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 US6951857(B2) 申请公布日期 2005.10.04
申请号 US20030434896 申请日期 2003.05.09
申请人 FREYNE EDDY JEAN EDGARD;BOECKX GUSTAAF MARIA;VAN WAUWE JEAN PIERRE FRANS;DIELS GASTON STANISLAS MARCELL 发明人 FREYNE EDDY JEAN EDGARD;BOECKX GUSTAAF MARIA;VAN WAUWE JEAN PIERRE FRANS;DIELS GASTON STANISLAS MARCELLA
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;(IPC1-7):C07D253/075 主分类号 C07D253/06
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