发明名称 Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
摘要 The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R<SUP>1 </SUP>is H, alkyl, cycloalkyl, cylcoalkylalkyl-, -CH<SUB>2</SUB>F, -CHF<SUB>2</SUB>, -CF<SUB>3</SUB>, -C(O)alkyl or -C(O)NR<SUP>18</SUP>R<SUP>19</SUP>; R<SUP>3 </SUP>and R<SUP>4</SUP>H, alkyl, hydroxyalkyl or -C(O)Oalkyl; R<SUP>5 </SUP>and R<SUP>6 </SUP>are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, -CH<SUB>2</SUB>F, -CHF<SUB>2</SUB>, -CF<SUB>3</SUB>, -C(O)OH or -C(O)Oalkyl; R<SUP>7 </SUP>is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R<SUP>17</SUP>-phenyl)alkyl or -CH<SUB>2</SUB>-C(O)-O-alkyl; and R<SUP>8 </SUP>comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R<SUP>7 </SUP>and R<SUP>8 </SUP>and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.
申请公布号 US2006106062(A1) 申请公布日期 2006.05.18
申请号 US20050130359 申请日期 2005.05.16
申请人 SCHERING CORPORATION 发明人 KUANG RONGZE;BLYTHIN DAVID;SHIH NENG-YANG;SHUE HO-JANE;CHEN XIAO;CAO JIANHUA;GU DANLIN;HUANG YING;SCHWERDT JOHN H.;TING PAULINE C.;WONG SHING-CHUN;XIAO LI
分类号 A61K31/4709;A61K31/496;A61K31/497;A61K31/498;A61K31/501;A61K31/506;A61K31/519;C07D401/04;C07D405/04;C07D405/14;C07D409/14;C07D413/02;C07D413/04;C07D413/14;C07D417/02;C07D417/04;C07D417/14 主分类号 A61K31/4709
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