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1. 发明申请

WO2022180416A1 PROCESS FOR OBTAINING AVAPRITINIB AND ITS INTERMEDIATES 审中-公开
公开(公告)号：WO2022180416A1
公开(公告)日：2022-09-01
申请号：PCT/HU2022/050019
申请日：2022-02-28
申请人： EGIS GYÓGYSZERGYÁR ZRT
发明人： PORCS-MAKKAY, Márta , BERTHA, Ferenc , MOLNÁR, Enikő , NÉMETH, Gábor , HORVÁTH, Simon , SZEBELÉDI, Ildikó , BALI, Beatrix , TELLÉR, Mónika , KÁTAINÉ FADGYAS, Katalin
IPC分类号： C07D487/04
摘要： The present invention relates to process for obtaining Avapritinib of the formula (I) and its intermediates. Avapritinib, is used for treatment of gastrointestinal stromal tumors (GIST) and for tumors of stomach and intestines.

2. 发明申请

WO2022157525A1 TOPICAL FORMULATION CONTAINING MODIFIED PHOSPHOLIPID COMPOUNDS 审中-公开
公开(公告)号：WO2022157525A1
公开(公告)日：2022-07-28
申请号：PCT/HU2022/050003
申请日：2022-01-24
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： GULYÁS, Anita , MÓRICZ, Krisztina , ULEJ, Dániel , GIGLER, Gábor , PAPP, Edit , PÁLVÖLGYI, Adrienn , GACSÁLYI, István , VARGA, Zoltán , WACHA, András Ferenc , BÓTA, Attila
IPC分类号： A61K31/197 , A61P25/00
摘要： The present invention relates to a topical pharmaceutical composition comprising pregabalin and a reduced micellar phospholipid as an active ingredient, which results in a prolonged analgesic effect of pregabalin. The product can reduce neuropathic pain by at least 5 hours.

3. 发明申请

WO2018007842A1 PIMAVANSERIN SALTS USEFUL FOR THE PRODUCTION OF A PHARMACEUTICAL PREPARATION 审中-公开
标题翻译：用于制备药物制剂的PIMAVansERIN盐
公开(公告)号：WO2018007842A1
公开(公告)日：2018-01-11
申请号：PCT/HU2017/050027
申请日：2017-07-07
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： TÓTHNÉ LAURITZ, Mária , VOLK, Balázs , KÁTAINÉ FADGYAS, Katalin , VARGA, Zoltán , NAGY, Tamás , DIETRICH, Ádám Dezső , MOLNÁRNÉ SAMU, Erika , KESZTHELYI, Adrienn , RÁCZ, Norbert , SZLÁVIK, László
IPC分类号： A61K31/4468 , A61P25/00
CPC分类号： A61K31/4468 , A61P25/00
摘要： The object of the present invention relates to the formula (1) 1-(4-fluorobenzyl)-1-(1- methylpiperidin-4-yl)-3-[4-(2-methylpropoxy)benzyl]carbamide (pimavanserin) besylate, cyclamate, tosylate, benzoate and mandelate salts, as well as to their amorphous and crystalline forms, their hydrates and solvates, to the production of these salts, and to pharmaceutical preparations containing these, as well as to the therapeutic use of these salts.
摘要翻译：本发明的目的涉及式（1）1-（4-氟苄基）-1-（1-甲基哌啶-4-基）-3- [4-（2-甲基丙氧基））苄基]脲（泊马金色林）苯磺酸盐，环磺酸盐，甲苯磺酸盐，苯甲酸盐和扁桃酸盐，以及它们的无定形和结晶形式，它们的水合物和溶剂化物，以及这些盐的制备，以及含有这些盐的药物制剂，到这些盐的治疗用途。

4. 发明申请

WO2017149332A1 MIRABEGRON COCRYSTAL 审中-公开
公开(公告)号：WO2017149332A1
公开(公告)日：2017-09-08
申请号：PCT/HU2016/050044
申请日：2016-09-22
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： VOLK, Balázs , KOVÁCS, József , KÁTAINÉ FADGYAS, Katalin , VARGA, Zoltán , MRAVIK, András , VIRÁG, Attila , NAGY, Tamás , HALÁSZ, Judit , TÓTHNÉ LAURITZ, Mária , JANINÉ VAKULYA, Gabriella
IPC分类号： C07D277/40 , A61K31/426
CPC分类号： C07D277/40
摘要： The subject of the present invention is the cocrystal form of ( R) -2-(2-aminothiazol-4-yl)-4'- {2-[(2-hydroxy-2-phenyl)ethylamino]ethyl}acetamide (mirabegron) of formula (1) and halide salt of an alkaline earth metal or halide salt of a d-yield metal and its solvates, where the alkaline earth metal is preferably calcium or magnesium and the d-yield metal is preferably zinc. The more specific subject of the present invention is the cocrystal form of mirabegron of formula (2) consisting of 2 molecules of mirabegron, 1 molecule of magnesium-chloride (MgC 2 ) and 2 molecules of water (H 2 O), its preparation method, a pharmaceutical composition comprising the cocrystal of formula (2) and the therapeutical use of the latter pharmaceutical composition.
摘要翻译：本发明的主题是（R）-2-（2-氨基噻唑-4-基）-4' - {2 - [（（1）的2-（2-羟基-2-苯基）乙氨基]乙基}乙酰胺（米拉贝隆）和碱土金属的卤化物盐或d-产物金属的卤化物盐及其溶剂化物，其中碱土金属优选为钙或镁，d产率金属优选为锌。本发明更具体的主题是由2分子米拉贝隆，1分子氯化镁（MgCl 2）和2分子水（H）组成的式（2）的米拉贝隆的共晶形式其制备方法，包含式（2）共结晶的药物组合物和后一种药物组合物的治疗用途。

