199586-66-8Relevant academic research and scientific papers
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 38, (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.
Medicaments for viral diseases
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, (2008/06/13)
Chromanone derivatives are highly active antiviral agents. Combinations of chromanones and/or chromanols with HBV polymerase inhibitors, HBV DNA inhibitors or HBV core protein inhibitors and/or isoxazoles and, where appropriate, interferon inhibit the replication of HBV viruses better than agents disclosed previously.
Sulfonamide-substituted chromans, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising them
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, (2008/06/13)
Sulfonamide-substituted chromans, processes for their preparation, their use as a medicament or a diagnostic, and medicament comprising them Chromans of the formula I and of the formula 1a having the meanings R(A), R(B), R(C) and R(1) to R(8) indicated in the claims are outstandingly suitable for preparing a medicament for blocking the K+channel which is opened by cyclic adenosine monophosphate (cAMP); and further for preparing a medicament for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and of the intestinal region, in particular of the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal illnesses, for the treatment and prevention of all types of arrhythmias including ventricular and supraventricular arrhythmias, and for the control of reentry arrhythmias and for the prevention of sudden heart death as a result of ventricular fibrillation.
