Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft

Merck Patent Gellschaft MIT Beschrankter

Henning Boettcher

Christoph Seyfried

Gerd Bartoszyk

Hartmut Greiner

Christoph Van Amsterdam

Juergen Harting

Ewen Sedman

Christoph Von Amsterdam

Dieter Dorsch

Andreas Bathe

Wilfried Rautenberg

Steffen Emmert

Timo Heinrich

Joachim Leibrock

Rudolf Gottschlich

Bernd Helfert

Andrew Barber

Helene Crassier

Michael Arlt

Helmut Pruecher

Uwe Eckert

Lisa Matzen

Joseph Maria Martinez

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

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

1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof, 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.

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

The present invention relates to a process for the preparation of (3-cyano-1H-indol-7-yl)[4-(4-fluorophenethyl)piperazin-1-yl]-methanone and salts thereof, characterised in that an indole ester of the formula II in which R is as defined in Claim 1, is converter into 3-cyano-1H-indole-7-carboxylic acid via steps (1) to (4) according to Claim 1, and this is reacted with 1-[2-(4-fluorophenyl)ethyl]piperazine of salts thereof to give the product.

Process for the preparation of (3-cyano-1h-indol-7-yl) (4-(4-fluorophenethyl) piperazin-1-yl)-methanone and salts thereof

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 

Substituted benzofuran-2-carboxamides derivatives

The invention relates to compounds of formula (I) wherein R, R, Rand Rhave the meaning given in Claim. Said compounds are potent 5-HT-antagonists and are suitable for the treatment of psychosis, schizophrenia, depression, neurological disorders, memory disorders. Parkinson's disease, amytrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, e.g. nervous bulimia and anorexia and premenstrual syndrome and/or for positively influencing compulsive behaviors (obsessive-compulsive disorder, OCD). 

N-(indolecarbonyl) piperazine derivatives

The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I:where

Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals

1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof, 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 salts is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.

Compounds of the formula Iin which R, R, Rand Rhave the meanings indicated in claim, are potent 5-HTantagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).

N-(indolcarbonyl-)piperazine derivatives

Process for the preparation of 5-(1-piperazinyl)benzofuran-2-carboxamide in which, as intermediate step, 5-bromosalicylaldehyde or one of its derivatives is reacted in a transition metal-catalysed amination with R -piperazine, in which R is as defined in claim

Method for producing 5-(1-piperazinyl)-benzofuran-2-carboxamide by transition metal-catalyzed amination

Amide and urea derivatives as 5-HT reuptake inhibitors and as 5-HT1B/1D ligands

The invention relates to piperidine derivatives of the formula I

3-Benzylpiperidine

Piperazinylbenzodioxane derivatives of formula I ##STR1## wherein B is an indol-3-yl or benzimidazol-1-yl radical which is unsubstituted or monosubstituted by CN, CO--R.sup.1, C.sub.n H.sub.2n --R.sup.1, Hal, OH, OA, O--C.sub.n H.sub.2n --CO--R.sup.1, or NHR.sup.2, and Q is C.sub.n H.sub.2n, or a physiologically acceptable salt thereof. The derivatives are active in the central nervous system, especially as serotonin agonists and antagonists.

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Darmstadt, Germany

Henning Boettcher