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1. 发明申请

WO2007147889A2 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：WO2007147889A2
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056251
申请日：2007-06-22
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , 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多米诺替米沙坦钾多晶型物质，并被包括在药物制剂中。

2. 发明申请

WO2010146187A2 PROCESS FOR THE PREPARATION OF TELMISARTAN 审中-公开
标题翻译：制备泰米斯坦的方法
公开(公告)号：WO2010146187A2
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058754
申请日：2010-06-21
申请人： KRKA, tovarna zdravil, d.d., Novo mesto , ZUPANCIC, Silvo , SEDMAK, Gregor
发明人： ZUPANCIC, Silvo , SEDMAK, Gregor
IPC分类号： C07D235/20 , A61K31/4184 , A61P9/12
CPC分类号： C07D235/20
摘要： The invention relates to processes for preparing telmisartan or a pharmaceutically acceptable salt thereof as well as to a process for preparing a telmisartan cyano intermediate. Moreover, the invention relates to a multilayer pharmaceutical tablet comprising (a) at least one first tablet layer comprising 1 to 50 wt. -% telmisartan or a pharmaceutically acceptable salt thereof by weight of the first tablet layer and (b) at least one second tablet layer comprising 1 to 50 wt.-% of a diuretic and 50 to 99 wt.-% of at least one filler by weight of the second tablet layer, wherein the combined weight of the diuretic and the at least one filler is at least 87 wt.-% by weight of the second tablet layer. The invention also relates to a process for the preparation of a multilayer pharmaceutical tablet.
摘要翻译：本发明涉及制备替米沙坦或其药学上可接受的盐以及制备替米沙坦氰基中间体的方法。此外，本发明涉及一种多层药物片剂，其包含（a）至少一种第一片剂层，其包含1至50重量％ - 替米沙坦或其药学上可接受的盐，和（b）至少一个第二片剂层，其包含1至50重量％的利尿剂和50至99重量％的至少一种填料的第二片剂层，其中利尿剂和至少一种填料的组合重量为第二片剂层的至少87重量％。本发明还涉及制备多层药物片剂的方法。

3. 发明申请

WO2010026255A1 PROCESS FOR PREPARING OLMESARTAN MEDOXOMIL INTERMEDIATE 审中-公开
标题翻译：制备OLMESARTAN MEDOXOMIL中间体的方法
公开(公告)号：WO2010026255A1
公开(公告)日：2010-03-11
申请号：PCT/EP2009/061583
申请日：2009-09-07
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPANCIC, Silvo
发明人： ZUPANCIC, Silvo
IPC分类号： C07D405/14 , A61K31/41 , A61P9/12
CPC分类号： C07D405/14
摘要： The present invention discloses a process for preparing tritylolmesartan medoxomil with purity greater than 98% and further converting such an intermediate to olmesartan medoxomil.
摘要翻译：本发明公开了一种制备纯度大于98％的三苯甲基马来酰吗啉的方法，并进一步将这种中间体转化为奥美沙坦酯。

4. 发明申请

WO2009004064A1 PROCESS FOR PREPARING TELMISARTAN 审中-公开
标题翻译：制备TELMISARTAN的方法
公开(公告)号：WO2009004064A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/058616
申请日：2008-07-03
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPET, Rok , JIANG, Xiangrui , OU, Yang , LIU, Yongjian , CHEN, Weiming , WU, Mingjun , SHEN, Jingshan , ZUPANCIC, Silvo , SEDMAK, Gregor
发明人： ZUPET, Rok , JIANG, Xiangrui , OU, Yang , LIU, Yongjian , CHEN, Weiming , WU, Mingjun , SHEN, Jingshan , ZUPANCIC, Silvo , SEDMAK, Gregor
IPC分类号： C07D235/08 , C07D235/18 , C07D235/20 , A61K31/4184 , A61P9/12
CPC分类号： C07D235/20 , C07D235/08 , C07D235/18
摘要： Novel processes for preparing a telmisaitan nitrile intermediate (4'-[{2-n-propyl-4- methyI-6-f l-methyJbenzimidazol-2-yl)-benzimidazol- l -yl)-methyl]-biphenyl-2-nitrile) and further converting it to telmisaitan and/or salts thereof are disclosed.
摘要翻译：制备替米沙坦腈中间体（4' - [{2-正丙基-4-甲基-6- [1-甲基-1H-咪唑-2-基] - 苯并咪唑-1-基） - 甲基]联苯-2-基的新方法腈）并进一步转化为替米沙坦和/或其盐。

