| 摘要 |
1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R<SUP>1 </SUP>is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C<SUB>1-4</SUB>alkyl)methanimidamidyl, Het<SUB>1 </SUB>or Het<SUB>2</SUB>; X is NR<SUB>2</SUB>, O, S, SO, SO<SUB>2</SUB>; R<SUP>2 </SUP>is hydrogen, C<SUB>1-10</SUB>alkyl, C<SUB>2-10</SUB>alkenyl, C<SUB>3-7</SUB>cycloalkyl, which are optionally substituted; R<SUP>2 </SUP>is aryl substituted with -COOR<SUP>4</SUP>; or R<SUP>2 </SUP>is: <?in-line-formulae description="In-line Formulae" end="lead"?>-C<SUB>p</SUB>H<SUB>2p</SUB>-CH(OR<SUP>14</SUP>)-C<SUB>q</SUB>H<SUB>2q</SUB>-R<SUP>15 </SUP>(b-3); -CH<SUB>2</SUB>-CH<SUB>2</SUB>-(O-CH<SUB>2</SUB>-CH<SUB>2</SUB>)<SUB>m</SUB>-OR<SUP>14 </SUP>(b-4); -CH<SUB>2</SUB>-CH<SUB>2</SUB>-(O-CH<SUB>2</SUB>-CH<SUB>2</SUB>)<SUB>m</SUB>-NR<SUP>5a</SUP>R<SUP>5b </SUP>(b-5); <?in-line-formulae description="In-line Formulae" end="tail"?> -a<SUP>1</SUP>=a<SUP>2</SUP>-a<SUP>3</SUP>=a<SUP>4</SUP>- is -CH-CH-CH-CH-; -N-CH-CH-CH-; -CH-N-CH-CH-; -CH-CH-N-CH-; -CH-CH-CH-N-; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R<SUP>3 </SUP>is a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted.
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