发明名称 IL-5 inhibiting 6-azauracil derivatives
摘要 The present invention is concerned with the compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR<3 >or a direct bond; R<1 >is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R<2 >is aryl, Het<1>, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR<3>, then R<2 >may also be a carbonyl or thiocarbonyl linked substituent; R<3 >is hydrogen or C1-4alkyl; R<4 >and R<5 >independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het<3>, R<6 >or NR<7>R<8>; R<6 >is substituted sulfonyl or sulfinyl; R<7 >and R<8 >are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het<3 >and R<6>; R<9 >and R<10 >are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het<3 >and R<6>; R<11 >is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R<6>, NR<7>R<8>, C(=O)NR<7>R<8>, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het<3 >and C(=O)Het<3>; R<12 >and R<13 >are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R<6>; aryl is optionally substituted phenyl; Het<1>, Het<
申请公布号 US6867207(B2) 申请公布日期 2005.03.15
申请号 US20010891888 申请日期 2001.06.26
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 LACRAMPE JEAN FERNAND ARMAND;FREYNE EDDY JEAN EDGARD;VENET MARC GASTON;BOECKX GUSTAAF MARIA
分类号 A61P37/08;C07D401/10;C07D403/10;C07D403/12;C07D413/10;C07D413/14;C07D417/10;C07D417/14;(IPC1-7):C07D253/065;A61K31/53;A61K17/00 主分类号 A61P37/08
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