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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：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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4.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：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：US09339543B2
公开(公告)日：2016-05-17
申请号：US14350839
申请日：2012-10-08
IPC分类号： A61K31/44 , A01N43/40 , A61K47/12 , A61K9/20 , A61K31/4439
CPC分类号： A61K47/12 , A61K9/2013 , A61K9/2054 , A61K31/4439
摘要： Pharmaceutical formulations comprising solid pharmaceutically acceptable organic acids, such as maleic acid or tartaric acid, that inhibit the disproportionation of pharmaceutically acceptable acid salts of active pharmaceutical ingredients, and methods of manufacturing such pharmaceutical compositions. The pharmaceutically acceptable acid salt of the active pharmaceutical ingredient has a pKa of less than about 6.0, and wherein the solid pharmaceutically acceptable organic acid has a pKa of less than about 4.0 and an aqueous solubility in the range of about 500 to about 2000 milligrams per milliliter. A pharmaceutical formulation comprising a pharmaceutical acceptable acid salt of pioglitazone, a solid pharmaceutically acceptable organic acid selected from the group consisting of maleic acid or tartaric acid, and an excipient that promotes disproportionation, wherein the ratio by weight of the solid pharmaceutically acceptable organic acid to excipient is from about 1:6 to about 1:1.
摘要翻译： 包含抑制活性药物成分的药学上可接受的酸盐的歧化的固体药学上可接受的有机酸如马来酸或酒石酸的药物制剂，以及制造这种药物组合物的方法。 活性药物成分的药学上可接受的酸盐的pKa小于约6.0，并且其中固体药学上可接受的有机酸的pKa小于约4.0，水溶解度在约500至约2000毫克/ 毫升。 一种药物制剂，其包含吡格列酮的药学上可接受的酸性盐，选自马来酸或酒石酸的固体药学上可接受的有机酸和促进歧化的赋形剂，其中所述固体药学上可接受的有机酸的重量比 赋形剂为约1:6至约1:1。
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