发明名称 6-azauracil derivatives as IL-5 inhibitors.
摘要 The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R<SUP>1 </SUP>represents hydrogen, C<SUB>1-6</SUB>alkyl, mono- or di(C<SUB>1-6</SUB>alkyl)aminoC<SUB>1-6</SUB>alkyloxy, mercapto, C<SUB>1-6</SUB>alkylthio, C<SUB>3-7</SUB>cycloalkyl, aryl or C<SUB>1-6</SUB>alkyl substituted with mono- or di(C<SUB>1-6</SUB>alkyl)amino, C<SUB>1-6</SUB>alkyloxy, aryl or Het; R<SUP>2 </SUP>represents cyano or a radical of formula -C(-X)-Y-R<SUP>5</SUP>; wherein X represents O or S; Y represents O, S, NR<SUP>6 </SUP>or a direct bond; R<SUP>5 </SUP>represents hydrogen; C<SUB>3-7</SUB>cycloalkyl; aryl or optionally substituted C<SUB>1-6</SUB>alkyl; and where Y is a direct bond, R<SUP>5 </SUP>may also be halo or Het; R<SUP>3 </SUP>and R<SUP>4 </SUP>each independently represents halo, haloC<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkyl, hydroxy, C<SUB>1-6</SUB>alkyloxy, C<SUB>1-6</SUB>alkylcarbonyloxy, mercapto, C<SUB>1-6</SUB>alkylthio, C<SUB>1-6</SUB>alkylsulfonyl, C<SUB>1-6</SUB>alkylsulfinyl, haloC<SUB>1-6</SUB>alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C<SUB>1-6</SUB>alkyl)amino or (C<SUB>1-6</SUB>alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.
申请公布号 ZA9806095(B) 申请公布日期 2000.01.10
申请号 ZA19980006095 申请日期 1998.07.09
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 EDDY JEAN EDGARD FREYNE;JEAN PIERRE FRANS VAN WAUWE;GUSTAAF MARIA BOECKX;GASTON STANISLAS MARCELLA DIELS
分类号 C07D253/06;A61K31/53;A61K51/00;A61K51/04;A61P11/06;A61P17/00;A61P27/02;A61P27/14;A61P37/08;A61P43/00;C07D253/075;C07D403/10;C07D417/10 主分类号 C07D253/06
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