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1. 发明申请

WO2019138362A1 PROCESS FOR THE PREPARATION OF 4-(4-AMINOPHENYL)MORPHOLIN-3-ONE 审中-公开
公开(公告)号：WO2019138362A1
公开(公告)日：2019-07-18
申请号：PCT/IB2019/050213
申请日：2019-01-11
申请人： RICHTER GEDEON NYRT.
发明人： SZABÓ, Tamás , NEU, József , GARADNAY, Sándor
IPC分类号： C07D265/32 , C07C231/02 , C07C51/16
摘要： The field of this invention relates to a novel process, suitable for industrial scale manufacture, for the preparation of 4-(4-aminophenyl)morpholin-3-one of Formula (I), the key intermediate of rivaroxaban according to the scheme. In the process 2-(2-chloroethoxy)ethanol of Formula (XI) is oxidized to 2-(2-chloroethoxy)- acetic acid with aqueous sodium- or calcium-hypochlorite and a catalyst. The 2-(2~ chloroethoxy)acetic acid of Formula (X) is reacted with 4-nitro-aniline of Formula (VII) with phenylboronic acid catalyst. Then the 2-(2-chloroetoxy)-N-(4-nitrophenyl)acetamide of Formula (IX) is transformed to 4-(4-nitrophenyl)morpholin-3-one of Formula (IV) in a „one- pot" procedure. The 4-(4-nitrophenyl)morpholin-3-one of Formula (IV) is hydrogenated to get 4-(4-aminophenyl)morpholin-3-one of Formula (I).

2. 发明申请

WO2018167630A1 PHARMACOLOGICALLY ACTIVE ALICYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2018167630A1
公开(公告)日：2018-09-20
申请号：PCT/IB2018/051599
申请日：2018-03-12
申请人： RICHTER GEDEON NYRT.
发明人： BORZA, István , ROMÁN, Viktor , ÉLES, János , HADADY, Zsuzsa
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P25/00
摘要： The present invention relates to new pyrazolo[l,5-a]pyrimidine derivatives of formula (I) or pharmaceutical ly acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.

3. 发明申请

WO2018015428A1 NOVEL CELL-BASED TNF-ALPHA BINDING ASSAY 审中-公开
标题翻译：新颖的基于细胞的TNF-α结合测定
公开(公告)号：WO2018015428A1
公开(公告)日：2018-01-25
申请号：PCT/EP2017/068221
申请日：2017-07-19
申请人： RICHTER GEDEON NYRT.
发明人： URBÁNYI, Zoltán , KERESZTESSY, Zsolt , BOZÓKI, Beáta , HAMBALKÓ, Szabolcs , RÁBAI, Erzsébet Mária , ZAHUCZKY, Gábor
IPC分类号： C07K14/525 , A61K38/00
CPC分类号： C07K14/525 , A61K38/00 , C07K14/70575 , C07K2319/00 , C07K2319/03 , C07K2319/70
摘要： Provided is a novel cellular assay for TNF-α binding molecules. In particular, a monoclonal mammalian cellline and its use in the assessment of the relative binding affinity and/or the complement-dependent cytotoxic (CDC) activity of a TNF-α binding molecule to a membrane- bound human TNF-α protein is described.
摘要翻译：提供了用于TNF-α结合分子的新型细胞测定法。具体而言，描述了单克隆哺乳动物细胞及其在评估TNF-α结合分子对膜结合的人TNF-α蛋白的相对结合亲和力和/或补体依赖性细胞毒性（CDC）活性中的用途。

