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

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专利权人:

发明人:

Ananda Hanumappa,Sharath Kumar Kothanahally S,Mahesh Hegde,Sathees C. Raghavan,Kanchugarakoppal S Rangappa

申请号：

US15753888

公开号：

US20180251425A1

申请日:

2016.02.26

申请国别(地区):

US

年份:

2018

代理人:

摘要：

The compounds of Formula (1) having topoisomerase inhibitory effect includeswherein, 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-C18heteroarylR2, 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-C18heteroarylR5 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-Ci18heteroarylor a pharmaceutically acceptable salt, N-oxide, or prodrug thereof.

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