Merck Patent Gmbh

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Regeneron Pharmaceuticals, Inc.

Max-planck-gesellschaft Zur F&#xf6;rderung Der Wissenschaften E. V.

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Merck Patent Gesellschaft

Joachim Leibrock

Christoph Seyfried

Kai Schiemann

Henning Böttcher

Gerd Bartoszyk

Timo Heinrich

Günter Hölzemann

Christoph Van Amsterdam

George D Yancopoulos

Friedrich Lottspeich

Hans Thoenen

Yves-Alain Barde

Oliver Schadt

Michael Wolf

Rudolf Gottschlich

Michael Gassen

Norbert Beier

Hans-Michael Eggenweiler

Helmut Prucher

Ronald M Lindsay

Thomas Ehring

Chrisoph Van Amsterdam

David Edgar

Hans F Thoenen

Hans-Peter Buchstaller

Rochus Jonas

Pierre Schelling

Wilfried Rautenberg

Hans-Jochen Schliep

Henning Boettcher

Gunter Holzemann

Michael Klockow

Karl-August Ackermann

Helene Crassier

Andrew Barber

Peter C Maisonpierre

Harry Schwartz

Helmut Pr&uuml;cher

Izaak Den Daas

Helmut Pruecher

Christian Noe

Michael Berger

Laurie Von Melchner

Rudlof Gottschlich

Ralph Alderson

Carolyn Hyman

Magdalena Hofer

Dan Lindholm

Francisco Zafra

Karen Bailey

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), in which R, R, Q, X, Y, m and n have the meanings indicated in Claim (), are potent 5-HTantagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, such as bulimia, anorexia nervosa, of premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD). 

Piperidine derivatives

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

Compounds of the formula I in which R, R, Rand Rare as defined in Claim, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.

6H-oxazolo[4,5 e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands

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. 

Triazine derivatives of the formula (I) and physiologically acceptable salts and solvates thereof, in which R, R, A and Rare as defined in Claim, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of allergic diseases, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, autoimmune diseases, such as, for example, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumour growth or tumour metastases, sepsis, memory disorders, atherosclerosis and AIDS, furthermore for inhibiting the formation of TNF&#x3b1;. 

4-(benzylidene-amino)-3-(methylsulfanyl)-4h-(1,2,4)triazin-5-one derivatives having a PDE-IV inhibiting and TNF-antagonistic effect for the treatment of cardiac diseases and allergies

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

This invention relates to compounds of the formula (I) in which R, R, R, X and Q are as defined above and their use as PDE IV inhibitors.

Benzoylpyridazines

Compounds of the formula I in which R, R, Rand Rare as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity 

6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands

Compounds of the formula (I) in which R, R, Rand Rare as defined in Claim, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, pre-menstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence. Strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity. 

Dihydroimidazo[4,5-e]indole and 7h-pyrrolo[3,2-f]quinoxaline derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands

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

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Pfungstadt, Germany

Joachim Leibrock