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Ariamide derivatives substituted with triazole and use thereof as antagonists of purinergic receptors P2X3 and / or P2X2 / 3
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
CHEN, LI,DILLON, MICHAEL PATRICK,FENG, LICHUN,HAWLEY, RONALD CHARLES,YANG, MINMIN
申请号:
ES08861017
公开号:
ES2541662T3
申请日:
2008.12.08
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compound of formula I: ** Formula ** or pharmaceutically acceptable salts thereof, in which: 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, hydroxy C1-6 alkyl, C1-6 alkylamino-C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl-C1-6 alkyl alkyl, R2 is 5-methyl-pyridine -2-yl, 5-chloro-pyridin-2-yl, 5-fluoro-pyridin-2-yl, 5-methyl-3-fluoro-pyridin-2-yl, 5-methyl-3-chloro-pyridine-2 -yl, 3,5-difluoro-pyridin-2-yl or 3,5-dichloro-pyridin-2-yl, R3 is hydrogen, R4 is hydrogen or methyl, R5 is hydroxymethyl, methoxymethyl, morpholin-4-ylmethyl, piperidine -1-ylmethyl optionally substituted in the 4-position with methyl, methanesulfonyl or acetyl, 1,1-dioxo-thiomorpholin-1-yl, piperidine-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 be optionally substituted once or twice with a group or groups independently selected from methyl, methylamino, dimethylamino and halo, R6, R7 and R8, each independently, it is hydrogen, C 1-6 alkyl, C 1-6 alkyloxy, halo, C 1-6 haloalkyl or cyano.Compuesto de fórmula I: **Fórmula** o sales farmacéuticamente aceptables de los mismos, en los que: R1 es [1,2,4]triazol-1-ilo sustituido opcionalmente en la posición 5 con alquilo C1-6, haloalquilo C1-6, alcoxi C1-6-alquilo C1-6, hidroxialquilo C1-6, alquilamino C1-6-alquilo C1-6, cicloalquilo C3-6 o cicloalquil C3-6-alquilo C1-6, R2 es 5-metil-piridín-2-ilo, 5-cloro-piridín-2-ilo, 5-fluoro-piridín-2-ilo, 5-metil-3-fluoro-piridín-2-ilo, 5-metil-3-cloro-piridín-2-ilo, 3,5-difluoro-piridín-2-ilo ó 3,5-dicloro-piridín-2-ilo, R3 es hidrógeno, R4 es hidrógeno o metilo, R5 es hidroximetilo, metoximetilo, morfolín-4-ilmetilo, piperidín-1-ilmetilo sustituido opcionalmente en la posición 4 con metilo, me
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