Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1985-05-08
1987-06-23
Schwartz, Richard A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514305, 514318, 546133, 546137, 546193, 546194, A61K 3146, C07D40112
Patent
active
046753265
ABSTRACT:
A novel series of antidotes against organophosphorus poisoning having both anti-muscarinic activity and reactivation potency, were synthesized 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.
REFERENCES:
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F. Mobbiger in Handbuch der Experimentellen Pharmakologie, O. Eichler et al. (Editors), Springer Verlag, Berlin, 1963, pp. 921-968.
H. Kewitz et al., Arch. Biochem. Biophys. 64, 456 (1956).
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G. Amitai, et al., Biochem. Pharmacol., 29, 483 (1980).
J. Gordon, et al., Toxicol. App. Pharmacol., 43, 207 (1978).
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M. D. Mashkovsky, First Intern. Pharmacol. Meeting, 7, 359 (1961).
Amitai Gabriel
Balderman David
Bruckstein-Davidovici Rachel
Spiegelstein Michael
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