发明名称 |
SUBSTITUTED O6-BENZYLGUANINES AND USE THEREOF |
摘要 |
The present invention provides 8-substituted O6-benzylguanine, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidine, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. 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 lesions at the O6-position of guanine, by administering to a mammal an effective amount of one of the aforesaid derivatives, 2,4-diamino-6-benzyloxy-s-triazine, 5-substituted 2,4-diamino-6-benzyloxypyrimidines, or 8-aza-O6-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine.
|
申请公布号 |
CA2632452(A1) |
申请公布日期 |
1996.02.15 |
申请号 |
CA19952632452 |
申请日期 |
1995.07.31 |
申请人 |
THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRETARY, DEPARTMENT OF HE;ARCH DEVELOPMENT CORPORATION, THE UNIVERSITY OF CHICAGO THE UNIVERSITY OF CH;THE PENN STATE RESEARCH FOUNDATION |
发明人 |
CHAE, MI-YOUNG;PEGG, ANTHONY E.;MOSCHEL, ROBERT C.;DOLAN, M. EILEEN |
分类号 |
C07D487/04;A61K31/505;A61K31/519;A61K31/52;A61K31/522;A61K31/53;A61P35/00;A61P43/00;C07D239/08;C07D239/46;C07D239/47;C07D239/48;C07D239/50;C07D251/52;C07D473/06;C07D473/18;C07D473/40 |
主分类号 |
C07D487/04 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|