Substitutes O.sup.6 -benzylguanines, compositions, and methods of using same
US5958932A · kind A · utility
Assignees
Inventors
Key dates
| Filing date | Apr 28, 1997 |
| Grant date | Sep 28, 1999 |
| Priority date | — |
| Expiry date | Apr 28, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides AGT inactivating compounds such as substituted O.sup.6 -benzylguanines of the formula ##STR1## wherein, for example, R.sub.1 is amino, hydroxy, or alkylamino, R.sub.2 is aminoalkyl, hydroxyalkyl, or alkylaminoalkyl, and R.sub.3 is halo, hydroxyalkyl, thiol or alkylthio, as well as pharmaceutical compositions comprising such compounds and 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 O.sup.6 -position of guanine comprising administering to a mammal an effective amount of one of the aforesaid compounds 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.