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5,6,7,8-tetrahydro [1,2,4] triazolo [4,3-a] pyrazine derivatives as modulators of P2X7
专利权人:
Glaxo Group Limited
发明人:
DEAN, David Kenneth,MUNOZ-MURIEDAS, Jorge,SIME, Mairi,STEADMAN, Jon Graham Anthony,THEWLIS, Rachel Elizabeth Anne,TRANI, Giancarlo,WALTER, Daryl Simon
申请号:
ES10720006
公开号:
ES2590987T3
申请日:
2010.04.28
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is hydrogen, C1-4 alkyl, C1-3 alkoxy, C1-2 fluoroalkyl, halogen, NR6R7, Het, or phenyl, wherein the phenyl is optionally substituted with one, two or three substituents that are independently fluorine, chlorine, C1-3 alkyl or methoxy; wherein Het is: i) a six-membered heteroaromatic monocyclic ring containing one, two or three nitrogen atoms in the ring, or ii) a five-membered heteroaromatic monocyclic ring containing one, two or three heteroatoms that are independently N, O or S, in which at most one of the heteroatoms of the 5-member ring is O or S; and wherein Het is optionally substituted with one or two substituents that are independently C1-3 alkyl, fluorine, chlorine, OH (including a tautomer thereof), or methoxy; and wherein: R1 is hydrogen, chlorine, fluorine, bromine, C1 fluoroalkyl, cyano or C1-3 alkyl; R2 is hydrogen, fluorine, chlorine, bromine, C1 fluoroalkyl, cyano or C1-3 alkyl; R3 is hydrogen, fluorine or chlorine; R4 is hydrogen; R5 is hydrogen, fluorine, chlorine or methyl; and R6 and R7 are independently hydrogen or C1-3 alkyl; or R6 and R7 are taken together and are - (CH2) 2-O- (CH2) 2-, - (CH2) 2-O- (CH2) 3-, or - (CH2) n1- in which n1 is 3 , 4, 5 or 6; wherein, when A is hydrogen, C1-4 alkyl, C1-3 alkoxy, C1-2 fluoroalkyl, halogen or NR6R7, then R1 is chloro, fluorine, bromine, C1 fluoroalkyl, cyano or C1-3 alkyl, and at least one of R2 and R3 is different from hydrogen; and when A is optionally substituted Het or phenyl, then R1 is hydrogen, chlorine, fluorine, bromine, C1 fluoroalkyl, cyano or C1-3 alkyl, and at least one of R1, R2 and R3 is different from hydrogen; and wherein, when R5 is fluorine, chlorine or methyl, then R1 is chlorine, fluorine, C1 or methyl fluoroalkyl and R2 is hydrogen.Un compuesto de fórmula (I) o una de sus sales farmacéuticamente aceptables: en la que: A es hidrógeno, alquilo C1-4, alcoxi C1-3, fluoroalquilo C1-2, halógeno, NR6R7,
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