Carbaphens: aprophen analogs that are binary antidotes for organ

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters

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560 57, C07C26900, C07C 6976

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active

049737341

ABSTRACT:
Novel carbaphens are provided of the formula ##STR1## wherein R is OH, OCON(CH.sub.3).sub.2 or OCONHCH.sub.3, and R' is H, OH or .sub.2 OCON(CH.sub.3).sub.2, stereoisomers thereof, pharmaceutically-acceptable salts thereof or mixtures thereof.
Compositions comprise the carbaphens with pharmaceutically acceptable carriers, and they may further comprise other drugs as well.
Methods of treating patients either prophylactically or therapeutically which suffer from organophosphate poisoning, coronary insufficiency, cerebral vasospasms, spastic cholitis and cholecystitis comprise the administration of the carbaphens of the invention.

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Leader et al. J. Med. Chem 32(7), 1989, 1522-1528.
Parris et al. J. Org. Chem 27, 1962 pp. 455-460.
Foye, Principles of Medicinal Chemistry, Philadelphia; Lea and Fibiger, (1), pp. 369-370.
Carroll, et al. J. Med. Chem. 30(5), 1987, pp. 805-809.
Mashkovskii, et al. Farmakol. Toksikol. 30(1) 36-41, (1967) Chemical Abstracts, vol. 66, 1967 Abstract. 93599c.

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