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1. 发明授权

US06806386B1 Process for the preparation of ketimines 失效
标题翻译：酮亚胺的制备方法
公开(公告)号：US06806386B1
公开(公告)日：2004-10-19
申请号：US10130198
申请日：2002-05-14
申请人： Marc Thommen , Andreas Hafner , Frédëric Brunner , Hans-Jörg Kirner , Roman Kolly
发明人： Marc Thommen , Andreas Hafner , Frédëric Brunner , Hans-Jörg Kirner , Roman Kolly
IPC分类号： C07C20900
CPC分类号： C07C249/02 , C07C251/20
摘要： The present invention relates to a process for the preparation of compounds of formula (1), in which R1, R2 and R3 independently of one another are hydrogen, halogen , trifluoromethyl of or C1-C4alkoxy, wherein a compound of formula (2), in which R1, R2 and R3 are as defined in formula (1), is reacted with methlyamine in the presence of a non-alcoholic solvent and, if desired, in the presence of a sulfonic acid catalyst to give the compound of formula (2) and, if desired, is subject to purification by recrystallization.
摘要翻译：本发明涉及制备式（1）化合物的方法，其中R 1，R 2和R 3彼此独立地是氢，卤素，或C 1 -C 4烷氧基的三氟甲基，其中式（2）的化合物，其中R 1，R 2和R 3如式（1）中所定义）与甲胺在非醇溶剂存在下反应，如果需要，在磺酸催化剂的存在下反应得到式（2）的化合物），如果需要，通过重结晶进行纯化。

2. 发明授权

US06693218B1 Process for the preparation of ketimines 失效
标题翻译：酮亚胺的制备方法
公开(公告)号：US06693218B1
公开(公告)日：2004-02-17
申请号：US10130199
申请日：2002-09-20
申请人： Marc Thommen , Andreas Hafner , Roman Kolly , Hans-Jörg Kirner , Frédéric Brunner
发明人： Marc Thommen , Andreas Hafner , Roman Kolly , Hans-Jörg Kirner , Frédéric Brunner
IPC分类号： C07C24902
CPC分类号： C07C249/02 , C07C251/20
摘要： Described is a process for the preparation of compounds of formula (1a) which comprises reacting an isomeric mixture consisting of from 75 to 95% of compound of formula (2a) and from 5 to 25% of a compound of formula (2b) with methylamine, in a suitable solvent, to form a sertraline-imine isomeric mixture consisting of from 75 to 95% of formula (1a) and from 5 to 25% of formula (1b)(A1), or reacting an isomeric mixture consisting of from 75 to 95% of a compound of formula (2a) and from 5 to 25% of a compound of formula (2b) with methylamine, in a suitable solvent, using suitable methods of isolation to form an enriched sertraline-imine isomeric mixture, consisting of >99% of a compound of formula (1a) and
摘要翻译：描述了制备式（1a）化合物的方法，其包括将由75至95％的式（2a）化合物和5至25％的式（2b）化合物组成的异构体混合物与甲胺在合适的溶剂中形成由75至95％的式（1a）和5至25％的式（1b）（A1）组成的舍曲林 - 亚胺异构体混合物，或将由75 至95％的式（2a）化合物和5至25％的式（2b）化合物与甲胺在合适的溶剂中，使用合适的分离方法形成富集的舍曲林 - 亚胺异构体混合物，其由 > 99％的式（1a）化合物和<1％式（1b）化合物（A2）的化合物; 然后根据反应路线（A1）或（A2）得到的舍曲林 - 亚胺异构体混合物在合适的溶剂中，按照式（Ⅰ）中式（Ⅰa）中R1，R2 和R 3各自独立地为氢，卤素，三氟甲基或C 1 -C 4烷氧基，式（1b），（2a）和（2b）如说明书中所定义。

3. 发明授权

US06872853B1 Polymorphic forms of sertraline hydrochloride 失效
标题翻译：盐酸舍曲林的多形态
公开(公告)号：US06872853B1
公开(公告)日：2005-03-29
申请号：US10111947
申请日：2000-10-23
申请人： Paul Adriaan Van Der Schaaf , Franz Schwarzenbach , Hans-Jörg Kirner , Martin Szelagiewicz , Claudia Marcolli , Andreas Burkhard , Regine Peter
发明人： Paul Adriaan Van Der Schaaf , Franz Schwarzenbach , Hans-Jörg Kirner , Martin Szelagiewicz , Claudia Marcolli , Andreas Burkhard , Regine Peter
IPC分类号： A61P3/04 , A61K31/135 , A61K31/137 , A61P15/10 , A61P25/22 , A61P25/24 , A61P25/30 , C07C209/84 , C07C211/42
CPC分类号： A61K31/137 , A61K31/135 , C07C211/42 , C07C2602/10
摘要： A cystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.
摘要翻译：发现盐酸舍曲林的结晶形式，以下称为具有令人惊奇地增加药物吸收速率的溶出速率的多晶型CSC2。此外，盐酸舍曲林盐酸盐溶剂合物的不同结晶形式，盐酸舍曲林盐酸盐水合物的结晶形式，以下称为多晶型CSC1，制备盐酸舍曲林无定形形式的方法，以及制备多晶型I， II，V和T1。

4. 发明授权

US06939992B2 Polymorphic forms of sertraline hydrochloride 失效
标题翻译：盐酸舍曲林的多形态
公开(公告)号：US06939992B2
公开(公告)日：2005-09-06
申请号：US10736195
申请日：2003-12-15
申请人： Paul Adriaan Van Der Schaaf , Franz Schwarzenbach , Hans-Jörg Kirner , Martin Szelagiewicz , Claudia Marcolli , Andreas Burkhard
发明人： Paul Adriaan Van Der Schaaf , Franz Schwarzenbach , Hans-Jörg Kirner , Martin Szelagiewicz , Claudia Marcolli , Andreas Burkhard
IPC分类号： A61P3/04 , A61K31/135 , A61K31/137 , A61P15/10 , A61P25/22 , A61P25/24 , A61P25/30 , C07C209/84 , C07C211/42 , C07C211/00
CPC分类号： A61K31/137 , A61K31/135 , C07C211/42 , C07C2602/10
摘要： A crystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug.Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.
摘要翻译：发现盐酸舍曲林的结晶形式，以下称为具有令人惊奇地增加药物吸收速率的溶出速率的多晶型CSC2。此外，盐酸舍曲林盐酸盐溶剂合物的不同结晶形式，盐酸舍曲林盐酸盐水合物的结晶形式，以下称为多晶型CSC1，制备盐酸舍曲林无定形形式的方法，以及制备多晶型I， II，V和T1。

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