摘要 |
1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indo l-2-ones of formula (I): the N- oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereo f, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy- methanimidamidyl, mono- o r di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl subst ituted with -COOR4 ; or R2 is: (b-1); (b-2); - CpH2p-CH(OR14)-CqH2q-R15 (b-3); -CH2-CH2-(O-CH2 -CH2)m-OR14 (b-4); -CH2-CH2- (O- CH2-CH2)m-NR5aR5b (b-5); -a1=a2-a3=a4- 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; R3 is a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted.
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申请人 |
TIBOTEC PHARMACEUTICALS LTD. |
发明人 |
WIGERINCK, PIET TOM BERT PAUL;PEETERS, ANNICK ANN;VENDEVILLE, SANDRINE MARIE HELENE;SURLERAUX, DOMINIQUE LOUIS NESTOR GHISLAIN;RABOISSON, PIERRE JEAN-MARIE BERNARD;HACHE, GEERWIN YVONNE PAUL;KESTELEYN, BART RUDOLF ROMANIE |