475094-98-5

Upstream product

• 41253-21-8 sodium triazole 
• 312638-89-4 4-cyclohexyl-4-methanesulfonyloxymethylpiperidine-1-carboxylic acid tert-butyl ester 
• 312638-87-2 4-cyclohexyl-4-hydroxymethylpiperidine-1-carboxylic acid tert-butyl ester 
• 624732-70-3 (4-cyclohexylpiperidin-4-yl)-methanol 
• 167262-68-2 N-(t-butyloxycarbonyl)-4-phenylpiperidine-4-carboxylic acid 
• 77-17-8 Normeperidine 
• 4220-08-0 (4-phenyl-piperidin-4-yl)-methanol 

Downstream Products

• 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 
• 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 [(S)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide 
• 312637-48-2 (R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(S)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide 

Relevant academic research and scientific papers

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.

MELANOCORTIN RECEPTOR AGONISTS

The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

Melanocortin receptor ligands

The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W1 is a carbocyclic unit, and W2 is a heteroatom comprising unit.

Melanocortin receptor ligands

The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W is a pendant unit having the formula: -L-Q L is a linking unit, Q is preferably a cyclic hydrocarbyl unit; W1 is preferably a carbocyclic unit and W2 is a heteroatom comprising unit.

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.

Substituted piperidines as melanocortin-4 receptor agonists

Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.