro-8H-pyrido[2,3-b]azepin-8-one 
• 864829-89-0 tert-butyl (3S*,4R*)-3-fluoro-4-o-tolylpiperidine-1-carboxylate 
• 864829-88-9 tert-butyl (3R*,4R*)-3-fluoro-4-o-tolylpiperidine-1-carboxylate 

Relevant academic research and scientific papers

Bioisosteric replacement and related analogs in the design, synthesis and evaluation of ligands for muscarinic acetylcholine receptors

Previous structure-activity relationship studies involving a series of lactone-based muscarinic ligands identified a lead compound containing a diphenylmethylpiperazine moiety (4; IC50 = 340 nM). The purpose of the present work is to investigate 1,3-benzodioxoles, 4,4-diethyl substituted tetrahydrofurans, 5-substituted oxazolidinones and chromones as bioisosteric replacements for the lactone ring in a novel series of muscarinic ligands. The approach provided compounds with improved % inhibition values and identified a non-selective muscarinic ligand with an IC50 value of 280 nM. The structure-activity relationship for this new series will be discussed. Selected compounds were evaluated in preliminary assays for subtype selectivity and were found to be non-selective.

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists

A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.

CYCLOALKANOPYRIDINE DERIVATIVE

Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2- yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist

High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified t