专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明公开

EP4183450A1 METHOD FOR PREPARING A HYDRATED FORM OF PERINDOPRIL L-ARGININE 审中-实审
公开(公告)号：EP4183450A1
公开(公告)日：2023-05-24
申请号：EP21215144.3
申请日：2021-12-16
申请人： Zupet, Rok
发明人： Zupet, Rok , Zupancic, Blaz
IPC分类号： A61P9/12 , C07D209/42
摘要： The present invention relates to a novel process for preparing a hydrated form of perindopril L-arginine with improved process properties.
In the process for the production of a hydrated form of perindopril L-arginine according to the invention, by precisely controlling and regulating the amount of water in the crystallisation solution comprising perindopril L-arginine, the isolation properties of the suspension of the hydrated form of perindopril L-arginine formed in the process are improved, i.e. the stability time of the resulting suspension is prolonged, the filtration time of the suspension is shortened and the amount of solvent and antisolvent in the final product - an isolated wet filter cake of the hydrated form of perindopril L-arginine - is reduced, wherein the wet filter cake has a high dry residue value after drying. The process according to the invention has a high molar yield and the resulting hydrated form of perindopril L-arginine has high chromatographic purity and adequate stability under storage conditions at room temperature.
The process according to the invention is suitable for use on an industrial scale and provides an efficient, economical and reproducible process for the production of a hydrated form of perindopril L-arginine using materials that can be regenerated with a minimal environmental footprint.

2. 发明申请

WO2011012322A3 SYNTHESIS AND USE OF VILDAGLIPTIN FOR THE PREPARATION OF PHARMACEUTICAL DOSAGE FORMS 审中-公开
标题翻译：维拉胶的合成和用途，用于制备药物剂型
公开(公告)号：WO2011012322A3
公开(公告)日：2011-06-30
申请号：PCT/EP2010004689
申请日：2010-07-30
申请人： KRKA D D NOVO MESTO , ZUPET ROK , SMODIS JANEZ , STROPNIK TADEJ , ANDERLUH MARKO , VRBINC MIHA , VRECER FRANC , PECAVAR ANICA , KUKEC SIMON
发明人： ZUPET ROK , SMODIS JANEZ , STROPNIK TADEJ , ANDERLUH MARKO , VRBINC MIHA , VRECER FRANC , PECAVAR ANICA , KUKEC SIMON
IPC分类号： C07D207/16 , A61K9/16 , A61K31/4015
CPC分类号： C07D207/16
摘要： The present invention relates the synthesis of vildagliptin in the presence of phase transfer catalysts; as well as the use of vildagliptin or its pharmaceutically acceptable salts for the preparation of solid oral dosage forms.
摘要翻译：本发明涉及在相转移催化剂存在下维格列汀的合成; 以及使用维格列汀或其药学上可接受的盐来制备固体口服剂型。

3. 发明申请

WO2011061292A1 A PROCESS FOR A PREPARATION OF MARBOFLOXACIN AND INTERMEDIATE THEREOF 审中-公开
标题翻译：一种制备马可氟菌素及其中间体的方法
公开(公告)号：WO2011061292A1
公开(公告)日：2011-05-26
申请号：PCT/EP2010/067828
申请日：2010-11-19
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPET, Rok , ISKRA, Jernej , RUZIC, Milos , PECAVAR, Anica , KOLENC, Ivanka , PUCELJ, Jože , PLAPER, Igor
发明人： ZUPET, Rok , ISKRA, Jernej , RUZIC, Milos , PECAVAR, Anica , KOLENC, Ivanka , PUCELJ, Jože , PLAPER, Igor
IPC分类号： C07D215/58
CPC分类号： C07D215/58
摘要： The present invention describes a novel process for the preparation of marbof loxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula (III), NR 1 R 2 R 3 R 4 , wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula (II), wherein R is selected from H, alkyl, arylalkyl, alkali metal cation,, NH 4 cation, NR 1 R 2 R 3 R 4 cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.
摘要翻译：本发明描述了一种新的制备马可福酯和其中间体的方法，其包括式（III）的氢氧化铵，NR1R2R3R4的反应，其中R 1，R 2，R 3和R 4独立地选自H，烷基，烷基芳基，芳基和/或杂芳基与式（II）化合物反应，其中R选自H，烷基，芳基烷基，碱金属阳离子，NH 4阳离子，NR 1 R 2 R 3 R 4; X是卤素，例如氯，溴，氟，哌嗪基，其可以是取代或未取代的，R'选自H，甲酰基或COOA烷基。

