Merck Patent Gmbh

Merck Patent Gesellschaft

Merck Patent Gesellschaft MIT Beschrankter Haftung

Christoph Van Amsterdam

Gerd Bartoszyk

Christoph Seyfried

Kai Schiemann

Timo Heinrich

Henning Böttcher

Günter Hölzemann

Joachim Leibrock

Oliver Schadt

Dieter Dorsch

Hartmut Greiner

Werner Mederski

Christos Tsaklakidis

Johannes Gleitz

Bertram Cezanne

Henning Boettcher

Wilfried Rautenberg

Henning B&ouml;ttcher

Juergen Harting

J&uuml;rgen Harting

Hanns Wurziger

Rudolf Gottschlich

Dirk Finsinger

Michel Brunet

Karl-August Ackermann

Jean Jacques Zeiller

Michael Arlt

Helmut Pr&uuml;cher

Joachim M&auml;rz

Jean Berthelon

Lisa Matzen

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

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

Novel compounds of the formula (I) in which R, D, X, W, Y and T have the meaning indicated in Patent Claim (1), e.g. (II), are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors. 

Carboxamide derivatives and their use as factor Xa inhibitors

Novel compounds of the formula (I), in which D, W, X, Y, T, m and Rhave the meaning indicated in Patent claim, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

Carboxamides

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

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 compounds of the formula (I), in which R, R, R, X and Y have the meaning indicated in Patent claimare inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors. 

Ethynyl derivatives as factor Xa inhibitors

Compound of the formula (I) in which R, Rand alk are as defined in Claim 1, are potent 5-HTantagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).

Piperazinylcarbonylquinolines and -isoquinolines

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 

Substituted benzodioxepines

Compounds of the formula (I), in which D, R, Rand n are defined in Claim, are potent 5-HTagonists and 5-HT reuptake inhibitors and are suitable for the treatment of depression, anxiety states, panic attacks, obsessive-compulsive disorders, psychiatric illnesses, cerebral infarction, cerebral ischaemia, tension states, side-effects in the treatment of high blood pressure, for the prophylaxis and therapy of cerebral illnesses, acromegaly, hypogonadism, secondary amenorrhoea, premenstrual syndrome, undesired puerperal lactation, pain, sleep disorders, narcolepsy, bipolar illnesses, mania, dementia, addiction illnesses, sexual dysfunction, eating disorders, obesity or fibromyalgia 

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Darmstadt, Germany

Christoph Van Amsterdam