312639-10-4

Upstream product

• 475094-99-6 [1-(4-chlorobenzyl)-2-(4-cyclohexyl-4-[1,2,4]triazole-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]carbamic acid tert-butyl ester 
• 4220-08-0 (4-phenyl-piperidin-4-yl)-methanol 
• 77-17-8 Normeperidine 
• 167262-68-2 N-(t-butyloxycarbonyl)-4-phenylpiperidine-4-carboxylic acid 
• 624732-70-3 (4-cyclohexylpiperidin-4-yl)-methanol 
• 312638-92-9 4-cyclohexyl-4-(1H-1,2,4-triazol-1-yl-methyl)piperidine 
• 312638-87-2 4-cyclohexyl-4-hydroxymethylpiperidine-1-carboxylic acid tert-butyl ester 
• 57292-44-1 N-Boc-D-(4-Cl)Phe-OH 
• 312638-89-4 4-cyclohexyl-4-methanesulfonyloxymethylpiperidine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 457895-19-1 {2-[1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethylcarbamoyl]-ethyl}-carbamic acid tert-butyl ester 
• 1347810-43-8 4-({(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethyl}amino)-N-phenylpiperidine-1-carboxamide 
• 312637-48-2 (R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide 
• 312637-48-2 (S)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide 
• 874897-05-9 N-{(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethyl}tetrahydro-2H-pyran-4-amine 
• 874897-12-8 tert-butyl 4-({(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethyl}amino)piperidine-1-carboxylate 

Relevant academic research and scientific papers

Chiral effect of a Phe residue in position 3 of the Dmt1-l (or d)-Tic2 analogues on opioid functional activities

In this letter, we describe a structure-activity relationships study, specifically related to the chirality of third amino acid residue in our H-Dmt-l(or d)-Tic analogues, of which C-terminus is attached to a piperidinyl moiety. Observed selectivities and functional activities of these analogues demonstrated that the chiralities of the second and third position residues are crucial for determining whether these ligands act as antagonists or agonists at the δ opioid receptor, but not at the μ opioid receptor.

OXOPIPERIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF

The present invention relates to compounds of formula (I) as defined herein that are melanocortin receptor agonists, to the preparation thereof and to the therapeutic use thereof in the treatment or prevention of a condition selected from obesity, diabetes and sexual dysfunctions that can affect both sexes, in the treatment of cardiovascular diseases, and also in anti-inflammatory uses or in the treatment of alcohol dependency.

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1- (4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl) piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist

Synthetic and natural peptides that act as nonselective melanocortin receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity.