The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Nov. 02, 2010
Filed:
Mar. 07, 2007
Robert C. Moschel, Frederick, MD (US);
Matthew Karl Moschel, Legal Representative, Baltimore, MD (US);
Natalia A. Loktionova, Hershey, PA (US);
Anthony E. Pegg, Hershey, PA (US);
Gary T. Pauly, Frederick, MD (US);
Robert C. Moschel, Frederick, MD (US);
Matthew Karl Moschel, legal representative, Baltimore, MD (US);
Natalia A. Loktionova, Hershey, PA (US);
Anthony E. Pegg, Hershey, PA (US);
Gary T. Pauly, Frederick, MD (US);
The United States of America as represented by the Department of Health and Human Services, Washington, DC (US);
The Penn State Research Foundation, University Park, PA (US);
Abstract
Disclosed are prodrugs of inactivators of O-alkylguanine-DNA alkyltransferase (AGT). The prodrugs are cleavable by the β-glucuronidase enzyme, which is either administered to the patient or produced by necrotic tumor cells. The prodrugs are represented by the formula A-B-C, wherein A is a glucuronosyl residue linked through its 1-oxygen to the phenyl ring of B; B is a benzyloxycarbonyl group, optionally ring-substituted with one or more electron withdrawing groups; and C is an inactivator of AGT, e.g., a substituted or unsubstituted O-benzylguanine or O-benzyl-2'-deoxyguanosine. Also disclosed are additional inactivators of AGT, pharmaceutical compositions comprising an inactivator or prodrug and a pharmaceutically acceptable carrier, and a method of use of the inactivator or prodrug in enhancing the chemotherapeutic treatment of tumor cells in a mammal, e.g., a human, with an antineoplastic alkylating agent that causes cytotoxic lesions at the O-position of guanine.