Discovery of piperidine carboxamide TRPV1 antagonists
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
Cheung, Wing S.,Calvo, Raul R.,Tounge, Brett A.,Zhang, Sui-Po,Stone, Dennis R.,Brandt, Michael R.,Hutchinson, Tasha,Flores, Christopher M.,Player, Mark R.
experimental part
p. 4569 - 4572
(2009/04/06)
4-Piperidinecarboxamide modulators of vanilloid VR1 receptor
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.
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Page/Page column 68; 69
(2010/11/08)
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