5. 发明申请

WO2017134476A1 METHOD FOR THE PRODUCTION OF POMALIDOMIDE 审中-公开
标题翻译：甲酰胺的生产方法
公开(公告)号：WO2017134476A1
公开(公告)日：2017-08-10
申请号：PCT/HU2017/050002
申请日：2017-01-19
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： VOLK, Balázs , KÁTAINÉ FADGYAS, Katalin , LUKÁCS, Gyula , TÓTHNÉ LAURITZ, Mária , DANCSÓ, András , KIRÁLY, Imre , PALOTAI, László , KORMÁNY, Róbert
IPC分类号： C07D401/04 , A61K31/454
CPC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.
摘要翻译：本发明的目的涉及可用作用于生产药物活性物质pomalidomide的中间体的通式20的新的一组化合物。本发明的目的还涉及一种用于生产pomalidomide的新型，成本有效的生产性方法，该方法也可以通过本发明的新型式20化合物以工业规模实施。

6. 发明申请

WO2017093773A1 NEW POLYMORPHIC AND SOLVATE FORM OF IDELALISIB 审中-公开
标题翻译：新的多晶型和溶剂型IDELALISIB
公开(公告)号：WO2017093773A1
公开(公告)日：2017-06-08
申请号：PCT/HU2016/050031
申请日：2016-07-01
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： FLORIÁN, Endréné , DETRICH, Ádám Dezső , KOVÁCS, József , LOZSI, Károly , GREGOR, Tamás , VARGA, Zoltán , SIMIG, Gyula , KÁTAINÉ FADGYAS, Katalin , VOLK, Balázs , PORCS-MAKKAY, Márta
IPC分类号： C07D473/34 , A61K31/52 , A61P35/02
CPC分类号： A61K31/52 , C07D473/34
摘要： The subject of our invention relates to a new polymorph and solvate form of idelalisib and to their production methods. The subject of the invention also relates to a pharmaceutical preparation containing the idelalisib polymorph according to the invention, as well as to the therapeutic use of the preparation.
摘要翻译：我们的发明的主题涉及idelalisib的新多晶型物和溶剂化物形式及其生产方法。本发明的主题还涉及含有根据本发明的爱德利昔布多晶型物的药物制剂，以及该制剂的治疗用途。

7. 发明申请

WO2016079549A1 PROCESS AND INTERMEDIATE FOR THE PREPARATION OF APIXABAN 审中-公开
标题翻译：制定APIXABAN的过程和中间
公开(公告)号：WO2016079549A1
公开(公告)日：2016-05-26
申请号：PCT/HU2015/050018
申请日：2015-11-18
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： NAGY, Tamas , MRAVIK, Andras , VOLK, Balazs , NEMETH, Gabor , CSONKA-KIS, Gyozo , FARAGO, Janos , SLEGEL, Peter , VARGA, Zoltan , MEZOVARI, Monika
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to a preparation process and an intermediate compound for the preparation of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H- pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban) of formula 1. Further, the invention is the cesium salt of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1- yl)phenyl]-4,5,6,7-tetrahydro-1 H -pyrazolo[3,4-c]pyridine-3-carboxylic acid of formula 4b - where M is cesium ion - and the ammonium salt of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2- oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1 H -pyrazolo[3,4-c]piridine-3-carboxylic acid of formula 4b - where M is ammonium ion.
摘要翻译：本发明涉及用于制备1-（4-甲氧基苯基）-7-氧代-6- [4-（2-氧代哌啶-1-基）苯基] -4,5,6的制备方法和中间体化合物，（4-甲氧基苯基）-7-氧代-6- [3-（4-甲氧基苯基）-7-氧代-6- [ 4-（2-氧代哌啶-1-基）苯基] -4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-3-甲酸，其中M是铯离子 - 和1-（4-甲氧基苯基）-7-氧代-6- [4-（2-氧代哌啶-1-基）苯基] -4,5,6,7-四氢-1H-吡唑并[3,3- 4-c]吡啶-3-羧酸，其中M是铵离子。

