Neurosearch A/s

A/s Ferrosan

Schering Aktiengesellschaft

Leif H Jensen

Frank Watjen

John Bondo Hansen

Mogens Engelstoft

Peter Moldt

Jorgen Drejer

Dieter Seidelmann

Jorgen Scheel-Kruger

Erling N Petersen

Per Sauerberg

Bjarne H Dahl

Soren-Peter Olesen

Jens W Kindtler

Gunnar M Olsen

Andreas Huth

Ralph Schmiechen

David N Stephens

Claus T Braestrup

Frank Waetjen

Tage Honore

Mikkel Thaning

Jo Slashedrgen Scheel-Kruger

Jo Slashedrgen Scheel-Kr Uger

Elsbet O Nielsen

Fused tropane-derivatives as neurotransmitter reuptake inhibitors

The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sup.3, and R.sub.4 each have the meanings set forth in the specification. The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

Substituted heterocyclic compounds as dopamine-reuptake inhibitors

The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.21 and R.sup.22 each independently are alkyl; and

Indole-derivatives, method of treatment therewith, and pharmaceutical

A compound having the formula ##STR1## wherein X is O, S

Benzimidazole derivatives, their preparation and pharmaceutical use

The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sub.3, and R.sup.4 each have the meanings set forth in the specification. The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

Phenyl substituted heterocyclic compounds

The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sup.3, and R.sup.4 each have the meanings set forth in the specification. The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

2,3-trans-disubstituted tropane compounds which have useful

Certain 2,3-diphenyl-2-(1,2,4-oxadiazol-5-yl)tropanes useful as dopamide

A method of antagonizing the biological effects of an excitatory amino acid of a subject in need of such antagonization comprising the step of administering to said subject an effective amount of a compound having the formula ##STR1## wherein R.sup.3 is hydrogen, C.sub.1-8 -alkyl which may be branched, or cycloalkylmethyl;

Method of antagonizing excitatory amino acids by administration of

A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 wherein

Isatinoxime derivatives, their preparation and use

A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;

Isatineoxime derivatives and their use

A method of treatment with compounds having the formula ##STR1## R.sup.1 is hydrogen, C.sub.1-6 -alkyl which may be branched, C.sub.3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C.sub.1-6 -alkoxy, CH.sub.2 CO.sub.2 R' wherein R' is hydrogen or C.sub.1-6 -alkyl which may be branched, CH.sub.2 CN, CH.sub.2 CONR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen or C.sub.1-6 -alkyl, or CH.sub.2 C(.dbd.NOH)NH.sub.2 ; R.sup.2 is hydrogen, benzyl, C.sub.1-6 -alkyl which may be branched, or C.sub.3-7 -cycloalkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently are hydrogen, C.sub.1-6 -alkyl which may be branched, phenyl, halogen, C.sub.1-6 -alkoxy, NO.sub.2, CN, CF.sub.3, OCF.sub.3, or SO.sub.2 NR'R'' wherein R' and R'' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl; or R.sup.6 and R.sup.7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO.sub.2, CF.sub.3, CN, OCF.sub.3, SO.sub.2 NR' R'' wherein R' and R'' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl, and R.sup.4 and R.sup.5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel. The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.

Isatine derivatives, their preparation and use

A method of treating a disease in a mammal, including a human, responsive to blockade of potassium channels, which comprises administering to a mammal in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 independently of each other are hydrogen, CF.sub.3, NO.sub.2, NH.sub.2, OH, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy or phenyl; and

Indole derivatives as potassium channel blockers

New piperidine compounds having the formula ##STR1## wherein at least one of R.sup.3, R.sup.4, and R.sup.5 are ##STR2## and the other independently are H, C.sub.1-6 -alkyl, wherein R' is H, C.sub.1-8 -alkyl, phenyl, thienyl, cyclopropyl, or C.sub.1-3 -alkoxymethyl; and

Lipophilically-substituted piperidine oxadiazolyl compounds and their

New piperidine compounds having the formula ##STR1## wherein at least one of R.sup.3, R.sup.4, and R.sup.5 are ##STR2## and the other independently are H, C.sub.1-6 -alkyl, wherein R' is H, C.sub.1-8 -alkyl, phenyl, thienyl, cyclopropyl, or C.sub.1-3 -alkoxymethyl; and R.sup.1 and R.sup.6 independently are H or C.sub.1-6 -alkyl, and wherein ##STR3## and salts thereof with pharmaceutically-acceptable acids. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are therefore useful in the treatment of Alzheimer's disease.

Lipophillically-substituted piperidine oxadiazolyl compounds and their

Compounds of formula I ##STR1## wherein X is COOR.sup.3 or an oxadiazolyl radical of the formula or

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Copenhagen, Denmark

Leif H Jensen