Abstract: Compounds useful for treating diseases of the central or peripheral nervous system in mammals have formulae I-XII ##STR1## wherein ring A or A' together with the spiro-carbon atom constitutes a bridged or unbridged ring containing one or two ring nitrogen atoms; and the other symbols have specified values, subject to certain conditions.

Abstract: Compounds useful for treating diseases of the central or peripheral nervous system in mammals have formulae I-XIII: ##STR1## wherein ring A or A' together with the spiro-carbon atom constitutes a bridged or unbridged ring containing one or two ring nitrogen atoms; and the other symbols have specified values, subject to certain conditions.

Abstract: The invention relates to compounds (I) for treating diseases of the central and peripheral nervous system, including enantiomers, racemates and acid addition and quaternary salts, ##STR1## wherein Q is selected from two H atoms, (CH.sub.2).sub.m and C(CH.sub.3).sub.2 where m is 1, 2 or 3 and n and p are; each independently 0, 1, 2 or 3, provided that n+p=1-3, and R.sup.0 is H, methyl or OH; the moiety ##STR2## R is selected from H, NH.sub.2, NH-C.sub.1-6 -alkyl, N(C.sub.1-6 -alkyl).sub.2, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, C.sub.3-7 - cycloalkyl, C.sub.1-6 -alkyl substituted by 1-6 halogen atoms, hydroxy- C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, carboxy-C.sub.1-6 -alkyl, (C.sub.1-6 -alkoxy)carbonyl-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, mono-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, di-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, 2-oxo-pyrrolidin-1-yl-methyl, aryl, diarylmethylol, and C.sub.

Abstract: 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.

Abstract: The invention relates to novel compounds (I) for treating diseases of the central and peripheral nervous system: ##STR1## including enantiomers, racemates and acid addition and quaternary salts thereof, wherein one of X and Y is O and the other of X and Y is N; Q is (CH.sub.2).sub.n or C(CH.sub.3).sub.2 where n is 1, 2 or 3 and the bridge --Q-- is attached at one end to position 1 and at the other end to position 4 or 5, and R.degree. is hydrogen, methyl or hydroxyl; in the moiety ##STR2## the line connecting Z and Y signifies a double bond when X--Z is O--C--R and Y is N, and a single bond when X--Z is N.dbd.C--R and Y is O; Z is C--R wherein R is selected from hydrogen, NH.sub.2, NH-R" (R"=C.sub.1-6 -alkyl), N(R").sub.2, R", C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, C.sub.3-7 -cycloalkyl, R" substituted by hydroxy or by 1-6 halogen atoms, R"O-C.sub.1-6 -alkyl, carboxy-C.sub.1-6 -alkyl, R"OCO-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, R""NH-C.sub.1-6 -alkyl, (R").sub.2 N-C.sub.

Abstract: 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.

Abstract: The invention thus provides a process for obtaining the preferential replacement by isotopes, of at least one of the hydrogen atoms selected from the group consisting of those attached to the .alpha.- or .alpha.'-carbon atoms in a compound containing the structural moiety (I) ##STR1## which comprises the steps of oxidizing the compound to the corresponding sulfoxide or sulfone which contains the corresponding structural moiety (II) ##STR2## wherein in the sulfoxide n is 1 and in the sulfone n is 2, effecting the isotopic replacement by a known method of said at least one hydrogen atom, and reducing the resultant isotope-labelled sulfoxide or sulfone to the correspondingly labelled compound containing the structural moiety (I).

Abstract: The present invention accordingly provides in one aspect, novel spiro-oxathiolane/quinuclidine compounds corresponding with the schematic structural formula (I) ##STR1## and geometrical isomers, enantiomers, diastereoisomers, racemates and acid addition salts thereof, wherein one of Y and Z is 0 and the other is S(.dbd.O).sub.n ; n is 0, 1 or 2; R' and R" are each selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl, C.sub.3-7 cycloalkyl, aryl, diarylmethylol, and alkyl substituted by at least one aryl group, provided that at least R' and R" is other than hydrogen; and each X is hydrogen, or when Y is 0 and Z is S(.dbd.O).sub.n simultaneously, then each X may also be selected from the group consisting of deuterium and tritium, and provided further that when each X is hydrogen, Y is 0 and Z is S simultaneously, then at least one of R' and R" is selected from the group consisting of alkenyl, alkynyl, cyclopropyl, cyclobutyl, cycloheptyl, hydroxyalkyl and aminoalkyl.

Abstract: 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 >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.

Abstract: The present invention describes novel tritium labelled nitrogen mustard type compounds, and their aziridinium type analog, and a process for the production of same. The compounds are of value in medical research and development and also as active ingredients of pharmaceutical compositions. The compounds can be used to develop analogs of human disease states and can also be used to evaluate the mechanism of neurotransmitter regulation and function, both in vitro and in vivo.

Abstract: 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.

Abstract: The invention relates to the production of compounds of the general formula: ##STR1## wherein X is selected from the group consisting of oxygen, CH.sub.2 and CH radicals, and when X designates oxygen, R designates alkyl, isoalkyl, aralkyl, and substituted aralkyl groups and when X designates CH.sub.2 then R designates alkyl, phenyl or substituted phenyl group, and A-B is a single bond, and when X designates CH.sub.2, R designates alkyl, phenyl or substituted phenyl groups and A-B is a double bond; and physiologically acceptable salts of these, and pharmaceutical composition containing the same as active ingredient.

Abstract: The invention relates to the production of compounds of the general formula: ##STR1## wherein X is selected from the group consisting of oxygen, CH.sub.2 and CH radicals, and when X designates oxygen, R designates alkyl, isoalkyl, aralkyl, and substituted aralkyl groups and when X designates CH.sub.2 then R designates alkyl, phenyl or substituted phenyl group, and A-B is a single bond, and when X designates CH.sub.2, R designates alkyl, phenyl or substituted phenyl groups and A-B is a double bond; and physiologically acceptable salts of these, and pharmaceutical compositions containing the same as active ingredient.

Abstract: Compounds of the general formula: ##STR1## wherein X is selected from the group consisting of oxygen, CH.sub.2 and CH radicals, and when X designates oxygen, R designates alkyl, isoalkyl, aralkyl, and substituted aralkyl groups and when X designates CH.sub.2 then R designates alkyl, phenyl or substituted phenyl group, and A-B is a single bond, and when X designates CH.sub.2 R designates alkyl, phenyl or substituted phenyl groups and A-B is a double bond; and physiologically acceptable salts of these, and mydriatic pharmaceutical compositions containing the same as active ingredient.

Abstract: Novel spiro (1,3-dioxolane-4,3') quinuclidine compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical or different, each designates a member of the group hydrogen, alkyl or aryl; a process for the production of these and pharmaceutical compositions of matter containing such compound as active ingredient.

Abstract: Compounds of the general formula ##STR1## wherein X is selected from the group consisting of oxygen CH.sub.2 and CH radicals, and when X designates oxygen, R designates alkyl, isoalkyl, aralkyl, and substituted aryl groups and when X designates ##STR2## then R designates alkyl, phenyl or substituted phenyl group, and A--B is a single bond and when X designates >CH, and A--B is a double bond, R designates alkyl, phenyl or substituted phenyl groups and physiologically acceptable salts of these, and pharmaceutical compositions containing same as active ingredient.