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

机译:吡啶鎓醛肟型胆碱酯酶活化剂的新型前药衍生物及其使用方法

摘要

There is provided, novel pro-drug forms of pyridinium aldoxime type cholinesterase reactivators, namely, dihydropyridinium aldoximes, having the formula:PPWHEREIN R represents a member selected from the group consisting of an alkyl (C.sub.1 -C.sub.4) group, aP PGROUP, AP PGROUP,PP GROUP, AND A PPWHEREIN 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.PPThese compounds are useful in reactivating cholinesterase, inhibited following exposure to and/or ingestion of conventional anti-cholinesterase agents, especially in the brain.
机译:提供了新颖的前药形式的吡啶醛醛肟型胆碱酯酶活化剂,即二氢吡啶醛醛肟,其具有下式:其中R代表选自由烷基(C.sub.1)组成的组的成员。 -C.sub.4)组,a

GROUP,A

GROUP,

GROUP和A

,其中Z表示选自以下的成员由--CH.sub.2 --CH.sub.2-组组成的组,即--CH.sub。 2 --O--CH.sub。 2-组,--CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2-组和--CH。 sub.2 O--CH.sub.2 --CH.sub.2 --O--CH.sub.2-组;其中R1代表选自氢原子,甲基,酰基和## EQU1 ##的基团;这些化合物可用于重新活化胆碱酯酶,在暴露于和/或摄入常规抗胆碱酯酶后,尤其是在胆碱酯酶中被抑制。大脑。

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