发明名称 Substituted acetophenones useful as PDE4 inhibitors
摘要 The present invention relates to a compound according to formula (I); wherein X1, X2, X3, X4 and X5 independently of each other represent -CH- or N; or X3, X4 and X5 independently of each other represent -CH- or N, and Xi and X2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, -CH2-C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
申请公布号 ZA200904358(B) 申请公布日期 2010.08.25
申请号 ZA20090004358 申请日期 2007.12.21
申请人 LEO PHARMA A/S 发明人 FELDING, JAKOB;NIELSEN, SIMON FELDBAEK
分类号 A61K;A61P;C07D 主分类号 A61K
代理机构 代理人
主权项
地址