| 主权项 |
1. A compound of general formula (I): in which R1 represents —(CH2)n—(CHR4)—(CH2)m—N(R5)(R5′) R2 represents a heteroaryl of structure: optionally substituted with 1, 2 or 3 R6 groups,in which:* represents the point of attachment of said heteroaryl with the rest of the compound of general formula (I),X represents N or C—R6,X′ represents O, S, NH, N—R6, N or C—R6,with the proviso that when X and X′ are both C—R6, then one C—R6 is C—H; R3 is methyl; R4 is hydroxy; R5 and R5′ are the same or different and are, independently of each other, a hydrogen atom, or a C1-C6-alkyl, C3-C6-cycloalkyl-C1-C6-alkyl, or C1-C6-alkoxy-C1-C6-alkyl, or R5 and R5′, taken together with the nitrogen atom to which they are bound, represent a 3- to 7-membered nitrogen containing heterocyclic ring optionally containing at least one additional heteroatom selected from oxygen, nitrogen or sulfur and which may be optionally substituted with 1 or more R6′ groups; each occurrence of R6 may be the same or different and is independently a hydrogen atom, a halogen atom, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C6-alkyl, aryl, aryl-C1-C6-alkyl, heteroaryl, heteroaryl-C1-C6-alkyl, 3- to 8-membered heterocyclic ring, 3- to 8-membered heterocyclyl-C1-C6-alkyl, —C1-C6-alkyl-OR7, —C1-C6-alkyl-SR7, —C1-C6-alkyl-N(R7)(R7′), —C1-C6-alkyl-C(═O)R7, —CN, —C(═O)OR7, —C(═O)N(R7)(R7′), —OR7, —SR7, —N(R7)(R7′), or —NR7C(═O)R7 each of which may be optionally substituted with 1 or more R8 groups; each occurrence of R6′ may be the same or different and is independently C1-C6-alkyl, C3-C6-cycloalkyl-C1-C6-alkyl, or C1-C6-alkyl-OR7; each occurrence of R7 and R7′ may be the same or different and is independently a hydrogen atom, or a C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C6-alklyl, C3-C6-cycloalkenyl, aryl, aryl-C1-C6-alkyl, heteroaryl, 3- to 8-membered heterocyclic ring, 3- to 8-membered heterocyclyl-C1-C6-alkyl, or heteroaryl-C1-C6-alkyl; each occurrence of R8 is independently a halogen atom, or nitro, hydroxy, cyano, formyl, acetyl, amino, C1-C6-alkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C6-alkyl, C1-C6-cycloalkenyl, aryl, aryl-C1-C6-alkyl, heteroaryl, 3- to 8-membered heterocyclic ring, heterocyclyl-C1-C6-alkyl, or heteroaryl-C1-C6-alkyl; n is an integer of 1 and m is an integer of 1; with the proviso that when:
said R5 and R5′, taken together with the nitrogen atom to which they are bound, represent: in which * represents the point of attachment with the rest of the structure of general formula (I), then
said R2 heteroaryl of structure: is not: in which * represents the point of attachment with the rest of the structure of general formula (I). or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same. |
