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    • 2. 发明申请
    • NOVEL N- (ALKOXYALKYL) CARBAMOYL - SUBSTITUTED 6-PHENYL-BENZONAPHTHYRIDINE DERIVATIVES AND THEIR USE AS PDE3/4 INHIBITORS
    • 新型N-(烷氧基)羰基 - 取代的6-苯基 - 苯并噻吩衍生物及其作为PDE3 / 4抑制剂的用途
    • WO2005090345A1
    • 2005-09-29
    • PCT/EP2005/051204
    • 2005-03-16
    • ALTANA PHARMA AGFLOCKERZI, Dieter
    • FLOCKERZI, DieterKAUTZ, UlrichHATZELMANN, ArminBARSIG, JohannesMARX, DegenhardKLEY, Hans-Peter
    • C07D471/04
    • C07D471/04
    • Compounds of formula (1), in which R1 is 1-4C-alkyl, R2 is hydroxyl, 1-4C-alkoxy. 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R3 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, or in which R2 and R3 together are a 1-2C-alkylenedioxy group, R4 is hydrogen, halogen, nitro, 1-4C-alkyl, trifluoromethyl or 1-4C-alkoxy, R5 is hydrogen, 1-8C-alkyl, 3-7C-cycloalkyl or phenyl-1-4C-alkyl, R6 is 1-4C-alkyl, phenyl-1-4C-alkyl, or Aryl-1-4C-alkyl, in which Aryl is R61 - and/or R62-substituted phenyl, in which R61 is 1-4C-alkoxy, trifluoromethyl or cyano, R62 is 1-4C-alkoxy, and in which either R7 is 1-4C-alkyl, and n is 1 or 2, or R7 is hydrogen, and n is 1, 2 or 3, the salts, the N-oxides of these compounds and the salts of the latter are novel effective PDE3/4 inhibitors.
    • 式(1)的化合物,其中R 1是1-4C-烷基,R 2是羟基,1-4C-烷氧基。 完全或主要被氟取代的3-7C-环烷氧基,3-7C-环烷基甲氧基或1-4C-烷氧基,R3是羟基,1-4C-烷氧基,3-7C-环烷氧基,3-7C-环烷基甲氧基或 完全或主要被氟取代的1-4C-烷氧基,或其中R2和R3一起是1-2C-亚烷基二氧基,R4是氢,卤素,硝基,1-4C-烷基,三氟甲基或1-4C- 烷氧基,R 5是氢,1-8C-烷基,3-7C-环烷基或苯基1-4C-烷基,R6是1-4C-烷基,苯基1-4C-烷基或芳基 - 1-4C-烷基 其中芳基是R61 - 和/或R62-取代的苯基,其中R61是1-4C-烷氧基,三氟甲基或氰基,R62是1-4C-烷氧基,其中R7是1-4C-烷基,和 n为1或2,或R7为氢,n为1,2或3,这些化合物的N-氧化物和后者的盐为新的有效的PDE3 / 4抑制剂。