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Ariamide derivatives substituted with triazole and use thereof as antagonists of purinergic receptors P2X3 and / or P2X2 / 3
Ariamide derivatives substituted with triazole and use thereof as antagonists of purinergic receptors P2X3 and / or P2X2 / 3
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机译:三唑取代的芳酰胺衍生物及其作为嘌呤能受体P2X3和/或P2X2 / 3的拮抗剂的用途
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摘要
Compound of formula I: ** Formula ** or pharmaceutically acceptable salts thereof, wherein: R1 is [1,2,4] triazol-1-yl optionally substituted in the 5-position with C1-6 alkyl, C1 haloalkyl -6, C1-6 alkoxy-C1-6 alkyl, hydroxyalkyl C1-6, C1-6 alkylamino-C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl-C1-6 alkyl, R2 is 5-methyl-pyridine -2-yl, 5-chloro-pyridine-2-yl, 5-fluoro-pyridine-2-yl, 5-methyl-3-fluoro-pyridine-2-yl, 5-methyl-3-chloro-pyridine-2 -yl, 3,5-difluoro-pyridine-2-yl or 3,5-dichloro-pyridine-2-yl, R3 is hydrogen, R4 is hydrogen or methyl, R5 is hydroxymethyl, methoxymethyl, morpholin-4-ylmethyl, piperidine -1-ylmethyl optionally substituted at the 4-position with methyl, methanesulfonyl or acetyl, 1,1-dioxo-thiomorpholin-1-yl, piperidin-1-yl optionally substituted once or twice with a group or groups independently selected from methyl , methoxy or halo, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrazolyl or thiazolyl, in wherein pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrazolyl, and thiazolyl each can optionally be substituted once or twice with a group or groups independently selected from methyl, methylamino, dimethyloamino, and halo, R6, R7, and R8, each independently, it is hydrogen, C1-6alkyl, C1-6alkyloxy, halo, haloC1-6alkyl or cyano.
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