Antidotes

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/12 (2006.01) C07D 211/36 (2006.01) C07D 213/20 (2006.01) C07D 453/02 (2006.01) C07D 453/04 (2006.01) C07D 519/00 (2006.01)

Patent

CA 1283412

ABSTRACT : A novel series of antidotes against organophosphorus poisoning having both anti-muscarinic activity and reactivation potency, were syn- thesized and evaluated for their pharmacological efficacy. The compounds are bisquarternary oxybismethylene(or:trimethylene)- - bis-N-heterocycles. The N-heterocycles are comprised of 2,3 or 4 mono-substituted pyridines, 3 substituted quinuclidines and 4-substituted N-methylpiperidines (exclusive of both groups in one molecule designating a substituted pyridine ring). Some of the compounds display a remarkably low acute toxicity in mice. These antidotes have been shown to be effective against poisoning by a variety of organophosphorus compounds as well as carbamates. The compounds are also of value as active ingredients in ophthalmic preparations.

489417

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