The title compds. I [A = CH or N; Z = (un)substituted Ph or pyridinyl], useful for the treatment of inflammatory diseases such as neuropathic pain, were prepd. and claimed. E.g., a multi-step synthesis of I [A = N; Z = 4-ClC6H4], starting from 6-chloronicotinoyl chloride and 4-chloroaniline, was given. Compds. I modulate the vanilloid TRPV1 receptor. For example, compd. I [A = N; Z = 4-ClC6H4] showed a Ki of 15 nM (13-17) in rat spinal cord and an IC50 of 0.83 nM (0.74-0.93) in cultured rat dorsal root ganglia neurons. Pharmaceutical compn. comprising the compd. I is disclosed.
Preparation of N-aryl biarylcarboxamides as vanilloid-1 receptor modulators.
BARALDI, Pier Giovanni;BOREA, Pier Andrea;PAVANI, Maria Giovanna;FRUTTAROLO, Francesca;TREVISANI, Marcello
2008
Abstract
The title compds. I [A = CH or N; Z = (un)substituted Ph or pyridinyl], useful for the treatment of inflammatory diseases such as neuropathic pain, were prepd. and claimed. E.g., a multi-step synthesis of I [A = N; Z = 4-ClC6H4], starting from 6-chloronicotinoyl chloride and 4-chloroaniline, was given. Compds. I modulate the vanilloid TRPV1 receptor. For example, compd. I [A = N; Z = 4-ClC6H4] showed a Ki of 15 nM (13-17) in rat spinal cord and an IC50 of 0.83 nM (0.74-0.93) in cultured rat dorsal root ganglia neurons. Pharmaceutical compn. comprising the compd. I is disclosed.File in questo prodotto:
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