5. 发明申请

WO2008107452A1 PHARMACEUTICAL COMPOSITION COMPRISING A SALT OF ROSIGLITAZONE 审中-公开
标题翻译：包含ROSIGLITAZONE盐的药物组合物
公开(公告)号：WO2008107452A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052655
申请日：2008-03-05
申请人： KRKA, tovarna zdravil, d.d., Novo Mesto , GERMAN, Tamara , VRBINC, Miha , ZUPANCIC, Silvo , STEFANIC, Marko
发明人： GERMAN, Tamara , VRBINC, Miha , ZUPANCIC, Silvo , STEFANIC, Marko
IPC分类号： A61K9/20 , A61K9/28 , A61K31/427
CPC分类号： A61K9/2059 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2077
摘要： The present invention relates to a pharmaceutical composition comprising (a) 0.1 - 10 % by weight of a salt of rosiglitazoneas active ingredient, and (b) 0.2 - 4.0 % by weight of disintegrant and a process for producing the same.
摘要翻译：本发明涉及药物组合物，其包含（a）0.1-10重量％的罗格列酮活性成分的盐，和（b）0.2-4.0重量％的崩解剂及其制备方法。

6. 发明申请

WO2006073376A2 PREPARATION OF TETRAZOLE DERIVATIVE 审中-公开
标题翻译：四唑衍生物的制备
公开(公告)号：WO2006073376A2
公开(公告)日：2006-07-13
申请号：PCT/SI2006/000001
申请日：2006-01-04
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , 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

7. 发明申请

WO2010081861A1 PROCESS FOR THE PREPARATION OF ROSUVASTATIN 审中-公开
标题翻译：制备罗司他汀的方法
公开(公告)号：WO2010081861A1
公开(公告)日：2010-07-22
申请号：PCT/EP2010/050425
申请日：2010-01-14
申请人： KRKA, tovarna zdravil, d.d., Novo Mesto , BENKIC, Primoz , BEVK, David , LENARSIC, Roman , ZUPANCIC, Silvo , VAJS, Anamarija , JAKSE, David
发明人： BENKIC, Primoz , BEVK, David , LENARSIC, Roman , ZUPANCIC, Silvo , VAJS, Anamarija , JAKSE, David
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The invention relates to a process for the preparation of a HMG - CoA reductase inhibitor such as rosuvastatin, as well as intermediates useful in such process. The invention also relates to salts of HMG-CoA reductase inhibitors and processes for preparing same as well as processes for preparing pharmaceutically acceptable salts of HMG-CoA reductase inhibitors.
摘要翻译：本发明涉及制备HMG-CoA还原酶抑制剂如罗苏伐他汀的方法，以及可用于该方法的中间体。本发明还涉及HMG-CoA还原酶抑制剂的盐及其制备方法以及制备HMG-CoA还原酶抑制剂的药学上可接受的盐的方法。

