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1. 发明授权

US5716960A Crystalline trimetrexate salts and the process for making the same 失效
公开(公告)号：US5716960A
公开(公告)日：1998-02-10
申请号：US372254
申请日：1995-01-13
申请人： Paul Kennedy , Ingomar Grafe , Johann Peter Morsdorf , Kurt-Henning Ahrens
发明人： Paul Kennedy , Ingomar Grafe , Johann Peter Morsdorf , Kurt-Henning Ahrens
IPC分类号： A61K31/505 , A61K31/517 , C07D239/95 , A61K31/495
CPC分类号： C07D239/95
摘要： The present invention provides for a crystalline form of trimetrexate either as a glucuronate, acetate, hydrochloride, methanosulfonate or lactate salt, which can be processed galenically as a stable, well-defined solid substance and processes for producing the crystalline forms. Such crystalline forms allow for prolonged stability in storage and for oral and intravenous administration of the drug.

2. 发明授权

US4973755A Stable solvent adducts of Z-1-(p-.beta.-dimethylaminoethoxy-phenyl)-1-(p-hydroxyphenyl)-2-phenyl-b ut-1-ene 失效
标题翻译： Z-1-（对 - 二甲基氨基乙氧基 - 苯基）-1-（对羟基苯基）-2-苯基 - 丁-1-烯的稳定的溶剂加合物
公开(公告)号：US4973755A
公开(公告)日：1990-11-27
申请号：US183068
申请日：1988-04-19
申请人： Ingomar Grafe , Helmut Schickaneder , Peter W. Jungblut , Kurt H. Ahrens
发明人： Ingomar Grafe , Helmut Schickaneder , Peter W. Jungblut , Kurt H. Ahrens
IPC分类号： A61K31/135 , A61P35/00 , C07C67/00 , C07C213/00 , C07C213/02 , C07C217/16 , C07C217/20 , C07C217/54
CPC分类号： A61K31/135
摘要： This invention relates to new stereochemically pure and stable adducts of Z-1-(p-.beta.-dimethylaminoethoxyphenyl)-1-(p-hydroxyphenyl)-2-phenyl-but-1-ene and certain solvents which by virtue of their marked antioestrogenic activities may be used for the therapeutic treatment of benign breast diseases and hormone-dependent mammary tumors, in particularly by percutaneous application.
摘要翻译：本发明涉及Z-1-（对 - β-二甲基氨基乙氧基苯基）-1-（对羟基苯基）-2-苯基 - 丁-1-烯的新的立体化学纯的和稳定的加合物以及由于其明显的抗雌激素活动可用于治疗良性乳腺疾病和激素依赖性乳腺肿瘤，特别是通过经皮应用。

3. 发明授权

US6140334A Polymorphic form of doxazosin mesylate (form III) 失效
标题翻译：甲磺酸多沙唑嗪的多晶型（形式III）
公开(公告)号：US6140334A
公开(公告)日：2000-10-31
申请号：US992251
申请日：1997-12-17
申请人： Johann Peter Morsdorf , Ingomar Grafe
发明人： Johann Peter Morsdorf , Ingomar Grafe
IPC分类号： A61K31/505 , A61P9/12 , A61P13/02 , A61P15/00 , C07D405/12 , C07D403/14 , A61K31/517
CPC分类号： C07D405/12
摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 8.49.degree., 11.72.degree., 16.03.degree., 18.29.degree., 21.03.degree., 22.87.degree. and 25.02.degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.
摘要翻译：描述了新的结晶和无水形式的甲磺酸多沙唑嗪。新型结晶无水，其特征在于X射线光谱中高强度的以下反射位置：8.49°，11.72°，16.03°，18.29°，21.03°，22.87°和25.02°。由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

4. 发明授权

US06017921A Crystalline trimetrexate salts and the process for making the same 失效
标题翻译：结晶三甲氧甲酸盐及其制备方法
公开(公告)号：US06017921A
公开(公告)日：2000-01-25
申请号：US18515
申请日：1998-02-04
申请人： Paul Kennedy , Ingomar Grafe , Johann Peter Morsdorf , Kurt-Henning Ahrens
发明人： Paul Kennedy , Ingomar Grafe , Johann Peter Morsdorf , Kurt-Henning Ahrens
IPC分类号： A61K31/505 , A61K31/517 , C07D239/95
CPC分类号： C07D239/95
摘要： The present invention provides for a crystalline form of trimetrexate either as a glucuronate, acetate, hydrochloride, methanosulfonate or lactate salt, which can be processed galenically as a stable, well-defined solid substance and processes for producing the crystalline forms. Such crystalline forms allow for prolonged stability in storage and for oral and intravenous administration of the drug.
摘要翻译：本发明提供了作为葡萄糖醛酸盐，乙酸盐，盐酸盐，甲磺酸盐或乳酸盐的三甲氧
磷酸盐的结晶形式，其可以作为稳定的，明确定义的固体物质进行加成以及制备结晶形式的方法。这种结晶形式允许在储存和口服和静脉内施用药物时延长稳定性。

