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TRPM8 receptor antagonists
专利权人:
Silvia Bovolenta;Chiara Liberati;Laura Brandolini;Andrea Aramini;Andrea Beccari;Gianluca Bianchini;Simone Lorenzi;Alessio Moriconi
发明人:
Alessio Moriconi,Gianluca Bianchini,Andrea Aramini,Laura Brandolini,Chiara Liberati,Silvia Bovolenta,Andrea Beccari,Simone Lorenzi
申请号:
US13982235
公开号:
US08906946B2
申请日:
2012.01.27
申请国别(地区):
US
年份:
2014
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:WhereinR 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 OHY is selected from: O, CH2, NH and SO2R1 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 alkylR5 is a residue selected from: H and linear or branched C1-C4 alkylHet 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.
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