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1.发明授权Detection of endotoxin levels in liposomes, lipid bilayers and lipid complexes 失效检测脂质体，脂质双层和脂质复合物中的内毒素水平
公开(公告)号：US06015716A
公开(公告)日：2000-01-18
申请号：US679046
申请日：1996-07-12
IPC分类号： G01N33/579 , A61K9/50 , C07F9/02 , G01N31/00
CPC分类号： G01N33/579 , G01N2400/50 , G01N2405/04 , Y10S436/829 , Y10T436/104165
摘要： Endotoxin incorporated into liposomes, lipid bilayers or lipid complexes can be detected by combining an aqueous suspension of the liposomes, lipid complexes or lipid bilayers with a suitable detergent. Preferable detergents, e.g., Lubrol-PX.TM. or a polyoxyethylene ether, solubilize the lipid bilayers, liposomes or lipid complexes at acceptable lipid concentrations, forming micelles therefrom which contain lipid bilayer, liposome or lipid complex lipid, detergent and endotoxin, should it be present. The micelles are then assayed for the presence of endotoxin.
摘要翻译： 可以通过将脂质体，脂质复合物或脂质双层的水性悬浮液与合适的洗涤剂组合来检测掺入脂质体，脂质双层或脂质复合物中的内毒素。 优选的洗涤剂，例如Lubrol-PX TM或聚氧乙烯醚，以可接受的脂质浓度溶解脂质双层，脂质体或脂质复合物，形成其中含有脂质双层，脂质体或脂质复合物脂质，洗涤剂和内毒素的胶束，如果存在 。 然后测定胶束的内毒素的存在。
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公开(公告)号：US6118011A
公开(公告)日：2000-09-12
申请号：US753650
申请日：1996-11-27
IPC分类号： A61K9/127 , A61K31/335 , A61K31/337 , A61K31/66 , A61P35/00 , C07D305/14 , C07F9/655
CPC分类号： B82Y5/00 , A61K9/127 , C07D305/14 , C07F9/65512
摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。
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公开(公告)号：US5939567A
公开(公告)日：1999-08-17
申请号：US988120
申请日：1997-12-10
IPC分类号： A61K9/127 , A61K31/335 , A61K31/337 , A61K31/66 , A61P35/00 , C07D305/14 , C07F9/655
CPC分类号： B82Y5/00 , A61K9/127 , C07D305/14 , C07F9/65512
摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。
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公开(公告)号：US5580899A
公开(公告)日：1996-12-03
申请号：US474888
申请日：1995-06-07
IPC分类号： A61K9/127 , A61K31/335 , A61K31/337 , A61K31/66 , A61P35/00 , C07D305/14 , C07F9/655
CPC分类号： B82Y5/00 , A61K9/127 , C07D305/14 , C07F9/65512
摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。
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公开(公告)号：US06291690B1
公开(公告)日：2001-09-18
申请号：US09567366
申请日：2000-05-09
IPC分类号： C07D30514
CPC分类号： B82Y5/00 , A61K9/127 , C07D305/14 , C07F9/65512
摘要： This invention provides a taxane derivative of the formula: wherein a hydrophobic organic moiety is attached to a taxane. R and R1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。
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公开(公告)号：US06392063B1
公开(公告)日：2002-05-21
申请号：US09618872
申请日：2000-07-19
申请人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
发明人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
IPC分类号： C07D30514
CPC分类号： C07D305/14 , A61K9/127
摘要： Provided herein is a taxane having a hydrocarbon attached at the 2′ and/or 7 positions, the hydrocarbon's alpha position being occupied by a “hydrolysis-promoting group” (“HPG”). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the a-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.
摘要翻译： 本文提供了具有在2'和/或7位上连接的烃的紫杉烷，烃的α位置被“水解促进基团”（“HPG”）占据。 在一个实施方案中，水解促进基团立体特异性地连接到疏水紫杉烷的α-碳上。 通常占据α位置的通常占据α位置的亚甲基单元的HPG的取代允许烃 - 紫杉烷键的体内水解增强，因此增强紫杉烷治疗活性。 本文还提供了含紫杉烷的组合物，以及向动物（包括患有癌症或炎性疾病的患者）施用紫杉烷的方法。
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公开(公告)号：US06482850B2
公开(公告)日：2002-11-19
申请号：US09940672
申请日：2001-08-29
申请人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
发明人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
IPC分类号： A01N4302
CPC分类号： C07D305/14 , A61K9/127
摘要： Provided herein is a taxane having a hydrocarbon attached at the 2′ and/or 7 positions, the hydrocarbon's alpha position being occupied by a “hydrolysis-promoting group” (“HPG”). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the &agr;-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.
