[EN] 2,3,5 TRISUBSTITUTED PYRROLE DERIVATIVES AS TOPOISOMERASE INHIBITORS AND THERAPEUTIC USES THEREOF<br/>[FR] DÉRIVÉS TRISUBSTITUÉS 2, 3, 5 DE PYRROLE EN TANT QU'INHIBITEURS DE TOPOISOMÉRASE ET LEURS UTILISATIONS THÉRAPEUTIQUES
申请人:UNIV OF MYSORE
公开号:WO2017029684A1
公开(公告)日:2017-02-23
The compounds of Formula (1) having topoisomerase inhibitory effect includes [Formula should be inserted here] 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.
具有拓扑异构酶抑制作用的Formula(1)化合物包括[在此插入公式]其中,R1从以下组中选择:H,OR5,可选择取代的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杂基烷基,C3-C12环烷基,C3-C12环烯基,C2-C12杂环烷基,C2-C2杂环烯基,C6-C18芳基和C1-C18杂芳基;R2、R3和R4分别从以下组中选择:H,卤素,CN,-NO2,SH,CF3,OH,CO2H,CONH2,OCF3,可选择取代的C1-C12烷基,可选择取代的C1-C12卤代烷基,可选择取代的C2-C12烯基,可选择取代的C2-C12炔基,可选择取代的C1-C12烷氧基,可选择取代的C1-C12卤代烷氧基,可选择取代的C2-C12杂基烷基,可选择取代的C3-C12环烷基,可选择取代的C3-C12环烯基,可选择取代的C2-C12杂环烷基,可选择取代的C2-C12杂环烯基,可选择取代的C6-C18芳基,可选择取代的C1-C18杂芳基;R5选择为H,可选择取代的C1-C12烷基,可选择取代的C2-C12烯基,可选择取代的可选择取代的C1-C12卤代烷基,可选择取代的C3-C12环烷基,可选择取代的C6-C18芳基,可选择取代的C1-Ci18杂芳基;或其药学上可接受的盐、N-氧化物或前药。