202859-31-2

Upstream product

• 94436-70-1 (1-benzyl-piperidin-4-yl)-p-tolyl-amine 
• 123-62-6 propionic acid anhydride 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 106-49-0 p-toluidine 

Downstream Products

• 202859-54-9 N-piperidin-4-yl-N-p-tolyl-propionamide 

Relevant academic research and scientific papers

NON-PEPTIDIC NEUROPEPTIDE Y RECEPTOR MODULATORS

The invention provides compounds that are modulators of neuropeptide Y (NPY) receptors, which can be selective inhibitors of NPY receptor Y2R. NPY receptor modulatory compounds are of the general formula Ar2-Y-Ar1-W-Ar3, wherein the variables are as defined herein. Compounds of the invention can be used for treatment of malconditions in patients wherein modulation of an NPY receptor is medically indicated, for example including drug or alcohol abuse, anxiety disorders, depression, stress-related disorders, neurological disorders, nerve degeneration, osteoporosis or bone loss, sleep/wake disorders, cardiovascular diseases, obesity, anorexia, inovulation, fertility disorders, angiogenesis, cell proliferation, learning and memory disorders, migraine and pain.

Pharmacological profile of a novel series of NK1, antagonists. In vitro and in vivo potency of benzimidazolone derivatives

By low throughput examination of our chemical library, compound 7 was selected as a lead NK1, antagonist with a K(i) of 7.1 nM. Modifications of its structure led to the finding that the in vitro potency could be markedly enhanced by disubstituting the anilino phenyl ring as in compounds 13 or 22. Human binding data correlated rather well with results obtained with in vitro animal smooth muscle preparations. Several agents proved to possess antinociceptive properties as exemplified in the hot-plate test in mice; compound 13 was the most active with ED50 of 0.001 and 0.3 mg/kg after iv and po administration respectively. Furthermore, antagonist 71 was found to be a potent inhibitor of SP-induced bronchoconstriction in guinea-pigs with an ED50 between 0.1 and 0.03 mg/kg iv. Furthermore, upon oral administration, 71 was observed to be active in a model of SP-induced bronchial hypersensitivity in mice, with an ID50 of around 3 mg/kg.