363191-04-2

Upstream product

• 674791-75-4 C₇H₈O₃S*C₁₂H₂₁NO₂ 
• 852323-76-3 1-tert-butoxycarbonyl 4-tert-butylcarbamoyl-4-cyclohexylpiperidine 
• 167262-68-2 N-(t-butyloxycarbonyl)-4-phenylpiperidine-4-carboxylic acid 
• 363191-02-0 N-(tert-butyl)-4-cyclohexylpiperidine-4-carboxamide 
• 363191-03-1 [(1R)-2-[4-Cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]carbamic Acid 1,1-dimethylethyl Ester 
• 852323-77-4 1-BOC-4-cyclohexyl-4-piperidinecarbonyl chloride 
• 273378-16-8 (1-tert-butoxycarbonyl)-4-cyclohexylpiperidine-4-carboxylic acid 

Downstream Products

• 363189-18-8 (2S)-2-[[[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]amino]carbonyl]-1,4-piperazinedicarboxylic Acid 1-(1,1-dimethylethyl) 4-(phenylmethyl) Ester 
• 852683-09-1 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-5-ethyl-4-methyl-piperazine-1-carboxylic acid tert-butyl ester 
• 363191-99-5 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-6-isopropyl-piperazine-1,4-dicarboxylic acid di-tert-butyl ester 
• 363190-28-7 (2S)-2-[[[(R)-2-[4-Cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]amino]carbonyl]-4-methyl-1-piperazinecarboxylic Acid 1,1-dimethylethyl Ester 
• 363191-06-4 4-(2-tert-butoxycarbonylamino-propionyl)-2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 363190-30-1 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-(2,2-difluoro-ethyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 363189-67-7 (S)-3-[(R)-2-(4-tert-Butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-methyl-piperazine-1-carboxylic acid benzyl ester 
• 363190-57-2 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-ethyl-piperazine-1-carboxylic acid tert-butyl ester 
• 363190-29-8 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-isopropyl-piperazine-1-carboxylic acid tert-butyl ester 
• 834888-53-8 2-[2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Melanocortin subtype 4 receptor agonists: Structure-activity relationships about the 4-alkyl piperidine core

SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino] carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl] -4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1- dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl] -2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin su

A novel isoquinuclidine containing selective melanocortin subtype-4 receptor small molecule agonist, 3 (RY764), is reported. Its in vivo characterization revealed mechanism-based food intake reduction and erectile activity augmentation in rodents.

PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS

Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders r