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公开(公告)号：EP1077070A2
公开(公告)日：2001-02-21
申请号：EP00118505.7
申请日：1994-04-22
发明人： Milstein, Sam J. , Barantsevitch, Evgueni N. , Sarubbi, Donald J. , Leone-Bay, Andrea , Paton, Duncan R.
CPC分类号： A61K31/16 , A61K9/1617 , A61K31/352 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/64 , C07C235/84 , C07C237/22 , C07C2601/02 , C07C2601/14 , C07C2601/18
摘要： The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form durg containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.
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公开(公告)号：EP0812212A1
公开(公告)日：1997-12-17
申请号：EP96907856.0
申请日：1996-01-16
发明人： SANTIAGO, Noemi, B. , HAAS, Susan , LEONE-BAY, Andrea , MILSTEIN, Sam, J. , BARANTSEVITCH, Evgueni
IPC分类号： A61K9 , A61K31 , A61K38 , A61K39 , A61K47 , C07C229 , C07C233 , C07C235 , C07C237 , C07C279 , C07K1 , C07K5 , C07K14
CPC分类号： A61K39/00 , A61K9/1617 , A61K9/1641 , A61K31/16 , A61K31/352 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , A61K47/183 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/64 , C07C235/84 , C07C237/22 , C07C279/14 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07K1/1077 , C07K5/06043 , Y02A50/464 , Y02A50/466
摘要： The present invention relates to the delivery of antigens. Delivery systems are provided that include the antigen and acylated or sulfonated amino acids or poly amino acids. Methods of preparation and administration of these compositions are also provided.
摘要翻译： 本发明涉及递送抗原。 提供递送系统，其包括抗原和酰化或磺化的氨基酸或聚氨基酸。 还提供了这些组合物的制备和给药方法。
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公开(公告)号：EP0726771A1
公开(公告)日：1996-08-21
申请号：EP94932077.0
申请日：1994-10-24
IPC分类号： A61K47 , A61K8 , A61K9 , A61K31 , A61K38 , A61P3 , A61P5 , A61P7 , A61P11 , A61P39 , A61Q13 , C07C229 , C07C233 , C07C235 , C07C237
CPC分类号： A61K8/64 , A61K8/11 , A61K9/1617 , A61K9/1641 , A61K9/167 , A61K31/16 , A61K31/28 , A61K31/35 , A61K31/352 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , A61K38/28 , A61Q13/00 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/64 , C07C235/84 , C07C237/22 , C07C2601/02 , C07C2601/14 , C07C2601/18
摘要： Modified amino acids and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The modified amino acids are preparable by reacting single amino acids or mixtures of two or more kinds of amino acids with an amino modifying agent such as benzene sulfonyl chloride, benzoyl chloride, and hippuryl chloride. The modified amino acids may form encapsulating microspheres in the presence of the active agent under sphere-forming conditions. Alternatively, the modified amino acids may be used as a carrier by simply mixing the amino acids with the active agent. The preferred acylated amino acid carrier is salicyloyl-phenylalanine. The modified amino acids are particularly useful in delivering biologically active agents, e.g., desferrioxamine, insulin or cromolyn sodium, or other agents which are sensitive to the denaturing conditions of the gastrointestinal tract.
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54.发明公开
公开(公告)号：EP0696192A1
公开(公告)日：1996-02-14
申请号：EP94915419.0
申请日：1994-04-22
CPC分类号： A61K9/1658
摘要： Modified hydrolyzed vegetable protein microspheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. Figure 1 illustrates levels of glucose detected in rat serum taken from rats orally administered microsphere encapsulated insulin or raw (unencapsulated) insulin as described in example 4. Figure 2 illustrates rat serum calcium levels after oral administration of calcitonin and calcitonin encapsulated in the vegetable protein microsphere of the present invention as described in example 5. Figure 3 illustrates an HPLC trace of the hydrolyzed vegetable protein before modification. Figure 4 illustrates the change in the hydrolyzed vegetable protein after modification with benzene sulfonyl chloride in an HPLC trace.
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55.发明授权
公开(公告)号：EP2129218B1
公开(公告)日：2016-10-19
申请号：EP08730114.9
申请日：2008-02-19
发明人： TANG, Pingwah , DINH, Steven
CPC分类号： C07C59/72 , C07C65/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
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56.发明授权ARYL KETONE COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 有权ARYLKETONVERBINDUNGEN和组合物-RELEASE
公开(公告)号：EP1745004B8
公开(公告)日：2016-07-27
申请号：EP05804827.3
申请日：2005-05-16
IPC分类号： A61K38/28 , A61K38/29 , A61K31/19 , A61K31/727
CPC分类号： C07C233/33 , A61K31/19 , A61K31/192 , A61K31/727 , A61K38/2271 , A61K38/28 , A61K38/29 , A61K45/06 , C07C59/90 , Y02A50/406 , A61K2300/00
摘要： The present invention provides aryl ketone compounds and compositions containing them which facilitate the delivery of active agents. The aryl ketone compounds have the formula or a salt thereof, where n=1 to 9, and R1 to R5 are independently hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, C2 to C4 alkenyl, halogen, hydroxyl, —NH—C(O)—CH3, or —O—C6H5.
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公开(公告)号：EP1461031B1
公开(公告)日：2016-06-29
申请号：EP02789934.3
申请日：2002-11-29
CPC分类号： A61K31/352 , A61K9/4858 , A61K47/183
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公开(公告)号：EP2007372B1
公开(公告)日：2015-03-04
申请号：EP07760847.9
申请日：2007-04-18
发明人： SONG, Jianfeng
IPC分类号： A61K47/12 , C07C53/134 , A61K31/192 , A61K9/00 , C07C59/66
CPC分类号： A61K31/192 , A61K9/0053 , A61K47/12 , C07C59/66
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公开(公告)号：EP1750718B1
公开(公告)日：2014-08-13
申请号：EP05751979.5
申请日：2005-05-19
发明人： ADAMS, Amy , MAJURU, Shingai , DHOOT, Nikhil , SINGH, Brahma
IPC分类号： A61K31/522 , A61K9/20 , A61P31/12
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/08 , A61K9/2013 , A61K31/522 , A61K47/12
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公开(公告)号：EP1246792B1
公开(公告)日：2014-08-13
申请号：EP01908609.9
申请日：2001-01-12
IPC分类号： C07C229/00 , A61K38/28 , A61K51/00
CPC分类号： A61K31/195 , A61K9/0053 , A61K9/0073 , A61K31/557 , A61K31/727 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/183 , A61K47/541 , C07C235/64 , A61K2300/00
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