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DERIVES DE HYDROXY-6-HETEROARYL-PHENANTHRIDINE ET LEUR UTILISATION ET TANT QU'INHIBITEURS DE PDE4
专利权人:
ALTANA PHARMA AG
发明人:
KAUTZ, ULRICH
申请号:
CA2557752
公开号:
CA2557752C
申请日:
2005.03.02
申请国别(地区):
CA
年份:
2012
代理人:
摘要:
Compounds of formula (I), in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or completely orpredominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or completely orpredominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 togetherare a 1-2C-alkylenedioxy group, R3 is hydrogen or 1-4C-alkyl, R31 is hydrogenor 1-4C-alkyl, either, in a first embodiment (embodiment a) according to thepresent invention, R4 is -O-R41, in which R41 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyl, or completely orpredominantly fluorine-substituted 1-4C-alkyl, and R5 is hydrogen or 1-4C-alkyl, or, in a second embodiment (embodiment b) according to the presentinvention, R4 is hydrogen or 1-4C-alkyl, and R5 is -O-R51, in which R51 ishydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyl, or completely or predominantly fluorine-substituted 1-4C-alkyl,Har is optionally substituted by R6 and/or R7 and/or R8, and is a 5- to 10-membered monocylic or fused bicyclic unsaturated or partially saturatedheteroaryl radical comprising 1 to 4 heteroatoms selected independently fromthe group consisting of oxygen, nitrogen and sulfur, are novel effective PDE4inhibitors.
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