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Triazole derivatives as Gaba receptor ligands
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GABRIEL, STEPHEN DEEMS,THOMAS, ANDREW
申请号:
ES11779633
公开号:
ES2536667T3
申请日:
2011.11.02
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of the formula (I): ** Formula ** in which: A is -CH2-O-, or -CH>; = CH-; X is S or CH; Y is O, NR9 or CR9, with the proviso that if X is S, then Y is CR9 and if X is CH, then Y is O or NR9; u, v represent in each case a single link or a double link, with the proviso that u and v are not both double links and are not both single links; R1, R2 are alkyl, aryl optionally substituted by 1 or 2 halogens or heteroaryl optionally substituted by 1 or 2 halogens, wherein one of R1 and R2 is alkyl; R3 is halogen, cyano, alkyl, haloalkyl, nitro, -C (O) R4 or -C (O) NR5R6; R4 is H, alkyl, aryl, hydroxy, alkoxy or aryloxy; R5 is H, alkyl, haloalkyl, hydroxyalkyl, - (CH2) n-cycloalkyl, - (CH2) n-heterocycloalkyl, - (CH2) n-aryl, - (CH2) nheteroaryl, - (CH2) m-NR7R8, or - (CH2) m-OR7, said cycloalkyl, heterocycloalkyl, aryl and heteroaryl are optionally substituted by halogen, alkyl, haloalkyl, hydroxyalkyl, or alkoxy; R6 is H, alkyl, or is alkylene together with R9; or R5 and R6 together with the nitrogen to which they are attached form a heterocycloalkyl; R7, R8 are independently H, alkyl or aryl; R9 is H, alkyl, or R9 is alkylene together with R6; n is an integer from 0 to 6; m is an integer from 2 to 6; and pharmaceutically acceptable salts thereof.Un compuesto de la fórmula (I):**Fórmula** en la que: A es -CH2-O-, o -CH>;=CH-; X es S o CH; Y es O, NR9 o CR9, con la condición de que si X es S, entonces Y sea CR9 y si X es CH, entonces Y sea O o NR9; u, v representan en cada caso un enlace sencillo o un doble enlace, con la condición de que u y v no sean ambos dobles enlaces y no sean ambos enlaces sencillos; R1, R2 son alquilo, arilo opcionalmente sustituido por 1 ó 2 halógenos o heteroarilo opcionalmente sustituido por 1 ó 2 halógenos, en los que uno de R1 y R2 es alquilo; R3 es halógeno, ciano, alquilo, haloalquilo, nitro, -C(O)R4 o -C(O)NR5R6; R4 es H, alquilo, arilo, hidroxi, alcoxi o ariloxi; R5 es H, alquilo, haloalquilo, hidroxialquilo, -(CH2)n-cicloalqu
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