823191-40-8Relevant academic research and scientific papers
INDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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Page/Page column 96, (2017/03/14)
The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores
Zhang, Deyi,Blanco, Maria-Jesus,Ying, Bai-Ping,Kohlman, Daniel,Liang, Sidney X.,Victor, Frantz,Chen, Qi,Krushinski, Joseph,Filla, Sandra A.,Hudziak, Kevin J.,Mathes, Brian M.,Cohen, Michael P.,Zacherl, Deanna,Nelson, David L.G.,Wainscott, David B.,Nutter, Suzanne E.,Gough, Wendy H.,Schaus, John M.,Xu, Yao-Chang
, p. 4337 - 4341 (2015/11/03)
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the indole nucleus in 2 (LY334370) with a monocyclic phenyl ketone moiety generated potent and more selective 5-HT1F receptor agonists. Focused SAR studies around this central phenyl ring demonstrated that the electrostatic and steric interactions of the substituent with both the amide CONH group and the ketone C=O group play pivotal roles in affecting the adopted conformation and thus the 5-HT1F receptor selectivity. Computational studies confirmed the observed results and provide a useful tool in the understanding of the conformational requirements for 5-HT1F receptor agonist activity and selectivity. Through this effort, the 2-F-phenyl and N-2-pyridyl series were also identified as potent and selective 5-HT1F receptor agonists.
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT 1F receptor agonists
Zhang, Deyi,Kohlman, Dan,Krushinski, Joseph,Liang, Sidney,Ying, Bai-Ping,Reilly, John E.,Dinn, Sean R.,Wainscott, David B.,Nutter, Suzanne,Gough, Wendy,Nelson, David L.G.,Schaus, John M.,Xu, Yao-Chang
, p. 6011 - 6016 (2007/10/03)
The synthesis and evaluation of structurally novel 5-HT1F receptor agonists are reported. Several fused bicyclic systems have been investigated to serve as the core structure of potent and selective 5-HT 1F receptor agonists. Replace
