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1. 发明申请

WO2012001156A2 PHARMACEUTICAL ORAL DOSAGE FORMS COMPRISING DABIGATRAN ETEXILATE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译：包含DABIGATRAN ETEXILATE的药物口服剂型及其药物可接受的盐
公开(公告)号：WO2012001156A2
公开(公告)日：2012-01-05
申请号：PCT/EP2011061140
申请日：2011-07-01
申请人： KRKA TOVARNA ZDRAVIL D D NOVO MESTO , KROSELJ VESNA
发明人： KROSELJ VESNA
IPC分类号： A61K9/50
CPC分类号： A61K9/1682 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K9/167 , A61K9/5078 , A61K31/4439
摘要： The invention relates to pharmaceutical oral dosage forms of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H- benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate (dabigatran etexilate) and the pharmacologically acceptable salts thereof, in particular dabigatran etexilate methanesulfonate.
摘要翻译：本发明涉及活性物质的3-[（2 - {[4-（己氧基羰基氨基 - 亚氨基 - 甲基） - 苯基氨基] - 甲基} -1-甲基-1H-苯并咪唑-5-羰基） - 吡啶-2-基 - 氨基]丙酸酯（达比加群酯）及其药理学上可接受的盐，特别是达比加群酯甲磺酸盐。

2. 发明申请

WO2009000909A8 SALTS OF PERINDOPRIL 审中-公开
标题翻译：佩林德的财产
公开(公告)号：WO2009000909A8
公开(公告)日：2009-02-12
申请号：PCT/EP2008058258
申请日：2008-06-27
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , MERSLAVIC MARJO , BOMBEK SERGEJA , GOJAK URSKA , SMRKOLJ MATEJ , ZUPET ROK
发明人： MERSLAVIC MARJO , BOMBEK SERGEJA , GOJAK URSKA , SMRKOLJ MATEJ , ZUPET ROK
IPC分类号： C07D209/34 , A61K31/404 , A61P9/00
CPC分类号： C07D209/34
摘要： The present invention relates to new salts of perindopril, particularly to a new calcium salt and new amine salts of perindopril, to a process for their preparation and to a pharmaceutical formulations containing the new salts.
摘要翻译：本发明涉及培哚普林的新盐，特别是涉及一种新的钙盐和培哚普利的新的胺盐，其制备方法和含有新盐的药物制剂。

3. 发明申请

WO2008092939A3 PROCESS FOR THE PREPARATION OF OPTICALLY PURE OMEPRAZOLE VIA SALT FORMATION WITH A CHIRAL AMINE OR TREATMENT WITH AN ENTIOMER CONVERTING ENZYME AND CHROMATOGRAPHIC SEPARATION 审中-公开
标题翻译：制备光学纯OMEPRAZOLE的方法，通过盐酸盐形成与原料胺或处理与转化酶和色谱分离的实验者
公开(公告)号：WO2008092939A3
公开(公告)日：2009-01-29
申请号：PCT/EP2008051230
申请日：2008-01-31
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , PLAPER IGOR , PECAVAR ANICA , KOTAR-JORDAN BERTA , ZAJC NATALIJA , VRBINC MIHA , KOCEVAR ANTON , PELKO MITJA , VEVERKA MIROSLAV , VEVERKOVA EVA , SMODIS JANEZ , ZUPET ROK
发明人： PLAPER IGOR , PECAVAR ANICA , KOTAR-JORDAN BERTA , ZAJC NATALIJA , VRBINC MIHA , KOCEVAR ANTON , PELKO MITJA , VEVERKA MIROSLAV , VEVERKOVA EVA , SMODIS JANEZ , ZUPET ROK
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D453/04
摘要： The present invention relates to a process for the preparation of substantially optically pure omeprazole, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to a process for preparing a pharmaceutical composition comprising the substantially optically pure omeprazole or the pharmaceutically acceptable salt or solvate thereof and to intermediates useful for the preparation of optically pure omeprazole.
摘要翻译：本发明涉及制备基本上光学纯的奥美拉唑或其药学上可接受的盐或溶剂合物的方法。本发明还涉及一种制备药物组合物的方法，该药物组合物包含基本上光学纯的奥美拉唑或其药学上可接受的盐或溶剂合物，以及可用于制备光学纯奥美拉唑的中间体。

