| 摘要 |
Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1′,2′, S3,4 and S3′,4′ are present, each of S1,2, S1′,2′, S3,4 and S3′,4′ independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2′, and 4′ are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5′ with C8′, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)− and (X2)− independently represent anions of pharmaceutically acceptable salts. |
| 主权项 |
1. Helquat derivatives of the general formula I wherein up to three of S1,2, S1′,2′, S3,4 and S3′,4′ linkers are present, each of S1,2, S1′,2′, S3,4 and S3′,4′ independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, more preferably hydrocarbon chain having 4 carbon atoms and two double bonds, or S1,2, S1′,2′, S3,4 and S3′,4′ are not present; and from one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2′, and 4′ are substituted with a substituent R3 of general formula II wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5′ with C8′, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms, wherein heteroaryl is an aromatic carbocyclic group containing: 4 to 26 and preferably 4 to 12 carbon atoms, and at least one aromatic ring or multiple aromatic rings, wherein at least one carbon atom of the ring is replaced with a heteroatom selected from a group comprising N, S and O; the heteroaryl can be unsubstituted or substituted with 1 to 5 substituents selected from a group comprising C1 to C6 alkyl, C3 to C12 cycloalkyl optionally having at least one carbon atom of the ring replaced with a heteroatom selected from a group comprising N, S and O; C6 to C16 aryl, C6 to C26 arylalkyl, C1 to C6 halogenoalkyl, C1 to C12 alkoxy, C6 to C16 aryloxy, benzyloxy, C1 to C6 alkylthio, C6 to C16 arylthio, halogeno, —OH, —SH, —NH2, C1 to C6 alkylamino, C6 to C16 arylamino, C1 to C6 acylamino, —CN, nitro, —SO3H and —COORn, —C(═O)N(Rn)2, wherein Rn is hydrogen or C1 to C6 alkyl or C6 to C16 C6 to C12aryl; and anions (X1)− and (X2)− independently represent anions of salts, in particular pharmaceutically acceptable salts. |
