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1. 发明申请

WO2014006091A1 TICAGRELOR ADDUCTS WITH DIVALENT METAL SALTS 审中-公开
公开(公告)号：WO2014006091A1
公开(公告)日：2014-01-09
申请号：PCT/EP2013/064031
申请日：2013-07-03
申请人： LEK PHARMACEUTICALS D.D. , ZUPANCIC, Borut
发明人： ZUPANCIC, Borut
IPC分类号： C07D487/04 , A61K31/519 , A61P7/02 , A61P9/10
CPC分类号： C07D487/04 , A61K31/519
摘要： The present invention relates to amorphous adducts of ticagrelor with divalent metal salts useful in the treatment or prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease.
摘要翻译：本发明涉及可用于治疗或预防冠状动脉，脑血管或外周血管疾病患者动脉血栓并发症的二价金属盐的替卡格雷的无定形加合物。

2. 发明申请

WO2013186326A1 NEW SYNTHETIC ROUTE FOR THE PREPARATION OF ß-AMINOBUTYRYL SUBSTITUTED 5,6,7,8-TETRAHYDRO[1,4]DIAZOLO[4,3-alpha]PYRAZIN-7-YL COMPOUNDS 审中-公开
标题翻译：制备β-氨基丁二烯的新合成路线5,6,7,8-四氢[1,4]二唑[4,3-α]吡嗪-7-基化合物
公开(公告)号：WO2013186326A1
公开(公告)日：2013-12-19
申请号：PCT/EP2013/062307
申请日：2013-06-13
申请人： LEK PHARMACEUTICALS D.D. , STARCEVIC, Stefan , MRAK, Peter , KOPITAR, Gregor
发明人： STARCEVIC, Stefan , MRAK, Peter , KOPITAR, Gregor
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10 , C07D205/08
CPC分类号： C07D487/04 , C07C227/18 , C07D205/08
摘要： The present invention relates to a process for preparing -aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-α]pyrazin-7-yl compounds.
摘要翻译：本发明涉及制备-氨基丁酰基取代的5,6,7,8-四氢[1,4]二唑并[4,3-a]吡嗪-7-基化合物的方法。

3. 发明申请

WO2012159981A2 PROCESS FOR THE PREPARATION OF α-SUBSTITUTED KETONES AND THEIR APPLICATION IN SYNTHESIS OF PHARMACEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：制备取代的酮的方法及其在药物活性化合物合成中的应用
公开(公告)号：WO2012159981A2
公开(公告)日：2012-11-29
申请号：PCT/EP2012/059236
申请日：2012-05-18
申请人： LEK PHARMACEUTICALS D.D. , GAZIC SMILOVIC, Ivana , SEECHURN, Carin , COLACOT, Thomas J.
发明人： GAZIC SMILOVIC, Ivana , SEECHURN, Carin , COLACOT, Thomas J.
IPC分类号： C07C45/68
CPC分类号： C07D295/088 , C07C45/68 , C07C49/67
摘要： The present invention relates to a novel one step preparation of 6-methoxy-2-phenyl-tetralone starting from 6-methoxy-tetralone and its use as an intermediate in the synthesis of pharmaceutically active compounds.
摘要翻译：本发明涉及从6-甲氧基 - 四氢萘酮开始的6-甲氧基-2-苯基 - 四氢萘酮的新一步制备及其作为药物活性化合物合成中的中间体。

4. 发明申请

WO2012045863A1 PHARMACEUTICAL COMPOSITIONS COMPRISING GLIMEPIRIDE AND POLYETHYLENE GLYCOL CASTOR OIL 审中-公开
标题翻译：包含水杨酸和聚乙烯甘油蓖麻油的药物组合物
公开(公告)号：WO2012045863A1
公开(公告)日：2012-04-12
申请号：PCT/EP2011/067552
申请日：2011-10-07
申请人： LEK PHARMACEUTICALS D.D. , JAKLIC, Miha Tomaz , REVEN, Sebastjan
发明人： JAKLIC, Miha Tomaz , REVEN, Sebastjan
IPC分类号： A61K9/20 , A61K31/4439 , A61K31/64 , A61K9/16
CPC分类号： A61K47/14 , A61K9/2054 , A61K9/2077 , A61K9/209 , A61K31/4015 , A61K31/4439 , A61K31/64 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the field of a pharmaceutical technology. More specifically, the present invention relates to a pharmaceutical composition comprising glimepiride and a surface active agent. Surface active agent obtainable by reacting castor oil or hydrogenated castor oil with ethylene oxide, preferably hydrogenated castor oil, substantially improves dissolution glimepiride active pharmaceutical ingredient and at the same time, when both formulated into a pharmaceutical composition, ensures satisfying or exceeding other parameters like for example stability, hardness, friability and handling of said pharmaceutical composition.
摘要翻译：本发明涉及制药技术领域。更具体地，本发明涉及包含格列美脲和表面活性剂的药物组合物。通过使蓖麻油或氢化蓖麻油与环氧乙烷（优选氢化蓖麻油）反应可获得的表面活性剂大大改善溶解格列美脲活性药物成分，同时当配制成药物组合物时，确保满足或超过其他参数，如所述药物组合物的稳定性，硬度，脆性和处理的实例。

