896127-78-9Relevant academic research and scientific papers
Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition
Berglund, Susanne,Egner, Bryan J.,Graden, Henrik,Graden, Joakim,Morgan, David G.A.,Inghardt, Tord,Giordanetto, Fabrizio
scheme or table, p. 4268 - 4273 (2010/04/30)
Herein, we disclose the discovery and optimization of 2-piperidin-4-yl-acetamide derivatives as MCH-R1 antagonists. Structural investigation of piperidin-4-yl-amide and piperidin-4-yl-ureas identified 2-piperidin-4-yl-acetamide-based MCH-R1 antagonists with outstanding in vivo efficacy but flawed with high affinity towards the hERG potassium channel. While existing hERG SAR information was employed to discover highly potent MCH-R1 antagonists with minimized hERG inhibition, additional hurdles prevented their subsequent clinical exploration.
HETEROCYCLIC MCHr1 ANTAGONISTS AND THEIR USE IN THERAPY
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Page/Page column 66-67, (2008/06/13)
Compounds of formula I depicted below, pharmaceutical compositions containing them, processes for preparing the compounds, and their use in the treatment of obesity, type II diabetes, metabolic syndrome, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy and related conditions, neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease, and pain related disorders. The compounds are melanin concentrating hormone receptor 1 (MCHr1) antagonists.