4. 发明申请

WO2014191964A1 NEW BIS-INDOLE ALKALOIDS AS ANTICANCER DRUGS 审中-公开
标题翻译：新的双硝酸盐作为抗生素药物
公开(公告)号：WO2014191964A1
公开(公告)日：2014-12-04
申请号：PCT/IB2014/061836
申请日：2014-05-30
申请人： RICHTER GEDEON NYRT.
发明人： SZÁNTAY, Csaba , HAZAI, László , KALAUS, György , KEGLEVICH, Péter
IPC分类号： C07D519/04 , A61K31/437 , A61P35/00
CPC分类号： C07D519/04
摘要： The field of this invention relates to novel cyclopropyl derivatives of the general formula (I) representing pharmaceutically applicable Vinca Rosea type alkaloid compounds, particularly having a cytostatic effect. The invention also is concerned processes for preparing these new alkaloids and their pharmacological compositions and the use of these compounds in treatment of cancer. R stands for a methyl or a formyl group, R 1 stands for a methoxy or an amino group, R 2 represents a hydroxy or acetoxy group, R 3 stands for a hydrogen atom or a hydroxy group, R 4 represents a hydrogen atom or R3 and R4 together represent a double bond, R 5 and R 6 represent hydrogen or fluorine atoms n = 1 or 2.
摘要翻译：本发明的领域涉及代表药学上适用的长春花玫瑰型生物碱化合物的通式（I）的新型环丙基衍生物，特别是具有细胞抑制作用。本发明还涉及制备这些新生物碱及其药物组合物的方法以及这些化合物在治疗癌症中的用途。 R表示甲基或甲酰基，R1表示甲氧基或氨基，R2表示羟基或乙酰氧基，R3表示氢原子或羟基，R4表示氢原子或R3和R4表示双键，R 5和R 6表示氢或氟原子n = 1或2。

5. 发明申请

WO2014136075A1 H3 ANTAGONISTS CONTAINING PHENOXYPIPERIDINE CORE STRUCTURE 审中-公开
标题翻译： H3拮抗剂含有羟基哌啶核心结构
公开(公告)号：WO2014136075A1
公开(公告)日：2014-09-12
申请号：PCT/IB2014/059489
申请日：2014-03-06
申请人： RICHTER GEDEON NYRT.
发明人： BARTÁNÉ SZALAI, Gizella , WÁGNER, Gábor András , KISS, Béla , SCHMIDT, Éva , BALÁZS, Ottília , NAGY, Noémi
IPC分类号： C07D211/44 , C07D401/12 , A61K31/4465 , A61K31/454 , A61P25/28
CPC分类号： C07D211/46 , A61K9/0019 , A61K9/0095 , A61K9/02 , A61K9/2059 , A61K9/4866 , A61K31/27 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/473 , A61K31/55 , A61K45/06 , C07D211/44 , C07D401/12 , A61K2300/00
摘要： The present invention relates to new histamine H 3 (H 3 ) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/ or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H 3 receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor.
摘要翻译：本发明涉及通式（I）的新型组胺H 3（H 3）受体亚型选择性配体和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂合物。本发明还涉及含有这些化合物的药物组合物以及这些化合物作为治疗和/或预防需要调节H 3受体的病症的药物的用途。本发明还涵盖通式（I）的化合物与乙酰胆碱酯酶抑制剂的组合。

6. 发明申请

WO2014080341A1 NEW PROCESS FOR THE SYNTHESIS OF TRICHLOROPYRIMIDINE-AMINE DERIVATIVES 审中-公开
标题翻译：合成二氯嘧啶胺衍生物的新方法
公开(公告)号：WO2014080341A1
公开(公告)日：2014-05-30
申请号：PCT/IB2013/060264
申请日：2013-11-20
申请人： RICHTER GEDEON NYRT.
发明人： CZIBULA, László , DOBAY, László , SZAVICSKÓ, Krisztina , KISS-BARTOS, Dorottya , NAGYNÉ BAGDY, Judit
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The invention relates to a new process for the synthesis of 2-(N-methyl)-amino-4,5,6- trichloro-l,3-pyrimidine, which is more economical than the known process, as well as the new compounds synthesized as intermediates in the process: 2-(N',N'-dimethylamino- methylene)-amino-4,5,6-trichloro-l,3-pyrimidine and 2-(N-formyl)-amino-4,5,6-trichloro-l,3- pyrimidine.
摘要翻译：本发明涉及一种合成2-（N-甲基） - 氨基-4,5,6-三氯-1,3-嘧啶的新方法，其比已知方法更经济，以及新化合物在该方法中合成的中间体：2-（N'，N'-二甲基氨基 - 亚甲基） - 氨基-4,5,6-三氯-1,3-嘧啶和2-（N-甲酰基） - 氨基-4,5 ，6-三氯-1,3-嘧啶。

