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:
Jun. 29, 1999
Filed:
Sep. 11, 1997
Robert C Moschel, Frederick, MD (US);
Anthony E Pegg, Hershey, PA (US);
M Eileen Dolan, Oak Park, IL (US);
Mi-Young Chae, Frederick, MD (US);
The United States of America as represented by the Department of Health, , US;
The Penn State Research Foundation, University Park, PA (US);
Arch Development Corporation, Chicago, IL (US);
Abstract
The present invention provides 8-substituted O.sup.6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. Thus, for example, the present invention provides a compound of the formula ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of amino, hydroxy, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.4 acylamino, R.sub.2 is a substituent selected from the group consisting of C.sub.1 -C.sub.4 aminoalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 dialkylamino alkyl, and C.sub.1 -C.sub.4 pivaloylalkyl, and R.sub.3 is a C.sub.1 -C.sub.4 alkyl. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lessons at the O.sup.6 -position of guanine by administering to a mammal an effective amount of one of the aforesaid derivatives and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.