| 主权项 |
1. A compound of formula (I):wherein
A is C1—R1 or N; R1 and R2 are selected from hydrogen, halogen, nitro, cyano, —S(O)nR7, amino, mono- or di-C1-C6-alkylamino, —NHCOR8, —NH(C═O)NHR9, —NHSO2R10, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, hydroxyl, C1-C6-alkoxy or C2-C6-alkenyloxy wherein C1-C6-alkyl and C1-C6-alkoxy can be further substituted with one to three identical or different radicals selected from the group consisting of halogen, hydroxy and C1-C4-alkoxy; n is 0, 1 or 2; R4 is hydrogen; R3 and R5 are independently selected from hydrogen, halogen and C1-C6-alkyl which can be further substituted with halogen; R6 is selected from hydrogen, nitrile (—CN), —COOH, —COORA, —CORA, —SO2RA—CONH2, —SO2NH2, —CONHRA, —SO2NHRA, CONRARB, SO2NRARB and heteroaryl, wherein RA and RB are independently an optionally substituted (C1-C6)alkyl, phenyl or monocyclic heteroaryl having 5 or 6 ring atoms, or RA and RB when attached to the same nitrogen atom form a cyclic amino ring; R7 is selected from C1-C6-alkyl, hydroxy-C1-C6-alkyl, C1-C4-alkoxy, amino, mono- or di-C1-C4-alkylamino, hydroxycarbonyl, aminocarbonyl, C3-C6-cycloalkyl, phenyl or C2-C6-alkenyl; wherein C3-C6-cycloalkyl can be substituted with one or more of C1-C4-alkyl, hydroxyl and C1-C4-alkoxy and phenyl can be substituted with one or more of halogen, cyano, C1-C4-alkyl, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy and C1-C4-alkoxy; R8 and R9 are independently selected from hydrogen and C1-C6-alkyl, and R10 is C1-C6 alkyl; —X1—X2— is —NR19—CO—; R15 and R19 each independently represent a radical of formula —[Y]m-[Alk1]p-[Q]t-[Alk2]q-Z, wherein
Y is —O—, —S—, —NRE—, —(C═O)—, —S(O)2—, —C(═O)O—, —(C═O)NRE—, —NRE(C═O)—, —NRE—C1-C4-alkyl-, or —C1-C4-alkyl-NRE—, —S(O)2NRE—, —NRES(O)2— wherein RE is hydrogen, C1-C6 alkyl;m, p, q and t are independently 0 or 1;Alk1 and Alk2 each independently represent a C1-C6 alkylene radical;Q represents a divalent mono- or bicyclic carbocyclic or heterocyclic radical having 3-9 ring members;Z is(i) a monocyclic heterocyclic ring of 5 or 6 ring members or a bridged heterocyclic ring system of 7 or 8 ring members, wherein the ring heteroatoms are nitrogen, said monocyclic ring or bridged ring system being linked to the rest of the molecule via a ring carbon, and wherein a ring nitrogen may be quaternized by substitution by C1-C3 alkyl or benzyl the latter being optionally substituted in the phenyl ring thereof; or(ii) —N(RA)(RB) wherein RA and RB are independently hydrogen, or a C1-C6-alkyl, C3-C6-cycloalkyl group, or a phenyl(C1-C6)alkyl- group optionally substituted in the phenyl ring thereof; or, taken together with the nitrogen to which they are attached form a monocyclic heterocyclic ring of 5 to 7 ring atoms which may contain a further heteroatom selected from N, O and S; or(iii) —N+(RA)(RB)(RC) wherein
RA, RB and RC are independently a C1-C6-alkyl, C3-C6-cycloalkyl group, or a phenyl(C1-C6)alkyl- group optionally substituted in the phenyl ring thereof; orRA is a C1-C6-alkyl, C3-C6-cycloalkyl group, or a phenyl(C1-C6)alkyl- group optionally substituted in the phenyl ring thereof and RB and RC taken together with the nitrogen to which they are attached form a monocyclic heterocyclic ring of 5 to 7 ring atoms which may contain a further heteroatom selected from N, O and S; orRA, RB and RC taken together with the nitrogen to which they are attached form a bridged heterocyclic ring system of 7 or 8 ring members;(iv) —NRAC(═NRB)NRCRD wherein
RA, RB, RC and RD are independently hydrogen or C1-C6-alkyl; or any two of RA, RB, RC and RD are independently hydrogen or C1-C6-alkyl, while the other two taken together represent a C1-C6 alkylene radical; or(v) —C(═NRA)NRBRC, wherein
RA, RB and RC are independently hydrogen or C1-C6-alkyl; or any one of RA, RB and RC is hydrogen or C1-C6-alkyl, while the other two taken together represent a C1-C6 alkylene radical;(vi) —NRAC(═NRC)RB, wherein
RA, RB and RC are independently hydrogen or C1-C6-alkyl; or any one of RA, RB and RC is hydrogen or C1-C6-alkyl, while the other two taken together represent a C1-C6 alkylene radical, or a pharmaceutically acceptable salt thereof. |