4. 发明申请

WO2006073376A3 PREPARATION OF IRBESARTAN 审中-公开
标题翻译： IRBESARTAN的制备
公开(公告)号：WO2006073376A3
公开(公告)日：2006-09-21
申请号：PCT/SI2006000001
申请日：2006-01-04
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , ZUPANCIC SILVO , PECAVAR ANICA , ZUPET ROK
发明人： ZUPANCIC SILVO , PECAVAR ANICA , ZUPET ROK
IPC分类号： C07D403/10
CPC分类号： C07D403/10 , Y02P20/55
摘要： The present invention relates to a process for the preparation of irbesartan or its pharmaceutically acceptable salts comprising a synthesis of trityl irbesartan by a reaction of 5-(4-(bromomethyl)biphenyl-2-yl)-1-(triphenylmethyl)tetrazole and 2-n-butyl-4-cyclopentane-2-imidazolin-5-one or a salt therof in an organic solvent in the presence of a phase transfer catalyst and a base, a removal of the protecting group and an isolation of irbesartan or its pharmaceutically acceptable salt.
摘要翻译：本发明涉及一种制备厄贝沙坦或其药学上可接受的盐的方法，其包括通过5-（4-（溴甲基）联苯-2-基）-1-（三苯基甲基）四唑和2 - 丁基-4-环戊烷-2-咪唑啉-5-酮或盐在有机溶剂中，在相转移催化剂和碱的存在下，除去保护基和分离厄贝沙坦或其药学上可接受的盐可接受的盐

5. 发明申请

WO2006011859A2 PREPARATION OF HYDROCHLORIDE SALTS OF TETRAZOLE DERIVATIVE 审中-公开
标题翻译：四唑衍生物的盐酸盐的制备
公开(公告)号：WO2006011859A2
公开(公告)日：2006-02-02
申请号：PCT/SI2005000023
申请日：2005-07-29
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , ZUPANCIC SILVO , SMRKOLJ MATEJ , JAKSE RENATA
发明人： ZUPANCIC SILVO , SMRKOLJ MATEJ , JAKSE RENATA
IPC分类号： C07D403/00
CPC分类号： C07D403/10
摘要： The present invention relates to sesquihydrate hydrochloride salt of irbesartan and anhydrous hydrochloride salts of irbesartan. Irbesartan used as the starting material for the preparation of the described hydrochlorides of irbesartan can be in any form, e.g. it can be used when contained in a reaction solution, in crude form, in a filtrate containing several solvents, or in anhydrous or any solvated or hydrated form, in amorphous form or any known crystal form or in a mixture thereof.
摘要翻译：本发明涉及厄贝沙坦的厄贝沙坦的盐酸倍半水合物盐和厄贝沙坦的无水盐酸盐。用作制备所述的厄贝沙坦的所述盐酸盐的起始原料的厄贝沙坦可以是任何形式，例如，当以含有几种溶剂的滤液或无水或任何溶剂化或水合形式的无定形形式或任何已知的晶形或其混合物中含有反应溶液时，可以使用它们。

6. 发明申请

WO2004065390A8 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF OLANZAPINE 审中-公开
标题翻译： OLANZAPINE的制备方法和中间体
公开(公告)号：WO2004065390A8
公开(公告)日：2004-12-16
申请号：PCT/EP2004000299
申请日：2004-01-16
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , LENARSIC ROMAN , ZUPET ROK , BENEDIK MILENA , MOHAR BARBARA , STIMAC ANTON
发明人： LENARSIC ROMAN , ZUPET ROK , BENEDIK MILENA , MOHAR BARBARA , STIMAC ANTON
IPC分类号： C07D243/14 , C07D495/04 , C07D295/04
CPC分类号： C07D495/04 , C07D243/14
摘要： The invention provides an improved process for preparing Olanzapine as well as intermediates therefor.
摘要翻译：本发明提供了制备奥氮平及其中间体的改进方法。

