Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft

Günter Hölzemann

Christoph Seyfried

Kai Schiemann

Gerd Bartoszyk

Timo Heinrich

Henning Böttcher

Joachim Leibrock

Christoph Van Amsterdam

Oliver Schadt

Chrisoph Van Amsterdam

Hartmut Greiner

Wilfried Rautenberg

Michel Brunet

Helene Crassier

Jean Jacques Zeiller

Jean Berthelon

Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R, D, E, R, p, X, E, G, Xand Z are as defined in Claim, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolyties and/or antihypertonics. They can furthermore be employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cerebral ischaemia, infarction or psychoses. 

Substituted indoles

Chromenoneindole derivatives of the formula (I), in which R, R, R, R, A and B are as defined in Claim, and pharmaceutically usable prodrugs, derivatives, solvates, stereoisomers and salts thereof, exhibit particular actions on the central nervous system, in particular 5-HT reuptake-inhibiting and 5-HT-agonistic and/or -antagonistic actions. They are distinguished by particularly high bioavailability and particularly high inhibition of 5-HT reuptake. 

Chromenoneindoles

Compounds of the formula (I), the use thereof for the preparation of a medicament for the treatment of diseases associated with the serotonin receptor and/or serotonin reuptake, in particular for the preparation of a medicament as anxiolytic, antidepressant, neuroleptic and/or antihypertonic and/or for positively influencing obsessive-compulsive disorder (OCD), sleeping disorders, tardive dyskinesia, learning disorders, age-dependent memory disorders, eating disorders, such as bulimia, and/or sexual dysfunctions. The compounds bind to the 5-HTreceptor. 

Indole derivatives as serotonin reuptake inhibitors

Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R, D, E, R, p, X, E, G, Xand Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics. They can furthermore be employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cerebral ischaemia, infarction or psychoses. 

The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above. 

Indol derivatives and their use as 5-HT ligands

Novel indole derivatives of the formula (I), in which X, Y, R, R, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HTand in some cases to the 5-HTreceptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics and for the treatment of neurodegenerative diseases 

Pyridinalkyl-aminoalkyl-IH-indole derivatives having an inhibitory action on 5-HT and serotonin reuptake as antidepressants and anxiolytics

Novel benzofuranoxyethylamines of the formula (I), in which R, R, R, R, m and n have the meanings indicated in Patent Claim (), which have a strong affinity to the 5 HTreceptors and/or 5HTreceptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics. 

Benzofuran oxyethylamines as antidepressants and anxiolytics

Novel benzofuran derivatives of the formula (I) in which R, R, X, Y, Z and m have the meanings indicated in Patent Claim, they have a strong affinity to the 5-HTreceptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics 

Benzofuran compounds and their use as antidepressants and anxiolytics

Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R, R, R, R, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases 

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Seeheim-Jugenheim, Germany

Günter Hölzemann