ANDREA BECCARI,ALESSIO MORICONI,ANDREA ARAMINI,GIANLUCA BIANCHINI,LAURA BRANDOLINI,CHIARA LIBERATI,SILVIA BOVOLENTA,SIMONE LORENZI
申请号：
PT12705078
公开号：
PT2668160E
申请日:
2012.01.27
申请国别(地区):
PT
年份:
2015
代理人:
摘要：
Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: wherein R is selected from: - H, CN, NO 2 , SO 2 NH 2 , SO 2 NHR' and SO 2 NR' 2 , where R' is selected from linear or branched C 1 -C 4 alkyl； X is selected from: - F, Cl, CH 3 , NH 2 and OH Y is selected from: - O, CH 2 , NH and SO 2 R1, R2, R3 and R4, indipendently one from the other, are selected from - H and linear or branched C 1 -C 4 alkyl； Z is selected from: - NR6 and R6R7N + , where R6 and R7 indipendently one from the other, are selected from: €¢ H and linear or branched C 1 -C 4 alkyl R5 is a residue selected from: - H and linear or branched C 1 -C 4 alkyl Het is a heteroaryl group selected from - a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or not substituted furanyl and a substituted or not substituted pyridinyl. Said compounds are useful in the treatment of pathologies depending on TRPM8 activity such as pain, cancer, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions, urological disorders.
