H. Lundbeck A/s

Other

A/s Gea

Erik Falch

Povl Krogsgaard-Larsen

Jens Kristian Perregaard

Henrik Pedersen

Hans Bundgaard

Sibylle Moltzen Lenz

Arne Schousboe

Bente Frolund

Anne V Christensen

Per Sauerberg

Jens-Jorgen Larsen

Thomas J Mikkelson

Claus S Larsen

The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.

4-aminotetrahydrobenzisoxazole or -isothiazole compounds

The present invention relates to novel compounds of the following formula: ##STR1## wherein R.sup.1 is alkyl, alkenyl, alkynyl, branched or unbranched, with 1-6 carbon atoms either unsubstituted or optionally substituted with fluoro, hydroxy or phenyl, in which the phenyl group may be substituted with halogen,trifluoromethyl, lower alkyl, hydroxy or lower alkoxy;

5,6,7,8-tetrahydro-4H-isoxazolo[4,5-c]-azepine derivatives

The present invention relates to novel compounds of the following formula: ##STR1## individual isomers and pharmaceutically acceptable acid addition salts thereof, wherein

4,5,6,7-Tetrahydroisothiazolo (4,5-c) pyridine derivatives

Compounds are disclosed of the general formula I ##STR1## wherein R.sub.1 is a group of the formula II

Pilocarpine prodrugs

Acyl- or acyloxymethyl-allopurinol prodrugs

The present invention relates to novel compounds of the following formula: ##STR1## individual isomers and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 is hydrogen, alkyl or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, lower alkyl or lower alkoxy; R.sub.2 is alkyl, alkenyl, alkynyl or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, lower alkyl or lower alkoxy; and R.sub.4 is hydrogen or alkyl. The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of the formula I.

Tetrahydroisoxazolo[4,5-c]pyridine derivatives useful in the treatment

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Vedbaek, Denmark

Erik Falch