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1. 发明申请

US20070208071A1 Oxidative Degradation Products of Atorvastatin Calcium 有权
标题翻译：阿托伐他汀钙的氧化降解产物
公开(公告)号：US20070208071A1
公开(公告)日：2007-09-06
申请号：US11632608
申请日：2005-07-15
申请人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
发明人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
IPC分类号： A61K31/403 , A61K31/401 , C07D487/02
CPC分类号： C07D498/14 , C07D207/416 , C07D301/00 , C07D303/48 , C07D493/04
摘要： The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
摘要翻译：本发明涉及阿托伐他汀钙的氧化降解产物及其制备方法。本发明还涉及基本上不含氧化降解产物的阿托伐他汀钙和含有这种阿托伐他汀钙的药物组合物。

2. 发明申请

US20070032549A1 Process for obtaining HMG-CoA reductase inhibitors of high purity 审中-公开
标题翻译：获得高纯度HMG-CoA还原酶抑制剂的方法
公开(公告)号：US20070032549A1
公开(公告)日：2007-02-08
申请号：US11581637
申请日：2006-10-16
申请人： Rok Grahek , Dusan Milivojevic , Andrej Bastarda
发明人： Rok Grahek , Dusan Milivojevic , Andrej Bastarda
IPC分类号： A61K31/22 , A61K31/366
CPC分类号： C07C67/52 , A61K31/22 , A61K31/366 , B01D15/422 , C07C69/33
摘要： Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment. The present invention relates to a new industrial process for the isolation of HMG-CoA reductase inhibitors using so-called displacement chromatography. Use of the invention enables one to obtain HMG-CoA reductase inhibitors of high purity, with high yields, lower production costs and suitable ecological balance.
摘要翻译：洛伐他汀，普伐他汀，辛伐他汀，美伐他汀，阿托伐他汀及其衍生物和类似物被称为HMG-CoA还原酶抑制剂，并用作抗高胆固醇血症药。其中大多数是通过使用不同种类的微生物鉴定为属于曲霉属，红曲霉属，诺卡氏菌属，无性系，毛霉属或青霉属，链霉菌属，放线菌属，微单孢菌属的发酵产生的，一些是通过使用化学方法处理发酵产物合成或它们是总化学合成的产物。活性成分的纯度是制造安全有效的药物的重要因素，特别是如果药物产品必须长期服用于治疗或预防高血浆胆固醇。来自低纯度药物的杂质的积累可能在治疗期间引起许多副作用。本发明涉及使用所谓的位移色谱法分离HMG-CoA还原酶抑制剂的新工业方法。使用本发明可以获得高纯度的HMG-CoA还原酶抑制剂，具有高产率，降低生产成本和合适的生态平衡。

3. 发明申请

US20110184172A1 PROCESS FOR THE PREPARATION OF METHYL ESTER OF ROSUVASTATIN 有权
标题翻译：制备罗司他汀甲酯的方法
公开(公告)号：US20110184172A1
公开(公告)日：2011-07-28
申请号：US12672119
申请日：2008-08-01
申请人： Andrej Bastarda , Rok Grahek , Martin Crnugelj
发明人： Andrej Bastarda , Rok Grahek , Martin Crnugelj
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.
摘要翻译：已经开发了用于制备罗苏伐他汀的对映体纯的甲基酯的方法，其中粗制甲基酯酯首先通过制备型色谱法纯化，随后结晶。

4. 发明申请

US20100056605A1 OXIDATIVE DEGRADATION PRODUCTS OF ATORVASTATIN CALCIUM 审中-公开
标题翻译： ATORVASTATIN钙的氧化降解产物
公开(公告)号：US20100056605A1
公开(公告)日：2010-03-04
申请号：US12613787
申请日：2009-11-06
申请人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
发明人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
IPC分类号： A61K31/40 , C07D498/14 , C07D493/04 , C07D207/30
CPC分类号： C07D498/14 , C07D207/416 , C07D301/00 , C07D303/48 , C07D493/04
摘要： The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
摘要翻译：本发明涉及阿托伐他汀钙的氧化降解产物及其制备方法。本发明还涉及基本上不含氧化降解产物的阿托伐他汀钙和含有这种阿托伐他汀钙的药物组合物。

