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1.发明授权公开(公告)号：US07435812B2
公开(公告)日：2008-10-14
申请号：US10499293
申请日：2002-12-02
CPC分类号： A61K31/7008 , C07H5/06
摘要： Method for preparing a compound comprising protonated glucosamine and Cl−, Na+ and SO42− ions, in which (a) glucosamine hydrochloride and a stoichiometric excess of sodium sulphate are placed in water, (b) the mixture obtained from the preceding step (a) is heated, (c) the mixture is cooled, and (d) the solid present in the said cooled mixture is recovered by filtration. Compound comprising protonated glucosamine and Cl−, Na+ and SO42− ions and having the X-ray diffraction diagram of FIG. 1.
摘要翻译： 用于制备包含质子化葡糖胺和Cl - ，Na +和/或SO 2 - 2 - 离子的化合物的方法， 将（a）葡萄糖胺盐酸盐和化学计量过量的硫酸钠置于水中，（b）将从前述步骤（a）获得的混合物加热，（c）将混合物冷却，和（d） 通过过滤回收所述冷却的混合物。 包含质子化葡糖胺和Cl - ，Na + +和SO 4 - 2 - / - 离子的化合物，并具有X射线 图的衍射图。 1。
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2.发明申请公开(公告)号：US20050171058A1
公开(公告)日：2005-08-04
申请号：US10499293
申请日：2002-12-02
IPC分类号： A61K31/7008 , C07H5/06
CPC分类号： A61K31/7008 , C07H5/06
摘要： Method for preparing a compound comprising protonated glucosamine and Cl−, Na+ and SO42− ions, in which (a) glucosamine hydrochloride and a stoichiometric excess of sodium sulphate are placed in water, (b) the mixture obtained from the preceding step (a) is heated, (c) the mixture is cooled, and (d) the solid present in the said cooled mixture is recovered by filtration. Compound comprising protonated glucosamine and Cl−, Na+ and SO42− ions and having the X-ray diffraction diagram of FIG. 1.
摘要翻译： 用于制备包含质子化葡糖胺和Cl - ，Na +和/或SO 2 - 2 - 离子的化合物的方法， 将（a）葡萄糖胺盐酸盐和化学计量过量的硫酸钠置于水中，（b）将从前述步骤（a）获得的混合物加热，（c）将混合物冷却，和（d） 通过过滤回收所述冷却的混合物。 包含质子化葡糖胺和Cl - ，Na + +和SO 4 - 2 - / - 离子的化合物，并具有X射线 图的衍射图。 1。
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公开(公告)号：US20120142699A1
公开(公告)日：2012-06-07
申请号：US13370735
申请日：2012-02-10
IPC分类号： A61K31/496 , A61P25/20 , A61P25/22 , C07D471/04 , A61P25/24
CPC分类号： A61K31/496 , A61K9/0053 , A61K9/08 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/44 , C07D249/18
摘要： A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
摘要翻译： 生产曲唑酮或曲唑酮盐酸盐的方法，其包括：（a）在至少一种有机溶剂中制备包含曲唑酮的有机相; （b）制备包含至少一种碱性化合物的水相; （c）将所述水相与所述有机相混合; （d）在至少40℃的温度下加热至少30分钟; （e）回收所述曲唑酮; 和（f）用盐酸处理所述曲唑酮以获得盐酸曲唑酮。 包含小于15ppm烷基化物质的曲唑酮或曲唑酮盐酸盐，以及包含所述曲唑酮盐酸盐的药物组合物。
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公开(公告)号：US20100056539A1
公开(公告)日：2010-03-04
申请号：US12513048
申请日：2008-07-23
IPC分类号： A61K31/496 , C07D471/04
CPC分类号： A61K31/496 , A61K9/0053 , A61K9/08 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/44 , C07D249/18
摘要： A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
摘要翻译： 生产曲唑酮或曲唑酮盐酸盐的方法，包括以下步骤：（a）在至少一种有机溶剂中制备含有曲唑酮的有机相; （b）制备包含至少一种碱性化合物的水相; （c）将所述水相与所述有机相混合; （d）在至少40℃的温度下加热至少30分钟; （e）回收所述曲唑酮; 和（f）用盐酸处理所述曲唑酮以获得盐酸曲唑酮。 包含小于15ppm烷基化物质的曲唑酮或曲唑酮盐酸盐，以及包含所述曲唑酮盐酸盐的药物组合物。
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公开(公告)号：US20130012520A1
公开(公告)日：2013-01-10
申请号：US13617907
申请日：2012-09-14
CPC分类号： A61K31/496 , A61K9/0053 , A61K9/08 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/44 , C07D249/18
摘要： A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
