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公开(公告)号：US06693073B2
公开(公告)日：2004-02-17
申请号：US10172582
申请日：2002-06-14
申请人： Sam J. Milstein , John E. Smart , Donald J. Sarubbi , Monica Leipold , Elizabeth Flanders , Doris O'Toole , Andrea Leone-Bay , David Gschneidner
发明人： Sam J. Milstein , John E. Smart , Donald J. Sarubbi , Monica Leipold , Elizabeth Flanders , Doris O'Toole , Andrea Leone-Bay , David Gschneidner
IPC分类号： A61K3828
CPC分类号： C07C235/64 , A61K9/0073 , A61K31/16 , A61K31/727 , A61K38/00 , A61K38/1709 , A61K38/1816 , A61K38/27 , A61K38/28 , A61K38/29 , A61K38/30 , A61K47/183
摘要： The present invention provides methods for administering an active agent to an animal in need of the agent by the pulmonary route. This method comprises administering via the pulmonary route, a composition comprising (a) an active agent and (b)(i) an acylated amino acid, (ii) a sulfonated amino acid, or (iii) a combination of (i) and (ii). Administration of the compositions of the present invention provide improved pulmonary delivery and greater bioavailability of the active agent than administration of the active agent alone. As a result, lesser amounts of the active agent may be administered to obtain a desired result when contained in the composition of the present invention than when administered alone.
摘要翻译： 本发明提供了通过肺部途径向需要该药物的动物施用活性剂的方法。 该方法包括通过肺部途径施用包含（a）活性剂和（b）（i）酰化氨基酸，（ii）磺化氨基酸或（iii）（i）和（i） ii）。 施用本发明的组合物比单独施用活性剂提供了改善的肺输送和活性剂的更大的生物利用度。 结果，当与本发明的组合物相比时，可以施用较少量的活性剂以获得期望的结果。
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公开(公告)号：US06440929B1
公开(公告)日：2002-08-27
申请号：US09744777
申请日：2001-04-26
申请人： Sam J. Milstein , John E. Smart , Donald J. Sarubbi , Monica Leipold , Elizabeth Flanders , Doris O'Toole , Andrea Leone-Bay , David Gschneidner
发明人： Sam J. Milstein , John E. Smart , Donald J. Sarubbi , Monica Leipold , Elizabeth Flanders , Doris O'Toole , Andrea Leone-Bay , David Gschneidner
IPC分类号： A61K3800
CPC分类号： C07C235/64 , A61K9/0073 , A61K31/16 , A61K31/727 , A61K38/00 , A61K38/1709 , A61K38/1816 , A61K38/27 , A61K38/28 , A61K38/29 , A61K38/30 , A61K47/183
摘要： The present invention relates to pulmonary delivery of active agents. Acylated or sufonated amino acids are used as carriers to facilitate pulmonary delivery of active agents to a target.
摘要翻译： 本发明涉及活性剂的肺部递送。 使用酰化或辅助氨基酸作为载体以促进活性剂向目标物的肺部递送。
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公开(公告)号：US06699467B2
公开(公告)日：2004-03-02
申请号：US10142009
申请日：2002-05-08
IPC分类号： A61K31195
CPC分类号： C07D333/38 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D213/81 , C07D295/215 , C07D317/68
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration and methods of preparation of the modified amino acid compounds are also provided.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 活性剂可以是肽。 还提供了口服，皮下，舌下和鼻内给药的给药方法和修饰的氨基酸化合物的制备方法。
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公开(公告)号：US6099856A
公开(公告)日：2000-08-08
申请号：US763183
申请日：1996-12-10
申请人： Sam J. Milstein , Evgueni Barantsevitch , Andrea Leone-Bay , Nai Fang Wang , Donald J. Sarubbi , Noemi B Santiago
发明人： Sam J. Milstein , Evgueni Barantsevitch , Andrea Leone-Bay , Nai Fang Wang , Donald J. Sarubbi , Noemi B Santiago
IPC分类号： A61K8/04 , A61K8/64 , A61K9/16 , A61K9/20 , A61K31/16 , A61K31/28 , A61K31/35 , A61K31/352 , A61K31/727 , A61K38/00 , A61K38/21 , A61K38/23 , A61K38/25 , A61K38/27 , A61K38/28 , A61K47/12 , A61K47/18 , A61K47/48 , A61Q13/00 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/54 , C07C235/64 , C07C235/84 , C07C237/22 , C07C279/14 , C07K1/107 , C07K5/06 , A61K9/127
CPC分类号： A61K8/64 , A61K31/16 , A61K31/28 , A61K31/35 , A61K31/352 , A61K31/715 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , A61K38/28 , A61K47/12 , A61K47/18 , A61K47/183 , A61K47/48238 , A61K8/0204 , A61K9/1617 , A61K9/1641 , A61K9/167 , A61K9/2013 , A61Q13/00 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/54 , C07C235/64 , C07C235/84 , C07C237/22 , C07C279/14 , C07K1/1077 , C07K5/06043 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of:(a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states;(b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and(c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.
