首页> 外国专利> 2,3,5 TRISUBSTITUTED PYRROLE DERIVATIVES AS TOPOISOMERASE INHIBITORS AND THERAPEUTIC USES THEREOF

2,3,5 TRISUBSTITUTED PYRROLE DERIVATIVES AS TOPOISOMERASE INHIBITORS AND THERAPEUTIC USES THEREOF

机译:2,3,5取代的吡咯衍生物作为拓扑异构酶抑制剂及其治疗用途

摘要

The compounds of Formula (1) having topoisomerase inhibitory effect includes; embedded image ;wherein, R1 is selected from a group consisting of H, OR5, optionally substituted C1-C12 alkyl, haloalkyl, C2-C12alkenyl, C2-C12alkynyl, C1-C12alkyloxy, C1-C12haloalkyloxy, C2-C10 heteroalkyl, C3-C12 cycloalkyl, C3-C12cycloalkenyl, C2-C12heterocycloalkyl, C2-C2 heterocycloalkenyl, C6-C18aryl, and C1-C18heteroaryl;R2, R3 and R4 are independently selected from a group consisting of H, halogen, CN, —NO2, SH, CF3, OH, CO2H, CONH2, OCF3, optionally substituted C1-C12alkyl, optionally substituted C1-C12haloalkyl optionally substituted C2-C12alkenyl, optionally substituted C2-C12alkynyl, optionally substituted C1-C12alkyloxy, optionally substituted C1-C12haloalkyloxy, optionally substituted C2-C12heteroalkyl, optionally substituted C3-C12cycloalkyl, optionally substituted C3-C12 cycloalkenyl, optionally substituted C2-C12 heterocycloalkyl, optionally substituted C2-C12 heterocycloalkenyl, optionally substituted C6-C18aryl, and optionally substituted C1-C18heteroaryl;R5 is selected H, optionally substituted C1-C12alkyl, optionally substituted C2-C12alkenyl, optionally substituted optionally substituted C1-C12 haloalkyl, optionally substituted C3-C12cycloalkyl, optionally substituted C6-C18aryl, and optionally substituted C1-Ci18heteroaryl;or a pharmaceutically acceptable salt, N-oxide, or prodrug thereof.
机译:具有拓扑异构酶抑制作用的式(1)化合物包括: “嵌入式图像” ;其中,R1选自H,OR5,任选取代的C1-C12烷基,卤代烷基,C2-C12烯基,C2-C12炔基,C1-C12烷氧基,C1-C12卤代烷氧基,C2-C10杂烷基,C3-C12环烷基, C 3 -C 12环烯基,C 2 -C 12杂环烷基,C 2 -C 2杂环烯基,C 6 -C 18芳基和C 1 -C 18杂芳基; R2,R3和R4独立选自H,卤素,CN,-NO2,SH,CF3,OH,CO2H,CONH2,OCF3,任选取代的C1-C12烷基,任选取代的C1- C 12卤代烷基,任选取代的C 2 -C 12炔基,任选取代的C 1 -C 12烷氧基,任选取代的C 1 -C 12卤代烷氧基,任选取代的C 2 -C 12杂烷基,任选取代的C 3 -C 12环烷基,任选取代的C 3 -C 12环烯基,任选取代的C 2 -C 12杂环烷基,任选取代的C2-C12杂环烯基,任选取代的C6-C18芳基和任选取代的C1-C18杂芳基; R5选择为H,任选取代的C1-C12烷基,可选取代的C2-C12烯基,可选取代的opti取代的C1-C12卤代烷基,任选取代的C3-C12环烷基,任选取代的C6-C18芳基和任选取代的C1-C18杂芳基; 或可药用盐,N-氧化物或其前药。

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