7. 发明申请

WO2010089105A3 MOISTURE-ACTIVATED GRANULATION PROCESS 审中-公开
标题翻译：水分活化成粒过程
公开(公告)号：WO2010089105A3
公开(公告)日：2011-01-13
申请号：PCT/EP2010000667
申请日：2010-02-03
申请人： KRKA TOVARNA ZDRAVIL D D NOVO MESTO , STUKELJ MITJA , SKRABANJA VIDA , FERLAN ANDREJ , VRECER FRANC , KUKEC SIMON
发明人： STUKELJ MITJA , SKRABANJA VIDA , FERLAN ANDREJ , VRECER FRANC , KUKEC SIMON
IPC分类号： A61K31/165 , A61K9/20 , A61K9/26 , A61K31/4985
CPC分类号： A61K9/2077 , A61K31/165 , A61K31/4985
摘要： The present invention relates to a moisture-activated granulation process for the manufacture of a pharmaceutical dosage form containing at least one moisture- sensitive active substance selected from the group consisting of aliskiren and its pharmaceutically acceptable salts, esters and cocrystals, said process comprising: a) mixing the active substance (s) with one or more dry excipients in solid form, said excipient being selected in particular from the group consisting of diluents, surfactants, binders, lubricants, disintegrators, granulation aids, buffering/alkalizing agents, fillers and antioxidants; b) contacting the mixture with a granulation liquid containing water and optionally one or more excipients to form a granulate, said excipient being selected in particular from the group consisting of binders, buffering/ alkalizing agents, surfactants and antioxidants, to form a granulate wherein the ratio of the total amount of water to the total amount of all the solid ingredients including the active substance (s) and all intragranular excipients is less than 30:100, based on weight; c) further processing the mixture including the addition of further dry excipients to obtain the pharmaceutical dosage form, said excipients being in particular selected from the group consisting of diluents, disintegrants, glidants and lubricants.
摘要翻译：本发明涉及一种用于制造含有至少一种选自阿利吉仑及其药学上可接受的盐，酯和共晶体的湿敏活性物质的药物剂型的水分激活造粒方法，所述方法包括：将活性物质与一种或多种固体形式的干燥赋形剂混合，所述赋形剂特别选自稀释剂，表面活性剂，粘合剂，润滑剂，崩解剂，造粒助剂，缓冲/碱化剂，填料和抗氧化剂 ; b）使混合物与含有水和任选的一种或多种赋形剂的造粒液接触以形成颗粒，所述赋形剂特别选自粘合剂，缓冲/碱化剂，表面活性剂和抗氧化剂，以形成颗粒，其中基于重量，水的总量与包括活性物质和所有颗粒内赋形剂的所有固体成分的总量的比例小于30：100; c）进一步处理混合物，包括加入另外的干燥赋形剂以获得药物剂型，所述赋形剂特别选自稀释剂，崩解剂，助流剂和润滑剂。

8. 发明申请

WO2009121946A2 PROCESS FOR THE PREPARATION OF OPTICALLY ENRICHED CLOPIDOGREL 审中-公开
标题翻译：制备光学加工玻璃的方法
公开(公告)号：WO2009121946A2
公开(公告)日：2009-10-08
申请号：PCT/EP2009053980
申请日：2009-04-02
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , 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
CPC分类号： C07D495/04
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.
摘要翻译：本发明涉及制备基本上光学纯的或光学富集的氯吡格雷或其药学上可接受的盐或溶剂合物的方法。本发明还涉及一种制备药物制剂的方法，其包含与至少一种药学上可接受的载体组合的基本上光学上纯的氯吡格雷或其药学上可接受的盐或溶剂化物。

9. 发明申请

WO2008110586A2 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：WO2008110586A2
公开(公告)日：2008-09-18
申请号：PCT/EP2008052970
申请日：2008-03-12
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , 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
CPC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.
摘要翻译：本发明描述了使用二甘醇酸或其衍生物和用于该方法的新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。

10. 发明申请

WO2007147889A3 PREPARATION OF TELMISARTAN SALTS 审中-公开
标题翻译：特米西坦盐的制备
公开(公告)号：WO2007147889A3
公开(公告)日：2008-05-08
申请号：PCT/EP2007056251
申请日：2007-06-22
申请人： KRKA TOVARNA ZDRAVIL D D NOVO , ZUPANCIC SILVO , SMRKOLJ MATEJ , STROPNIK TADEJ , VRBINC MIHA , OSOLNIK RENATA , SEDMAK GREGOR
发明人： ZUPANCIC SILVO , SMRKOLJ MATEJ , STROPNIK TADEJ , VRBINC MIHA , OSOLNIK RENATA , SEDMAK GREGOR
IPC分类号： C07D235/20 , A61K31/4184 , A61P9/12
CPC分类号： C07D235/20
摘要： New salts of telmisartan, in amorphous and crystalline forms, together with two new polymorphic forms of telmisartan potassium, have been prepared by crystallization, evaporation of solvent, spray-drying or lyophilization and were included into a pharmaceutical formulation.
摘要翻译：已经通过结晶，溶剂蒸发，喷雾干燥或冻干来制备替米沙坦的无定形和结晶形式的新盐以及两种新的替米沙坦钾的多晶型物质，并被包括在药物制剂中。

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