1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indol-2-ones

Details 1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indol-2-ones 1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indol-2-ones

C - Chemistry, Metallurgy

07

D

C07D 519/00 (2006.01) A61K 31/437 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2564027

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- or 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.

1-hétérocyclyl-1,5-dihydro-pyrido[3,2-b]indo l-2-ones représentés par la formule (I): les >N</i>-oxides, sels, formes stéréo-isomères, mélanges racémiques, promédicaments, esters et métabolites de ces composés, dans laquelle n vaut 1, 2 ou 3; R?1¿ est hydrogène, cyano, halo, carbonyle substitué, méthanimidamidyle, <i>N</i>-hydroxy- méthanimidamidyle, mono- ou di(C¿1-4?alkyl)méthanimidamidyle, Het¿1? ou Het¿2?; X est NR¿2?, O, S, SO, SO¿2?; R?2¿ est hydrogène, C¿1-10?alkyle, C¿2-10?alcényle, C¿3-7?cycloalkyle, qui sont éventuellement substitués; R?2¿ est un aryle subst itué par -COOR?4¿; ou R?2¿ est: (b-1); (b-2); -C¿p?H¿2p?-CH(OR?14¿)-C¿q?H¿2q?-R?15¿ (b-3); -CH¿2?-CH¿2?-(O-CH¿2? -CH¿2?)¿m?-OR?14¿ (b-4); -CH¿2?-CH¿2?-(O-CH¿2?-CH¿2?)¿m?-NR?5a¿R?5b¿ (b-5); -a?1¿=a?2¿-a?3¿=a?4¿- is -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; les atomes d'hydrogène de (c-1) - (c-5) pouvant être remplacés par certains radicaux; R?3¿ est un système à motif hétérocyclique aromatique monocyclique ou bicyclique pouvant être substitué.

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