PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS

Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl...

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Hauptverfasser: LINDERS, JOANNES THEODORUS MARIA, JAROSKOVA, LIBUSE, BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR, VAN DER VEKEN, LOUIS JOZEF ELISABETH, DIMITROV, VLADIMIR DIMTCHEV, NIKIFOROV, THEO TEOFANOV
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Sprache:eng ; spa
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Zusammenfassung:Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine. (ver formula (I)) sus formas N-oxido, sus sales de adicion farmaceuticamente aceptables y sus formas estereoquimicamente isomeras, en donde: N es 1 o 2; L representa un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de alquilo C1-4; alquiloxi C1-3-alquilo C1-4-; hidroxi-alquilo C1-4; hidroxi; alquiloxi C1-3- o fenil-alquilo C1-4; M representa un enlace directo o un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi; alquilo C1-4; o alquiloxi C1-4; R1 y R2 representan, cada uno de manera independiente, hidrogeno; halo; ciano; hidroxi; alquilo C1-4 opcionalmente sustituido con halo; alquiloxi C1-4 opcionalmente sustituido con uno, o cuando es posible, con dos o tres sustituyentes seleccionados de hidroxi, Ar1 y halo; o R1 y R2 tomados junto con el anillo fenilo al cual estan unidos forman naftilo o 1,3-benzodioxolilo, en donde dichos naftilo o 1,3-benzodiozolilo estan opcionalmente sustituidos con halo; R3 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R4 representa hidrogeno; halo; alq