Patent Number: 6,166,065

Title: 2,3-dioxabicyclo[3.3.1]nonane derivatives and antimalarial pharmaceutical compositions comprising them

Abstract: 2,3-Dioxabicyclo[3.3.1]nonane derivatives, carrying, at position 4, a sulfur-containing functionality selected from the group consisting of sulfonyl, sulfinyl and sulfenyl, adhered to C(4) vie methylene group, represented by structural formula (A) wherein: X is hydrogen, hydroxy, alkoxy, optionally substituted by alkoxy or acyloxy, aralkoxy optionally substituted by alkoxy or aryloxy, and M is hydrogen, hydroxy, alkoxy, alkenyloxy, acyloxy, optionally substituted by acyl or acyloxy, aralokoxy, arylalkenyloxy, oxalyloxy substituted by alkoxy, di(alkyl)amino or alkyl(aryl)amino, di(aralalkyl)amino or carbonyloxy substituted by arloxy, di(alkyl)amino, di(aralkyl)amino and alkyl(aryl)amino; or X and M together represent a carbon-carbon bond or an oxygen atom; L is hydrogen or L and M together represent a carbon-carbon bond; and either Z is a radical R--S(=O).sub.n -- and Y is hydrogen, or Y is R--S(=O).sub.n -- and Z is hydrogen, wherein R is alkyl optionally substituted by alkoxy or alkoxycarbonyl, cycloalkyl, or aryl or araklkyl optionally substituted by alkyl, halogen or CF.sub.3 ; and n is 0, 1, or 2, are useful for the prevention and/or treatment of malaria.

Inventors: Bachi; Mario (Rehovot, IL), Posner; Gary H. (Baltimore, MD), Korshin; Edward (Rehovot, IL)

Assignee: Yeda Research and Development Co., Ltd.

International Classification: C07D 319/00 (20060101); C07D 319/02 (20060101); A61K 031/335 (); C07D 319/02 ()

Expiration Date: 12/26/2017