7. 发明申请

WO2013068774A1 THERAPEUTIC COMBINATION OF MEMANTINE AND BACLOFEN AND PHARMACEUTICAL COMPOSITION CONTAINING THEM 审中-公开
标题翻译：记忆和硼酸和含有它们的药物组合物的治疗组合
公开(公告)号：WO2013068774A1
公开(公告)日：2013-05-16
申请号：PCT/HU2012/000119
申请日：2012-11-06
申请人： RICHTER GEDEON NYRT.
发明人： KOVÁCS, Péter , KITKA, Tamás , MISNYOVSZKI, Melinda , VARGA, Balázs , FARKAS, Sándor , HORVÁTH, Csilla Mária
IPC分类号： A61K31/13 , A61K31/195 , A61P3/04
CPC分类号： A61K31/197 , A61K31/13 , A61K31/195 , A61K2300/00
摘要： The present invention relates to the combination of memantine and baclofen active ingredients, and also to the method for achieving body weight loss and thereby treating obesity and related co-morbidities by co-administration of baclofen and memantine.
摘要翻译：本发明涉及美金刚和巴氯芬活性成分的组合，也涉及通过共同给予巴氯芬和美金刚来实现体重减轻，从而治疗肥胖和相关并发症的方法。

8. 发明申请

WO2013068603A2 METHODS FOR REFOLDING G-CSF FROM INCLUSION BODIES 审中-公开
标题翻译：从包裹体反转G-CSF的方法
公开(公告)号：WO2013068603A2
公开(公告)日：2013-05-16
申请号：PCT/EP2013/055531
申请日：2013-03-18
申请人： RICHTER GEDEON NYRT.
发明人： FELFÖLDI, Ferenc , BALLAGI, Andras , BÉCSI, János
IPC分类号： C07K14/435
CPC分类号： C07K14/245 , C07K14/535
摘要： New methods for the refolding of recombinant granulocyte colony stimulating factor (G-CSF) from inclusion bodies are disclosed. The methods comprise two refolding steps. In particular, the methods comprise the solubilising of G-CSF with a solubilising agent, the oxidative refolding (first refolding step) of G-CSF in the presence of the solubilising agent and an oxidizing agent, the efficient removal of the solubilising agent, and a second refolding step to complete the folding of G-CSF in the absence of the solubilising agent. Various methods are described for the efficient removal of the solubilising agent from partially refolded G-CSF.
摘要翻译：公开了用于从包涵体重新折叠重组粒细胞集落刺激因子（G-CSF）的新方法。该方法包括两个重折叠步骤。特别地，所述方法包括用增溶剂溶解G-CSF，在增溶剂和氧化剂存在下G-CSF的氧化重折叠（第一重折叠步骤），有效除去增溶剂，以及第二次重折叠步骤以在不存在增溶剂的情况下完成G-CSF的折叠。描述了从部分重折叠的G-CSF有效去除增溶剂的各种方法。

