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。

公开(公告)号：US08614331B2

公开(公告)日：2013-12-24

申请号：US13001936

申请日：2009-07-08

申请人： Dejan Mandic

发明人： Dejan Mandic

IPC分类号： C07D401/12

CPC分类号： C07D401/12 ,  A61K31/4439

摘要： A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallization of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.

摘要翻译： 一种制备艾美拉唑钠的方法包括以下步骤：将艾美拉唑钠溶于主要由甲醇或甲醇构成的溶剂中; 并从所述溶液中进行埃索美拉唑钠的沉淀或结晶。 艾美拉唑钠优选通过使用基于甲醇的流动相的手性色谱法和随后与钠源的反应从纯形式的中性外消旋体获得。 艾美拉唑钠的新型晶体和半晶形式可以重复提供，物理上稳定和高纯度的形式。

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。

公开(公告)号：US20110166183A1

公开(公告)日：2011-07-07

申请号：US13001936

申请日：2009-07-08

申请人： Dejan Mandic

发明人： Dejan Mandic

IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61P1/00

CPC分类号： C07D401/12 ,  A61K31/4439

摘要： A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallisation of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.

摘要翻译： 一种制备艾美拉唑钠的方法包括以下步骤：将艾美拉唑钠溶于主要由甲醇或甲醇构成的溶剂中; 并从所述溶液中进行埃索美拉唑钠的沉淀或结晶。 艾美拉唑钠优选通过使用基于甲醇的流动相的手性色谱法和随后与钠源的反应从纯形式的中性外消旋体获得。 艾美拉唑钠的新型晶体和半晶形式可以重复提供，物理上稳定和高纯度的形式。

公开(公告)号：US07875723B2

公开(公告)日：2011-01-25

申请号：US12416537

申请日：2009-04-01

申请人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

发明人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

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％。

公开(公告)号：US07553857B2

公开(公告)日：2009-06-30

申请号：US11318236

申请日：2005-12-23

申请人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

发明人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

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％。

公开(公告)号：US20100087652A1

公开(公告)日：2010-04-08

申请号：US12416537

申请日：2009-04-01

申请人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

发明人： Lidija Vranicar Savanovic ,  Dejan Mandic ,  Renata Toplak Casar

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％。

公开(公告)号：US20070149573A1

公开(公告)日：2007-06-28

申请号：US11318236

申请日：2005-12-23

申请人： Lidija Savanovic ,  Dejan Mandic ,  Renata Casar

发明人： Lidija Savanovic ,  Dejan Mandic ,  Renata Casar

IPC分类号： A61K31/4439 ,  C07D403/02

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％。