Trisbenzimidazoles useful as topoisomerase I inhibitors

US5767142A · kind A · utility

Assignee

• Rutgers, the State University of New Jersey · US

Inventors

• Edmond J. LaVoie · Princeton Junction, US
• Leroy F. Liu · Bound Brook, US
• Qun Sun · Princeton, US

Key dates

• Filing date: Mar 20, 1996
• Grant date: Jun 16, 1998
• Expiry date: Mar 20, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D235/18
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention provides anti-neoplastic topoisomerase I inhibitors of the formula: ##STR1## wherein Ar is (C.sub.6 -C.sub.12)aryl or (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with (C.sub.1 -C.sub.4)alkyl; X is H, CN, CHO, OH, acetyl, CF.sub.3, O(C.sub.1 -C.sub.4)alkyl, NO.sub.2, NH.sub.2, halogen or halo-(C.sub.1 -C.sub.4)alkyl; each Y is individually H, (C.sub.1 -C.sub.4)alkyl or aralkyl; Y' is H or (C.sub.1 -C.sub.4)alkyl; n is 0 or 1; and each Z is individually H, (C.sub.1 -C.sub.4)alkyl, halogen or halo(C.sub.1 -C.sub.4)alkyl; or a pharmaceutically acceptable salt therein.