Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft

Merck Patent Gesellschaft MIT

Henning Bottcher

Christoph Seyfried

Klaus-Otto Minck

Hans-Heinrich Hausberg

Rudolf Gottschlich

Gerd Bartoszyk

Andreas Bathe

Bernd Helfert

Hartmut Greiner

Steffen Neuenfeld

Susanne Rudolph

Heike Kniel

Matthias Bartels

Rolf Bergmann

Helmut Prucher

Andreas Fuchs

Anton Haase

Kurt Schuster

Ulrich Heywang

Michael Casutt

Roland Martin

Jean-Jacques Berthelon

Ingeborg Stein

Michel Brunet

Jean-Jacques Zeiller

Ralf M Devant

Michael Arlt

Harry Schwartz

Hans-Peter Wolf

Marc Noblet

Joachim Marz

Gunther Holzemann

The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.

Polymorphic forms of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl) piperazine hydrochloride

D4 receptor selectivity piperazine derivatives

Benzofurans of the formula I ##STR1## and their salts in which R.sup.1, R.sup.2 and X have the meanings indicated in claim 1, are suitable as intermediates in the synthesis of medicaments and show effects on the central nervous system.

Process of making substituted benzofurans

Amino(thio)ether derivatives of formula I ##STR1## wherein R.sup.0, R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X and Z are as defined herein, and their salts, are active on the central nervous system.

Pyridyl chroman

Benzofurans

3-Indolylpiperidines of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are in each case independently of one another H, A, OH, OA, F, Cl, Br, Z, CN, CF.sub.3, COOH, CONH.sub.2, CONHA, CONA.sub.2, or COOA, or

3-indolylpiperidines

Piperidine and piperazine derivatives of the formula I ##STR1## wherein Ind is an indol-3-yl radical which is unsubstituted or mono- or polysubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2,

Piperidines and piperazines

Indole derivatives of formula I ##STR1## wherein Ind, Q and Ar are as defined herein, and their salts, are active on the central nervous system.

Indole derivatives

The invention relates to benzylidene-quinuclidinone derivatives of the formula I ##STR1## in which R.sup.1 is A;

Benzylidenequinuclidinones

Indole derivatives of the general formula I ##STR1## wherein Ind is an indol-3-yl radical which is substituted by a hydroxymethyl or COW group and can additionally be monosubstituted or disubstituted by alkyl, O-alkyl, OH, F, Cl or Br,

Indole-3-yl-A-tetrahydropyridyl or piperidyl compounds

Novel oxazolidinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Z and n have the meanings defined herein, and their salts have effects on the central nervous system, in particular calming effects.

Oxazolidinones

3-(3-Indolyl)quinuclidines for the formula I

The invention relates to a novel process for the preparation of carebastine and similar materials from ebastine or terfenadine by oxidization using microorganisms. Carebastine and similar materials are used for the treatment of allergic disorders and as antihistamines.

Process for the preparation of carebastine and similar materials

Growing community of inventors

Darmstadt, Germany

Henning Bottcher