Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gmbh

Merck Patent Gesellschaft

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Tioga Pharmaceuticals, Inc.

Merck Patent Gesellschaft MIT

Merck Patent Gellschaft MIT Beschrankter

Christoph Seyfried

Gerd Bartoszyk

Henning Bottcher

Hans-Heinrich Hausberg

Klaus-Otto Minck

Rudolf Gottschlich

Hartmut Greiner

Christoph Van Amsterdam

Kai Schiemann

Joachim Leibrock

Henning Böttcher

Timo Heinrich

Henning Boettcher

Günter Hölzemann

Helmut Prucher

Oliver Schadt

Andrew Barber

Jurgen Uhl

Henning B&ouml;ttcher

Karl-August Ackermann

Klaus Otto Minck

Michael Arlt

Frank Weber

Ewen Sedman

Christoph Von Amsterdam

Rolf Bergmann

Matthias Wiesner

Juergen Harting

Hermann Russ

Andreas Fuchs

Helmut Pr&uuml;cher

J&uuml;rgen Harting

Helmut Pruecher

Joachim Marz

Chrisoph Van Amsterdam

Eike Poetsch

Dieter Dorsch

Michael Wolf

Rochus Jonas

Peter Raddatz

Wilfried Rautenberg

Dirk Finsinger

Hans-Jochen Schliep

Frank Mauler

Gunter Holzemann

Michael Klockow

Herbert Nowak

Michel Brunet

Rolf Pohlke

Helene Crassier

Ralf M Devant

Jean Jacques Zeiller

Wighard Strehlow

Hans-Peter Wolf

Anton Haase

Wolf-Dietrich Weber

Helmut Muller-Calgan

Dieter Marx

Otto Saiko

Joachim M&auml;rz

Maria Devant, Legal Representative

Helmut Mueller-Calgan

Jean Berthelon

Volker Koppe

Henning Bottch

Herman Russ

Joseph Maria Martinez

Karl Ulrich B&uuml;hring

Rudlof Gottschlich

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

The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the pharmaceutical composition.

Derivatives of asimadoline with covalently bonded acids

(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

The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R, R, R, R, p, k, E, G, Z and Q are as defined in claim, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses. 

Cyclic amides

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

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

Growing community of inventors

Seeheim-Jugenheim, Germany

Christoph Seyfried