C10-substituted camptothecin analogs

US7687497B2 · kind B2 · utility

Assignee

• BioNumerik Pharmaceuticals, Inc. · US

Inventors

• Kesavaram Narkunan · San Antonio, US
• Xinghai Chen · San Antonio, US
• Harry Kochat · San Antonio, US
• Frederick H. Hausheer · Boerne, US

Key dates

• Filing date: Oct 16, 2007
• Grant date: Mar 30, 2010
• Expiry date: Oct 16, 2027

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).