Neurosearch A/s

A/s Ferrosan

Novo Nordisk A/s

Meiji Seika Kaisha, Ltd.

Schering Aktiengesellschaft

Frank Watjen

Mogens Engelstoft

Leif H Jensen

Jorgen Drejer

Holger C Hansen

Lene Teuber

John Bondo Hansen

Peter Moldt

Per Sauerberg

Jens W Kindtler

Bjarne H Dahl

Erling N Petersen

Preben H Olesen

Dieter Seidelmann

Toshiro Sasaki

Yoshimasa Fukuda

Osamu Ushiroda

Andreas Huth

Christopher Franklin Bigge

Oskar Axelsson

Thomas C Malone

Lone Kierstein Nielsen

Jorgen Scheel-Kruger

Tage Honore

Soren-Peter Olesen

Jo Slashedrgen Scheel-Kruger

Trevor John Grinter

Lone Nielson

Lein H Jensen

The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

Hydrochloride salt of an azabicyclo[3.2.1]octane derivative

The present invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAreceptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

Benzimidazole derivatives and pharmaceutical compositions comprising these compounds

Quinoxalinedione derivatives, their preparation and use

Indole-2,3-dione-3-oxime derivatives

The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R is &mdash;CR&prime;&boxH;NOR&Prime; wherein R&prime; and R&Prime; each independently are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkylalkenyl, alkynyl, cycloalkylalkynyl, aryl or benzyl; R is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF , CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF , CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF , CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF , CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.

Piperidine derivatives as neurotransmitter re-uptake inhibitors

The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.

Indole-2,3-dione-3-oxime derivatives for therapeutic use

The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2 or 3; R,represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino and nitro; or R,represents a cyano group or a group of the formula -alkyl-CO,R,, alkenyl-CO,R,, &mdash;CO&mdash;R,, &mdash;CO,(CH,),R,, or &mdash;C(R,)&boxH;N&mdash;OR,, R,represents a group of formula &mdash;CO,&mdash;R,, or R,represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R,may represent a group of general formula (III), in which n is 0, 1, 2 or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA,receptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.

1-phenyl-benzimidazole compounds and their use as GABA-a receptor modulators

Benzimidazole compounds and their use as modulators of the GABA a

Benzimidazole compounds and their use as modulators of the GABA.sub.A

Indole-2,3-dione-3-oxime derivatives, their preparation and use

Benzimidazole compounds, pharmaceutical compositions containing the

The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders. ##STR1##

AMPA antagonists and a method of treatment

Fused indole and quinoxaline derivatives, their preparation and use

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Herlev, Denmark

Frank Watjen