487057-86-3

Upstream product

• 35944-64-0 3-iodo-4-methylaniline 

Downstream Products

• 762297-54-1 N-{3-[1-(3-aminopropyl)piperidin-4-yl]-4-methylphenyl}isobutyramide 
• 949096-76-8 N-(3-{1-[3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)propyl]piperidin-4-yl}-4-methylphenyl)isobutyramide 
• 486451-46-1 2-methyl-N-[4-methyl-3-(4-piperidinyl)phenyl]propanamide 
• 487057-87-4 4-(5-isobutyrylamino-2-methylphenyl)piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit

Melanin-concentrating hormone (MCH) is involved in the regulation of feeding, water balance, energy metabolism, general arousal and attention state, memory, cognitive functions, and psychiatric disorders. Herein, two new chemical series exemplified by N-[5-(1-{3-[2,2-bis-(4-fluoro-phenyl)-acetylamino]- propyl}-piperidin-4-yl)-2,4-difluoro-phenyl]-isobutyramide (SNAP 102739, 5m) and N-[3-(1-{3-[(S)-2-(4-fluorophenyl)-propionylamino]-propyl}-piperidin-4-yl)-4- methylphenyl]-isobutyramide ((S)-6b) are reported. These compounds were designed to improve the pharmacokinetic properties of the high-throughput screening lead compound 1 (SNAP 7941). The MCH1 receptor antagonists 5m and (S)-6b show reasonable pharmacokinetic profiles (rat bioavailability = 48 and 81%, respectively). Compounds 5m and (S)-6b demonstrated the inhibition of a centrally administered MCH-evoked drinking effect, and compound 5m exhibited oral in vivo efficacy in the rat social interaction model of anxiety, with a minimum effective dose = 0.3 mg/kg.

SUBSTITUTED ANILINIC PIPERIDINES AS MCH SELECTIVE ANTAGONISTS

This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.