4. 发明申请

WO2010072759A1 PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE 审中-公开
标题翻译：制备异喹诺酮的方法
公开(公告)号：WO2010072759A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/067743
申请日：2009-12-22
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , KOTAR-JORDAN, Berta , ZUPET, Rok , SMRKOLJ, Matej
发明人： KOTAR-JORDAN, Berta , ZUPET, Rok , SMRKOLJ, Matej
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to an improved process for preparation of esomeprazole or salts thereof by optical resolution of omeprazole with BINOL (1,1'-bi-2-naphthol).
摘要翻译：本发明涉及通过用BINOL（1,1'-双-2-萘酚）光学拆分奥美拉唑来制备艾美拉唑或其盐的改进方法。

5. 发明申请

WO2009150147A1 NEW PROCESS FOR THE PREPARATION OF LEVOCETIRIZINE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：用于制备左旋胆碱酯酶及其中间体的新方法
公开(公告)号：WO2009150147A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/057081
申请日：2009-06-09
申请人： KRKA, tovarna zdravil, d.d., Novo Mesto , TIHI, Jaroslav , PECAVAR, Anica , ZUPET, Rok , RZEN, Janez , STROPNIK, Tadej , HVALEC, Miran , KLOBCAR, Andrej , BENKIC, Primoz , SMODIS, Janez , KRASOVEC, Dusan
发明人： TIHI, Jaroslav , PECAVAR, Anica , ZUPET, Rok , RZEN, Janez , STROPNIK, Tadej , HVALEC, Miran , KLOBCAR, Andrej , BENKIC, Primoz , SMODIS, Janez , KRASOVEC, Dusan
IPC分类号： C07D295/185
CPC分类号： C07D295/185
摘要： The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof via a ketocetirizine ester and new ketocetirizine ester intermediates used in that process. reaction of ketocetirizine of the formula (IIIb) to a ketocetirizine ester of the formula (IV) or a salt thereof.
摘要翻译：本发明描述了一种用于通过酮替西嗪酯和该方法中使用的新的酮替卡里嗪酯中间体制备左西替利嗪及其药学上可接受的酸加成盐的新方法。式（IIIb）的酮替卡因与式（IV）的酮替卡瑞嗪酯或其盐的反应。

6. 发明申请

WO2008110586A3 NEW PROCESS FOR THE PREPARATION OF LEVOCETIRIZINE AND INTERMEDIATES THEREOF 审中-公开
公开(公告)号：WO2008110586A3
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052970
申请日：2008-03-12
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , TIHI, Jaroslav , ZUPET, Rok , PECAVAR, Anica , KOLENC, Ivanka , PAVLIN, Darja
发明人： TIHI, Jaroslav , ZUPET, Rok , PECAVAR, Anica , KOLENC, Ivanka , PAVLIN, Darja
IPC分类号： C07D295/088 , C07D295/185
摘要： The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.

7. 发明申请

WO2006010620A3 OLANZAPINE SALTS AND THEIR CONVERSION TO OLANZAPINE FREE BASE 审中-公开
标题翻译： OLANZAPINE SALTS及其转化为OLANZAPINE FREE BASE
公开(公告)号：WO2006010620A3
公开(公告)日：2006-06-08
申请号：PCT/EP2005008218
申请日：2005-07-28
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , SIMONIC IGOR , LENARSIC ROMAN , KOTAR-JORDAN BERTA , ZUPET ROK , GNIDOVEC JOZE
发明人： SIMONIC IGOR , LENARSIC ROMAN , KOTAR-JORDAN BERTA , ZUPET ROK , GNIDOVEC JOZE
IPC分类号： C07D495/04 , A61K31/5513 , A61P25/18
CPC分类号： C07D495/04
摘要： The present invention provides salts olanzapine useful as intermediates in the isolation of olanzapine from complex reaction mixtures. These salts can be used for the production of olanzapine base which has a suitable purity for pharmaceutical use and can easily be converted to anhydrous olanzapine polymorphic form I, in high yields.
摘要翻译：本发明提供盐奥氮平可用作从复杂的反应混合物中分离奥氮平的中间体。这些盐可以用于生产具有适用于药物用途的纯度的奥氮平碱，并且可以以高产率容易地转化为无水奥氮平多晶型I。

