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ANTAGONISTES DES RÉCEPTEURS TRPM8
专利权人:
ARAMINI, Andrea;BOVOLENTA, Silvia;LORENZI, Simone;MORICONI, Alessio;DOMPE' S.P.A.;BRANDOLINI, Laura;BIANCHINI, Gianluca;DOMPE S.P.A.;BECCARI, Andrea;LIBERATI, Chiara
发明人:
MORICONI, Alessio,BIANCHINI, Gianluca,BRANDOLINI, Laura,ARAMINI, Andrea,LIBERATI, Chiara,BOVOLENTA, Silvia,BECCARI, Andrea,LORENZI, Simone
申请号:
EPEP2012/051292
公开号:
WO2012/101244A1
申请日:
2012.01.27
申请国别(地区):
EP
年份:
2012
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 (I), 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, C1, 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.La présente invention concerne des composés constituant des antagonistes sélectifs du type 8 de la sous-famille M des canaux perméables aux cations TRP (ci-dessous TRPM8), de formule (I), dans laquelle R est choisi parmi H, Br, CN, NO2, SO2NH2, SO2NHR' et SO2NR'2, R' étant choisi parmi des groupes alkyle linéaires ou ramifiés en C1 à C4 ; X est choisi parmi F, Cl, un groupe alkyle en C1 à C3, NH2 et OH, Y est choisi parmi O, CH2, NH et SO2, R1 et R2, sont choisis, indépendamment l'un de l'autre, parmi H, F et des groupes alkyle linéaires ou ramifiés en C1 à C4 ; R3 et R4 sont choisis, indépendamment l'un de l'autre, parmi H et des groupes alkyle linéaires ou ramifié
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