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6- (5-hydroxy-1H-pyrazol-1-yl) nicotinamide derivatives and their use as PHD inhibitors
专利权人:
Takeda Pharmaceutical Company Limited
发明人:
BROWN, Jason,DAVIS, Melinda,IVETAC, Anthony,JONES, Benjamin,KIRYANOV, Andre,KUEHLER, Jon,LANIER, Marion,MIURA, Joanne,MURPHY, Sean,WANG, Xiaolun
申请号:
ES14726246
公开号:
ES2660914T3
申请日:
2014.03.26
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of the formula ** (See formula) ** or a pharmaceutically acceptable salt thereof, wherein q is 0, 1 or 2; s is 0, 1 or 2; R3, each time it is taken, is independently selected from the group consisting of hydrogen, hydroxyl, amino, C1-8 alkylamino, cyano, halo, optionally substituted C1-6 alkyl, and C1-4 alkoxy; R4 is selected from the group consisting of hydrogen, cyano, halo, methyl, ethyl, methoxy, and trifluoromethyl; R5 is selected from the group consisting of ** (See formula) ** G is carbon; A is selected from the group consisting of N, O, S, CR6 and NR6; E is selected from the group consisting of N, O, S, and CR6; with the proviso that only one of A and E can be O or S; or G is N and A and E are CR6; or G and A are N and E is CR6; or G, A, and E are N; R6, each time it is taken, is independently selected from the group consisting of hydrogen, cyano, halo, C3-8 cycloalkyl, optionally substituted C1-6 alkyl, C1-4 alkoxy, and trifluoromethyl; R7 is selected from the group consisting of cyano and cyanomethyl; R8, each time it is taken, is independently selected from the group consisting of hydrogen, cyano, halo, C1-4 alkyl, C1-4 alkoxy, and trifluoromethyl; and R9 is selected from the group consisting of hydrogen, C1-6 alkyl optionally substituted with 1 to 3 fluorine, and C3-8 cycloalkyl.Un compuesto de la fórmula **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que q es 0, 1 o 2; s es 0, 1 o 2; R3, cada vez que se toma, se selecciona independientemente del grupo que consiste en hidrógeno, hidroxilo, amino, alquilamino C1-8, ciano, halo, alquilo C1-6 opcionalmente sustituido, y alcoxi C1-4; R4 se selecciona del grupo que consiste en hidrógeno, ciano, halo, metilo, etilo, metoxi, y trifluorometilo; R5 se selecciona del grupo que consiste en **(Ver fórmula)** G es carbono; A se selecciona del grupo que consiste en N, O, S, CR6 y NR6; E se selecciona del grupo que consiste en N, O, S, y CR6; con la condición de que solamente uno de
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