5. 发明申请

WO2012013325A1 PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF STATINS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制定合理统计资料的主要中间人或药物可接受的费用的程序
公开(公告)号：WO2012013325A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/003714
申请日：2011-07-25
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , STERK, Damjan , JUKIC, Marko
发明人： CASAR, Zdenko , STERK, Damjan , JUKIC, Marko
IPC分类号： C07D215/14 , C07D239/46 , C07C49/233 , C07C49/235
CPC分类号： C07D239/42 , C07C45/68 , C07C49/807 , C07C49/86 , C07D215/12 , C07D215/14 , C07D239/46
摘要： The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
摘要翻译：本发明涉及用于合成用于制备他汀类药物的关键中间体的商业上可行的方法，特别是罗苏伐他汀和匹伐他汀或其各自的药学上可接受的盐。提出了一种关键中间体的简单且简短的合成路线，其优点是可以使用便宜且易于获得的起始原料，可以避免常规使用的DIBAL-H作为还原剂。

6. 发明申请

WO2011080346A3 PELLETS AND MICROPARTICLES OF PRAVASTATIN SODIUM AND A PROCESS OF MAKING THEM 审中-公开
公开(公告)号：WO2011080346A3
公开(公告)日：2011-07-07
申请号：PCT/EP2011/050054
申请日：2011-01-04
申请人： LEK PHARMACEUTICALS D.D. , JURKOVIC, Polona , SVETE, Peter , KERC, Janez
发明人： JURKOVIC, Polona , SVETE, Peter , KERC, Janez
IPC分类号： A61K9/16 , A61K9/50 , A61K31/22
摘要： The present invention belongs to the field of pharmaceutical industry and relates to a pharmaceutical composition comprising one or more cores, an enteric coating and a non- acidic protective coating between the core and the enteric coating comprising polymorphic pravastatin sodium. Furthermore, the present invention relates to pharmaceutical compositions comprising one or more cores comprising pravastatin sodium and specific excipients, and to a process for the preparation of said cores. Moreover, the present invention relates to a dosage form comprising said pharmaceutical compositions and to the use of said dosage form for the prevention or treatment of hypercholesterolemia and hyperlipidemia.

7. 发明申请

WO2011042463A2 PHARMACEUTICAL COMPOSITION COMPRISING POORLY SOLUBLE ACTIVE INGREDIENT AND HYPERBRANCHED POLYMER 审中-公开
标题翻译：包含不溶性活性成分和高分子聚合物的药物组合物
公开(公告)号：WO2011042463A2
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064916
申请日：2010-10-06
申请人： LEK PHARMACEUTICALS D.D. , REVEN, Sebastjan , ZAGAR, Ema
发明人： REVEN, Sebastjan , ZAGAR, Ema
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K47/34 , A61K31/64
CPC分类号： A61K31/00 , A61K9/1647 , A61K9/1676 , A61K9/204 , A61K31/122 , A61K31/404 , A61K31/4985 , A61K31/501 , A61K31/64
摘要： The present invention belongs to the field of pharmaceutical industry and relates to a pharmaceutical composition comprising at least one hyperbranched polymer and at least one pharmaceutically active ingredient, wherein the polymer and the pharmaceutically active ingredient are present in a specific weight ratio, and to a process for the preparation of said pharmaceutical composition. The present invention is also directed to a powder or granulate comprising at least one hyperbranched polymer and at least one pharmaceutically active ingredient in a specific weight ratio, to a process for the preparation of said powder or granulate, and to a pharmaceutical dosage form comprising the pharmaceutical composition, powder or granulate. Furthermore, the present invention relates to a process for preparing a solid dispersion of a hyperbranched polymer and at least one API. Moreover, it relates to the use of a crystalline carrier for the preparation of a mixture of hyperbranched polymer and a pharmaceutically active ingredient, as well as to the use of polyesteramide hyperbranched polymers for the preparation of a pharmaceutical composition, to the use of a hydrophilic or hydrophobic carrier for the preparation of said composition comprising a specific group of API, and to the use of a specific API and at least one hyperbranched polymer for the preparation of a pharmaceutical composition.
摘要翻译：本发明属于制药工业领域，涉及包含至少一种超支化聚合物和至少一种药物活性成分的药物组合物，其中聚合物和药物活性成分以特定重量比存在，并且涉及一种方法用于制备所述药物组合物。本发明还涉及包含至少一种超支化聚合物和至少一种特定重量比的药物活性成分的粉末或颗粒，与制备所述粉末或颗粒的方法，以及药物剂型，其包含药物组合物，粉剂或颗粒剂。此外，本发明涉及制备超支化聚合物和至少一种API的固体分散体的方法。此外，它涉及使用结晶载体制备超支化聚合物和药物活性成分的混合物，以及使用聚酯酰胺超支化聚合物制备药物组合物，使用亲水性或疏水载体，用于制备包含特定API组的所述组合物，以及使用特定的API和至少一种超支化聚合物来制备药物组合物。

