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公开(公告)号：US11655251B2
公开(公告)日：2023-05-23
申请号：US16767057
申请日：2018-11-27
发明人： Gábor Berecz , Bálint Nyulasi , Mátyás Milen , Gyula Simig , András Mravik , Gábor Németh , Adrienn Keszthelyi , Beatrix Bali , Balázs Volk , László Szlávik , Zoltán Varga , Daniel Ulej
IPC分类号： C07D471/16 , C07B57/00 , C07C235/74 , C07C309/30 , C07C309/35
CPC分类号： C07D471/16 , C07B57/00 , C07C235/74 , C07C309/30 , C07C309/35 , C07B2200/07 , C07B2200/13
摘要： Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS
is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X=I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.-
公开(公告)号：US10023566B2
公开(公告)日：2018-07-17
申请号：US15314255
申请日：2015-05-26
发明人： Ede Laszlo Marvanyos , Attila Virag , Tamas Gregor , Balazs Volk , Maria Tothne Lauritz , Laszlo Pongo , Balazs Peregi , Gyula Lukacs , Zoltan Varga , Andras Dancso
IPC分类号： C07D417/12
摘要： The invention relates to normal or acidic salts of dasatinib and the hydrate and solvate forms thereof. More specifically the invention concerns: dasatinib cyclamic acid salt, dasatinib cyclamic acid (1:1) salt Form I, dasatinib cyclamic acid (1:1) salt Form II, dasatinib hydrogen bromide (1:2) salt, dasatinib methane sulfonic acid (1:2) salt, dasatinib p-toluenesulfonic acid (1:1) dihydrate salt, anhydrous dasatinib p-toluenesulfonic acid (1:1) salt Form I, anhydrous dasatinib p-toluenesulfonic acid (1:1) salt Form II, dasatinib p-toluenesulfonic acid (1:1) salt methanol solvate. Moreover the invention relates process for preparing dasatinib salts, pharmaceutical compositions comprising thereof and the use of dasatinib salts the treatment of cancer.
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公开(公告)号：US20210070755A1
公开(公告)日：2021-03-11
申请号：US16767057
申请日：2018-11-27
发明人： Gábor BERECZ , Bálint NYULASI , Mátyás MILEN , Gyula SIMIG , András MRAVIK , Gábor NÉMETH , Adrienn KESZTHELYI , Beatrix BALI , Balázs VOLK , László SZLÁVIK , Zoltán VARGA , Daniel ULEJ
IPC分类号： C07D471/16 , C07B57/00 , C07C309/35 , C07C309/30 , C07C235/74
摘要： Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X═I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.
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公开(公告)号：US20230331727A1
公开(公告)日：2023-10-19
申请号：US18110570
申请日：2023-02-16
发明人： Gábor BERECZ , Bálint NYULASI , Mátyás MILEN , Gyula SIMIG , András MRAVIK , Gábor NÉMETH , Adrienn KESZTHELYI , Beatrix BALI , Balázs VOLK , László SZLÁVIK , Zoltán VARGA , Daniel ULEJ
IPC分类号： C07D471/16 , C07B57/00 , C07C235/74 , C07C309/30 , C07C309/35
CPC分类号： C07D471/16 , C07B57/00 , C07C235/74 , C07C309/30 , C07C309/35 , C07B2200/07 , C07B2200/13
摘要： Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS
is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X = I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.-
公开(公告)号：US09926332B2
公开(公告)日：2018-03-27
申请号：US15113083
申请日：2015-01-20
发明人： Agnes Kenez , Ferenc Bertha , Jozsef Barkoczy , Ferenc Antoni , Istvan Gacsalyi , Balazs Mihalik , Gabor Gigler , Krisztina Moricz , Gabor Nemeth , Agnes Angyalne Pataki , Gabor Laszlo Kapus , Adrienn Palvolgyi , Istvan Ling , Janos Petho , Gyula Simig , Balazs Volk , Lax Gyorgyi Kovanyine , Andras Dancso
IPC分类号： A61K31/551 , C07D498/04 , C07D265/36 , C07D413/06
CPC分类号： C07D498/04 , C07D265/36 , C07D413/06
摘要： Compounds of formula (I) having a selective dual action on the central GABAergic system, and a process for their preparation and to pharmaceutical compositions containing them.
