发明名称 TRPM8 RECEPTOR ANTAGONISTS
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, Br, CN, NO2, SO2NH2, SO2NHR' and SO2NR'2, where R' is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 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 furyl and a substituted or not substituted pyridinyl. Said compounds are useful in the prevention and treatment of pathologies depending on TRPM8 activity such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.
申请公布号 US2014031398(A1) 申请公布日期 2014.01.30
申请号 US201213982235 申请日期 2012.01.27
申请人 MORICONI ALESSIO;BIANCHINI GIANLUCA;ARAMINI ANDREA;BRANDOLINI LAURA;LIBERATI CHIARA;BOVOLENTA SILVIA;BECCARI ANDREA;LORENZI SIMONE 发明人 MORICONI ALESSIO;BIANCHINI GIANLUCA;ARAMINI ANDREA;BRANDOLINI LAURA;LIBERATI CHIARA;BOVOLENTA SILVIA;BECCARI ANDREA;LORENZI SIMONE
分类号 C07D333/20;C07D207/335;C07D213/38;C07D307/52 主分类号 C07D333/20
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