5. 发明授权

US4978773A Process for the preparation of 2,6-dichlorodiphenylaminoacetic acid derivatives 失效
标题翻译： 2,6-二氯二苯基氨基乙酸衍生物的制备方法
公开(公告)号：US4978773A
公开(公告)日：1990-12-18
申请号：US369618
申请日：1989-06-21
申请人： Ingomar Grafe , Helmut Schickaneder , Kurt H. Ahrens
发明人： Ingomar Grafe , Helmut Schickaneder , Kurt H. Ahrens
IPC分类号： C07D209/46 , A61K31/195 , C07C67/31 , C07C69/712 , C07C209/50 , C07C211/45 , C07C227/12 , C07C227/18 , C07C227/22 , C07C229/42 , C07C235/16 , C07C235/24
CPC分类号： C07C227/22 , C07C227/18 , C07C229/42
摘要： A new process for the preparation of 2,6-dichlorodiphenylamine derivatives is described, which process provides the desired active compound in a high yield and with a very high degree of purity by a technically simple and realizable procedure.
摘要翻译：描述了制备2,6-二氯二苯胺衍生物的新方法，该方法通过技术上简单且可实现的方法以高产率提供所需的活性化合物并具有非常高的纯度。

6. 发明授权

US4816455A Crystalline, anhydrous sigma-form of 2-(4-(2-furoyl)-(2-piperazin)-1-yl)-4-amino-6,7-dimethoxy-quinazoline hydrochloride and a process for its preparation 失效
标题翻译： 2-（4-（2-糠基） - （2-哌嗪）-1-基）-4-氨基-6,7-二甲氧基 - 喹唑啉的结晶无水西格玛形式及其制备方法
公开(公告)号：US4816455A
公开(公告)日：1989-03-28
申请号：US21161
申请日：1987-03-03
申请人： Helmut Schickaneder , Ingomar Grafe , Kurt H. Ahrens
发明人： Helmut Schickaneder , Ingomar Grafe , Kurt H. Ahrens
IPC分类号： A61K31/505 , C07D405/12 , C07D405/14
CPC分类号： C07D405/12 , A61K31/505
摘要： A new anhydrous crystalline form of prazosine hydrochloride characterized by the following bands in the infra-red spectrum in potassium bromide is described:3445 cm.sup.-1 (2.90 .mu.m),1010 cm.sup.-1 (9.90 .mu.m) (duplet), and768 cm.sup.-1 (13.03 .mu.m).This new form is distinguished by its surprisingly great stability in storage compared with known polymorphous forms of prazosine.
摘要翻译：描述了一种新的无水结晶形式的盐酸哌唑嗪，其特征在于溴化钾在红外光谱中具有以下条带：3445cm-1（2.90μm），1010cm-1（9.90μm）（双重）和768 cm-1（13.03μm）。与已知的多形态的吡唑嗪相比，这种新形式的特征在于其在储存中令人惊奇的极大的稳定性。

7. 发明授权

US6133269A Polymorphic form of doxazosin mesylate (form II) 失效
标题翻译：甲磺酸多沙唑嗪多晶型（Ⅱ型）
公开(公告)号：US6133269A
公开(公告)日：2000-10-17
申请号：US992474
申请日：1997-12-17
申请人： Johann Peter Morsdorf , Ingomar Grafe
发明人： Johann Peter Morsdorf , Ingomar Grafe
IPC分类号： A61K31/505 , A61P13/02 , A61P15/00 , C07D405/12 , C07D407/14 , A61K31/517
CPC分类号： C07D405/12
摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 10.68.degree., 14.45.degree., 17.37.degree., 23.45.degree., 23.82.degree. and 24.30 .degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.
摘要翻译：描述了新的结晶和无水形式的甲磺酸多沙唑嗪。新型结晶和无水，其特征在于X射线谱由高和中强度的以下反射位置：10.68°，14.45°，17.37°，23.45°，23.82°和24.30°。由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

