H. Lundbeck A/s

Bristol-myers Company

Povl Krogsgaard-Larsen

Erik Falch

Sibylle Moltzen Lenz

Jens Kristian Perregaard

Henrik Pedersen

Arne Schousboe

Bente Frolund

Benny Bang-Andersen

Michael S Eison

Klaus Peter B&oslash;ges&oslash;

Anne V Christensen

Per Sauerberg

Jens-Jorgen Larsen

(3-Alkoxyisoxazol-4-yl)-substituted 2-amino carboxylic acid derivatives and sulfur analogues thereof having general formula (I) or (II),

3-Alkoxyisoxazol-4-yl-substituted 2-amino carboxylic acid compounds

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

Tetrahydro-isoxazolo[4,5-d]azepine derivatives possess antiamnesic properties and are cognition enhancers.

THAZ derivatives for enhancement of cerebral function

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.

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Allerød, Denmark

Povl Krogsgaard-Larsen