8. 发明申请

WO2014044721A1 NOVEL CRYSTALLINE FORM OF VORTIOXETINE HYDROBROMIDE 审中-公开
标题翻译：氢溴酸伏立酮的新型结晶形式
公开(公告)号：WO2014044721A1
公开(公告)日：2014-03-27
申请号：PCT/EP2013/069401
申请日：2013-09-18
申请人： SANDOZ AG
发明人： HOTTER, Andreas , ENDERS, Michael , GRIESSER, Ulrich
IPC分类号： C07D295/096 , A61K31/495 , A61P25/00
CPC分类号： C07D295/096 , A61K31/495
摘要： The present invention is directed to a crystalline compound comprising a hydrobromide acid (HBr) salt of a compound of formula (I) (1-{2-[(2,4-dimethylphenyl)sulfanyl]phenyl}piperazine, INN: vortioxetine), having an XRPD pattern with characteristic peaks (expressed in 2θ ± 0,2° 2θ (CuKα radiation)) at 5.5°, 14.8°, 16.7° and 20.0° and processes for obtaining the same.
摘要翻译：本发明涉及包含式（I）化合物（1- {2 - [（2,4-二甲基苯基）硫烷基]苯基}哌嗪，INN：vortoxetine）的氢溴酸（HBr）盐的结晶化合物，具有在5.5°，14.8°，16.7°和20.0°具有特征峰（表示为2＆amp; t;±0,2°2;（CuKα辐射））的XRPD图案和获得相同的方法。

9. 发明申请

WO2013153161A2 NOVEL POLYMORPH OF RILPIVIRINE HYDROCHLORIDE 审中-公开
标题翻译：吡咯烷酮氯化氢的新型聚合物
公开(公告)号：WO2013153161A2
公开(公告)日：2013-10-17
申请号：PCT/EP2013/057596
申请日：2013-04-11
申请人： SANDOZ AG
发明人： HOTTER, Andreas , PICHLER, Arthur , ADAMER, Verena , GRIESSER, Ulrich
IPC分类号： C07D239/48
CPC分类号： C07D239/48
摘要： The present invention relates to a novel polymorph and to novel solvates of rilpivirine hydrochloride, as well as to their preparation. The novel solvates are valuable intermediates for the preparation of the novel polymorph of rilpivirine hydrochloride of the present invention. Moreover the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and additional therapeutic agents.
摘要翻译：本发明涉及一种新型多晶型物和盐酸利乐普林的新型溶剂合物及其制备方法。新型溶剂合物是制备本发明的盐酸利乐结济新型多晶型物的有价值的中间体。此外，本发明涉及新型多晶型物在制备药物中的用途。此外，本发明涉及包含有效量的盐酸利乐普林新型多晶型物的药物组合物及其制备方法。最后，本发明涉及药物组合，其包含有效量的盐酸利乐瑞林的新型多晶型物和另外的治疗剂。

10. 发明申请

WO2011080148A2 AN AQUEOUS INTRAVENOUS NANOSUSPENSION WITH REDUCED ADVERSE EFFECTS 审中-公开
标题翻译：具有降低不良反应的水肿性静息纳豆
公开(公告)号：WO2011080148A2
公开(公告)日：2011-07-07
申请号：PCT/EP2010/070304
申请日：2010-12-20
申请人： LEK PHARMACEUTICALS D.D. , HOMAR, Miha , CEGNAR, Mateja , LOVSE BARLE, Ester , PETERNEL, Luka , KERC, Janez
发明人： HOMAR, Miha , CEGNAR, Mateja , LOVSE BARLE, Ester , PETERNEL, Luka , KERC, Janez
IPC分类号： A61K9/107 , A61K9/00 , A61K47/10 , A61K47/26 , A61K31/343
CPC分类号： A61K31/343 , A61K9/0019 , A61K9/1075 , A61K47/10 , A61K47/26
摘要： The present invention relates to an aqueous nanosuspension formulation comprising a drug possessing low intrinsic water solubility, e.g. amiodarone. It also provides a method for the preparation of intravenous formulation comprising amiodarone, with markedly decreased adverse effects.
摘要翻译：本发明涉及包含具有低固有水溶性的药物的水性纳米悬浮液制剂，胺碘酮。它还提供了制备包含胺碘酮的静脉内制剂的方法，其具有显着降低的不良反应。

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