Bionumerik Pharmaceuticals, Inc.

Shijie Yao

Frederick H Hausheer

Kochat Haridas

Dhanabalan Murali

Dasharatha Gauravaram Reddy

Pavankumar Nv Petluru

Peddaiahgari Seetharamulu

Frederick Herman Hausheer

P Seetharamulu

Pavankumar Petluru

This invention relates to novel derivatives of camptothecin, and will, particularly to derivatives having a substitution at the C-7 position, or at one of the C-9, C-10, C-11 or C-12 positions, or to disubstituted derivatives having a first substitution at C-7 and a second at one of C-9, C-10, C-11 or C-12. The invention also includes methods of using the compounds as Topoisomerase I inhibitors to treat patients with cancer. The invention also includes pharmaceutical formulations which consist of the novel compounds in solution or suspension with one or more pharmaceutical excipients or dilutes.

Highly lipophilic camptothecin derivatives

Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.

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San Antonio, TX, United States of America

Shijie Yao