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公开(公告)号：US6107332A
公开(公告)日：2000-08-22
申请号：US249004
申请日：1999-02-12
申请人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
发明人： Shaukat Ali , J. Craig Franklin , Imran Ahmad , Eric Mayhew , Soumendu Bhattacharya , Gil Koehane , Andrew S. Janoff
IPC分类号： A61K9/127 , A61P35/00 , C07D305/14 , A61K31/337
CPC分类号： C07D305/14 , A61K9/127
摘要： Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a "hydrolysis-promoting group" ("HPG"). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the .alpha.-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.
摘要翻译： 本文提供了具有在2'和/或7位上连接的烃的紫杉烷，烃的α位置被“水解促进基团”（“HPG”）占据。 在一个实施方案中，水解促进基团立体特异性地连接到疏水紫杉烷的α-碳上。 通常占据α位置的通常占据α位置的亚甲基单元的HPG的取代允许烃 - 紫杉烷键的体内水解增强，因此增强紫杉烷治疗活性。 本文还提供了含紫杉烷的组合物，以及向动物（包括患有癌症或炎性疾病的患者）施用紫杉烷的方法。
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公开(公告)号：US6030639A
公开(公告)日：2000-02-29
申请号：US652259
申请日：1996-05-23
申请人： Andrew S. Janoff , David F. Eierman
发明人： Andrew S. Janoff , David F. Eierman
IPC分类号： A61K9/127 , A61K31/557 , A61K9/133 , A61K9/16
CPC分类号： A61K9/127 , A61K31/557
摘要： Provided herein is a method of administering a free arachidonic acid metabolite to an animal, the method involving administration of the free metabolite and an endocytosable particle. This method can be used to treat animals afflicted with disorders characterized by cell activation and adhesion, inflammation or toxemia. Also provided is a method of treating a animal for such disorders by administration to the animals of a composition containing an anti-disorder effective amount of an endocytosable particle.
摘要翻译： 本文提供了向动物施用游离花生四烯酸代谢物的方法，该方法涉及施用游离代谢物和可内吞颗粒。 该方法可用于治疗以细胞活化和粘附，炎症或毒血症为特征的疾病。 还提供了通过向动物施用含有抗障碍有效量的可内吞颗粒的组合物来治疗动物以治疗这种疾病的方法。
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10.发明授权Peptide-containing liposomes, immunogenic liposomes and methods of preparation and use 失效含肽的脂质体，免疫原性脂质体及其制备和使用方法
公开(公告)号：US5916588A
公开(公告)日：1999-06-29
申请号：US452549
申请日：1995-05-25
申请人： Mircea C. Popescu , Alan L. Weiner , Marie S. Recine , Andrew S. Janoff , Leonard Estis , Lynn D. Keyes , Carl R. Alving
发明人： Mircea C. Popescu , Alan L. Weiner , Marie S. Recine , Andrew S. Janoff , Leonard Estis , Lynn D. Keyes , Carl R. Alving
CPC分类号： A61K39/39 , A61K9/1271 , A61K2039/55555
摘要： A high integrity liposome comprising at least one stabile lipid and at least one peptide-like therapeutic agent associated with the liposome, adapted for parenteral administration to an animal, including a human, and method according to manufacture and use.Immunizing dosage forms comprising a liposome and an immunogen, wherein the liposome and immunogen are present in an immunization dose. Additionally, a dosage form, including such form particularly adapted to producing an immune response, comprising a salt according to an organic acid derivative of a sterol and an immunogen are present in an immunization dose, and method according to uses is disclosed. Further, a dosage form, including such form particularly adapted to producing an immune response, comprising dimyristolyphosphatidylcholine (DMPC)/cholesterol liposomes, optionally in an aluminum hydroxide gel, and an immunogen wherein the DMPC/cholesterol and immunogen are present in an immunization dose, and method according to use.
摘要翻译： 包含至少一种稳定脂质和至少一种与脂质体相关的肽样治疗剂的高完整性脂质体，其适于肠胃外给予动物，包括人类，以及根据制造和使用的方法。 包含脂质体和免疫原的免疫剂型，其中所述脂质体和免疫原以免疫剂量存在。 此外，包含特定适于产生免疫应答的形式的剂型，其包含根据固醇和免疫原的有机酸衍生物的盐，其以免疫剂量存在，并且公开了根据用途的方法。 此外，包括特别适于产生免疫应答的剂型，包括任选在氢氧化铝凝胶中的二肉豆蔻基磷脂酰胆碱（DMPC）/胆固醇脂质体和免疫原，其中DMPC /胆固醇和免疫原以免疫剂量存在， 和方法根据用途。
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