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11. 发明授权

US6007839A Preparation of pharmaceutical compositions containing etherlipid-containing multiple lipid liposomes 失效
标题翻译：含有含醚脂的多种脂质体的药物组合物的制备
公开(公告)号：US6007839A
公开(公告)日：1999-12-28
申请号：US17439
申请日：1998-02-02
申请人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
发明人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
IPC分类号： A61K9/127
CPC分类号： A61K9/1272 , Y10T428/2984
摘要： Described herein are methods of preparing liposome-containing pharmaceutical compositions, the liposomes containing headgroup-derivatized lipids and etherlipids having the formula: ##STR1## Such compositions are useful in the treatment of a variety of conditions, including various cancers and inflammatory disorders.
摘要翻译：本文描述了制备含脂质体的药物组合物的方法，所述脂质体含有头团衍生的脂质和具有下式的醚脂：这样的组合物可用于治疗多种病症，包括各种癌症和炎症性疾病。

12. 发明授权

US5965159A Etherlipid-containing multiple lipid liposomes 失效
公开(公告)号：US5965159A
公开(公告)日：1999-10-12
申请号：US17440
申请日：1998-02-02
申请人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
发明人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
IPC分类号： A61K9/127
CPC分类号： A61K9/1272 , A61K31/685 , A61K9/1271 , Y10T428/2984
摘要： Described herein are liposomes containing etherlipids of the formula: ##STR1## as well as a phosphatidylcholine, a sterol, and a headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.

13. 发明授权

US5762958A Multilipid component ether lipid liposomes 失效
标题翻译：多脂组分醚脂质体
公开(公告)号：US5762958A
公开(公告)日：1998-06-09
申请号：US602669
申请日：1996-02-16
申请人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
发明人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
IPC分类号： A61K9/127 , A61K47/06
CPC分类号： A61K31/685 , A61K9/1271 , Y10T428/2984
摘要： Liposomes are provided which contain ether lipids having the formula: ##STR1## as well as an underivatized phosphatidylethanolamine, a sterol, and a phosphatidylethanolamine-dicarboxylic acid headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.
摘要翻译：提供脂质体，其含有具有下式的醚脂质以及未衍生的磷脂酰乙醇胺，固醇和磷脂酰乙醇胺 - 二羧酸头基衍生的脂质。这些脂质体可用于各种治疗方案，包括治疗癌症和炎症性疾病。

14. 发明授权

US5677337A Methods of treatment using pharmaceutically active ceramide-related compositions 失效
标题翻译：使用药物活性神经酰胺相关组合物治疗的方法
公开(公告)号：US5677337A
公开(公告)日：1997-10-14
申请号：US547688
申请日：1995-10-19
申请人： Yong Wei , Eric Mayhew , Imran Ahmad , Andrew S. Janoff
发明人： Yong Wei , Eric Mayhew , Imran Ahmad , Andrew S. Janoff
IPC分类号： A61K9/127 , A61K31/13 , A61K31/135 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/18 , A61K31/695 , A61K38/00 , A61P35/00 , B01J13/02 , C07C211/21 , C07C211/22 , C07C211/45 , C07C211/49 , C07C215/02 , C07C219/02 , C07C229/02 , C07C233/18 , C07C233/31 , C07C311/03 , C07C311/11 , C07C317/28 , C07F7/18 , C07F9/06 , A61K31/22
CPC分类号： A61K9/1271 , C07F7/1852 , Y10T428/2984
摘要： This invention provides a compound having the formula R.sup.1 --Y.sup.1 --CHZ.sup.1 --CH(NY.sup.2 Y.sup.3)--CH.sub.2 --Z.sup.2, wherein: R.sup.1 is a straight-chained alkyl, alkenyl or alkynyl group having from 8 to 19 carbon atoms in the aliphatic chain; Y.sup.1 is --CH.dbd.CH--, --C.tbd.C-- or --CH(OH)CH(OH)--; Z.sup.1 is OH or a conversion-inhibiting group; Z.sup.2 is a conversion-inhibiting group; Y.sup.2 is H, a phenyl group, an alkyl-substituted phenyl group having from 1 to about 6 carbons in the alkyl chain, or an alkyl chain having from 1 to 6 carbons; Y.sup.3 is H or a group having the formula --C(O)R.sup.2 or --S(O).sub.2 R.sup.2 ; R.sup.2 is a straight-chained alkyl, alkenyl or alkynyl group having from 1 to 23 carbon atoms in the chain; and when Z.sup.2 is an amino, R.sup.2 is an aliphatic chain having from 1 to 9 or from 19 to 23 carbon atoms in the aliphatic chain.
摘要翻译：本发明提供具有式R1-Y1-CHZ1-CH（NY2Y3）-CH2-Z2的化合物，其中：R1是在脂族链中具有8至19个碳原子的直链烷基，烯基或炔基; Y1是-CH = CH-，-C3BON或-CH（OH）CH（OH） - ; Z1是OH或转化抑制基团; Z2是转化抑制基团; Y2是H，苯基，在烷基链中具有1至约6个碳的烷基取代的苯基或具有1至6个碳的烷基链; Y 3是H或具有式-C（O）R 2或-S（O）2 R 2的基团; R2是链中具有1至23个碳原子的直链烷基，烯基或炔基; 当Z 2是氨基时，R 2是在脂族链中具有1至9个或19至23个碳原子的脂族链。

15. 发明授权

US5580899A Hydrophobic taxane derivatives 失效
标题翻译：疏水紫杉烷衍生物
公开(公告)号：US5580899A
公开(公告)日：1996-12-03
申请号：US474888
申请日：1995-06-07
申请人： Eric Mayhew , J. Craig Franklin , Suresh Bhatia , Paul A. Harmon , Andrew S. Janoff
发明人： Eric Mayhew , J. Craig Franklin , Suresh Bhatia , Paul A. Harmon , Andrew S. Janoff
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。