5. 发明授权

US08044086B2 Oxidative degradation products of atorvastatin calcium 有权
标题翻译：阿托伐他汀钙的氧化降解产物
公开(公告)号：US08044086B2
公开(公告)日：2011-10-25
申请号：US11632608
申请日：2005-07-15
申请人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
发明人： Rok Grahek , Darko Kocjan , Andrej Bastarda , Andrej Kocijan , Matjaz Kracun
IPC分类号： A01N43/38 , A01N43/36
CPC分类号： C07D498/14 , C07D207/416 , C07D301/00 , C07D303/48 , C07D493/04
摘要： The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
摘要翻译：本发明涉及阿托伐他汀钙的氧化降解产物及其制备方法。本发明还涉及基本上不含氧化降解产物的阿托伐他汀钙和含有这种阿托伐他汀钙的药物组合物。

6. 发明授权

US5854390A Chromatographic purification of vancomycin hydrochloride by use of preparative HPLC 失效
标题翻译：使用制备型HPLC对盐酸万古霉素进行色谱纯化
公开(公告)号：US5854390A
公开(公告)日：1998-12-29
申请号：US875442
申请日：1997-07-28
申请人： Rok Grahek , Andrej Bastarda
发明人： Rok Grahek , Andrej Bastarda
IPC分类号： C07K1/16 , A61K38/00 , C07K9/00 , G01N30/02 , C07K5/12 , A61K38/12
CPC分类号： C07K9/008 , A61K38/00 , G01N30/02
摘要： The present invention discloses a new method for the purification of vancomycin hydrochloride by preparative HPLC (method of displacement chromatography), whereby the chromatographic purity of the product is essentialy improved. The chromatography is performed on a reverse stationary phase with a mobile phase consisting of an organic or inorganic acid or of a buffer with possible additives, with different displacing agents, at a defined pH and temperature as well as the amount and concentration of vancomycin hydrochloride. The process is distinguished by the excellent yield and exceptional chromatographic purity 95.5% area of the obtained product and, besides, it represents an ecologically irreproachable process. The vancomycin hydrochloride purified according to the present invention is useful for all types of application since the portion of impurities it contains is for one third lower than in hitherto known commercially available products.
摘要翻译： PCT No.PCT / SI96 / 00002 Sec。 371日期1997年7月28日第 102（e）日期1997年7月28日PCT提交1996年2月6日PCT公布。第WO96 / 24614号公报日期1996年8月15日本发明公开了一种通过制备型HPLC（置换色谱法）纯化万古霉素盐酸盐的新方法，从而提高了产品的色谱纯度。色谱法在反相固定相上进行，流动相由有机或无机酸组成的流动相或具有可能的添加剂的缓冲液，不同的置换剂在规定的pH和温度以及盐酸万古霉素的量和浓度下进行。该方法的优点是获得的产品的优异的产率和卓越的色谱纯度达95.5％，此外，它代表了一个生态无法应对的过程。根据本发明纯化的万古霉素盐酸盐可用于所有类型的施用，因为其含有的杂质的部分比目前已知的市售产品低三分之一。

7. 发明授权

US08309719B2 Process for the preparation of methyl ester of rosuvastatin 有权
标题翻译：罗苏伐他汀甲酯制备方法
公开(公告)号：US08309719B2
公开(公告)日：2012-11-13
申请号：US12672119
申请日：2008-08-01
申请人： Andrej Bastarda , Rok Grahek , Martin Crnugelj
发明人： Andrej Bastarda , Rok Grahek , Martin Crnugelj
IPC分类号： C07D239/02
CPC分类号： C07D239/42
摘要： Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.
摘要翻译：已经开发了用于制备罗苏伐他汀的对映体纯的甲基酯的方法，其中粗制甲基酯酯首先通过制备型色谱法纯化，随后结晶。

