624732-70-3

Upstream product

• 4220-08-0 (4-phenyl-piperidin-4-yl)-methanol 
• 10462-00-7 4-cyclohexylpiperidine-4-carboxylic acid ethyl ester 
• 167262-68-2 N-(t-butyloxycarbonyl)-4-phenylpiperidine-4-carboxylic acid 
• 77-17-8 Normeperidine 

Downstream Products

• 312638-87-2 4-cyclohexyl-4-hydroxymethylpiperidine-1-carboxylic acid tert-butyl ester 
• 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 
• 475095-00-2 [1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 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 
• 852319-26-7 2-amino-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-propan-1-one 
• 312639-10-4 (2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxo-propan-2-amine 
• 312638-89-4 4-cyclohexyl-4-methanesulfonyloxymethylpiperidine-1-carboxylic acid tert-butyl ester 
• 475094-98-5 4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidine-1-carboxylic acid tert-butyl ester 
• 312638-92-9 4-cyclohexyl-4-(1H-1,2,4-triazol-1-yl-methyl)piperidine 

Relevant academic research and scientific papers

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.

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.

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.