Patents by Inventor Janos Galambos
Janos Galambos has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8569496Abstract: 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}-carbType: GrantFiled: December 17, 2009Date of Patent: October 29, 2013Assignee: Richter Gedeon Nyrt.Inventors: Laszlo Czibula, Eva Againe Csongor, Katalin Nogradi, Balint Juhasz, Ferenc Sebok, Janos Galambos, Istvan Vago
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Patent number: 8569497Abstract: 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° 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.Type: GrantFiled: December 18, 2009Date of Patent: October 29, 2013Assignee: Richter Gedeon Nyrt.Inventors: Eva Againe Csongor, Laszlo Czibula, Ferenc Sebok, Balint Juhasz, Janos Galambos, Katalin Nogradi
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Patent number: 8569498Abstract: The invention relates to a new process for the preparation of compounds of general formula (I) wherein R1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in aType: GrantFiled: December 18, 2009Date of Patent: October 29, 2013Assignee: Richter Gedeon Nyrt.Inventors: Laszlo Czibula, Balint Juhasz, Eva Againe Csongor, Ferenc Sebok, Janos Galambos, Katalin Nogradi
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Patent number: 8063220Abstract: 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.Type: GrantFiled: June 23, 2008Date of Patent: November 22, 2011Assignee: Richter Gedeon Nyrt.Inventors: Janos Galambos, Gyorgy Keseru, Krisztina Gal, Monika Vastag, Amrita Agnes Bobok, Csaba Weber, Ibolya Prauda, Gabor Wagner
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Publication number: 20110275816Abstract: 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 aluminium 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]-cyclohexylType: ApplicationFiled: December 17, 2009Publication date: November 10, 2011Inventors: Laszlo Czibula, Eva Againe Csongor, Katalin Nogradi, Balint Juhasz, Ferenc Sebok, Janos Galambos, Istvan Vago
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Publication number: 20110275804Abstract: The invention relates to a new process for the preparation of compounds of general formula (I) wherein R1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in anType: ApplicationFiled: December 18, 2009Publication date: November 10, 2011Inventors: Laszlo Czibula, Balint Juhasz, Eva Againe Csongor, Ferenc Sebok, Janos Galambos, Katalin Nogradi
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Publication number: 20110269959Abstract: 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° 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.Type: ApplicationFiled: December 18, 2009Publication date: November 3, 2011Inventors: Eva Againe Csongor, Laszlo Czibula, Ferenc Sebok, Balint Juhasz, Janos Galambos, Katalin Nogradi
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Patent number: 7858791Abstract: A process for preparing cabergoline (I) from ergoline-8?-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.Type: GrantFiled: March 2, 2005Date of Patent: December 28, 2010Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Janos Galambos, Laszlo Czibula, Ferenc Sebök, Sandorné Balint, Ferencné Kassai, Gyorgyi Ignaczné Szendrei, Adam Demeter
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Publication number: 20100240640Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may 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.Type: ApplicationFiled: May 12, 2010Publication date: September 23, 2010Applicant: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Patent number: 7737142Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may 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.Type: GrantFiled: January 20, 2006Date of Patent: June 15, 2010Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Patent number: 7705003Abstract: The present invention relates to new dopamine D3 and D2 and serotonin 5-HT1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula —NR1R2, wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R1 and R2 form 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-HT1A receptors.Type: GrantFiled: February 2, 2006Date of Patent: April 27, 2010Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Eva Againe Csongor, Janos Galambos, Istvan Gyertyan, Bela Kiss, Katalin Saghy, Eva Schmidt, Gyoergy Domany
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Publication number: 20090042934Abstract: 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.Type: ApplicationFiled: June 23, 2008Publication date: February 12, 2009Inventors: Janos Galambos, Gyorgy Keseru, Krisztina Gal, Monika Vastag, Amrita Agnes Bobok, Csaba Weber, Ibolya Prauda, Gabor Wagner
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Patent number: 7473692Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).Type: GrantFiled: September 25, 2002Date of Patent: January 6, 2009Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: János Galambos, Katalin Nógrádi, Éva Ágainé Csongor, György Miklós Keserü, István Vágó, György Domány, Béla Kiss, István Gyertyán, István Laszlovszky, Judit Laszy
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Publication number: 20080103140Abstract: The present invention relates to new dopamine D3 and D2 and serotonin 5-HT1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula —NR1R2, wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R1 and R2 form 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-HT1A receptors.Type: ApplicationFiled: February 2, 2006Publication date: May 1, 2008Applicant: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Gyorgy Domany, Janos Galambos, Istvan Gyertyan, Bela Kiss, Katalin Saghy, Eva Schmidt
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Publication number: 20070293677Abstract: A process for preparing cabergoline (I) from ergoline-8?-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.Type: ApplicationFiled: March 2, 2005Publication date: December 20, 2007Inventors: Janos Galambos, Laszio Czibula, Ferenc Sebok, Sandorne Balint, Ferencne Kassai, Gyorgyi Ignaczne Szendrei, Adam Demeter
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Publication number: 20060229297Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may 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.Type: ApplicationFiled: January 20, 2006Publication date: October 12, 2006Applicant: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Publication number: 20050107397Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their us in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's desases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).Type: ApplicationFiled: September 25, 2002Publication date: May 19, 2005Inventors: Janos Galambos, Katalin Nogradi, Eva Againe Csongor, Gyorgy Keseru, Istvan Vago, Gyorgy Domany, Bela Kiss, Irstvan Gyertyan, Istvan Laszlovszky, Judit Laszy
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Patent number: 5204355Abstract: 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;R.sup.2 stands for hydrogen or a C.sub.1-6 alkyl group; and the symbolrepresents a single or double bond as well as their salts.The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for the preparation of the above compounds of formula (I) and of the pharmaceutical compositions.The compounds of formula (I) exert a reducing or inhibitory effect on cerebral edema and show antihypoxic properties. Thus, they are useful for the prevention or treatment of brain injuries of various origin induced by hypoxia of the brain.Type: GrantFiled: December 12, 1991Date of Patent: April 20, 1993Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Bela Zsadon, Margit Barta n/e/ e Bukovecz, Maria Szilasi, Tibor Keve, Janos Galambos, Viktoria Bolya nee Kassay, Sandor Szabo, Emilia Repasi, nee Balogh, Laszlo Szporny, Bela Kiss, Egon Karpati, Eva Palosi, Zsolt Szombathelyi, Adam Sarkadi, Erzsebet Lapis, Aniko Gere, Mih,acu/a/ ly Bodo, Katalin Csomor, Judit Laszy, Zsolt Szentirmay
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Patent number: 4758666Abstract: 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.Type: GrantFiled: May 9, 1986Date of Patent: July 19, 1988Assignee: Richter Gedeon Vegyeszeti Gyar R.T.Inventors: Janos Galambos, Tibor Keve, Bela Stefko, Gyorgy Fekete, Bela Zsadon, Anna Kassai nee Zieger, Klara Horvath nee Otta
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Patent number: 4753949Abstract: 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.Type: GrantFiled: June 23, 1986Date of Patent: June 28, 1988Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Gabor Megyeri, Tibor Keve, Bala Stefko, Erik Bogsch, Janos Galambos, Anna Kassi nee Zieger, Ferenc Trischler, Eva Palosi, Dora Groo, Egon Karpati, Zsolt Szombathelyi, Laszlo Szporny, Bela Kiss, Istvan Laszlovszky, Erzsebet Lapis