摘要翻译： 运输生物活性剂穿过细胞膜或脂质双层的方法。 第一种方法包括以下步骤：（a）提供可以以天然构象状态，变性构象状态和中和构象状态存在的生物活性剂，其可天然状态是可逆的，并且在天然和/或 变性状态 （b）将生物活性剂暴露于络合扰动剂以将生物活性剂可逆地转化为中间状态并形成可运输的超分子复合物; 和（c）将膜或双层暴露于超分子复合物，以将生物活性剂转运穿过膜或双层。 扰动剂具有约150至约600道尔顿之间的分子量，并且含有至少一个亲水部分和至少一个疏水部分。 超分子复合物包括与生物活性剂非共价结合或络合的扰动剂。 在本发明中，生物活性剂在与扰动剂相互作用后不形成微球体。 还提供了包含上述步骤（a）和（b）的可口服给药的生物活性剂的制备方法，口服递送组合物也是如此。 另外，可以考虑用于制备模拟物的模拟物和方法。
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公开(公告)号：US07417022B2
公开(公告)日：2008-08-26
申请号：US11104173
申请日：2005-04-11
IPC分类号： A61K9/48 , A61K9/64 , A61K9/20 , A61K9/14 , A61K38/00 , A61K31/715 , A61K31/20 , A01N37/18 , A01N43/04 , A01N37/00
CPC分类号： C07D209/48 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C229/42 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/69 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C235/82 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 也提供给药和制备方法。
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公开(公告)号：US5866536A
公开(公告)日：1999-02-02
申请号：US798033
申请日：1997-02-06
IPC分类号： C07D295/20 , A61K9/00 , A61K9/08 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/197 , A61K31/198 , A61K31/40 , A61K31/44 , A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/12 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C53/126 , C07C53/134 , C07C229/08 , C07C229/10 , C07C229/42 , C07C231/12 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/62 , C07C235/64 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C239/06 , C07C239/08 , C07C259/06 , C07C271/22 , C07C303/22 , C07C303/40 , C07C309/59 , C07C311/19 , C07D207/34 , C07D207/416 , C07D213/75 , C07D213/81 , C07D295/215 , C07D317/68 , C07D333/38 , A61K31/725 , C07C229/06
CPC分类号： C07D333/38 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/4803 , A61K9/0019 , A61K9/1617 , A61K9/4858 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07D207/34 , C07D213/81 , C07D295/215 , C07D317/68 , A61K9/0043 , A61K9/0056 , C07C2101/14 , C07C2101/18 , C07C2103/74
摘要： Carrier compounds, compositions, and dosage unit forms therefor which are useful in the delivery of active agents are provided. The present invention provides a compound having the formula: ##STR1## or a salt thereof, wherein the compound may be used in a composition or dosage unit form for delivery of at least one active agent, including a peptide, mucopolysaccharide, carbohydrate, or a lipid. Methods of administration and preparation of the compounds and compositions of the invention are provided as well, including oral administration. Further, the compositions of the invention may be prepared by mixing at least one active agent, at least one carrier compound, and, optionally, a dosing vehicle.
