| 摘要 |
Substituted C-(imidazo-(1,2-a)-pyridin-3-yl)-methylamines (I) are new. Imidazo-pyridine derivatives of formula (I), optionally in the form of racemates, pure stereoisomers (especially enantiomers or diastereomers) or their mixtures in all proportions and in acid, base, salt or solvate (specifically hydrate) form, are new. R1 = OH, SH, NH2, NHMe, NMe2, Me, CH2Cl, CH2F, CHF2, CF3, OMe, OCH2Cl, OCH2F, OCHF2, OCF3, SMe, SCF3, Et, CHClMe, CH2CH2Cl, CHFMe, CH2CH2F, CH2CHF2, CH2CF3, OEt, COOH, CH2OH, CH(OH)Me, CH2CH2 (sic), CN, NO2 or halo; R2 = H or Me; R = H or COOR10; or (all optionally substituted) optionally unsaturated 1-6C alkyl, optionally unsaturated 3-8C cycloalkyl, 2-methylcyclopropyl, cyclopropylmethyl, 2- or 3-methylcyclobutyl, cyclobutylmethyl, aryl or heteroaryl; R4 = H or heterocyclic group of formula (a); or (all optionally substituted) optionally unsaturated 1-12C alkyl, optionally unsaturated 3-8C cycloalkyl, 2-methylcyclopropyl, cyclopropylmethyl, 2- or 3-methylcyclobutyl or cyclobutylmethyl; n, m = 0-6, provided that n + m = 1-6; X = O, S, SO, SO2 or NR7; R = H, halo, OH, SH, NH2, NO2, Me, Et, OMe, OEt or OCF3; R5 = H; or (all optionally substituted) optionally unsaturated 1-6C alkyl, optionally unsaturated 3-8C cycloalkyl, 2-methylcyclopropyl, cyclopropylmethyl, 2- or 3-methylcyclobutyl or cyclobutylmethyl; R6 = H; or (all optionally substituted) optionally unsaturated 1-6C alkyl, optionally unsaturated 3-8C cycloalkyl, 2-methylcyclopropyl, cyclopropylmethyl, 2- or 3-methylcyclobutyl, cyclobutylmethyl, aryl, heteroaryl, 1-4C aryl (sic) or 1-4C heteroaryl (sic); or NR5R6 = morpholino, 4-(R11)-piperazino, azetidino, pyrrolidino, piperidino or homopiperidino; R7 = H, 1-6C alkyl, 3-8C cycloalkyl, 2-methylcyclopropyl, cyclopropylmethyl, 2- or 3-methylcyclobutyl, cyclobutylmethyl, COR8 or SO2R9; R8 - R10 = H, 1-6C alkyl or aryl; R11 = H, 1-6C alkyl, 3-8C cycloalkyl, aryl, heteroaryl, aryl-(1-3C) alkyl, heteroaryl-(1-3C) alkyl, COR12 or SO2R13; and R12, R13 = H, 1-6C alkyl or aryl. Provided that the compounds (7-methyl-imidazo-(1,2-a)-pyridin-3-ylmethyl)-dimethylamine and C-(7-methyl-imidazo-(1,2-a)-pyridin-3-yl)-methylamine are excluded.
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