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Pyrimidinecarboxamides as sodium channel blockers
专利权人:
Purdue Pharma LP
发明人:
LOCKMAN, Jeffrey,NI, Chiyou,PARK, Jae Hyun,PARK, Minnie,SHAO, Bin,TAFESSE, Laykea,YAO, Jiangchao,YOUNGMAN, Mark
申请号:
ES14710633
公开号:
ES2680246T3
申请日:
2014.03.03
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound having Formula V: ** Formula ** or a pharmaceutically acceptable salt or solvate thereof, A1 is selected from the group consisting of: ** Formula ** R28a is selected from the group consisting of hydrogen, fluoro , chloro, cyano, C1-4 halogenoalkyl, C1-4 halogenoalkoxy, (C1-C4 halogenoalkoxy) alkyl, C1-4 alkoxy, C1-C4 alkyl and C1-C6 cycloalkyl; R28b is selected from the group consisting of hydrogen, fluoro, chloro, cyano, C1-4 halogenoalkyl, C1-4 halogenoalkoxy, (C1-C4 halogenoalkoxy) alkyl, C1-4 alkoxy, C1-C4 alkyl and C1-C6 cycloalkyl; or R28a and R28b taken together with the two adjacent carbon atoms form a 5- or 6-membered cycloalkyl or heterocycle; R28c is selected from the group consisting of hydrogen, heteroaryl and (heterocycle) alkyl, or Z is selected from the group consisting of -NR5- and -O-; R4 is selected from the group consisting of: ** Formula ** R1a is selected from the group consisting of hydrogen and (heterocycle) alkyl; R10a is selected from the group consisting of alkyl and hydroxyalkyl; R12 is selected from the group consisting of hydrogen, alkyl, alkenyl and hydroxyalkyl; R5 is hydrogen; or R4 and R5 taken together with the nitrogen atom to which they are attached form an optionally substituted heterocycle selected from the group consisting of: ** Formula ** R14 is selected from the group consisting of hydrogen and C1-C4 alkyl.Un compuesto que tiene la Fórmula V:**Fórmula** o una sal o solvato farmacéuticamente aceptable del mismo, A1 se selecciona de entre el grupo consistente en:**Fórmula** R28a se selecciona de entre el grupo consistente en hidrógeno, fluoro, cloro, ciano, halogenoalquilo C1-4, halogenoalcoxi C1-4, (halogenoalcoxi C1-C4)alquilo, alcoxi C1-4, alquilo C1-C4 y cicloalquilo C1-C6; R28b se selecciona de entre el grupo consistente en hidrógeno, fluoro, cloro, ciano, halogenoalquilo C1-4, halogenoalcoxi C1-4, (halogenoalcoxi C1-C4)alquilo, alcoxi C1-4, alquilo C1-C4 y cicloalquilo C1-C6; o R28a y R28b tomados junto con l
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