Richter Gedeon Vegyeszeti Gyar Rt

Richter Gedeon Nyrt.

Janos Galambos

Tibor Keve

Laszlo Szporny

Bela Kiss

Egon Karpati

Eva Againe Csongor

Bela Zsadon

Laszlo Czibula

Gyorgy Fekete

Katalin Nogradi

Eva Palosi

Bela Stefko

Erzsebet Lapis

Ferenc Trischler

Istvan Laszlovszky

Erik Bogsch

Zsolt Szombathelyi

Arpad Kiraly

Maria Zajer Nee Balazs

Gabor Megyeri

Ferenc Sebok

Balint Juhasz

Istvan Gyertyan

Katalin Saghy

Dora Groo

Judit Laszy

Csaba Lorincz

Lilla Forgach

Gyongyver Kiraly Nee Soos

Bela Rosdy

Istvan Vago

Csaba Szantay

Lajos Szabo

Gyorgy Kalaus

Lajos Dancsi

Aniko Gere

Katalin Csomor

Adam Sarkadi

Sandor Szabo

Eva Schmidt

Lajos Kovacs

Lilla Forgacs

Tibor Acs

Adam Demeter

Monika Vastag

Zsolt Szentirmay

Maria Szilasi

Amrita Agnes Bobok

Anna Kassai Nee Zieger

Gyorgyi Ignaczné Szendrei

Ferenc Vezekenyi

Anna Kassainee Zieger

Gyongyver Soos

Margit Barta Nee Bukovecz

Klara Horvath Nee Otta

Bala Stefko

Anna Kassi Nee Zieger

Mih,acu/a/ Ly Bodo

Viktoria Bolya Nee Kassay

Emilia Repasi, Nee Balogh

Margit Barta N/e/ E Bukovecz

Krisztina Gal

Csaba Weber

Ibolya Prauda

Gabor Wagner

Ferenc Sebök

Sandorné Balint

Ferencné Kassai

Gyoergy Domany

Krisztina Gál

Gabor Andras Wagner

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 new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in treatment and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.

Sulfonyl-quinoline derivatives

A process for preparing cabergoline (I) from ergoline-8&#x3b2;-carboxylic acid ester (XIII) comprising the following steps. (XIII), (XVI), (XVII), (XVIII), (XIX), (I). The present case also relates to the intermediates (XVI), (XVII), (XVIII) and (XIX) as well as the polymorphic amorphous form of Cabergoline (I) and the production thereof. 

Process for the preparation of cabergoline

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. 

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The invention relates to novel 15-nitro-2.beta.,3.beta.-dihydro- and 15-nitro-2.beta.,3.beta.,6,7-tetrahydrotabersonine derivatives of the formula (I), ##STR1## wherein R.sup.1 stands for hydrogen;

15-nitro-2.beta., 3.beta.-dihydro- and

The invention relates to a new process for the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) ##STR1## and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) ##STR2## and/or 17,18-dehydro-epivincamine of formula (IIb) ##STR3## by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.

Process for the preparation of an apovincaminol derivative

The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts. The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt. The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.

2-chloronicergoline having antihypoxic activity

The invention relates to a novel process for the preparation of 2-bromo-.alpha.-ergocryptine and its acid addition salt by brominating .alpha.-ergocryptine in such a way that the bromination is carried out at room temperature by using a dimethylsulphoxide-hydrogen bromide mixture containing no more 0.02% of water and, if desired, converting the thus-obtained 2-bromo-.alpha.-ergocryptine to an acid addition salt in a known manner.

Process for the preparation of 2-bromo-.alpha.-ergocryptine

The invention relates to pharmaceutical compositions with a neuroleptic action as well as to a process for preparing these compositions. The active ingredients of the compositions of the invention are 2-halo-6-methyl-9-ergolene derivatives of the formula (I), ##STR1## wherein X represents a chlorine, bromine or iodine atom as well as their acid addition salts. The compositions of the invention contain an effective dose of compound of the general formula (I) or an acid addition salt thereof.

Pharmaceutical compositions with a neuroleptic action and process for

The invention relates to new apovincaminol derivatives of the formula /I/ ##STR1## wherein R.sub.1 is hydrogen, nitro or halogen,

Apovincaminol derivative

The invention relates to a new process for the preparation of alkoxyvincaminic acid esters of the formula (I) ##STR1## and/or alkoxyapovincaminic acid esters of the formula (II) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently stand for alkyl groups having from one to 6 carbon atoms. The compounds of the formulae (I) and (II) are pharmaceutically active, thus some of them show psychostimulant activity.

1.alpha.-Ethyl-1.beta.-(2'-alkoxy

The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.

Polycyclic compounds containing a double bond in the D-ring

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Budapest, Hungary

Janos Galambos