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1. 发明授权

US07659311B2 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 有权
标题翻译：用于递送活性剂的二钠盐，一水合物和乙醇溶剂化物
公开(公告)号：US07659311B2
公开(公告)日：2010-02-09
申请号：US12111750
申请日：2008-04-29
申请人： William Elliott Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
发明人： William Elliott Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C231/00 , A61K9/2013 , A61K47/183 , C07C235/60 , C07D265/26 , C07C235/58
摘要： The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above. The invention also provides a hydrate of a disodium salt of a delivery agent of the formula above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.
摘要翻译：发明人已经发现，某些递送剂的二钠盐比相应的单钠盐具有惊人的更大的递送活性剂的功效。此外，本发明人已经发现，这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。递送剂具有下式：其中R 1，R 2，R 3和R 4独立地是氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基; 取代或未取代的C 2 -C 16亚烯基，取代或未取代的C 1 -C 12烷基（亚芳基）或取代或未取代的芳基（C 1 -C 12亚烷基）。本发明的水合物和溶剂合物对于递送活性剂（例如肝素和降钙素）比其相应的单钠盐和游离酸具有惊人的更大的功效。本发明提供了一种醇溶剂合物，例如乙醇溶剂化物，其具有上式的递送剂的二钠盐。本发明还提供了上式的递送剂的二钠盐的水合物。优选的递送剂包括但不限于N-（5-氯水杨酰基）-8-氨基辛酸（5-CNAC），N-（10- [2-羟基苯甲酰基]氨基）癸酸（SNAD）和N - （8- [2-羟基苯甲酰基]氨基）辛酸酯（SNAC）。本发明还提供了制备二钠盐，乙醇溶剂合物和水合物的方法以及含有二钠盐，乙醇溶剂合物和/或水合物的组合物。

2. 发明授权

US08658695B2 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 有权
标题翻译：用于递送活性剂的二钠盐，一水合物和乙醇溶剂化物
公开(公告)号：US08658695B2
公开(公告)日：2014-02-25
申请号：US13481310
申请日：2012-05-25
申请人： William Elliott Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
发明人： William Elliott Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C231/00 , A61K9/2013 , A61K47/183 , C07C235/60 , C07D265/26 , C07C235/58
摘要： The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.
摘要翻译：发明人已经发现，某些递送剂的二钠盐比相应的单钠盐具有惊人的更大的递送活性剂的功效。此外，本发明人已经发现，这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。优选的递送剂包括但不限于N-（5-氯水杨酰基）-8-氨基辛酸（5-CNAC），N-（10- [2-羟基苯甲酰基]氨基）癸酸（SNAD）和N - （8- [2-羟基苯甲酰基]氨基）辛酸酯（SNAC）。本发明还提供了制备二钠盐，乙醇溶剂合物和水合物的方法以及含有二钠盐，乙醇溶剂化物和/或水合物的组合物。

3. 发明申请

US20080269108A1 Crystalline forms of the Di-Sodium Salt of N-(5-Chlorosalicyloyl)-8-Aminocaprylic Acid 有权
标题翻译： N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶形式
公开(公告)号：US20080269108A1
公开(公告)日：2008-10-30
申请号：US12067239
申请日：2006-09-18
申请人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
发明人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
IPC分类号： A61K47/18 , C07C229/00 , A61K38/22 , A61K38/29 , A61K38/27 , A61K38/28
CPC分类号： A61K47/18 , C07B2200/13 , C07C231/24 , C07C235/52 , C07C235/60
摘要： The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.
摘要翻译：本发明涉及N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶多晶型物，含有它们的药物组合物，其制备方法和促进活性剂递送方法，一样。

4. 发明申请

US20120065128A1 CRYSTALLINE FORMS OF THE DI-SODIUM SALT OF N-(5-CHLOROSALICYLOYL)-8-AMINOCAPRYLIC ACID 有权
标题翻译： N-（5-氯乙酰氧基）-8-氨基丙酸的二钠盐的晶体形式
公开(公告)号：US20120065128A1
公开(公告)日：2012-03-15
申请号：US13207750
申请日：2011-08-11
申请人： Nikhil DHOOT , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
发明人： Nikhil DHOOT , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
IPC分类号： A61K47/12 , A61K38/27 , A61K38/29 , A61K38/28 , C07C229/04 , A61K38/23
CPC分类号： A61K47/18 , C07B2200/13 , C07C231/24 , C07C235/52 , C07C235/60
摘要： The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.
摘要翻译：本发明涉及N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶多晶型物，含有它们的药物组合物，其制备方法和促进活性剂递送方法，一样。

