H. Lundbeck A/s

H. Lunbeck A/s

Henrik Pedersen

Jens Kristian Perregaard

Ejner Knud Moltzen

Kim Andersen

Ivan Mikkelsen

Robert Dancer

Benny Bang-Andersen

Klaus P Boegesoe

Klaus Gjervig Jensen

Klaus P Bogeso

Povl Krogsgaard-Larsen

Erik Falch

Thomas Ruhland

Klaus Peter B&oslash;ges&oslash;

Mario Rottl&auml;nder

Klaus Peter Bo Slashedgeso Slashed

Darcy Mulford

Barbara Bopp

Andre Pernet

Kiyoshi Sakamoto

Indane or dihydroindole derivatives

Benzofuran derivatives, their preparation and use

The present invention relates to substituted indane or dihydroindole compounds of Formula (I), wherein A and B are independently O or S; D is an optionally substituted methylene group; X is N or optionally substituted C; and W is a spacer group. The compounds are either selective dopamine D,ligands or they have combined effects at dopamine D,and serotonergic receptors and/or the serotonergic transporter. These compounds are therefore useful in the treatment of certain psychiatric and neurologic disorders, including psychosis, depression and anxiety.

The present invention relates to substituted indane or dihydroindole compounds of Formula (I)

##STR1## Fused benzo compounds of formula (I), wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from SO, SO.sub.2, and a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including, a group --COOR.sup.9 and a group --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also disclosed.

Fused benzo compounds for the treatment of central nervous system

Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including --COOR.sup.9 and --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also provided.

Fused benzo compounds containing a nitrogen heterocycle for the

Phenyl indole compounds

A substituted indole compound having the formula I: ##STR1## where Ar is one of a phenyl group, a phenyl group substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and cyano, and a hetero aromatic group selected from 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, 2-oxazolyl, 2-imidazolyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl; each dotted line is an optional double bond; X and X' are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, lower alkylthio, lower alkylsulfonyl, lower alkylamino, lower dialkylamino, cyano, trifluoromethyl, and trifluoromethylthio; or X and X' are taken together to form a 5 to 7 membered carbocyclic ring; R.sup.1 is selected from the group consisting of hydrogen, lower alkyl and lower alkyl substituted with one or two hydroxy groups; with the proviso that when X is hydrogen or fluoro then R.sup.1 cannot be hydrogen; R is a substituent having the formula Ib: ##STR2## wherein n is an integer from 2-6 inclusive; W is oxygen or sulfur; V.sup.1 is selected from OR.sup.4, SR.sup.5, CHR.sup.6 R.sup.7, and NR.sup.8 R.sup.9 ;

Indole derivatives

Specific 2- and 2,5-substituted indoles or 2,3-dihydroindole compounds of the following formula ##STR1## wherein, R is formula 1a ##STR2## and X, X', Ar, R.sup.1, n, U, Z, V and W are defined in the specification are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.

Specific 6-substituted or 2-alkyl substituted indole or 2,3-dihydroindole compounds are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.

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, where the dotted line designates an optional bond: ##STR1## wherein 'het' designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that 'het' may not designate a 1,2,4- or 1,3,4-oxadiazole; R.sup.1 -R.sup.5 are as defined in the specification; as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof. 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 formula I.

Oxazole and thiazole derivatives and their use for treating disorders

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

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Broenshoej, Denmark

Henrik Pedersen