8. 发明申请

WO2005085256A1 ISOPROPANOL WATER SOLVATE OF OLANZAPINE 审中-公开
标题翻译：奥兰波星的异丙酚水溶剂
公开(公告)号：WO2005085256A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/002389
申请日：2005-03-07
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , KOTAR-JORDAN, Berta , LENARSIC, Roman , GRCMAN, Marija , SMRKOLJ, Matej , MEDEN, Anton , SIMONIC, Igor , ZUPET, Rok , GNIDOVEC, Joze , BENKIC, Primoz
发明人： KOTAR-JORDAN, Berta , LENARSIC, Roman , GRCMAN, Marija , SMRKOLJ, Matej , MEDEN, Anton , SIMONIC, Igor , ZUPET, Rok , GNIDOVEC, Joze , BENKIC, Primoz
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a novel and well defined Oolvate form of olanzapine which contains 2 molecules of water and 1 molecule of isopropanol per 2 molecules of olanzapine, and which can be converted into other, forms of olanzapine, in particular form (I) of olanzapine, as well as processes for preparing form (I) olanzapine.
摘要翻译：本发明涉及一种新颖且明确定义的奥氮平的奥曲斯酸盐形式，其每2分子奥氮平含有2分子水和1分子异丙醇，并且其可以转化成其他形式的奥氮平，特别是奥氮平（I）形式，以及制备形式（I）奥氮平的方法。

9. 发明申请

WO1996033984A1 N-SULFOXY ANHYDRIDES, A PROCESS FOR THE PREPARATION THEREOF AND ITS USE FOR THE PREPARATION OF BIOACTIVE SUBSTANCES HAVING ACE INHIBITORY ACTION 审中-公开
标题翻译： N-SULFOXY ANHYDRIDES，其制备方法及其用于制备具有ACE抑制作用的生物活性物质的用途
公开(公告)号：WO1996033984A1
公开(公告)日：1996-10-31
申请号：PCT/SI1996000009
申请日：1996-04-22
申请人： CENTRO GENESIS PARA LA INVESTIGACION, S.L. , SERRA MORTES, Sonia , PALOMO COLL, Alberto , ZUPET, Rok
发明人： CENTRO GENESIS PARA LA INVESTIGACION, S.L.
IPC分类号： C07D291/04
CPC分类号： C07D291/04 , A61K38/00 , C07D209/42 , C07K5/0222 , Y02P20/55
摘要： Novel N-sulfoxy anhydrides, a process for the preparation thereof and its use for the preparation of bioactive substances having ACE inhibitory action. Novel compounds of formula (III), wherein R1 represents PhCH2-CH2- or CH3CH2-CH2- and R2 represents methyl or R3-NH-(CH2)3-CH2-, wherein R3 has the meaning of amino protective group, are disclosed. They are used as intermediates in the synthesis of ACE inhibitors, especially of enalapril and trandolapril.
摘要翻译：新型N-磺酰基酸酐，其制备方法及其用于制备具有ACE抑制作用的生物活性物质的用途。公开了新的式（III）化合物，其中R 1表示PhCH 2 -CH 2 - 或CH 3 CH 2 -CH 2 - ，R 2表示甲基或R 3 -NH-（CH 2）3 -CH 2 - ，其中R 3具有氨基保护基的含义。它们用作合成ACE抑制剂，特别是依那普利和群多普利的中间体。

10. 发明申请

WO2009121946A3 PROCESS FOR THE PREPARATION OF OPTICALLY ENRICHED CLOPIDOGREL 审中-公开
公开(公告)号：WO2009121946A3
公开(公告)日：2009-10-08
申请号：PCT/EP2009/053980
申请日：2009-04-02
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , SMODIS, Janez , ZUPET, Rok , VEVERKOVA, Eva , VEVERKA, Miroslav , SIMONIC, Igor
发明人： SMODIS, Janez , ZUPET, Rok , VEVERKOVA, Eva , VEVERKA, Miroslav , SIMONIC, Igor
IPC分类号： C07D495/04 , A61K31/4365
摘要： The invention relates to a process for the preparation of substantially optically pure or optically enriched clopidogrel or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to a process for the preparation of a pharmaceutical formulation comprising substantially optically pure clopidogrel, or a pharmaceutically acceptable salt or solvate thereof, in combination with at least one pharmaceutically acceptable carrier.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式