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公开(公告)号：US09822086B2
公开(公告)日：2017-11-21
申请号：US15115063
申请日：2015-01-30
发明人： Istvan Ling , Gyorgy Jeges , Gyorgyi Kovanyine Lax , Balazs Volk , Peter Gregor , Jeno Peter Seres , Andras Dancso , Zoltan Varga , Eva Szabo
IPC分类号： C07D295/08 , A61K31/495 , C07D295/096 , C07C55/07 , C07C59/265 , C07C65/10 , C07C55/08 , C07C309/29 , C07C53/10 , C07C55/10
CPC分类号： C07D295/096 , C07B2200/13 , C07C53/10 , C07C55/07 , C07C55/08 , C07C55/10 , C07C59/265 , C07C65/10 , C07C309/29 , C07D295/08
摘要： The invention relates to an improved process for the preparation of pharmaceutical active ingredients and also to high purity salts and pharmaceutical compositions prepared by said process. More particularly the invention relates to an economical process for the preparation of the compound having the international non-proprietary name (INN) vortioxetine and the chemical nomenclature 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine. Vortioxetine corresponds to the following Formula Still more particularly the invention relates to the preparation of high purity vortioxetine L-(+)-mandelate salt of the Formula IX, the conversion of this salt into other highly pure salts and also to the formulation of said salts.
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7.发明申请NEW DIHYDRO-OXAZINOBENZODIAZEPINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITONS CONTAINING THEM 有权新型二氢氧杂环己烷酮化合物，其制备方法和含有它们的药物组合物公开(公告)号：US20170002020A1
公开(公告)日：2017-01-05
申请号：US15113083
申请日：2015-01-20
发明人： Agnes KENEZ , Ferenc BERTHA , Jozsef BARKOCZY , Ferenc ANTONI , Istvan GACSALYI , Balazs MIHALIK , Gabor GIGLER , Krisztina MORICZ , Gabor NEMETH , Agnes ANGYALNE PATAKI , Gabor Laszlo KAPUS , Adrienn PALVOLGYI , Istvan LING , Janos PETHO , Gyula SIMIG , Balazs VOLK , Lax Gyorgyi KOVANYINE , Andras DANCSO
IPC分类号： C07D498/04 , C07D413/06 , C07D265/36
CPC分类号： C07D498/04 , C07D265/36 , C07D413/06
摘要： Compounds of formula (I) having a selective dual action on the central GABAergic system, and a process for their preparation and to pharmaceutical compositions containing them.
摘要翻译： 对中枢GABA能系统具有选择性双重作用，以及其制备方法和含有它们的药物组合物。
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公开(公告)号：US20200087269A1
公开(公告)日：2020-03-19
申请号：US16615468
申请日：2018-05-18
发明人： Marta PORCS-MAKKAY , Gyula SIMIG , Eniko MOLNAR , Janos PETHO , Balazs VOLK , Laszlo SZLAVIK , Eva SZABO , Judit HALASZ
IPC分类号： C07D271/06
摘要： The present invention relates a new process for the preparation of ozanimod of the formula and acid addition salts, via new intermediates and a new polimop form of ozanimod base.
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公开(公告)号：US20190040037A1
公开(公告)日：2019-02-07
申请号：US16075371
申请日：2017-01-19
发明人： Balazs VOLK , Katalin KATAINE FADGYAS , Gyula LUKACS , Maria TOTHNE LAURITZ , Andras DANCSO , Imre KIRALY , Laszlo PALOTAI , Robert KORMANY
IPC分类号： C07D401/04 , C07D209/48
摘要： The object of the invention relates to a novel group of compounds of general formula 20 that may be used as an intermediate for the production of the pharmaceutical active substance pomalidomide. The object of the invention also relates to a novel, cost-effective, productive method for the production of pomalidomide that can also be implemented on industrial scales via the novel compound of formula 20 according to the invention.
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公开(公告)号：US20170183334A1
公开(公告)日：2017-06-29
申请号：US15314255
申请日：2015-05-26
发明人： Ede Laszlo MARVANYOS , Attila VIRAG , Tamas GREGOR , Balazs VOLK , Maria TOTHNE LAURITZ , Laszlo PONGO , Balazs PEREGI , Gyula LUKACS , Zoltan VARGA , Andras DANCSO
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , C07B2200/13
摘要： The invention relates to normal or acidic salts of dasatinib and the hydrate and solvate forms thereof. More specifically the invention concerns: dasatinib cyclamic acid salt, dasatinib cyclamic acid (1:1) salt Form I, dasatinib cyclamic acid (1:1) salt Form II, dasatinib hydrogen bromide (1:2) salt, dasatinib methane sulfonic acid (1:2) salt, dasatinib p-toluenesulfonic acid (1:1) dihydrate salt, anhydrous dasatinib p-toluenesulfonic acid (1:1) salt Form I, anhydrous dasatinib p-toluenesulfonic acid (1:1) salt Form II, dasatinib p-toluenesulfonic acid (1:1) salt methanol solvate. Moreover the invention relates process for preparing dasatinib salts, pharmaceutical compositions comprising thereof and the use of dasatinib salts the treatment of cancer.
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