State of Israel, Represented by the Prime Minister's Office, Israel

State of Israel, Represented by Prime Minister's Office Israel Institute

State of Israel, Represented by Prime Minister's Office, Israel

Aharon Levy

Abraham Fisher

Yona Grunfeld

Eliahu Heldman

Ishai Karton

Ishal Karton

Michael Y Spiegelstein

Jacob Grunwald

Eliahu Heidman

Moshe Kushnir

Drora Levy

A pharmaceutical composition is disclosed comprising (-)-cis-2-methylspiro(1,3-oxathiolan-5,3')quinuclidine, and/or the pharmaceutically compatible acid addition salts thereof, together with at least one of physostigmine, tetrahydroaminoacridine, choline, lecithin, piracetam, aniracetam, pramiracetam, oxiracetam, 4-aminopyridine, 3,4-diaminopyridine, somatostatin, pirenzepine, N-methylatropine, N-butylscopolamine, scopolamine, clonidine, quanfamicine and Nerve Growth Factor. Also disclosed is a method for treating senile dementia of Alzheimer's type, which comprises coadministering to a patient in need thereof an effective dose of the spiro compound together with at least one other compound selected from those listed above.

Pharmaceutical composition comprising a spiro oxathiolon/quinuclidine

The (+)-cis-, (-)-cis-, (+)-trans- and (-)-trans- forms of 2-methylspiro(1,3-oxathiolan-5,3')quinuclidine are prepared by optical resolution of each of the (.+-.)-cis- and (.+-.)-trans-isomers. These compounds find application in treating diseases of the central nervous system in mammals, especially diseases due to a deficiency in the central cholinergic system. Biological tests indicate that the (-)-cis-form, as well as the (.+-.)-cis-isomer, shows particular promise for treating senile dementia of Alzheimer's type.

Optical isomers

Quinuclidine derivatives having the general formula (I) ##STR1## and geometrical isomers, enantiomers, diastereoisomers, racemates and/or acid addition salts thereof, wherein Z represents the group &gt;CR.sup.1 R.sup.2 or two hydrogen atoms; and R.sup.1 and R.sup.2, which may be identical or different, are each alkyl, cyclopentyl, cyclohexyl, aryl, or diarylmethylol, or alkyl which is substituted by one or more aryl groups, or one of R.sup.1 and R.sup.2 may be hydrogen.

Derivatives of quinuclidine

There is provided a composition for the transdermal application of basic drugs which have a high specific activity. The drug is provided in combination with a fatty acid having a low molecular weight. Amongst others, the delivery system is suited for cholinergic and anticholinergic basic drugs. The compositions can be supported by a pad, bandage or the like. It is one of the advantages of the compositions of the invention that a prolonged effect can be obtained, with an essentially constant therapeutic level of the active ingredient.

Drug delivery system

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Beit Hanan, Israel

Aharon Levy