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1. 发明授权

US07799770B2 Solid body forms of mesoprogestin 11β-{4E-(hydroxyiminomethyl)-phenyl}-17α methoxymethyl-17β-methoxy-estra-4,9-dien-3-one 有权
标题翻译：中孕素11和bgr的固体形式 - {4E-（羟基亚氨基甲基） - 苯基}-17α甲氧基甲基-17β-甲氧基 - 雌-4,9-二烯-3-酮
公开(公告)号：US07799770B2
公开(公告)日：2010-09-21
申请号：US10296463
申请日：2001-05-09
申请人： Detlef Grawe , Peter Hosel , Uwe Muller , Gabriele Winter
发明人： Detlef Grawe , Peter Hosel , Uwe Muller , Gabriele Winter
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J41/00 , C07J41/0083 , Y10S514/843
摘要： The invention relates to novel solid body forms of mesoprogestin 11β-[4E-(hydroxyiminomethyl)-phenyl]-17α-methoxymethyl-17β-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.
摘要翻译：本发明涉及中孕素11β-[4E-（羟基亚氨基甲基） - 苯基]-17α-甲氧基甲基-17β-甲氧基 - 雌-4,9-二烯-3-酮（肟J 867）的新型固体形式，特别是化合物J 867的高纯度和稳定的无定形或高度结晶形式（无溶剂/无水合物）。本发明还涉及制备所述新型固体形式的方法及其在药物组合物中的用途。新颖的固体形式的特征在于表现出高度的稳定性。猕猴J 867的固体形式特别可用于生育控制和激素替代治疗领域。

2. 发明授权

US06902741B1 Laminates containing an active substance transdermal system 有权
标题翻译：含有活性物质透皮系统的层压体
公开(公告)号：US06902741B1
公开(公告)日：2005-06-07
申请号：US09913112
申请日：2000-02-08
申请人： Detlef Grawe , Peter Hoesel , Wilfried Fischer
发明人： Detlef Grawe , Peter Hoesel , Wilfried Fischer
IPC分类号： A61K9/14 , A61K9/70 , A61K31/568 , A61P5/24 , A61F13/02 , A61L15/16
CPC分类号： A61K9/7053 , A61K9/146
摘要： The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.
摘要翻译：透皮系统包括含有性激素的粘合剂基质，其在溶解或分散形式的亲水性非交联聚合物中含有性激素的夹杂物。夹杂物的浓度为性激素的20〜90重量％，超过50重量％的非晶体。亲水性非交联聚合物可以是聚乙烯吡咯烷酮，甲基纤维素，乙基纤维素或羟乙基纤维素。粘合剂基质可以是聚异丁烯，乙烯 - 乙酸乙烯酯共聚物或聚苯乙烯 - 丁二烯嵌段共聚物。

3. 发明申请

US20110144071A1 CRYSTALLINE ACTIVE INGREDIENT MICROPARTICLES, METHOD FOR PRODUCING THE SAME AND USE THEREOF IN DRUGS 有权
标题翻译：晶体活性成分微生物，其生产方法及其在药物中的应用
公开(公告)号：US20110144071A1
公开(公告)日：2011-06-16
申请号：US13058168
申请日：2009-06-30
申请人： Detlef Grawe , Sabine Gliesing , Robert Eilers
发明人： Detlef Grawe , Sabine Gliesing , Robert Eilers
IPC分类号： A61K31/58 , C07J53/00 , C07J1/00 , C07J7/00 , C07J3/00 , A61K31/56 , A61P5/00
CPC分类号： A61K9/1694 , A61K9/1652 , H04R5/00
摘要： A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.
摘要翻译：一种生产具有非常窄尺寸分布的活性物质的高度结晶和稳定的微粒的方法。微粒从由活性物质的一次粒子，活性物质的溶液，活性物质的非溶剂和惰性成形体构成的悬浮液中结晶出来。所得到的微粒在很大程度上高度稳定地与活性物质的物理化学性质无关，并且特别适用于药物的快速释放剂型。

4. 发明申请

US20110065952A1 ARRANGEMENT AND METHOD FOR PRODUCING HIGH-PURITY CRYSTALS 有权
标题翻译：用于生产高纯度晶体的布置和方法
公开(公告)号：US20110065952A1
公开(公告)日：2011-03-17
申请号：US12992861
申请日：2009-04-29
申请人： Detlef Grawe , Robert Eilers , Sabine Gliesing
发明人： Detlef Grawe , Robert Eilers , Sabine Gliesing
IPC分类号： C07C63/00 , B01D9/00
CPC分类号： B01D9/0022 , B01D9/004 , B01D9/0059 , B01D9/0063
摘要： An arrangement and a method for producing high-purity crystals, such as temperature-sensitive pharmaceutical agents, in a countercurrent crystallization process. The arrangement comprises a plurality of crystallizers, mother liquor lines, each of which has a shut-off valve, and crystallization product lines, each of which has a shut-off valve, so that a mother liquor flow can be generated which is directed from a crystallizer to the second-next crystallizer in the direction of decreasing purity, and a crystallization product flow can be generated which is directed from a to dissolved crystallization product that is about to crystallize to the next crystallizer in the direction of higher purity.
摘要翻译：在逆流结晶方法中制备高纯度晶体（如温度敏感性药剂）的方法和装置。该装置包括多个结晶器，每个具有截止阀的母液液体管线和每个都具有截止阀的结晶产物管线，从而可以产生从母液中引导的母液流在纯度降低的方向向第二次结晶器的结晶器，并且可以产生结晶产物流，其从高纯度方向结晶到下一个结晶器的溶解结晶产物。

5. 发明授权

US09173843B2 Crystalline active ingredient microparticles, method for producing the same and use thereof in drugs 有权
标题翻译：结晶活性成分微粒，其制备方法及其在药物中的应用
公开(公告)号：US09173843B2
公开(公告)日：2015-11-03
申请号：US13058168
申请日：2009-06-30
申请人： Detlef Grawe , Sabine Gliesing , Robert Eilers
发明人： Detlef Grawe , Sabine Gliesing , Robert Eilers
IPC分类号： A61K31/58 , A61K31/56 , A61P5/00 , C07J53/00 , C07J1/00 , C07J7/00 , C07J3/00 , A61K9/16 , H04R5/00
CPC分类号： A61K9/1694 , A61K9/1652 , H04R5/00
摘要： A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare are highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.
摘要翻译：一种生产具有非常窄尺寸分布的活性物质的高度结晶和稳定的微粒的方法。微粒从由活性物质的一次粒子，活性物质的溶液，活性物质的非溶剂和惰性成形体构成的悬浮液中结晶出来。所得的微粒野兔在很大程度上与活性物质的物理化学性质无关，高度稳定，特别适用于药物的快速释放剂型。

6. 发明申请

US20130040141A1 METHOD FOR PRODUCING CRYSTALLINE ACTIVE INGREDIENT PARTICLES 有权
标题翻译：生产结晶活性成分颗粒的方法
公开(公告)号：US20130040141A1
公开(公告)日：2013-02-14
申请号：US13640025
申请日：2011-03-30
申请人： Detlef Grawe , Sabine Gliesing
发明人： Detlef Grawe , Sabine Gliesing
IPC分类号： A61K9/16 , B02C23/18 , B02C19/18
CPC分类号： B01D9/0013 , A61K9/1688 , B01D9/0036 , B01D9/0054 , B01D9/0081 , Y10T428/2982
摘要： A method and device for producing crystalline active ingredient particles. The active ingredient is crystallized from a supersaturated solution on the surface of particles of the active ingredient. A suspension of active ingredient particles is subjected to wet grinding in a supersaturated solution of the active ingredient in a first module. At least a part of the suspension is fed from the first module into the second module where it is cooled and simultaneously subjected to ultrasound. The suspension is fed back into the first module after cooling and being subjected to ultrasound. Active ingredient solution and optionally antisolvent are added to the suspension and active ingredient particles and liquid phase are extracted. A relative supersaturation of the active ingredient in the liquid phase of the suspension, relative to the entire liquid phase, is ≦90%, and the extracted active ingredient particles comprise a mean particle size of 10-500 μm.
摘要翻译：一种生产结晶活性成分颗粒的方法和装置。活性成分从活性成分颗粒表面的过饱和溶液中结晶。将活性成分颗粒的悬浮液在第一模块中的活性成分的过饱和溶液中进行湿磨。悬浮液的至少一部分从第一模块进入第二模块，在其中冷却并同时进行超声波。冷却后将悬浮液反馈回第一组件并进行超声波处理。将活性成分溶液和任选的反溶剂加入悬浮液中，提取活性成分颗粒和液相。相对于整个液相，悬浮液的液相中活性成分的相对过饱和度为90％，提取的活性成分颗粒的平均粒径为10-500μm。

