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公开(公告)号:US20020119910A1
公开(公告)日:2002-08-29
申请号:US09746548
申请日:2000-12-19
发明人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold , Koc-Kan Ho , David Gschneidner , Eugene N. Barantsevich
IPC分类号: A61K009/00
CPC分类号: C07D209/48 , A61K9/1617 , A61K31/195 , A61K31/445 , A61K31/4965 , A61K31/727 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K45/06 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , 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 , A61K2300/00
摘要: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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公开(公告)号:US20020040061A1
公开(公告)日:2002-04-04
申请号:US09939511
申请日:2001-08-24
IPC分类号: A61K031/195 , A61K031/165 , C07C317/32 , C07C235/42
CPC分类号: C07D207/27 , A61K9/0053 , A61K45/06 , A61K47/18 , C07C235/60 , C07C2601/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/13
摘要: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译: 提供用于递送活性剂的化合物和组合物。 也提供给药和制备方法。
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公开(公告)号:US20020013497A1
公开(公告)日:2002-01-31
申请号:US09922961
申请日:2001-08-03
IPC分类号: C07C237/28
CPC分类号: A61K9/0014 , A61K9/0031 , A61K9/2013 , A61K47/18 , A61K47/183 , C07C231/00 , C07C233/51 , C07C235/24 , C07C235/34 , C07C235/64 , C07C235/74 , C07C271/28 , C07C271/54 , C07C271/58 , C07C275/42 , C07C309/59 , C07C317/44 , C07D239/91 , C07D239/94 , C07D239/96 , C07D265/26 , C07D311/18 , C07D317/68 , C07C235/58
摘要: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a nullprotected/activated salicylamidenull). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.
摘要翻译: 本发明涉及由保护和活化的水杨酰胺(以下称为“保护/活化的水杨酰胺”)制备烷基化水杨酰胺的方法。 该方法包括以下步骤:(a)用烷基化剂烷基化保护/活化的水杨酰胺以形成受保护/活化的烷基化水杨酰胺,和(b)同时或以任何顺序使受保护/活化的烷基化水杨酰胺脱保护和失活以形成 烷基化水杨酰胺。 通过该方法制备的烷基化水杨酰胺适用于通过口服或其它给药途径向动物递送活性剂的组合物。
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公开(公告)号:US6100285A
公开(公告)日:2000-08-08
申请号:US967486
申请日:1997-11-11
申请人: Martin L. Kantor
发明人: Martin L. Kantor
IPC分类号: A61K9/16 , A61K31/4174 , A61K31/496 , A61K47/12 , B01J13/02 , A61K31/415 , A01N43/50
CPC分类号: A61K47/12 , A61K31/4174 , A61K31/496 , A61K9/1617 , A61K9/1641 , B01J13/02 , Y10S514/963
摘要: Solutions comprising itraconazole solubilized in a solvent comprising at least one volatile organic acid are provided. Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.
摘要翻译: 提供了包含伊曲康唑溶解在包含至少一种挥发性有机酸的溶剂中的溶液。 提供了制备含有咪唑衍生物的微球的方法。 还提供了含有微球的咪唑衍生物用于治疗真菌感染的用途。 还提供了口服给药的口服剂型。
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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:US6051561A
公开(公告)日:2000-04-18
申请号:US797813
申请日:1997-02-07
申请人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
发明人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
IPC分类号: A61K9/16 , A61K38/00 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K31/725 , A01N43/04 , A61K39/00
CPC分类号: C07D209/48 , A61K9/1617 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , 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 , A61K38/00
摘要: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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公开(公告)号:US06051258A
公开(公告)日:2000-04-18
申请号:US475885
申请日:1995-06-07
申请人: Martin L. Kantor
发明人: Martin L. Kantor
CPC分类号: A61K47/183 , A61K47/42 , A61K9/107 , Y10S514/937 , Y10S514/975
摘要: The present invention provides emulsions, and a method for preparing emulsions, comprising (A) an aqueous phase, (B) an non-aqueous phase, and (C) (i) a proteinoid emulsifier, (ii) a modified hydrolyzed vegetable protein emulsifier wherein said modified hydrolyzed vegetable protein is modified with an amine reactive modifying agent, (iii) an acylated non-.alpha.-amino acid emulsifier, (iv) an acylated poly amino acid emulsifier, (v) an acylated peptide emulsifier, (vi) a sulfonated non-.alpha.-amino acid emulsifier, (vii) a sulfonated poly amino acid emulsifier, (viii) a sulfonated peptide emulsifier, or (ix) any combination of any of (i), (ii), (iii), (iv), (v), (vi), (vii), and (viii). The proteinoids, modified hydrolyzed vegetable proteins, modified non-.alpha.-amino acids, modified poly amino acids, and modified peptides used in the present invention provide emulsions having improved stability against degradation and/or decomposition.
摘要翻译: 本发明提供乳液和一种制备乳液的方法,其包括(A)水相,(B)非水相和(C)(i)一种类蛋白质乳化剂,(ii)改性水解植物蛋白乳化剂 其中所述改性水解植物蛋白用胺反应性改性剂,(iii)酰化非α-氨基酸乳化剂,(iv)酰化聚氨基酸乳化剂,(v)酰化肽乳化剂,(vi) 磺化非α-氨基酸乳化剂,(vii)磺化聚氨基酸乳化剂,(viii)磺化肽乳化剂,或(ix)任何(i),(ii),(iii),(iv) ),(v),(vi),(vii)和(viii)。 本发明中使用的蛋白质类,修饰的水解植物蛋白,修饰的非α-氨基酸,修饰的聚氨基酸和修饰的肽提供具有改善的降解和/或分解稳定性的乳液。
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公开(公告)号:US5939381A
公开(公告)日:1999-08-17
申请号:US796340
申请日:1997-02-07
申请人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
发明人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
IPC分类号: A61K9/16 , A61K38/00 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K38/17
CPC分类号: C07D209/48 , A61K9/1617 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , 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 , A61K38/00
摘要: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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公开(公告)号:US5876710A
公开(公告)日:1999-03-02
申请号:US796335
申请日:1997-02-07
申请人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
发明人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
IPC分类号: A61K9/16 , A61K38/00 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K31/70 , A61K47/12 , C07C229/06
CPC分类号: C07D209/48 , A61K9/1617 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , 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 , A61K38/00
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.
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公开(公告)号:US5804688A
公开(公告)日:1998-09-08
申请号:US796339
申请日:1997-02-07
申请人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
发明人: Andrea Leone-Bay , Eric Wang , Donald J. Sarubbi , Harry Leipold
IPC分类号: A61K9/16 , A61K38/00 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , C07C229/00
CPC分类号: C07D209/48 , A61K9/1617 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , 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 , A61K38/00
摘要: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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