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ANTAGONISTI RECEPTORA TRPM8
专利权人:
DOMPÉ FARMACEUTICI S.P.A.
发明人:
MORICONI, ALESSIO,BIANCHINI, GIANLUCA,BRANDOLINI, LAURA,ARAMINI, ANDREA,LIBERATI, CHIARA,BOVOLENTA, SILVIA,BECCARI, ANDREA,LORENZI, SIMONE,MORICONI, Alessio,BIANCHINI, Gianluca,BRANDOLINI, Laura,ARAMINI, Andrea,LIBERATI, Chiara,BOVO
申请号:
RSP20150718
公开号:
RS54337B1
申请日:
2012.01.27
申请国别(地区):
RS
年份:
2016
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, CN, NO2, SO2NH2, SO2NHR' and SO2NR'2, where R' is selected from linear or branched C1-C4 alkyl;X is selected from:- F, Cl, CH3, NH2 and OHY is selected from:- O, CH2, NH and SO2R1, R2, R3 and R4, indipendently 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 indipendently 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 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.Patenti zahtevii njihove farmaceutski prihvatljive soli, u kojoj:R je odabrano između:- H, Br, CN, NO2, SO2NH2, SO2NHR' i SO2N(R')2, gde je R' izabrano između ravnog ili razgranatog C1-C4 alkila;X je odabrano između:- F, Cl, C1-C3 alkila, NH2 i OH Y je odabrano između:- -O-, CH2, NH i S O 2R1 i R2, nezavisno jedan od drugog, odabrani su između- H, F i ravnog ili razgranatog C1-C4 alkila;R3 i R4, nezavisno jedan od drugog, odabrani su između- H i ravnog ili razgranatog C1-C4 alkila;Z je odabrano između:- NR6 i R6R7N+, gde su R6 i R7, nezavisno jedan od drugog, odabrani između:- H i ravnog ili razgranatog C1-C4 alkilaR5 je ostatak odabran između:- H i ravnog ili razgranatog C1-C4 alkilaHet je heteroaril grupa odabrana između pirolila, N-metilpirolila, tiofenil
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