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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

US20110251125A1 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盐，单酯和乙醇溶剂
公开(公告)号：US20110251125A1
公开(公告)日：2011-10-13
申请号：US13053641
申请日：2011-03-22
申请人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , Joanne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
发明人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , Joanne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
IPC分类号： A61K38/23
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-C16alkylene, 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亚烷基，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，乙醇溶剂化物和/或水合物的组合物。

4. 发明申请

US20100099621A1 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盐，单酯和乙醇溶剂
公开(公告)号：US20100099621A1
公开(公告)日：2010-04-22
申请号：US12642508
申请日：2009-12-18
申请人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
发明人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
IPC分类号： A61K38/22 , A61P43/00
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，乙醇溶剂化物和/或水合物的组合物。

5. 发明申请

US20080269134A1 DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS 有权
公开(公告)号：US20080269134A1
公开(公告)日：2008-10-30
申请号：US12111750
申请日：2008-04-29
申请人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
发明人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Corvino , Moise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L. Zielinski
IPC分类号： A61K47/16 , C07C235/46 , A61K31/727 , A61K38/23
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.

6. 发明授权

US08207227B2 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：US08207227B2
公开(公告)日：2012-06-26
申请号：US13053641
申请日：2011-03-22
申请人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , Joanne P. Corvino , Shingai Majuru , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
发明人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , Joanne P. Corvino , Shingai Majuru , 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. 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-C16alkylene, 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亚烷基，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，乙醇溶剂化物和/或水合物的组合物。

7. 发明授权

US08003697B2 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：US08003697B2
公开(公告)日：2011-08-23
申请号：US12642508
申请日：2009-12-18
申请人： William Elliot Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , JoAnne P. Corvino , Shingai Majura , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
发明人： William Elliot Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , JoAnne P. Corvino , Shingai Majura , 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. 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，乙醇溶剂化物和/或水合物的组合物。

8. 发明授权

US07915314B2 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 有权
公开(公告)号：US07915314B2
公开(公告)日：2011-03-29
申请号：US12642508
申请日：2009-12-18
申请人： William Elliot Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , JoAnne P. Corvino , Shingai Majura , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
发明人： William Elliot Bay , Rajesh K. Agarwal , Kiran Chaudhary , Michael M. Goldberg , JoAnne P. Corvino , Shingai Majura , Moise Azria , Joseph Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph Zielinski
IPC分类号： A61K31/195 , C07C229/00
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.

9. 发明授权

US07384982B2 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 有权
公开(公告)号：US07384982B2
公开(公告)日：2008-06-10
申请号：US10615213
申请日：2003-07-07
申请人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Russo , Mosise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L Zielinski
发明人： William E. Bay , Rajesh K. Agarwal , Kiran Chaudhary , Shingai Majuru , Michael M. Goldberg , JoAnne P. Russo , Mosise Azria , Joseph M. Ault , Simon D. Bateman , Subash Patel , Joseph Sikora , Rebecca F. Yang , Joseph L Zielinski
IPC分类号： A61K31/195 , C07D229/04 , C07D229/14
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 indepedently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substitued 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.

10. 发明授权

US08697686B2 Crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-thtrahydro-1H-3-benzazepine hydrochloride 有权
标题翻译：（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-苯并吖庚因盐酸盐的结晶形式
公开(公告)号：US08697686B2
公开(公告)日：2014-04-15
申请号：US13425669
申请日：2012-03-21
申请人： Rajesh K. Agarwal , William L. Betts, III , James A. Henshilwood , Yuan-Hon Kiang , Noah Post
发明人： Rajesh K. Agarwal , William L. Betts, III , James A. Henshilwood , Yuan-Hon Kiang , Noah Post
IPC分类号： A61K31/55 , C07D223/16
CPC分类号： C07D223/16
摘要： The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.
摘要翻译：本发明涉及（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂的结晶形式，其含有该组合物及其应用的组合物。

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