9. 发明申请

WO2013027073A1 HISTAMINE H3 ANTAGONIST STEROIDAL CARBOXAMIDES 审中-公开
标题翻译：组胺H3 ANTAGONIST STEROIDAL CARBOXAMIDES
公开(公告)号：WO2013027073A1
公开(公告)日：2013-02-28
申请号：PCT/HU2012/000075
申请日：2012-08-17
申请人： RICHTER GEDEON NYRT. , SCHMIDT, Éva , KISS, Béla , MAHÓ, Sándor , LEDNECZKI, István , GÁBOR, Eszter , TAPOLCSÁNYI, Pál , BALÁZS, Ottília
发明人： SCHMIDT, Éva , KISS, Béla , MAHÓ, Sándor , LEDNECZKI, István , GÁBOR, Eszter , TAPOLCSÁNYI, Pál , BALÁZS, Ottília
IPC分类号： C07J41/00 , A61K31/566
CPC分类号： C07J41/0072 , C07J1/0055 , C07J1/0059 , C07J1/0077 , C07J43/003
摘要： The present invention relates to new histamine-3 (H 3 ) receptor subtype preferring ligands of formula (I) (as defined in the claims) and/or geometric isomers and/or stereoisomers and/or diastereoisomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions comprising such compounds and the use of these compounds in methods for treating or preventing of conditions which require modulation of histamine-3 (H 3 ) receptors. The invention also provides a method for manufacturing medicaments useful in the treatment or prevention of such conditions.˙
摘要翻译：本发明涉及式（I）（如权利要求中所定义）和/或几何异构体和/或立体异构体和/或非对映异构体和/或盐和/或水合物的新的组胺-3（H3）受体亚型优选配体， /或其溶剂合物。本发明还涉及包含这些化合物的药物组合物和这些化合物在治疗或预防需要调节组胺-3（H3）受体的病症的方法中的用途。本发明还提供了用于制备治疗或预防这些病症的药物的方法。

10. 发明申请

WO2012153154A1 OXETANE SUBSTITUTED THIENO PYRIMIDINONES 审中-公开
标题翻译： OXETANE取代三硝基吡啶酮
公开(公告)号：WO2012153154A1
公开(公告)日：2012-11-15
申请号：PCT/HU2012/000032
申请日：2012-05-04
申请人： RICHTER GEDEON NYRT. , ÉLES, János , BORZA, István , BEKE, Gyula , BOROS, András , SZALAI, Krisztina
发明人： ÉLES, János , BORZA, István , BEKE, Gyula , BOROS, András , SZALAI, Krisztina
IPC分类号： C07D495/04 , A61K31/519 , A61P3/00
CPC分类号： C07D495/04
摘要： The present invention provides a compound of Formula (I) or pharmaceutically acceptable salt thereof wherein is selected from the group consisting of unsubstituted aryl and heteroaryl groups and aryl and heteroaryl groups substituted with Q; Q represents fluoro, chloro, bromo, C 1-6 straight or branched alkyl, alkylthio, cyano, trihaloalkyl, trihaloalkoxy; Y represents CH or N; R is selected from a group consisting of hydrogen, C 1-6 straight or branched alkyl, C 1-6 alkoxy, trihaloalkyl, trihaloalkoxy, amino, alkylamino, dialkylamino, hydroxy cyano, acetyl, alkylthio and halo; k is independently an integer 2 or 3; n is an integer from 0 to 2 and m is an integer from 1 to 4 provided that sum of the integers m and n is equal to an integer from 2 to 4. The invention also relates to pharmaceutical compositions containing them, to processes for their preparation, new intermediate compounds thereof and to their use in the treatment and/or prophylaxis of a melanin concentrating hormone receptor 1 and optionally H3 receptor related disease or condition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中选自未取代的芳基和杂芳基，被Q取代的芳基和杂芳基; Q表示氟，氯，溴，C 1-6直链或支链烷基，烷硫基，氰基，三卤代烷基，三卤代烷氧基; Y表示CH或N; R选自氢，C 1-6直链或支链烷基，C 1-6烷氧基，三卤代烷基，三卤代烷氧基，氨基，烷基氨基，二烷基氨基，羟基氰基，乙酰基，烷硫基和卤素; k独立地为2或3的整数; n是0至2的整数，m是1至4的整数，条件是整数m和n的总和等于2至4的整数。本发明还涉及含有它们的药物组合物，用于其制备，其新的中间体化合物及其在治疗和/或预防黑色素浓缩激素受体1和任选的H3受体相关疾病或病症中的用途。

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