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Ethynyl derivatives
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GREEN, LUKE,GUBA, WOLFGANG,JAESCHKE, GEORG,JOLIDON, SYNESE,LINDEMANN, LOTHAR,STADLER, HEINZ,VIEIRA, ERIC
申请号:
ES10790960
公开号:
ES2551582T3
申请日:
2010.12.14
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Ethynyl derivatives of the formula I ** Formula ** in which: X is N or C-R1; Y is N or C-R2; Z is CH or N; R4 is a 6-link aromatic substituent containing 0, 1 or 2 nitrogen atoms, optionally substituted 1 to 3 times by groups chosen from halogen, C1-C4 alkyl, C1-C4 alkoxy and NRR '; R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy, hydroxy, C1-4 hydroxyalkyl, C1-4 cycloalkyl or is heterocycloalkyl optionally substituted by hydroxy or C1-4 alkoxy, R2 is hydrogen, CN, C1-4 alkyl or heterocycloalkyl ; R and R 'are independently from each other hydrogen or C1-4 alkyl, or to a pharmaceutically acceptable salt or an acid addition salt, to a racemic mixture, or to their corresponding enantiomers and / or optical and / or stereoisomers, with the condition that compounds 6- (3-chlorophenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine 6- (3-fluorophenylethynyl) - [1,2,4] triazolo [1,5 -a] pyridine 6- (3-methylphenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine 6- (4-chlorophenylethynyl) - [1,2,4] triazolo [1,5-a ] pyridine 6- (4-fluorophenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine 6- (4-methylphenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine 6- (3,4-Difluorophenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine 6- (2-chlorophenylethynyl) - [1,2,4] triazolo [1,5-a] pyridine and 6- (6-methylpyridin-2-ethynyl) - [1,2,4] triazolo [1,5-a] pyridine.Derivados de etinilo de la fórmula I**Fórmula** en la que: X es N o C-R1; Y es N o C-R2; Z es CH o N; R4 es un sustituyente aromático de 6 eslabones que contiene 0, 1 ó 2 átomos de nitrógeno, opcionalmente sustituido de 1 a 3 veces por grupos elegidos entre halógeno, alquilo C1-C4, alcoxi C1-C4 y NRR'; R1 es hidrógeno, alquilo C1-4, alcoxi C1-4, hidroxi, hidroxialquilo C1-4, cicloalquilo C1-4 o es heterocicloalquilo opcionalmente sustituido por hidroxi o alcoxi C1-4, R2 es hidrógeno, CN, alquilo C1-4 o heterocicloalquilo; R y R' son con independencia entre sí hidrógeno o alquilo C1-4, o a una sal farmacéuticamente aceptable o una sal de adición de
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