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1.发明授权Process for the preparation of enantiomerically enriched proton pump inhibitors 有权用于制备对映体富集的质子泵抑制剂的方法公开(公告)号：US08889873B2
公开(公告)日：2014-11-18
申请号：US13124082
申请日：2009-10-13
申请人： Barbara Mohar , Renata Toplak Casar
发明人： Barbara Mohar , Renata Toplak Casar
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.
摘要翻译： 本发明公开了一种通过在对映选择性氧化步骤中使用特定的金属催化剂来制备具有对映体富集形式的质子泵抑制剂典型结构的化合物的方法。 还公开了有用的进一步方法和纯中间体和随后的最终产物。
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2.发明申请公开(公告)号：US20120046319A1
公开(公告)日：2012-02-23
申请号：US13124082
申请日：2009-10-13
申请人： Barbara Mohar , Renata Toplak Casar
发明人： Barbara Mohar , Renata Toplak Casar
IPC分类号： A61K31/4439 , A61P1/00 , A61P29/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.
摘要翻译： 本发明公开了一种通过在对映选择性氧化步骤中使用特定的金属催化剂来制备具有对映体富集形式的质子泵抑制剂典型结构的化合物的方法。 还公开了有用的进一步方法和纯中间体和随后的最终产物。
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公开(公告)号：US20100087652A1
公开(公告)日：2010-04-08
申请号：US12416537
申请日：2009-04-01
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1% by weight as determined by high performance liquid chromatography (HPLC).
摘要翻译： 本发明公开了一种制备S-奥美拉唑镁盐的方法。 S-奥美拉唑盐的水含量优选低于约4.8重量％，镁含量为约3.4-4.0重量％，以无水，无溶剂的S-奥美拉唑镁的重量计，其光学纯度为 至少约85％的对映异构体过量（“ee”）。 此外，本发明提供了基本上不含中性奥美拉唑的S-奥美拉唑的镁盐，意味着该产品含有小于约3重量％的中性S-奥美拉唑和中性奥美拉唑的总和。 此外，根据本发明的S-奥美拉唑镁优选具有通过高效液相色谱（HPLC）测定的相关物质和降解产物的测定值小于约0.1重量％。
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公开(公告)号：US08247567B2
公开(公告)日：2012-08-21
申请号：US12523025
申请日：2008-01-09
申请人： Dejan Mandic , Renata Toplak Casar
发明人： Dejan Mandic , Renata Toplak Casar
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.
摘要翻译： 本发明涉及从奥美拉唑盐，特别是奥美拉唑镁盐中除去有机溶剂的方法，包含奥美拉唑盐，特别是可通过这种方法获得的奥美拉唑镁盐的组合物和药物组合物 包括所述组合物或奥美拉唑的盐，特别是奥美拉唑的镁盐，特别是奥美拉唑是S-奥美拉唑。
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公开(公告)号：US07875723B2
公开(公告)日：2011-01-25
申请号：US12416537
申请日：2009-04-01
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1% by weight as determined by high performance liquid chromatography (HPLC).
摘要翻译： 本发明公开了一种制备S-奥美拉唑镁盐的方法。 S-奥美拉唑盐的水含量优选低于约4.8重量％，镁含量为约3.4-4.0重量％，以无水，无溶剂的S-奥美拉唑镁的重量计，其光学纯度为 至少约85％的对映异构体过量（“ee”）。 此外，本发明提供了基本上不含中性奥美拉唑的S-奥美拉唑的镁盐，意味着该产品含有小于约3重量％的中性S-奥美拉唑和中性奥美拉唑的总和。 此外，根据本发明的S-奥美拉唑镁优选具有通过高效液相色谱（HPLC）测定的相关物质和降解产物的测定值小于约0.1重量％。
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公开(公告)号：US07553857B2
公开(公告)日：2009-06-30
申请号：US11318236
申请日：2005-12-23
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a-sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1 % by weight as determined by high performance liquid chromatography (HPLC).
摘要翻译： 本发明公开了一种制备S-奥美拉唑镁盐的方法。 S-奥美拉唑盐的水含量优选低于约4.8重量％，镁含量为约3.4-4.0重量％，以无水，无溶剂的S-奥美拉唑镁的重量计，其光学纯度为 至少约85％的对映异构体过量（“ee”）。 此外，本发明提供了基本上不含中性奥美拉唑的S-奥美拉唑镁盐，意味着该产品含有小于约3重量％的中和S-奥美拉唑和中性奥美拉唑的总和。 此外，根据本发明的S-奥美拉唑镁优选具有通过高效液相色谱（HPLC）测定的相关物质和降解产物的测定值小于约0.1重量％。
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公开(公告)号：US08362259B2
公开(公告)日：2013-01-29
申请号：US12506662
申请日：2009-07-21
申请人： Renata Toplak Casar
发明人： Renata Toplak Casar
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
摘要翻译： 提供了制备纯化的艾美拉唑镁的方法，包括以下步骤：提供艾美拉唑镁; 使所述艾美拉唑镁与包含水性组分的非溶剂接触，直到在非溶剂中由水饱和度限定的最大含量; 并回收由接触步骤形成的纯化的埃索美拉唑镁。 该方法特别适用于获得艾美拉唑镁二水合物，特别是A型。所得到的艾美拉唑镁非常纯净，稳定，具有互换性。
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公开(公告)号：US20110224271A1
公开(公告)日：2011-09-15
申请号：US12672264
申请日：2008-08-07
申请人： Renata Toplak Casar
发明人： Renata Toplak Casar
IPC分类号： A61K31/41 , C07D403/10 , A61P9/12
CPC分类号： C07D405/14
摘要： The present invention relates to a process for the preparation and purification of trityl olmesartan medoxomil and olmesartan medoxomil.
摘要翻译： 本发明涉及一种三苯甲基奥美沙坦酯和奥美沙坦酯的制备和纯化方法。
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公开(公告)号：US20100076025A1
公开(公告)日：2010-03-25
申请号：US12523025
申请日：2008-01-09
申请人： Dejan Mandic , Renata Toplak Casar
发明人： Dejan Mandic , Renata Toplak Casar
IPC分类号： A61K31/435 , C07D401/12 , A61P1/00
CPC分类号： C07D401/12
摘要： The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.
摘要翻译： 本发明涉及从奥美拉唑盐，特别是奥美拉唑镁盐中除去有机溶剂的方法，包含奥美拉唑盐，特别是可通过这种方法获得的奥美拉唑镁盐的组合物和药物组合物 包括所述组合物或奥美拉唑的盐，特别是奥美拉唑的镁盐，特别是奥美拉唑是S-奥美拉唑。
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公开(公告)号：US20100016370A1
公开(公告)日：2010-01-21
申请号：US12506662
申请日：2009-07-21
申请人： Renata Toplak Casar
发明人： Renata Toplak Casar
IPC分类号： A61K31/4439 , C07D401/12 , A61P29/00
CPC分类号： C07D401/12
摘要： There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
摘要翻译： 提供了制备纯化的艾美拉唑镁的方法，包括以下步骤：提供艾美拉唑镁; 使所述艾美拉唑镁与包含水性组分的非溶剂接触，直到在非溶剂中由水饱和度限定的最大含量; 并回收由接触步骤形成的纯化的埃索美拉唑镁。 该方法特别适用于获得艾美拉唑镁二水合物，特别是A型。所得到的艾美拉唑镁非常纯净，稳定，具有互换性。
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