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(Pyridin-4-yl) benzylamides as allosteric modulators of nAChR alpha 7
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
DE BOECK, Benoît Christian Albert Ghislain,ROMBOUTS, Geert,LEENAERTS, Joseph Elisabeth,MACDONALD, Gregor James
申请号:
ES12704845
公开号:
ES2563113T3
申请日:
2012.02.23
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound having the formula (I) ** Formula ** or a stereoisomer thereof, wherein n is 0, 1 or 2; X is fluoro or chloro; Y is N or CH; Z is O or CH2; R1 is C1-8 alkyl, C1-8 alkyl substituted with 1, 2 or 3 halogen substituents; C3-6 cycloalkyl; (C3-6 cycloalkyl) -C1-6 alkyl; (C 1-6 alkyloxy) -C 1-6 alkyl; (trihalo-C 1-4 alkyloxy) - C 1-6 alkyl; tetrahydrofuryl; tetrahydropyranyl; phenyl; or phenyl substituted with 1, 2 or 3 substituents selected from halogen, trifluoromethyl, trifluoromethoxy, cyano, C1-6 alkyl and C1-4 alkyloxy; or a monocyclic aromatic heterocyclic radical containing at least one heteroatom selected from N, O and S, optionally substituted with 1, 2 or whenever possible with 3 substituents selected from halogen, C1-4 alkyl, C1-4 alkyloxy, C3 cycloalkyl- 6 and trifluoromethyl; R2 and R3 are independently H, C1-4 alkyl or trifluoromethyl; or R2 and R3 are taken together to form 1,2-ethanediyl or 1,3-propanediyl; R4 and R5 are independently H, C1-4 alkyl, trifluoromethyl, C3-6 cycloalkyl or C1-4 alkyloxy; or a salt by the addition of acid thereof, or a solvate thereof.Un compuesto que tiene la fórmula (I) **Fórmula** o un estereoisómero del mismo, en donde n es 0, 1 o 2; X es fluoro o cloro; Y es N o CH; Z es O o CH2; R1 es alquilo C1-8, alquilo C1-8 sustituido con 1, 2 o 3 sustituyentes halógeno; cicloalquilo C3-6; (cicloalquil C3-6)- alquilo(C1-6); (alquiloxi C1-6)-alquilo(C1-6); (trihalo-alquiloxi(C1-4))-alquilo(C1-6); tetrahidrofurilo; tetrahidropiranilo; fenilo; o fenilo sustituido con 1, 2 o 3 sustituyentes seleccionados de halógeno, trifluorometilo, trifluorometoxi, ciano, alquilo C1-6 y alquiloxi C1-4; o un radical heterocíclico aromático monocíclico que contiene al menos un heteroátomo seleccionado de N, O y S, opcionalmente sustituido con 1, 2 o cuando sea posible con 3 sustituyentes seleccionados de halógeno, alquilo C1-4, alquiloxi C1-4, cicloalquilo C3-6 y trifluorometilo; R2 y R3 son independientemente H, alquilo C1-4 o trifluorometilo;
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