发明授权
US06803364B1 Il-5 inhibiting 6-azauracil derivatives 失效
Il-5抑制6-氮尿嘧啶衍生物

Il-5 inhibiting 6-azauracil derivatives
摘要:
The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or —X—R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are —C(═O)—Z—R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(═O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with —C(═O)—Z—R14, Het3, R6 or NR7R8; Z is O, S, NH, —CH2O or —CH2—S—; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het5, phenyl; or R14 is an oxygen containing radical; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het5 are optionally substituted heterocycles; Het4 is a monocyclic heterocycle; provided however that R2 is other than NH2C(═O), C1-6alkylOC(═O)C1-6alkyl; and R11 is other than COOH, C1-4alkylOC(═O), NH2C(═O), C1-4alkylNH2C(═O), OHC1-4alkylNH2C(═O), C1-4alkylC(═O)NH2C(═O), C3-7cycloalkylNH2C(═O); and R7, R8, R9, R10, R12, R13, R15 and R16 are other than C1-4alkylC(═O)OC1-4alkylC(═O), OHC1-4alkylC(═O); and Het3 is other than a monocyclic heterocycle substituted with COOH or C1-4alkylOC(═O); and the compounds of formula (I) contain at least one —C(═O)—Z—R14 moiety: to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
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