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公开(公告)号：US08314236B2
公开(公告)日：2012-11-20
申请号：US13370735
申请日：2012-02-10
IPC分类号： C07D471/04
CPC分类号： A61K31/496 , A61K9/0053 , A61K9/08 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/44 , C07D249/18
摘要： A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
摘要翻译： 生产曲唑酮或曲唑酮盐酸盐的方法，其包括：（a）在至少一种有机溶剂中制备包含曲唑酮的有机相; （b）制备包含至少一种碱性化合物的水相; （c）将所述水相与所述有机相混合; （d）在至少40℃的温度下加热至少30分钟; （e）回收所述曲唑酮; 和（f）用盐酸处理所述曲唑酮以获得盐酸曲唑酮。 包含小于15ppm烷基化物质的曲唑酮或曲唑酮盐酸盐，以及包含所述曲唑酮盐酸盐的药物组合物。
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公开(公告)号：US20130261160A1
公开(公告)日：2013-10-03
申请号：US13990974
申请日：2012-01-17
申请人： Tommaso Iacoangeli , Mario Chiavarini , Antonello Fazio , Marcello Marchetti , Giovanni Battista Ciottoli
发明人： Tommaso Iacoangeli , Mario Chiavarini , Antonello Fazio , Marcello Marchetti , Giovanni Battista Ciottoli
IPC分类号： C07D263/24
CPC分类号： C07D263/24 , C07D405/06 , C07D405/14
摘要： The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30° C. and 50° C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80° C. and 180° C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25° C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production.
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公开(公告)号：US08133893B2
公开(公告)日：2012-03-13
申请号：US12513048
申请日：2008-07-23
IPC分类号： A61K31/496 , C07D471/04
CPC分类号： A61K31/496 , A61K9/0053 , A61K9/08 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/44 , C07D249/18
摘要： A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
摘要翻译： 生产曲唑酮或曲唑酮盐酸盐的方法，包括以下步骤：（a）在至少一种有机溶剂中制备含有曲唑酮的有机相; （b）制备包含至少一种碱性化合物的水相; （c）将所述水相与所述有机相混合; （d）在至少40℃的温度下加热至少30分钟; （e）回收所述曲唑酮; 和（f）用盐酸处理所述曲唑酮以获得盐酸曲唑酮。 包含小于15ppm烷基化物质的曲唑酮或曲唑酮盐酸盐，以及包含所述曲唑酮盐酸盐的药物组合物。
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公开(公告)号：US20110092751A1
公开(公告)日：2011-04-21
申请号：US12972955
申请日：2010-12-20
IPC分类号： C07C19/00
CPC分类号： C07D265/30 , C07D295/088 , C07F3/02
摘要： A process for the preparation of delmopinol (3-(4-propylheptyl)-4-morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including a hydrate, comprises reacting oxazolidin [2,3-c]morpholine and a Grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2,3-c]morpholine and the Grignard reagent are useful as intermediates in the production process.
摘要翻译： 制备地莫莫丁（3-（4-丙基庚基）-4-吗啉代甲醇）或其衍生物或药学上可接受的盐或其溶剂化物，包括水合物的方法包括使恶唑烷并[2,3-c]吗啉与 格利雅试剂，并且任选地将德莫可诺（或衍生物）游离碱转化为药学上可接受的盐。 恶唑烷并[2,3-c]吗啉和格氏试剂可用作生产过程中的中间体。
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公开(公告)号：US07910730B2
公开(公告)日：2011-03-22
申请号：US12779288
申请日：2010-05-13
IPC分类号： C07D498/04
CPC分类号： C07D265/30 , C07D295/088 , C07F3/02
摘要： A process for the preparation of delmopinol (3-(4-propylheptyl)-4-morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including a hydrate, comprises reacting oxazolidin [2,3-c] morpholine and a Grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2,3-c] morpholine and the Grignard reagent are useful as intermediates in the production process.
摘要翻译： 制备地莫莫丁（3-（4-丙基庚基）-4-吗啉代甲醇）或其衍生物或药学上可接受的盐或其溶剂化物，包括水合物的方法包括使恶唑烷并[2,3-c]吗啉与 格利雅试剂，并且任选地将德莫可诺（或衍生物）游离碱转化为药学上可接受的盐。 恶唑烷并[2,3-c]吗啉和格氏试剂可用作生产过程中的中间体。
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