8. 发明授权

US06130218A Polymorphic form of doxazosin mesylate (Form I) 失效
标题翻译：甲磺酸多沙唑嗪的多晶型（I型）
公开(公告)号：US06130218A
公开(公告)日：2000-10-10
申请号：US992252
申请日：1997-12-17
申请人： Johann Peter Morsdorf , Ingomar Grafe
发明人： Johann Peter Morsdorf , Ingomar Grafe
IPC分类号： A61K31/505 , A61P9/12 , A61P13/02 , A61P15/00 , C07D405/12 , C07D407/14 , A61K31/517
CPC分类号： C07D405/12
摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 15.40.degree., 16.85.degree., 18.06.degree., 24.15.degree. and 25.81.degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.
摘要翻译：描述了新的结晶和无水形式的甲磺酸多沙唑嗪。新型结晶无水，其特征在于其X射线光谱由高，中强度的以下反射位置：15.40°，16.85°，18.06°，24.15°和25.81°。由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

9. 发明授权

US06258952B1 Thermally stable trimetrexates and processes for producing the same 失效
标题翻译：热稳定性三甲氧戊酸及其制备方法
公开(公告)号：US06258952B1
公开(公告)日：2001-07-10
申请号：US09436708
申请日：1999-11-09
申请人： Martin Stogniew , Ingomar Grafe , Johann Mörsdorf
发明人： Martin Stogniew , Ingomar Grafe , Johann Mörsdorf
IPC分类号： A61K31517
CPC分类号： C07D239/95
摘要： The present invention provides for thermally stable forms of 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P{overscore (1)}(#2) and having a triclinic cell with dimensions of about a=7.699 Å, b=9.606 Å and c=13.012 Å is disclosed. A novel Schiff base compound, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyphenylimino)-methinyl]quinazoline, is also disclosed. The present invention further provides novel methods of producing stable trimetrexate free base compounds, including crystalline trimetrexate monohydrate. The crystalline monohydrate form provides increased stability over the anhydrous form.
摘要翻译：本发明提供2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯胺基）甲基]喹唑啉或三甲氧甲酸酯的热稳定形式。属于空间群P {overscore（1）}（＃2）的结晶的2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯胺基）甲基]喹唑啉一水合物或三甲
铵一水合物具有尺寸为约a =7.699，b =9.606和c =13.012的三斜晶细胞。还公开了一种新型席夫碱化合物，2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯基亚氨基） - 甲基苯基]喹唑啉。本发明还提供了生产稳定的三甲氧铵游离碱化合物，包括结晶三甲氧甲酸一水合物的新方法。结晶一水合物形式比无水形式提供了更高的稳定性。

10. 发明授权

US6017922A Thermally stable trimetrexates and processes for producing the same 失效
标题翻译：热稳定性三甲氧戊酸及其制备方法
公开(公告)号：US6017922A
公开(公告)日：2000-01-25
申请号：US80290
申请日：1998-05-18
申请人： Martin Stogniew , Ingomar Grafe , Johann Morsdorf
发明人： Martin Stogniew , Ingomar Grafe , Johann Morsdorf
IPC分类号： A61K31/517 , A61P31/04 , A61P33/10 , A61P35/00 , C07D239/95 , A61K31/505
CPC分类号： C07D239/95
摘要： The present invention provides for thermally stable forms of 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P1(#2) and having a triclinic cell with dimensions of about a=7.699 .ANG., b=9.606 .ANG. and c=13.012 .ANG. is disclosed. A novel Schiff base compound, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyphenylimino)-methinyl]quinazoline, is also disclosed. The present invention further provides novel methods of producing stable trimetrexate free base compounds, including crystalline trimetrexate monohydrate. The crystalline monohydrate form provides increased stability over the anhydrous form.
摘要翻译：本发明提供2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯胺基）甲基]喹唑啉或三甲氧甲酸酯的热稳定形式。属于空间群P + E，ov 1 + EE（＃2）的结晶的2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯胺基）甲基]喹唑啉一水合物或三甲氧甲酸一水合物，并且具有尺寸为约a = 7.699 ANGSTROM，b = 9.606 ANGSTROM和c = 13.012 ANGSTROM的三斜晶胞。还公开了一种新型席夫碱化合物，2,4-二氨基-5-甲基-6 - [（3,4,5-三甲氧基苯基亚氨基） - 甲基苯基]喹唑啉。本发明还提供了生产稳定的三甲氧铵游离碱化合物，包括结晶三甲氧甲酸一水合物的新方法。结晶一水合物形式比无水形式提供了更高的稳定性。

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