Title: Novel pro-drug derivatives of pyridinium aldoxime type cholinesterase reactivators and method of using same

Abstract: There is provided, novel pro-drug forms of pyridinium aldoxime type cholinesterase reactivators, namely, dihydropyridinium aldoximes, having the formula: ##SPC1## Wherein R represents a member selected from the group consisting of an alkyl (C.sub.1 -C.sub.4) group, a ##SPC2## Group, a ##SPC3## Group, ##SPC4## Group, and a ##SPC5## Wherein Z represents a member selected from the group consisting of a --CH.sub.2 --CH.sub.2 -- group, a --CH.sub.2 --O--CH.sub.2 -- group, a --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- group, and a --CH.sub.2 O--CH.sub.2 --CH.sub.2 --O--CH.sub.2 -- group; wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a methyl group, an acyl group and a ##EQU1## group; and wherein X.sup.- represents an anion derived from a pharmaceutically acceptable acid addition salt. These compounds are useful in reactivating cholinesterase, inhibited following exposure to and/or ingestion of conventional anti-cholinesterase agents, especially in the brain.

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Inventors: Higuchi, Takeru (Lawrence, KS, US)
Bodor, Nicolae S. (Lawrence, KS, US)
Shek, Efraim (Lawrence, KS, US)

Application Number: 603612
Filing Date: 1975-08-11
Publication_date: 1976-06-08
Assignee: Interx Research Corporation (Lawrence, KS)
Primary Class(es): 514/89 514/332
Other Classes:
US Patent Ref:
Other Refs:
Primary Examiner: Friedman, Stanley J.
Assistant Examiner:
Attorney: Blitzer; Charles N.