114741-22-9Relevant academic research and scientific papers
SUBSTITUTED CYCLOLAKYLS AS MODULATORS OF THE INTEGRATED STRESS PATHWAY
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Page/Page column 255; 258, (2020/11/12)
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: Assessment of potency, efficacy, and cardiovascular safety
Lynch, John K.,Freeman, Jennifer C.,Judd, Andrew S.,Iyengar, Rajesh,Mulhern, Mathew,Zhao, Gang,Napier, James J.,Wodka, Dariusz,Brodjian, Sevan,Dayton, Brian D.,Falls, Doug,Ogiela, Christopher,Reilly, Regina M.,Campbell, Thomas J.,Polakowski, James S.,Hernandez, Lisa,Marsh, Kennan C.,Shapiro, Robin,Knourek-Segel, Victoria,Droz, Brian,Bush, Eugene,Brune, Michael,Preusser, Lee C.,Fryer, Ryan M.,Reinhart, Glenn A.,Houseman, Kathryn,Diaz, Gilbert,Mikhail, Ann,Limberis, James T.,Sham, Hing L.,Collins, Christine A.,Kym, Philip R.
, p. 6569 - 6584 (2007/10/03)
Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to the identification of a chromone-2-carboxamide series as having excellent safety against the chosen cardiovascular endpoints at high drug concentrations in the plasma and brain. Optimization of this series led to considerable improvements in affinity, functional potency, and pharmacokinetic profile. This led to the identification of a 7-fluorochromone-2-carboxamide (22) that was orally efficacious in a diet-induced obese mouse model, retained a favorable cardiovascular profile in rat, and demonstrated dramatic improvement in effects on mean arterial pressure in our dog cardiovascular model compared to other series reported by our group. However, this analogue also led to prolongation of the QT interval in the dog that was linked to affinity for hERG channel and unexpectedly potent functional blockade of this ion channel.
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
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Page/Page column 22, (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.
SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
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Page 101, (2010/02/08)
The present invention relates to novel substituted piperidine and piperazine derivatives as melanocortin-4 receptor (MC-4R) modulators. MC-4R agonists of the invention can be used for the treatment of disorders and diseases such as obesity, diabetes and s