8. 发明申请

WO2008012372A1 PROCESS FOR THE PREPARATION OF CANDESARTAN CILEXETIL FORM I 审中-公开
标题翻译： CANDESARTAN CILEXETIL FORM的制备方法I
公开(公告)号：WO2008012372A1
公开(公告)日：2008-01-31
申请号：PCT/EP2007/057804
申请日：2007-07-27
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPANCIC, Silvo , BENKIC, Primoz , SMRKOLJ, Polona , SENICAR, Suzana , SOSTARIC-VIRC, Nives , HVALA, Jernej
发明人： ZUPANCIC, Silvo , BENKIC, Primoz , SMRKOLJ, Polona , SENICAR, Suzana , SOSTARIC-VIRC, Nives , HVALA, Jernej
IPC分类号： C07D309/12 , C07D403/10 , C07D407/14 , A61K31/4184 , A61P9/00 , C07C22/00
CPC分类号： C07D403/10 , C07C69/96 , C07C2601/14
摘要： The present invention provides an improved process for the manufacture of candesartan cilexetil form I. Further disclosed is a candesartan cilexetil preparation containing less than 0.15%, preferably less than 0.10%, of (+-)-1 -Hydroxyethyl candesartan oxanyl carbonate (ester) of the following formula (V) wherein one of A, B and C is an oxygen atom and the other two are -CH 2 - groups.
摘要翻译：本发明提供了一种制备坎地沙坦片塞霉素形式I的改进方法。还公开了含有少于0.15％（优选小于0.10％）（+ - ） - 1 - 羟基乙基坎地沙坦碳酸亚根酯（酯）的坎地沙坦碳酸酯制剂，的下式（Ⅴ）其中A，B和C中的一个为氧原子，另外两个为-CH 2 2 - 基团。

9. 发明申请

WO2003080591A1 PROCESS FOR THE PREPARATION OF 4-OXYTETRAHYDROPYRAN-2-ONES 审中-公开
标题翻译：制备4-氧化二氢吡喃-2-酮的方法
公开(公告)号：WO2003080591A1
公开(公告)日：2003-10-02
申请号：PCT/SI2003/000009
申请日：2003-03-17
申请人： KRKA TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPANCIC, Silvo , KRASOVEC, Dusan , ZUPET, Pavel
发明人： ZUPANCIC, Silvo , KRASOVEC, Dusan , ZUPET, Pavel
IPC分类号： C07D309/10
CPC分类号： C07D309/30
摘要： A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents. It is characteristic of this reaction that no additional impurities are obtained and that it takes place without the use of additional catalysts and with low excesses of the reagent.
摘要翻译：描述了用作为去硅烷化试剂的四乙酸三氢氟酸4-甲硅烷氧基四氢吡喃-2-酮的HMG-CoA还原酶抑制剂如辛伐他汀的制备方法。该反应在有机溶剂，其混合物或无溶剂中进行。该反应的特征在于没有额外的杂质获得，并且在没有使用额外的催化剂和低过量的试剂的情况下进行。

10. 发明申请

WO2008012371A1 PROCESS FOR THE PREPARATION OF AMORPHOUS AND CRYSTALLINE FORMS OF CANDESARTAN CILEXETIL USING COLUMN CHROMATOGRAPHY 审中-公开
标题翻译：使用色谱法制备CANDESARTAN CILEXETIL的非晶态和结晶形式的方法
公开(公告)号：WO2008012371A1
公开(公告)日：2008-01-31
申请号：PCT/EP2007/057803
申请日：2007-07-27
申请人： KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO , ZUPANCIC, Silvo , BENKIC, Primoz , STROPNIK, Tadej , PECAVAR, Anica , PUCELJ, Joze , PLAPER, Igor , HVALEC, Miran , SMRKOLJ, Matej , OSOLNIK, Renata , SMRKOLJ, Polona , SENICAR, Suzana , SOSTARIC-VIRC, Nives , HVALA, Jernej
发明人： ZUPANCIC, Silvo , BENKIC, Primoz , STROPNIK, Tadej , PECAVAR, Anica , PUCELJ, Joze , PLAPER, Igor , HVALEC, Miran , SMRKOLJ, Matej , OSOLNIK, Renata , SMRKOLJ, Polona , SENICAR, Suzana , SOSTARIC-VIRC, Nives , HVALA, Jernej
IPC分类号： C07D309/12 , C07D403/10 , C07D407/14 , A61K31/4184 , A61P9/00 , C07C22/00
CPC分类号： C07D403/10 , C07C69/96 , C07C2601/14
摘要： The present invention provides processes for the preparation of amorphous and crystalline candesartan cilexetil with quality that complies to Ph.Eur./ICH Guidelines by an economical way using easy accessible substances and pure starting compounds.
摘要翻译：本发明提供了通过使用容易获得的物质和纯起始化合物的经济方法制备质量符合Ph.Eur./ICH指南的无定形和结晶坎地沙坦酯的方法。

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