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Pyridine-2-carboxamide derivatives as antagonists of MGLUR5
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JAESCHKE, GEORG,KOLCZEWSKI, SABINE,PORTER, RICHARD HUGH PHILIP,VIEIRA, ERIC
申请号:
ES06707197
公开号:
ES2476840T3
申请日:
2006.02.23
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compounds of the general formula (I) ** Formula ** in which R1 is a 5- or 6- member ring respectively of formulas (II) and (III): R2 is H, C1-C7-alkyl, C3-C6-cycloalkyl - (CH2) m-Ra; R3 is aryl or heteroaryl qu45 and are optionally substituted by: CN, Cl, F, Br, CF3, CHF2, or -O-C1-C7-alkyl, - (CO) -Rb, - (CH2) m-Rc, -NH- (CO) -C1-C7-alkyl; -O-CH2F, -OCHF2, -O-CF3, -S (O) 2-Rd, C3-C6-cycloalkyl heteroaryl which is optionally substituted by C1-C7-alkyl; R4 is H, -OH, Cl, F, Br, CN, -CHF2, CF3, C1-C7-alkyl, -O- (CO) -C1-C7-alkyl, C3-C6-cycloalkyl, or - (CH2) m-Re; R5 is C1-C7-alkyl or C1-C7-alkyl-C3-C6-cycloalkyl; - (CH2) n-O-Rf, C3-C8-alkenyl-O-Rf, - (CH2) n-NRgRh; -C2-C6- alkenyl-NRgRh or - (CH2) n-Re; Ra is -O-C1-C7-alkyl or -OH; Rb is C1-C7-alkyl, NH2, or -O-C1-C7-alkyl; Rc is -OH, NH2, or NH- (CO) -O-C1-C7-alkyl; Rd is C1-C7-alkyl, -NH2, -NH-C1-C7-alkyl or -N-di (C1-C7-alkyl); Re is -OH, -CH2F, -CHF2, -CF3 or -O- (CO) -C1-C7-alkyl; Rf is C1-C7-alkyl, C3-C8-alkenyl, C3-C6-cycloalkyl, phenyl, benzyl or - (CO) -R '; Rg, Rh are, independently, H, C1-C7-alkyl, C3-C6-cycloalkyl, C3-C8-alkenyl, phenyl, benzyl, or - (CO) -R 'or Rg and Rh also, together with the atom of nitrogen to which they are attached, can form a 5- to 7- membered heteroaryl or heterocyclic ring that can optionally be substituted with 1 or 2 OH; R 'is NH2, -NH-C1-C7-alkyl, C1-C7-alkyl or C1-C7-alkoxy; m is 1 to 4; n is 2 to 6; as well as its pharmaceutically accepted salts.Los compuestos de la fórmula general (I)**Fórmula** en la cual R1 es un anillo de 5- o 6- miembros respectivamente de las fórmulas (II) y (III): R2 es H, C1-C7-alquilo, C3-C6-cicloalquilo -(CH2)m-Ra; R3 es arilo o heteroarilo qu 45 e son opcionalmente sustituidos por: CN, Cl, F, Br, CF3, CHF2, o -O-C1-C7-alquilo, -(CO)-Rb, -(CH2)m-Rc, -NH-(CO)-C1-C7-alquilo; -O-CH2F, -OCHF2, -O-CF3, -S(O)2-Rd, C3-C6-cicloalquilo heteroarilo que es opcionalmente sustituido por C1-C7-alquilo; R4 es H, -OH, Cl, F, Br, CN, -CHF2, CF3, C1-C7-alquilo, -O-
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