摘要翻译： 提供了可用于递送活性剂的载体化合物，组合物和剂量单位形式。 本发明提供具有下式的化合物或其盐，其中所述化合物可以组合物或剂量单位形式用于递送至少一种活性剂，包括肽，粘多糖，碳水化合物或 脂质。 还提供了本发明化合物和组合物的施用和制备方法，包括口服给药。 此外，本发明的组合物可以通过混合至少一种活性剂，至少一种载体化合物和任选的给药载体来制备。
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公开(公告)号：US06972300B2
公开(公告)日：2005-12-06
申请号：US10623142
申请日：2003-07-18
IPC分类号： C07D295/20 , A61K9/00 , A61K9/08 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/197 , A61K31/198 , A61K31/40 , A61K31/44 , A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/12 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C53/126 , C07C53/134 , C07C229/08 , C07C229/10 , C07C229/42 , C07C231/12 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/62 , C07C235/64 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C239/06 , C07C239/08 , C07C259/06 , C07C271/22 , C07C303/22 , C07C303/40 , C07C309/59 , C07C311/19 , C07D207/34 , C07D207/416 , C07D213/75 , C07D213/81 , C07D295/215 , C07D317/68 , C07D333/38 , A61K31/195 , C07C229/00
CPC分类号： C07D333/38 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D213/81 , C07D295/215 , C07D317/68
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 活性剂可以是肽，例如rhGH。 提供口服，皮下，舌下和鼻内给药的给药方法，提供修饰的氨基酸化合物的制备方法。
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公开(公告)号：US06348207B1
公开(公告)日：2002-02-19
申请号：US08941609
申请日：1997-09-30
申请人： Sam J. Milstein , Evgueni Barantsevitch , Andrea Leone-Bay , Nai Fang Wang , Donald J. Sarubbi , Noemi B Santiago
发明人： Sam J. Milstein , Evgueni Barantsevitch , Andrea Leone-Bay , Nai Fang Wang , Donald J. Sarubbi , Noemi B Santiago
IPC分类号： A01N2512
CPC分类号： A61K8/64 , A61K9/1617 , A61K9/1641 , A61K9/167 , A61K9/2013 , A61K31/16 , A61K31/28 , A61K31/35 , A61K31/352 , A61K31/715 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , A61K38/28 , A61K47/12 , A61K47/18 , A61K47/183 , A61K47/62 , A61Q13/00 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/54 , C07C235/64 , C07C235/84 , C07C237/22 , C07C279/14 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07K1/1077 , C07K5/06043
摘要： Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.
摘要翻译： 运输生物活性剂穿过细胞膜或脂质双层的方法。 第一种方法包括以下步骤：（a）提供可以以天然构象状态，变性构象状态和中和构象状态存在的生物活性剂，其可天然状态是可逆的，并且在天然和/或 变性状态;（b）将生物活性剂暴露于络合扰动剂以将生物活性剂可逆地转化为中间状态并形成可运输的超分子复合物; 和（c）将膜或双层暴露于超分子复合物，以将生物活性剂转运穿过膜或双层。 扰动剂具有约150至约600道尔顿之间的分子量，并且含有至少一个亲水部分和至少一个疏水部分。 超分子复合物包括与生物活性剂非共价结合或络合的扰动剂。 在本发明中，生物活性剂在与扰动剂相互作用后不形成微球体。 还提供了包含上述步骤（a）和（b）的可口服给药的生物活性剂的制备方法，口服递送组合物也是如此。 另外，可以考虑用于制备模拟物的模拟物和方法。
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公开(公告)号：US07005141B2
公开(公告)日：2006-02-28
申请号：US10225104
申请日：2002-08-20
申请人： Sam J. Milstein , Evgueni N. Barantsevitch , Donald J. Sarubbi , Andrea Leone-Bay , Duncan R. Paton
发明人： Sam J. Milstein , Evgueni N. Barantsevitch , Donald J. Sarubbi , Andrea Leone-Bay , Duncan R. Paton
IPC分类号： A61K9/20
CPC分类号： A61K9/1617 , A61K9/1641 , A61K31/16 , A61K31/352 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/25 , A61K38/27 , A61K39/12 , A61K39/39 , A61K47/183 , A61K2039/5252 , A61K2039/542 , A61K2039/552 , A61K2039/55544 , A61K2039/55555 , 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 , C12N2720/10034
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 drug 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：US06428780B2
公开(公告)日：2002-08-06
申请号：US09305506
申请日：1999-05-05
IPC分类号： A61K3800
CPC分类号： C07D333/38 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D213/81 , C07D295/215 , C07D317/68
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration are provided, and methods of preparation of the modified amino acid compound are provided.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 活性剂可以是肽。 提供口服，皮下，舌下和鼻内给药的给药方法，提供修饰氨基酸化合物的制备方法。
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