发明名称 DERIVATIVES OF 1,3-DIHYDRO-1-(PHENYLALKYL)-2H-IMODAZOL-2-ONE OF PDE IV AND CYTOKINIC ACTIVITY
摘要 The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy; R4 is hydrogen; halo; optionally substituted C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or R4 is a radical of formula: -O-R6; or -NH-R7; R5 is hydrogen, halo, hydroxy or C1-6alkyl; or R4 and R5 taken together may form a bivalent radical of formula: -(CH2)n-; -CH2-CH2-O-CH2-CH2-; -CH2-CH2-N(R8)-CH2-CH2-; or -CH2-CH=CH-CH2-; Y is a direct bond, haloC1-4alkanediyl or C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR9=CR10-; or -CHR9-CHR10-; and L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 </superscript><
申请公布号 PL187375(B1) 申请公布日期 2004.06.30
申请号 PL19960322654 申请日期 1996.03.28
申请人 JANSSEN PHARMACEUTICA NV 发明人 FREYNE EDDY J. E.;DIELS GASTON S. M.;ANDRES-GIL JOSE I.;FERNANDEZ GADEA FRANCISCO J.
分类号 C07D233/32;A61K31/415;A61K31/4166;A61K31/44;A61K31/4427;A61K31/443;A61P11/00;A61P17/00;A61P29/00;A61P37/08;C07D233/36;C07D233/38;C07D233/70;C07D401/06;C07D401/12;C07D405/06;C07D405/12 主分类号 C07D233/32
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