8. 发明申请

US20100305087A1 ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY 审中-公开
标题翻译：活性药物成分在固体支持，无定形和改善溶解度
公开(公告)号：US20100305087A1
公开(公告)日：2010-12-02
申请号：US12809576
申请日：2008-12-18
申请人： Rok Grahek , Aleksander Resman , Andrej Bastarda , Martin Crnugelj
发明人： Rok Grahek , Aleksander Resman , Andrej Bastarda , Martin Crnugelj
IPC分类号： A61K31/397 , A61K31/122
CPC分类号： A61K31/122 , A61K9/143 , A61K31/397
摘要： A combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support, wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed.
摘要翻译：包含活性药物成分（API）和药学上可接受的固体支持物的组合制剂，其中所述固体支持物为水不溶性颗粒形式，并且包含选自硅酸，氢氧化铝和氢氧化钛的材料。 API是具有至少一个引起API在水中或在水溶液中具有低溶解度的至少一个疏水性结构部分的化合物，以及与包含极性或离子或氢的固体支持物形成多个分子间相互作用的多个亲水基团粘接。 API的亲水基团独立地相同或不同，并且包含由OH-和卤素基团组成的组中的至少一个。 API通过吸附与固体支持物结合，并且所述API的主要比例处于非晶状态。还公开了相关药物和制备方法。

9. 发明申请

US20090012150A1 Stablized Pharmaceutical Composition Comprising an Amorphous Active Substance 审中-公开
标题翻译：包含无定形活性物质的稳定药物组合物
公开(公告)号：US20090012150A1
公开(公告)日：2009-01-08
申请号：US11923059
申请日：2007-10-24
申请人： Rok Grahek , Andrej Bastarda , Mateja Salobir
发明人： Rok Grahek , Andrej Bastarda , Mateja Salobir
IPC分类号： A61K31/40
CPC分类号： A61K31/40 , A61K9/2013 , A61K9/2018 , A61K9/2054
摘要： The invention relates to the pharmaceutical composition comprising the amorphous active substance which is atorvastatin calcium. The process of stabilization of the pharmaceutical composition comprising the pharmaceutical formulation with amorphous atorvastatin calcium, the process of stabilization of the pharmaceutical formulation comprising amorphous atorvastatin calcium and the process of stabilization of atorvastatin calcium in an amorphous form is described.
摘要翻译：本发明涉及包含阿托伐他汀钙的无定形活性物质的药物组合物。描述了包含药物制剂与无定形阿托伐他汀钙的药物组合物的稳定化过程，包含无定形阿托伐他汀钙的药物制剂的稳定化过程和以无定形形式稳定阿托伐他汀钙的方法。

10. 发明授权

US07141602B2 Process for obtaining HMG-CoA reductase inhibitors of high purity 失效
标题翻译：获得高纯度HMG-CoA还原酶抑制剂的方法
公开(公告)号：US07141602B2
公开(公告)日：2006-11-28
申请号：US10698009
申请日：2003-10-30
申请人： Rok Grahek , Dusan Milivojevic , Andrej Bastarda
发明人： Rok Grahek , Dusan Milivojevic , Andrej Bastarda
IPC分类号： A61K31/351 , C07D309/30
CPC分类号： C07C67/52 , A61K31/22 , A61K31/366 , B01D15/422 , C07C69/33
摘要： Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment. The present invention relates to a new industrial process for the isolation of HMG-CoA reductase inhibitors using so-called displacement chromatography. Use of the invention enables one to obtain HMG-CoA reductase inhibitors of high purity, with high yields, lower production costs and suitable ecological balance.
摘要翻译：洛伐他汀，普伐他汀，辛伐他汀，美伐他汀，阿托伐他汀及其衍生物和类似物被称为HMG-CoA还原酶抑制剂，并用作抗高胆固醇血症药。其中大多数是通过使用不同种类的微生物鉴定为属于曲霉属，红曲霉属，诺卡氏菌属，无性系，毛霉属或青霉属，链霉菌属，放线菌属，微单孢菌属的发酵产生的，一些是通过使用化学方法处理发酵产物合成或它们是总化学合成的产物。活性成分的纯度是制造安全有效的药物的重要因素，特别是如果药物产品必须长期服用于治疗或预防高血浆胆固醇。来自低纯度药物的杂质的积累可能在治疗期间引起许多副作用。本发明涉及使用所谓的位移色谱法分离HMG-CoA还原酶抑制剂的新工业方法。使用本发明可以获得高纯度的HMG-CoA还原酶抑制剂，具有高产率，降低生产成本和合适的生态平衡。

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