79557-77-0Relevant academic research and scientific papers
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: The effects of chirality on substituted indan-1-ylamines
Souers, Andrew J.,Iyengar, Rajesh R.,Judd, Andrew S.,Beno, David W.A.,Gao, Ju,Zhao, Gang,Brune, Michael E.,Napier, James J.,Mulhern, Mathew M.,Lynch, John K.,Freeman, Jennifer C.,Wodka, Dariusz,Chen, Chong J.,Falls, H. Doug,Brodjian, Sevan,Dayton, Brian D.,Diaz, Gilbert J.,Bush, Eugene N.,Shapiro, Robin,Droz, Brian A.,Knourek-Segel, Victoria,Hernandez, Lisa E.,Marsh, Kennan C.,Reilly, Regina M.,Sham, Hing L.,Collins, Christine A.,Kym, Philip R.
, p. 884 - 889 (2007)
The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the identification of a series of chiral racemic compounds that displayed good to excellent functional potency, binding affinity, and selectivity over the hERG channel. Further separation of two distinct chiral racemic compounds into their corresponding pairs of enantiomers revealed a considerable selectivity for MCHr1 for one configuration, in addition to a striking difference in oral exposure between one pair of enantiomers in diet-induced obese mice. Oral administration of the most potent compound in this class in the same animal model led to significant reduction of fat mass in a semi-chronic model for weight loss.
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
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Page/Page column 48, (2010/02/14)
The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