8. 发明申请

WO2015114395A9 PROCESS FOR THE PREPARATION OF VORTIOXETINE SALTS 审中-公开
标题翻译：制备VORTIOXETINE SALTS的方法
公开(公告)号：WO2015114395A9
公开(公告)日：2015-12-03
申请号：PCT/HU2015000007
申请日：2015-01-30
申请人： EGIS GYÓGYSZERGYÁR ZRT
发明人： LING ISTVÁN , JEGES GYÖRGY , KOVÁNYNÉ LAX GYÖRGYI , VOLK BALÁZS , GREGOR PÉTER , SERES JENŐ PÉTER , DANCSÓ ANDRÁS , VARGA ZOLTÁN , SZABÓ ÉVA
IPC分类号： C07D295/08 , A61K31/495 , A61P25/28
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 l-[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.
摘要翻译：本发明涉及一种制备药物活性成分的改进方法，还涉及通过所述方法制备的高纯度盐和药物组合物。更具体地说，本发明涉及一种制备具有国际非专利名称（INN）vortoxetine和化学名称1- [2-（2,4-二甲基 - 苯硫基） - 苯基] - 哌嗪的化合物的经济方法。 Vortoxetine对应于下列公式。更具体地说，本发明涉及制备式IX的高纯度维生素D（+） - 扁桃酸盐，将该盐转化为其它高纯度盐，还涉及所述盐的配制。

9. 发明申请

WO2022157524A1 TOPICAL PHARMACEUTICAL COMPOSITION CONTAINING PHOSPHOLIPIDS 审中-公开
公开(公告)号：WO2022157524A1
公开(公告)日：2022-07-28
申请号：PCT/HU2022/050002
申请日：2022-01-24
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： GULYÁS, Anita , MÓRICZ, Krisztina , ULEJ, Dániel , GIGLER, Gábor , PAPP, Edit , PÁLVÖLGYI, Adrienn , GACSÁLYI, István , VARGA, Zoltán , WACHA, András Ferenc , BÓTA, Attila
IPC分类号： A61K31/197 , A61P25/00
摘要： The present invention relates to a topical pharmaceutical composition comprising pregabalin and a reduced micellar phospholipid as an active ingredient, which results in a prolonged analgesic effect of pregabalin. The product can reduce neuropathic pain by at least 5 hours.

10. 发明申请

WO2017072543A1 PALBOCICLIB SALTS 审中-公开
公开(公告)号：WO2017072543A1
公开(公告)日：2017-05-04
申请号：PCT/HU2016/050050
申请日：2016-10-26
申请人： EGIS GYÓGYSZERGYÁR ZRT.
发明人： LUKÁCS, Gyula , MÁRVÁNYOS, Ede László , BERECZ, Gábor , HÉDER, János Levente , MILEN, Mátyás , PEREGI, Balázs , GUDOR, Róbert , VOLK, Balázs , TÓTHNÉ LAURITZ, Mária
IPC分类号： C07D401/14 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04
摘要： The subject of the invention relates to various new salts of palbociclib, furthermore to their hydrate and solvate forms, such as the palbociclib hydrogen bromide (1:1) salt, the palbociclib hydrogen bromide (1:2) dihydrate salt, the palbociclib hydrogen chloride (1:1) salt Form E, the palbociclib sulphate (2:1) dihydrate salt, the palbociclib camsylate (1:1) salt, the palbociclib napsylate (1:1) salt, the palbociclib napsylate (1:2) dihydrate salt, the palbociclib tosylate (1:1) salt, the palbociclib citrate (1:1) monohydrate salt, the palbociclib maleate (1:1) salt Form I, the palbociclib maleate (1:1) salt Form II and the palbociclib oxalate (1:1) salt. The subject of the invention also relates to the production of the above palbociclib salts, medicinal preparations containing these and the medical use of the above forms.
摘要翻译：本发明的主题涉及palbociclib的各种新盐，此外还涉及它们的水合物和溶剂合物形式，例如palbociclib溴化氢（1:1）盐，palbociclib溴化氢（1：2））二水合物盐，palbociclib氯化氢（1：1）盐形式E，palbociclib硫酸盐（2:1）二水合物盐，palbociclib樟脑磺酸盐（1:1）盐，palbociclib萘磺酸盐（1:1）盐，palbociclib 萘磺酸盐（1:2）二水合物盐，palbociclib甲苯磺酸盐（1:1）盐，palbociclib柠檬酸盐（1:1）一水合物盐，palbociclib马来酸盐（1:1）盐，palbociclib马来酸盐（1:1）盐II型和palbociclib草酸盐（1：1）盐。本发明的主题还涉及上述palbociclib盐的生产，含有这些的药物制剂以及上述形式的医学用途。

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