专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明授权

US08729016B2 Oral insulin therapies and protocol 有权
标题翻译：口服胰岛素治疗和方案
公开(公告)号：US08729016B2
公开(公告)日：2014-05-20
申请号：US12485521
申请日：2009-06-16
申请人： Ehud Arbit , Michael Goldberg , Shingai Majuru
发明人： Ehud Arbit , Michael Goldberg , Shingai Majuru
IPC分类号： A61K38/28
CPC分类号： A61K38/28 , A61B5/14532 , A61K31/192 , A61K38/00
摘要： Methods for treating impaired glucose tolerance and early and late stage diabetes in mammals, for prophylactically sparing β-cell function, aiding in preventing β-cell death, preventing the onset of overt diabetes in a mammal with type 2 diabetes, treating the current level of glycemic control dysfunction of a mammal with impaired glucose tolerance or diabetes, comprising orally administering insulin and a delivery agent that facilitates insulin absorption from the gastrointestinal tract at the time of or shortly before mealtime, e.g., within about 10 minutes prior to ingestion of a meal, on a chronic basis. The methods also comprise, in addition to administering a rapid-acting insulin to provide a first insulin peak, administering a slow acting insulin to provide a second insulin peak occurring at a later time but of a longer duration. These methods achieve improved glycemic control without the risks of hypoglycemia, hyperinsulinemia and weight gain and the need for frequent blood glucose monitoring that are normally associated with insulin therapy.
摘要翻译：用于治疗哺乳动物葡萄糖耐量异常和早期和晚期糖尿病的方法，用于预防性保护和细胞功能，有助于预防和细胞死亡，预防2型糖尿病哺乳动物的明显糖尿病发作，治疗目前的包括葡萄糖耐量降低或糖尿病患者的血糖控制功能障碍的水平，包括口服给药胰岛素和促进胰岛素在进食之前或之后的胰岛素从胃肠道吸收的递送剂，例如在摄取前约10分钟内一顿饭，慢性的。除了施用快速作用的胰岛素以提供第一胰岛素峰之外，所述方法还包括施用缓慢作用的胰岛素以提供在稍后时间但持续时间更长的时间发生的第二胰岛素峰。这些方法可以改善血糖控制，没有低血糖，高胰岛素血症和体重增加的风险，以及通常与胰岛素治疗相关的频繁血糖监测的需要。

3. 发明申请

US20120238591A1 ACYCLOVIR FORMULATIONS 审中-公开
标题翻译： ACYCLOVIR制剂
公开(公告)号：US20120238591A1
公开(公告)日：2012-09-20
申请号：US13482668
申请日：2012-05-29
申请人： Shingai MAJURU , Moses Oyewumi
发明人： Shingai MAJURU , Moses Oyewumi
IPC分类号： A61K31/522 , A61P31/22
CPC分类号： A61K45/06 , A61K31/522 , A61K2300/00
摘要： The present invention relates to acyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
摘要翻译：本发明涉及具有改善的生物利用度的阿昔洛韦制剂，其导致更好的功效和/或需要较不频繁的施用。

4. 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。

5. 发明授权

US07462368B2 Polymorphs of sodium 4-[(4-chloro-2-hydroxybenzoyl) amino]butanoate 有权
标题翻译： 4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的多晶型物
公开(公告)号：US07462368B2
公开(公告)日：2008-12-09
申请号：US11686341
申请日：2007-03-14
申请人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
发明人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
IPC分类号： A61F13/00 , C07C229/00
CPC分类号： C07C235/60 , A61K31/00 , A61K38/28 , A61K45/06 , A61K47/16 , A61K2300/00
摘要： The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.
摘要翻译：本发明涉及4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的无定形和多晶型形式及其用于促进活性剂如胰岛素向靶标递送的用途。

