TODAY’S PATENT – DI-N-HETEROCYCLIC COMPOUNDS, METHODS, AND COMPOSITIONS FOR INHIBITING PARP ACTIVITY

The Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity was invented by Paul F. Jackson, Keith M. Maclin, and Jie Zhang. which is been patented by USPTO on 19^th September 2000 bearing patent no. US6121278A. This patent has been assigned to Eisai Inc. This invention covers pharmaceutically acceptable salts, hydrates, esters, solvates, prodrugs, metabolites, and stereoisomers with formulas I–VI.

The compounds have a fused 5- to 6-membered heterocyclic ring with a nitrogen heteroatom. These compounds can be substituted with alkyl, alkenyl, cycloalkyl, cycloalkyl, aralkyl, aryl, double-bonded oxygen, or other non-hydrogen, non-phenyl substituents. In another embodiment, a pharmaceutically acceptable carrier and a compound of formula I am present in an amount sufficient to inhibit PARP activity, treat or prevent tissue damage, affect neuronal activity not mediated by NMDA toxicity, treat neural tissue damage, neurological disorders, vascular stroke, cardiovascular disorders, and other conditions.

As with the pharmaceutical compositions of the invention, the formula I compound inhibits PARP activity. These methods treat tissue damage, neural tissue damage, neurological disorders, vascular stroke, cardiovascular disorders, and other conditions with enough compounds.