发明名称 PHTHALAZINE DERIVATIVES AS PHOSPHODIESTERASE 4 INHIBITORS
摘要 Compounds of formula (I) wherein B is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalk yl residue; A is phenyl or heterocycle optionally substituted; R represents two hydrogen atoms or a C=O group when ----- is a single bond or, when <u >-- --- is a double bond, is hydrogen, optionally substituted aryl or heterocycle, (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl optionally substituted by aryl or heterocycle; aryloxy, heterocyclyloxy, aryl-C1-4- alkoxy, heterocyclyl-C1-4-alkoxy, amino substituted by 1 or 2 C1-4-alkyl group(s), aryl-amino, heterocyclyl-amino, aryl-C1-4-alkylamino, heterocyclyl - C1-4-alkylamino; R1 is a C1-6-alkyl, aryl, aryl-C1-10-alkyl, C4-7-cycloalkyl group optionally containing an oxygen atom and/or substituted; R2 is a C1-6- alkyl, polyfluoroC1-6-alkyl group; R3, when ----- is a single bond, i s (a) hydrogen; (b) C1-6-alkyl optionally substituted by aryl, by heterocycle or by a COR5 group wherein R5 is hydroxy, C1-4-alkoxy or hydroxyamino; (c) -COR 6 wherein R6 is hydrogen, aryl, aryl-C1-6-alkyl, amino optionally alkylated or monohydroxylated, hydroxy, C1-4-alkoxy, carboxy, C1-4-alkoxycarbonyl, formul a (II) or C1-4-alkyl optionally substituted by heterocycle; (d) C1-4 alkyl- sulfonyl; the NO derivatives of the compounds of formula (I) and the pharmaceutically acceptable salts thereof; are PDE 4 inhibitors.
申请公布号 CA2337954(A1) 申请公布日期 2000.02.03
申请号 CA19992337954 申请日期 1999.07.16
申请人 ZAMBON GROUP S.P.A. 发明人 MORAZZONI, GABRIELE;GRANCINI, GIANCARLO;NORCINI, GABRIELE;PELLACINI, FRANCO;NAPOLETANO, MAURO
分类号 A61K31/502;A61P11/00;A61P29/00;A61P37/08;C07D237/30;C07D237/32;C07D237/34;C07D401/04;C07D401/06;C07D401/14;C07D405/06;C07D405/12;C07D405/14;C07D417/14;(IPC1-7):C07D237/30 主分类号 A61K31/502
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