Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-09-11
1999-06-29
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514 45, 514263, 514264, 544265, 544266, 544267, A61K 3152, C07D47304, C07D47318
Patent
active
059168943
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.
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Chae Mi-Young
Dolan M. Eileen
Moschel Robert C.
Pegg Anthony E.
ARCH Development Corporation
Gupta Yogendra N.
The Penn State Research Foundation
The United States of America as represented by the Department of
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