7. 发明申请

US20090054387A1 Method for preparing 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxestra-4,9-dien-11beta-yl]benzaldehyde (E)-oxime (asoprisnil) 审中-公开
标题翻译：制备4- [17β-甲氧基-17α-甲氧基甲基-3-硫代雌-4,9-二烯-11β-基]苯甲醛（E） - 肟（asoprisnil）
公开(公告)号：US20090054387A1
公开(公告)日：2009-02-26
申请号：US11785421
申请日：2007-04-17
申请人： Detlef Grawe , Sabine Gliesing , Hagen Gerecke , Peter Heesel , Uwe Mueller , Thomas Michel , Robert Eilers
发明人： Detlef Grawe , Sabine Gliesing , Hagen Gerecke , Peter Heesel , Uwe Mueller , Thomas Michel , Robert Eilers
IPC分类号： A61K31/56 , C07J3/00
CPC分类号： C07J3/00 , Y10T428/2982
摘要： The present invention relates to a method for the reliable and reproducible preparation of 4-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-11β-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
摘要翻译：本发明涉及一种可靠和可重复地制备4- [17β-甲氧基-17α-甲氧基甲基-3-氧代雌-4,9-二烯-11β-基]苯甲醛（E） - 肟（asoprisnil）的方法试点和制造规模。通过该方法制备的麻醉药具有非常好的物理稳定性，因此特别适用于制备固体药物形式（片剂，包衣片剂等）。

8. 发明授权

US09095783B2 Arrangement and method for producing high-purity crystals 有权
标题翻译：制备高纯度晶体的方法和方法
公开(公告)号：US09095783B2
公开(公告)日：2015-08-04
申请号：US12992861
申请日：2009-04-29
申请人： Detlef Grawe , Robert Eilers , Sabine Gliesing
发明人： Detlef Grawe , Robert Eilers , Sabine Gliesing
IPC分类号： B01D9/02 , B01D9/00
CPC分类号： B01D9/0022 , B01D9/004 , B01D9/0059 , B01D9/0063
摘要： An arrangement and a method for producing high-purity crystals, such as temperature-sensitive pharmaceutical agents, in a countercurrent crystallization process. The arrangement comprises a plurality of crystallizers, mother liquor lines, each of which has a shut-off valve, and crystallization product lines, each of which has a shut-off valve, so that a mother liquor flow can be generated which is directed from a crystallizer to the second-next crystallizer in the direction of decreasing purity, and a crystallization product flow can be generated which is directed from a to dissolved crystallization product that is about to crystallize to the next crystallizer in the direction of higher purity.
摘要翻译：在逆流结晶方法中制备高纯度晶体（如温度敏感性药剂）的方法和装置。该装置包括多个结晶器，每个具有截止阀的母液液体管线和每个都具有截止阀的结晶产物管线，从而可以产生从母液中引导的母液流在纯度降低的方向向第二次结晶器的结晶器，并且可以产生结晶产物流，其从高纯度方向结晶到下一个结晶器的溶解结晶产物。

9. 发明授权

US07192942B2 Process for production of crystals of 11μ-benzaldoxim-estra-4,9-diene derivatives, crystals obtained thereby and pharmaceutical preparations containing them 有权
标题翻译：制备11M-亚苄基肟 - 雌-4,9-二烯衍生物的晶体的方法，由此获得的晶体和含有它们的药物制剂
公开(公告)号：US07192942B2
公开(公告)日：2007-03-20
申请号：US10417559
申请日：2003-04-17
申请人： Detlef Grawe , Hagen Gerecke , Peter Hoesel , Annette Eichardt , Sabine Gliesing , Uwe Mueller
发明人： Detlef Grawe , Hagen Gerecke , Peter Hoesel , Annette Eichardt , Sabine Gliesing , Uwe Mueller
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J41/0083 , A61K9/14
摘要： The process for making crystals of a 11 β-benzaldoxim-estra-4,9-diene derivative having an average particle size of from 3 μm to 25 μm and a maximum particle size of 100 μm, includes subjecting a supersaturated solution containing a special 11β-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, In order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described and are part of the invention.
摘要翻译：制备平均粒度为3μm〜25μm，最大粒径为100μm的11β-苯甲醛肟 - 雌-4,9-二烯衍生物的晶体的方法包括使含有特殊的11beta的过饱和溶液 - 苯甲醛 - 雌-4,9-二烯衍生物在结晶时通过湿式研磨装置进行湿法研磨，以获得初级颗粒悬浮液。还描述了根据该方法获得的晶体和含有它们的药物制剂，并且是本发明的一部分。

10. 发明授权

US06974885B2 Method for isolating pharmaceutically exploitable etidronate disodium 失效
标题翻译：用于分离药学上可利用的依替膦酸二钠的方法
公开(公告)号：US06974885B2
公开(公告)日：2005-12-13
申请号：US10381535
申请日：2001-09-28
申请人： Detlef Grawe , Barbara Schmidt , Harald Raethe
发明人： Detlef Grawe , Barbara Schmidt , Harald Raethe
IPC分类号： C07F9/38 , C07C409/04
CPC分类号： C07F9/386
摘要： 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.
摘要翻译：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。

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