64798-38-5Relevant articles and documents
α-Methylation at benzylic fragment of N-aryl-N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
Gomtsyan, Arthur,Bayburt, Erol K.,Keddy, Ryan,Turner, Sean C.,Jinkerson, Tammie K.,Didomenico, Stanley,Perner, Richard J.,Koenig, John R.,Drizin, Irene,McDonald, Heath A.,Surowy, Carol S.,Honore, Prisca,Mikusa, Joe,Marsh, Kennan C.,Wetter, Jill M.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 3894 - 3899 (2008/02/09)
SAR studies for N-aryl-N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties. Further structural manipulations that included replacement of isoquinoline core with indazole and isolation of single enantiomer led to TRPV1 antagonists like (R)-16a with superior pharmacokinetic properties and greater potency in animal model of inflammatory pain.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Page/Page column 34-35; 97, (2010/02/11)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.