6. 发明申请

US20080175907A1 ORAL INSULIN THERAPIES AND PROTOCOL 审中-公开
标题翻译：口服胰岛素治疗和协议
公开(公告)号：US20080175907A1
公开(公告)日：2008-07-24
申请号：US12040293
申请日：2008-02-29
申请人： Ehud Arbit , Michael Goldberg , Shingai Majuru
发明人： Ehud Arbit , Michael Goldberg , Shingai Majuru
IPC分类号： A61K9/20 , A61K38/28 , A61P3/10
CPC分类号： A61K38/28 , A61B5/14532 , A61K31/192 , A61K38/00
摘要： Methods for treating impaired glucose tolerance and early and late stage diabetes in mammals, for prophylactically sparing β-cell function, aiding in preventing β-cell death, preventing the onset of overt diabetes in a mammal with type 2 diabetes, treating the current level of glycemic control dysfunction of a mammal with impaired glucose tolerance or diabetes, comprising orally administering insulin and a delivery agent that facilitates insulin absorption from the gastrointestinal tract at the time of or shortly before mealtime, e.g., within about 10 minutes prior to ingestion of a meal, on a chronic basis. The methods also comprise, in addition to administering a rapid-acting insulin to provide a first insulin peak, administering a slow acting insulin to provide a second insulin peak occurring at a later time but of a longer duration. These methods achieve improved glycemic control without the risks of hypoglycemia, hyperinsulinemia and weight gain and the need for frequent blood glucose monitoring that are normally associated with insulin therapy.
摘要翻译：用于治疗哺乳动物葡萄糖耐量异常和早期和晚期糖尿病的方法，用于预防性节省β-细胞功能，有助于预防β-细胞死亡，预防2型糖尿病哺乳动物的明显糖尿病发作，治疗目前的水平具有葡萄糖耐量降低或糖尿病的哺乳动物的血糖控制功能障碍，包括在摄食之前或之后约10分钟内口服胰岛素和促进胰岛素从胃肠道吸收的输送剂，长期的。除了施用快速作用的胰岛素以提供第一胰岛素峰之外，所述方法还包括施用缓慢作用的胰岛素以提供在稍后时间但持续时间更长的时间发生的第二胰岛素峰。这些方法可以改善血糖控制，没有低血糖，高胰岛素血症和体重增加的风险，以及通常与胰岛素治疗相关的频繁血糖监测的需要。

7. 发明申请

US20080033204A1 POLYMORPHS OF SODIUM 4-[(4-CHLORO-2-HYDROXYBENZOYL) AMINO] BUTANOATE 有权
标题翻译： 4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的多元醇
公开(公告)号：US20080033204A1
公开(公告)日：2008-02-07
申请号：US11734591
申请日：2007-04-12
申请人： Satej Bhandarkar , Shingai Majuru , Halina Leuchyk
发明人： Satej Bhandarkar , Shingai Majuru , Halina Leuchyk
IPC分类号： C07C229/34
CPC分类号： C07C235/60 , A61K31/00 , A61K38/28 , A61K45/06 , A61K47/16 , A61K2300/00
摘要： The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.
摘要翻译：本发明涉及4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的无定形和多晶型形式及其用于促进活性剂如胰岛素向靶标递送的用途。

8. 发明申请

US20070161708A1 POLYMORPHS OF SODIUM 4-[(4-CHLORO-2-HYDROXYBENZOYL) AMINO] BUTANOATE 有权
标题翻译： 4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的多元醇
公开(公告)号：US20070161708A1
公开(公告)日：2007-07-12
申请号：US11686341
申请日：2007-03-14
申请人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
发明人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
IPC分类号： A61K31/195 , C07C237/20
CPC分类号： C07C235/60 , A61K31/00 , A61K38/28 , A61K45/06 , A61K47/16 , A61K2300/00
摘要： The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.
摘要翻译：本发明涉及4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的无定形和多晶型形式及其用于促进活性剂如胰岛素向靶标递送的用途。

9. 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。

10. 发明申请

US20100069410A1 ACYCLOVIR FORMULATIONS 审中-公开
标题翻译： ACYCLOVIR制剂
公开(公告)号：US20100069410A1
公开(公告)日：2010-03-18
申请号：US12516798
申请日：2007-11-30
申请人： Shingai Majuru , Moses Oyewumi
发明人： Shingai Majuru , Moses Oyewumi
IPC分类号： A61K31/522 , A61P31/22
CPC分类号： A61K45/06 , A61K31/522 , A61K2300/00
摘要： The present invention relates to acyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
摘要翻译：本发明涉及具有改善的生物利用度的阿昔洛韦制剂，其导致更好的功效和/或需要较不频繁的施用。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式