公开(公告)号：US11655251B2

公开(公告)日：2023-05-23

申请号：US16767057

申请日：2018-11-27

申请人： EGIS GYOGYSZERGYAR ZRT.

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：US20170114034A1

公开(公告)日：2017-04-27

申请号：US15115063

申请日：2015-01-30

申请人： EGIS GYÓGYSZERGYÁR ZRT.

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： C07D295/096 ,  C07C59/265 ,  C07C55/10 ,  C07C55/08 ,  C07C309/29 ,  C07C53/10 ,  C07C55/07 ,  C07C65/10

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.

公开(公告)号：US20210070755A1

公开(公告)日：2021-03-11

申请号：US16767057

申请日：2018-11-27

申请人： EGIS GYOGYSZERGYAR ZRT.

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.

公开(公告)号：US20150094345A1

公开(公告)日：2015-04-02

申请号：US14379382

申请日：2012-02-17

申请人： Andras Feher ,  Zsolt Zsigmond ,  György Újfalussy ,  Péter Tonkanagy ,  György Morovjan

发明人： Andras Feher ,  Zsolt Zsigmond ,  György Újfalussy ,  Péter Tonkanagy ,  György Morovjan

IPC分类号： A61K47/38 ,  A61K45/06 ,  A61K47/32 ,  A61K47/36 ,  A61K31/403 ,  A61K31/44

CPC分类号： A61K47/38 ,  A61K9/1635 ,  A61K9/1652 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4422 ,  A61K45/06 ,  A61K47/32 ,  A61K47/36 ,  A61K2300/00

摘要： The present invention is related to a pharmaceutical formulation containing ramipril with improved stability, which comprises ramipril and a desintegrant directly granulated with a binder.

摘要翻译： 本发明涉及含有具有改善的稳定性的雷米普利的药物制剂，其包含雷米普利和用粘合剂直接造粒的脱脂剂。

公开(公告)号：US20230331727A1

公开(公告)日：2023-10-19

申请号：US18110570

申请日：2023-02-16

申请人： EGIS GYOGYSZERGYAR ZRT.

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

申请人： Egis Gyogyszergyar Zrt.

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.

公开(公告)号：US09822086B2

公开(公告)日：2017-11-21

申请号：US15115063

申请日：2015-01-30

申请人： Egis Gyogyszergyar Zrt.

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.

公开(公告)号：US20170002020A1

公开(公告)日：2017-01-05

申请号：US15113083

申请日：2015-01-20

申请人： Egis Gyogyszergyar Zrt.

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。

公开(公告)号：US10023566B2

公开(公告)日：2018-07-17

申请号：US15314255

申请日：2015-05-26

申请人： EGIS GYOGYSZERGYAR ZRT

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.

公开(公告)号：US20200087269A1

公开(公告)日：2020-03-19

申请号：US16615468

申请日：2018-05-18

申请人： EGIS GYOGYSZERGYAR ZRT.

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.