5. 发明授权

US08431736B2 Crystalline forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid 有权
标题翻译： N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶形式
公开(公告)号：US08431736B2
公开(公告)日：2013-04-30
申请号：US13207750
申请日：2011-08-11
申请人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
发明人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
IPC分类号： C07C229/00
CPC分类号： A61K47/18 , C07B2200/13 , C07C231/24 , C07C235/52 , C07C235/60
摘要： The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.
摘要翻译：本发明涉及N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶多晶型物，含有它们的药物组合物，其制备方法和促进活性剂递送方法，一样。

6. 发明授权

US08026392B2 Crystalline forms of the di-sodium salt of N-(5-Chlorosalicyloyl)-8-aminocaprylic acid 有权
标题翻译： N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶形式
公开(公告)号：US08026392B2
公开(公告)日：2011-09-27
申请号：US12067239
申请日：2006-09-18
申请人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
发明人： Nikhil Dhoot , Steven Dinh , Shingai Majuru , William Elliott Bay , JoAnne P. Corvino , Doris C. O'Toole
IPC分类号： C07C229/00
CPC分类号： A61K47/18 , C07B2200/13 , C07C231/24 , C07C235/52 , C07C235/60
摘要： The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.
摘要翻译：本发明涉及N-（5-氯水杨酰基）-8-氨基辛酸的二钠盐的结晶多晶型物，含有它们的药物组合物，其制备方法和促进活性剂递送方法，一样。

7. 发明授权

US08927015B2 Formulations for delivering insulin 有权
标题翻译：输送胰岛素的配方
公开(公告)号：US08927015B2
公开(公告)日：2015-01-06
申请号：US12297147
申请日：2007-04-12
申请人： Halina Levchik , Moses O. Oyewumi , Shingai Majuru , William Elliott Bay , Jun Liao , Puchun Liu , Steven Dinh , Nikhil Dhoot
发明人： Halina Levchik , Moses O. Oyewumi , Shingai Majuru , William Elliott Bay , Jun Liao , Puchun Liu , Steven Dinh , Nikhil Dhoot
IPC分类号： A61K38/28 , A61K9/20 , A61K47/02 , A61K47/42 , A61K9/14
CPC分类号： A61K9/2013 , A61K9/06 , A61K9/145 , A61K9/2009 , A61K9/2027 , A61K9/2063 , A61K9/2077 , A61K9/2095 , A61K38/28
摘要： Oral insulin formulations and processes for preparing oral insulin formulations are provided.
摘要翻译：提供口服胰岛素制剂和制备口服胰岛素制剂的方法。

8. 发明授权

US07544833B2 Methods for producing N-(8-[2-hydroxybenzoyl]-amino) caprylic acid 有权
标题翻译：制备N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的方法
公开(公告)号：US07544833B2
公开(公告)日：2009-06-09
申请号：US11847415
申请日：2007-08-30
申请人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
发明人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
IPC分类号： C07C229/02 , C07C231/10
CPC分类号： C07C231/10 , C07C231/24 , C07C235/60
摘要： Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.
摘要翻译：公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的改进方法。已经发现某些化合物在包含在酯水解反应中时可用于防止形成有色杂质。还发现在厌氧条件下进行酯水解使色彩杂质的形成最小化。还公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的钠盐的改进方法。

9. 发明申请

US20080064890A1 METHODS FOR PRODUCING N-(8-[2-HYDROXYBENZOYL]-AMINO) CAPRYLIC ACID 有权
标题翻译：生产N-（8- [2-羟基苯甲酰基] - 氨基）丙烯酸的方法
公开(公告)号：US20080064890A1
公开(公告)日：2008-03-13
申请号：US11847415
申请日：2007-08-30
申请人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
发明人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
IPC分类号： C07C229/02
CPC分类号： C07C231/10 , C07C231/24 , C07C235/60
摘要： Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.
摘要翻译：公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的改进方法。已经发现某些化合物在包含在酯水解反应中时可用于防止形成有色杂质。还发现在厌氧条件下进行酯水解使色彩杂质的形成最小化。还公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的钠盐的改进方法。

10. 发明授权

US5686619A Chloroalkyl pyridinium hydrochloride compounds and processes for their preparation 失效
标题翻译：氯烷基吡啶盐酸盐化合物及其制备方法
公开(公告)号：US5686619A
公开(公告)日：1997-11-11
申请号：US399302
申请日：1995-03-06
申请人： William Elliott Bay , Matthew A. Brown , David R. Kilanowski
发明人： William Elliott Bay , Matthew A. Brown , David R. Kilanowski
IPC分类号： C07D213/26 , C07D213/30 , C07D213/61
CPC分类号： C07D213/26
摘要： Provided is a process for preparing chloroalkyl pyridinium hydrochloride compounds and various regioisomers and analogs thereof having substantially high purity levels and yields and a free-flowing, non-dusting form.
摘要翻译：提供了制备氯烷基吡啶盐酸盐化合物及其各种区域异构体及其类似物的方法，其具有基本上高的纯度水平和产率以及自由流动的无粉尘形式。

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