16. 发明授权

US5415869A Taxol formulation 失效
标题翻译：紫杉醇制剂
公开(公告)号：US5415869A
公开(公告)日：1995-05-16
申请号：US151215
申请日：1993-11-12
申请人： Robert M. Straubinger , Amarnath Sharma , Eric Mayhew
发明人： Robert M. Straubinger , Amarnath Sharma , Eric Mayhew
IPC分类号： A61K47/24 , A61K9/127 , A61K31/335 , A61K31/70 , A61P35/00 , A61K9/133
CPC分类号： A61K31/70 , A61K31/335 , A61K9/127
摘要： The present invention relates to a pharmaceutical composition for use in treatment of cancer patients. The composition includes at least one taxane present in a pharmaceutical effective amount and a mixture of one or more negatively charged phospholipids and one or more zwitterion (i.e. uncharged) phospholipids. This mixture entraps the at least one taxane in what is believed to be a liposome. The mixture contains a ratio of negatively charged phospholipids to zwitterion phospholipids of 1:9 to 7:3. The taxol is present in an amount of 1.5-8.0 mole percent taxane. The composition is in the form of particles having a size of 0.025 to 10 microns with substantially no taxane crystals.
摘要翻译：本发明涉及用于治疗癌症患者的药物组合物。组合物包含至少一种以药物有效量存在的紫杉烷和一种或多种带负电荷的磷脂与一种或多种两性离子（即不带电荷的）磷脂的混合物。这种混合物在所谓的脂质体中截留至少一种紫杉烷。该混合物含有负电荷的磷脂与两性离子磷脂的比例为1:9至7:3。紫杉醇的量为1.5-8.0摩尔百分数紫杉烷。该组合物为具有0.025至10微米尺寸的颗粒形式，基本上不含紫杉烷晶体。

17. 再颁专利

USRE39042E1 Etherlipid-containing multiple lipid liposomes 失效
标题翻译：含脂质的多种脂质体
公开(公告)号：USRE39042E1
公开(公告)日：2006-03-28
申请号：US09976936
申请日：2001-10-11
申请人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
发明人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
IPC分类号： A61K9/127
CPC分类号： A61K9/1272 , Y10T428/2984
摘要： Described herein are liposomes containing etherlipids of the formula: as well as a phosphatidylcholine, a sterol, and a headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.
摘要翻译：本文描述了含有下式的醚脂的脂质体：以及磷脂酰胆碱，固醇和头团衍生的脂质。这些脂质体可用于各种治疗方案，包括治疗癌症和炎症性疾病。

18. 发明授权

US06500461B2 Particulate formulations 失效
标题翻译：颗粒配方
公开(公告)号：US06500461B2
公开(公告)日：2002-12-31
申请号：US09314338
申请日：1999-05-19
申请人： Walter Perkins , Xingong Li , Donald Hirsh , Eric Mayhew , Imran Ahmad , Shaukat Ali , Andrew Janoff
发明人： Walter Perkins , Xingong Li , Donald Hirsh , Eric Mayhew , Imran Ahmad , Shaukat Ali , Andrew Janoff
IPC分类号： A61K914
CPC分类号： A61K47/6929 , A61K47/542
摘要： This invention provides vehicles capable of delivering high concentrations of poorly hydrophilic/poorly lipophilic compounds to animals, by combining compounds having biocompatible hydrophobic domains with conjugates having both hydrophobic and hydrophilic regions. Such formulations are suitable for a number of uses in animals, particularly the administration thereto of high concentrations of therapeutically useful compound, without an undue level of side effects.
摘要翻译：本发明提供能够通过将具有生物相容性疏水域的化合物与具有疏水和亲水区两者的缀合物组合的化合物，将能够将高浓度亲水性差/亲脂性差的化合物递送给动物的载体。这样的制剂适用于动物中的许多用途，特别是其给予高浓度的治疗有用的化合物，而没有不适当的副作用水平。

19. 发明授权

US06291690B1 Hydrophobic taxane derivatives 失效
标题翻译：疏水紫杉烷衍生物
公开(公告)号：US06291690B1
公开(公告)日：2001-09-18
申请号：US09567366
申请日：2000-05-09
申请人： Eric Mayhew , J. Craig Franklin , Suresh Bhatia , Paul A. Harmon , Andrew S. Janoff
发明人： Eric Mayhew , J. Craig Franklin , Suresh Bhatia , Paul A. Harmon , Andrew S. Janoff
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。

20. 发明授权

US5942246A Etherlipid containing multiple lipid liposomes 失效
标题翻译：含有多种脂质体的醚脂
公开(公告)号：US5942246A
公开(公告)日：1999-08-24
申请号：US17366
申请日：1998-02-02
申请人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
发明人： Eric Mayhew , Andrew S. Janoff , Imran Ahmad , Suresh K. Bhatia
IPC分类号： A61K9/127 , A61K9/133
CPC分类号： A61K9/1272 , A61K31/685 , A61K9/1271 , Y10T428/2984
摘要： Liposomes are provided which contain etherlipids having the formula: ##STR1## as well as an unsaturated or partially unsaturated phospholipid, a sterol, and a phosphatidylethanolamine-based headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.
摘要翻译：提供了含有具有下式的醚脂的脂质体：以及不饱和或部分不饱和的磷脂，固醇和基于磷脂酰乙醇胺的头组衍生的脂质。这些脂质体可用于各种治疗方案，包括治疗癌症和炎症性疾病。

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