Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Merck Patent Gesellschaft MIT

Gerd Bartoszyk

Christoph Seyfried

Hartmut Greiner

Christoph Van Amsterdam

Kai Schiemann

Joachim Leibrock

Henning Böttcher

Timo Heinrich

Rudolf Gottschlich

Günter Hölzemann

Henning Boettcher

Henning B&ouml;ttcher

Oliver Schadt

Henning Bottcher

Helmut Prucher

Andrew Barber

Karl-August Ackermann

Michael Arlt

Ewen Sedman

Juergen Harting

Frank Weber

Helmut Pr&uuml;cher

Christoph Von Amsterdam

Dieter Dorsch

Wilfried Rautenberg

Michel Brunet

Ralf M Devant

Hermann Russ

J&uuml;rgen Harting

Joachim Marz

Chrisoph Van Amsterdam

Bertram Cezanne

Dirk Finsinger

Frank Mauler

Jean-Jacques Berthelon

Helene Crassier

Jean-Jacques Zeiller

Jean Jacques Zeiller

Gerhard Barnickel

Anton Haase

Marc Noblet

Joachim M&auml;rz

Maria Devant, Legal Representative

Jean Berthelon

Lisa Matzen

Herman Russ

Karl Ulrich B&uuml;hring

Andrew Barbar

Manfred Stohrer

Jürgen Harting

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) and salts and solvates thereof, in which X, R, R, R, R, Rand Rhave the meanings indicated in Claim, are suitable as ligands of 5 HT receptors. 

Pyrazole compounds

(R)-(&#x2212;)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof is useful for treatment of adverse effects in treating Parkinson's disease.

Use of(R)-(&#x2212;) -2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane and its physiologically acceptable salts

(R/S)-(&#x2212;/+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof and/or (S)-(+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof are used for the manufacture of a medicament for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders.

Use of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane and its physiologically acceptable salts

Compounds of formula (I) and salts thereof, in which the following definitions apply: X is N or CH; Ris H, A, Hal, (CH)Het, (CH)Ar, C-cycloalkyl, CF, NO, CN, C(NH)(OH), or OCF; Ris (CH)Het, (CH)Ar, or C-cycloalkyl, or CF; Rand Rdenote H or an organic radical. Compounds of formula (I) are useful as ligands of 5-HT receptors and useful in the treatment of disorders such as anxiety, depression, obsessive-compulsive disorder and pain. 

Substituted pyrazole compounds

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

1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.

Use of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and its physiologically acceptable salts

Compounds of formula I in which R has a meaning as indicated in claim, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics. 

Use of substituted aminomethyl chromans

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. 

Compounds of the formula (I) and salts and solvates thereof, in which X, R, R, Rand Q have the meanings indicated in Claim, are suitable as ligands of 5 HT receptors; as well as intermediate compounds of the formula (IA). 

1,3,4-Substituted pyrazoles as 5-HT receptor antagonists for the treatment of psychoses and neurological disorders

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

The present invention relates to the use of compounds being combined selective serotonin (5-HT) reuptake inhibitors (SSRIs) and 5-HTreceptor agonists, in particular of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof or 3-{4-[4-(4-cyano-phenyl)-piperazin-1-yl]-butyl}-1H-indole-5-carbonitrile or a physiologically acceptable salt thereof, for the manufacture of a medicament for the treatment of chronic pain disorders or in treating other conditions where there is hyper-sensitization to painful signals, hyperalgesia, allodynia, enhanced pain perception, and enhanced memory of pain, as well as for the treatment of irritable bowel syndrome (IBS).

[object Object]

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

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Weiterstadt, Germany

Gerd Bartoszyk