公开(公告)号：US06974885B2

公开(公告)日：2005-12-13

申请号：US10381535

申请日：2001-09-28

Applicant: Detlef Grawe ,  Barbara Schmidt ,  Harald Raethe

Inventor： Detlef Grawe ,  Barbara Schmidt ,  Harald Raethe

IPC: C07F9/38 ,  C07C409/04

CPC classification number: C07F9/386

Abstract: The method of isolating an anhydrous etidronate disodium particulate includes preparing a liquid-liquid dispersion consisting of an aqueous-organic phase and an etidronate-disodium-salt-containing aqueous phase; adjusting a temperature of the liquid-liquid dispersion to between 0 and 30° C. and intensely agitating so that a coarse-particle fraction precipitates from the liquid-liquid dispersion, then drawing off a fine-particle suspension and allowing a fine-particle fraction to precipitate from it and filtering and drying the coarse particle fraction. In a preferred embodiment the fine-particle fraction is separated from the fine-particle suspension for recycling The resulting anhydrous etidronate disodium particulate has a grain size of from about 0.1 to 1 mm and a bulk density of 0.4 to 0.6 g/cm2 with good properties for pharmaceutical applications.

Abstract translation: 分离无水依替膦酸二钠颗粒的方法包括制备由水 - 有机相和含有硝酸根 - 二钠盐的水相组成的液 - 液分散体; 将液 - 液分散体的温度调节在0和30℃之间并强烈搅拌，使得粗液颗粒分数从液 - 液分散体中沉淀出来，然后除去细粒悬浮液，并使细颗粒分数 从中沉淀并过滤并干燥粗颗粒级分。 在一个优选的实施方案中，将细颗粒级分与细颗粒悬浮液分离以进行再循环。得到的无水埃硝膦酸二钠颗粒的颗粒尺寸为约0.1至1mm，堆积密度为0.4至0.6g / 2 具有良好的药物应用性能。

公开(公告)号：US20070072836A1

公开(公告)日：2007-03-29

申请号：US11352898

申请日：2006-02-13

Applicant: Sabine Fricke ,  Hagen Gericke ,  Ralf Ladwig ,  Alexander Buske ,  Harald Raethe

Inventor： Sabine Fricke ,  Hagen Gericke ,  Ralf Ladwig ,  Alexander Buske ,  Harald Raethe

IPC: A61K31/57

CPC classification number: A61K31/57 ,  A61K31/567 ,  A61K2300/00

Abstract: The solid peroral contraceptive contains an effective ingredient combination of dienogest in a daily dosage of equal to or less than 2.0 mg and ethinyl estradiol in a daily dosage of less than 0.03 mg together with one or more pharmaceutically acceptable carriers. The dienogest is released in two stages, while the ethinyl estradiol is released with the first stage portion of the dienogest.

Abstract translation: 固体口服避孕药含有日剂量等于或小于2.0mg的地那诺酯和乙炔雌二醇的有效成分组合，日剂量小于0.03mg，以及一种或多种药学上可接受的载体。 乙酰雌二醇分两个阶段释放，而乙炔雌二醇与去乙内酯的第一阶段部分一起释放。

公开(公告)号：US20060205701A1

公开(公告)日：2006-09-14

申请号：US11354681

申请日：2006-03-27

Applicant: Sabine Fricke ,  Hagan Gericke ,  Ralf Ladwig ,  Alexander Buske ,  Harald Raethe

Inventor： Sabine Fricke ,  Hagan Gericke ,  Ralf Ladwig ,  Alexander Buske ,  Harald Raethe

IPC: A61K31/56

CPC classification number: A61K31/565 ,  A61K31/56 ,  A61K31/567 ,  A61K31/57 ,  A61K2300/00

Abstract: The solid peroral contraceptive contains an effective ingredient combination of dienogest in a daily dosage of equal to or less than 2.0 mg and ethinyl estradiol in a daily dosage of less than 0.03 mg together with one or more pharmaceutically acceptable carriers. The dienogest is released in two stages, while the ethinyl estradiol is released with the first stage portion of the dienogest.

Abstract translation: 固体口服避孕药含有日剂量等于或小于2.0mg的地那诺酯和乙炔雌二醇的有效成分组合，日剂量小于0.03mg，以及一种或多种药学上可接受的载体。 乙酰雌二醇分两个阶段释放，而乙炔雌二醇与去乙内酯的第一阶段部分一起释放。

公开(公告)号：US5831104A

公开(公告)日：1998-11-03

申请号：US303662

申请日：1994-09-09

Applicant: Sven Ring ,  Gerhard Teichmueller ,  Gisela Weber ,  Sigfrid Schwarz ,  Bernd Erhart ,  Bernd Undeutsch ,  Harald Raethe ,  Peter Moellmann ,  Carmen Pfeiffer ,  Hans-Joachim Palme

Inventor： Sven Ring ,  Gerhard Teichmueller ,  Gisela Weber ,  Sigfrid Schwarz ,  Bernd Erhart ,  Bernd Undeutsch ,  Harald Raethe ,  Peter Moellmann ,  Carmen Pfeiffer ,  Hans-Joachim Palme

IPC: C07J1/00 ,  C07J11/00 ,  C07J71/00 ,  C07J21/00

CPC classification number: C07J71/0026 ,  C07J1/007 ,  C07J11/00

Abstract: The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel). Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.

Abstract translation: 本发明涉及通式I的新型类固醇中间产物（I）可根据本发明分离的类固醇中间体产物适用于合成13-乙基-11-亚甲基-18,19-双 -17α-孕甾-4-烯-20- -17-醇（去氧孕烯）。 另外，对通式I的类固醇中间产物的制造方法进行了说明。 11-氧基类固醇的烯化在超声波的影响下进行。