- ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
-
The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
- -
-
Page/Page column 15-16
(2008/12/06)
-
- N,N-disubstituted aminomethyl benzofuran derivatives: Synthesis and preliminary binding evaluation
-
A series of new N-substituted 2,3-dihydro-2-aminomethyl-2H-1-benzofuran derivatives was prepared and evaluated for affinity at 5-HT(1A), 5-HT(2A), 5-HT(2C), 5-HT3, D2, and D3 receptors. Compound 9, 8-[4-[N-propyl-N-(7-hydroxy-2,3-dihydro-2H-1-benzofuran-2-yl)methyl]aminobutyl]-8-azaspiro[4,5]decane-7,9-dione, bound at 5-HT(1A) sites with nanomolar affinity (IC50=1.5nM) and high selectivity over 5-HT(2A), 5-HT(2C), 5-HT3, D2, and D3 receptors. Copyright (C) 1999 Elsevier Science Ltd.
- Boye, Sophie,Pfeiffer, Bruno,Renard, Pierre,Rettori, Marie-Claire,Guillaumet, Gerald,Viaud, Marie-Claude
-
p. 335 - 341
(2007/10/03)
-