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2,3,5 TRISUBSTITUTED PYRROLE DERIVATIVES AS TOPOISOMERASE INHIBITORS AND THERAPEUTIC USES THEREOF
专利权人:
UNIVERSITY OF MYSORE
发明人:
HANUMAPPA, Ananda,KOTHANAHALLY S., Sharath Kumar,HEGDE, Mahesh,RAGHAVAN, Sathees C.,RANGAPPA, Kanchugarakoppal S.
申请号:
ININ2016/050069
公开号:
WO2017/029684A1
申请日:
2016.02.26
申请国别(地区):
WO
年份:
2017
代理人:
摘要:
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.Selon linvention, les composés de formule (1) ayant un effet inhibiteur de la topoisomérase comprennent [Formule à insérer ici] dans laquelle R1 est choisi dans un groupe constitué des composants suivants : H, OR5, alkyle C1-C12 éventuellement substitué, haloalkyle, alcényle C2-C12, alcynyle C2-C12, alkyloxy C1-C12, haloalkyloxy C1-C12, hétéroalkyle C2-C10, cycloalkyle C3-C12, cycloalcényle C3-C12, hétérocycloalkyle C2-C12, hétérocycloalcényle C2-C2, aryle C6-C18, et hétéroaryle C1-C18 R2, R3 et R4 sont indépendamment choisis dans un groupe constitué des
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