Richter Gedeon Nyrt.

Richter Gedeon Vegyeszeti Gyar Rt

Eva Againe Csongor

Bela Kiss

Istvan Gyertyan

Janos Galambos

Gyorgy Domany

Laszlo Czibula

Katalin Saghy

Katalin Nogradi

Eva Schmidt

Ferenc Sebok

Judit Laszy

Balint Juhasz

Kalman Harsanyi

Bela Hegedus

Sandor Farkas

Gizella Bartane Szalai

Istvan Vago

Andras Rado

Zsolt Komlodi

Janos Kreidl

Gyorgy Fekete

Istvan Laszlovszky

Lajos Toldy

Tibor Balogh

Endre Kasztreiner

Jozsef Reiter

Tibor Lang

Janos Borvendeg

Maria Farkas Nee Kirjak

Margit Bidlo Nee Igloy

Ida Deutsch Nee Juhasz

Ferenc Morasz

Bela Benke

Hajnalka V Petho

Arpad Lazar

Béla Kiss

Istvan Greiner

István Laszlovszky

János Galambos

Gyoergy Domany

Tibor Somogyi

Norbert Antal Kirschner

Oszkar Fuchs

István Vago

István Gyertyan

György Miklos Keseru

The present invention relates to new dopamine Dand Dligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.

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The present invention relates to metabolites of(thio)-carbamoyl cyclohexane derivatives, particularly, metabolites of trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing the same and to their use in the treatment and/or prevention of a conditions which requires modulation of dopamine receptors.

Metabolites of (thio) carbamoyl-cyclohexane derivatives

The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminum trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester;d) heating trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester obtained to a temperature between 40-100&#xb0; C. in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate.

Piperazine salt and a process for the preparation thereof

The invention relates to a new process for the preparation of compounds of general formula (I) wherein Rand Rrepresent independently hydrogen or 

Process for the preparation of piperazine compounds and hydrochloride salts thereof

The invention relates to a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of general formula (I) by reacting the compound of formula (III) with a carbamoylchloride of general formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100&#xb0; C. in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.

Process for the preparation of piperazine derivatives

The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.

The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein Rand Rrepresent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or Rand Rmay form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.

(Thio) carbamoyl-cyclohexane derivatives as D3/D2 receptor antagonists

The present invention relates to new dopamine Dand Dand serotonin 5-HTreceptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula &#x2014;NRR, wherein Rand Rrepresent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or Rand Rform with the adjacent nitrogen atom and optionally with further heteroatom(s) a heterocyclic ring; m is an integer of 0 to 1; n is an integer of 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine and/or 5-HTreceptors. 

The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne monohydrate.

Cimetidine monohydrate

The invention relates to a new crystal modification of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne (cimetidine), a histamine H-2 receptor antagonist having the Formula (I) ##STR1## as well as to a process for preparing same. In the description, this new modification is named N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N'-cyanoguanidi ne Z (cimetidine Z).

Cimetidine Z, a new crystal modification of cimetidine

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Budapest, Hungary

Eva Againe Csongor