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41. 发明授权

US5662930A Reduction of liposome-induced adverse physiological reactions 失效
标题翻译：减少脂质体诱导的不良生理反应
公开(公告)号：US5662930A
公开(公告)日：1997-09-02
申请号：US433665
申请日：1995-05-04
申请人： Patrick L. Ahl , Suresh K. Bhatia , Sharma R. Minchey , Andrew S. Janoff
发明人： Patrick L. Ahl , Suresh K. Bhatia , Sharma R. Minchey , Andrew S. Janoff
IPC分类号： A61K9/127 , A61P9/02 , A61K9/133
CPC分类号： A61K9/1271 , Y10T428/2984
摘要： Provided herein is a method of administering a liposome composition to an animal, the method involving adminstering to the animal a liposome composition containing an adverse physiological reaction-reducing effective amount of a liposome which has, in addition to a bioactive agent, a lipid bilayer containing a lipid and a surface agent-modified molecule. An adverse physiological reaction which may be experienced by the animal upon administration of a liposome composition is reduced by way of the presence of the surface agent-modified molecule in the liposome's lipid bilayer.
摘要翻译：本文提供了向动物施用脂质体组合物的方法，该方法涉及向动物施用含有不利的生理学降低反应的有效量的脂质体的脂质体组合物，该有效量除了生物活性剂外还含有含有脂质和表面活性剂改性分子。通过在脂质体脂质双层中存在表面活性剂修饰的分子，减少了在施用脂质体组合物时可能经历的不良生理反应。

42. 发明授权

US5614216A Synthetic lung surfactant 失效
标题翻译：合成肺表面活性剂
公开(公告)号：US5614216A
公开(公告)日：1997-03-25
申请号：US442079
申请日：1995-05-16
申请人： Andrew S. Janoff
发明人： Andrew S. Janoff
IPC分类号： A61K9/127
CPC分类号： A61K31/685 , Y10S514/958
摘要： A synthetic lung surfactant composition and process for depositing a monolayer of a phosphatidylcholine lung surfactant to the alveoli of a mammal. The composition comprises a phosphatidylcholine lung surfactant, a phosphatidylethanolamine, and cholesterol in proportions such that the composition is in lamellar form at or below a first temperature and in non-lamellar form at a second temperature which is higher than the first temperature. A preferred phosphatidylcholine lung surfactant for use in this invention is dipalmitoyl phosphatidylcholine (DPPC), which is known to be the major lipid constituent of natural mammalian lung surfactant, and a preferred phosphatidylethanolamine is dioleoyl phosphatidylethanolamine (DOPE). In particular embodiments, the composition is in lamellar form at about room temperature (25.degree. C.), and in non-lamellar form at a temperature in the range of about 30.degree. to 37.degree. C., which is at or below normal human body temperature (37.degree. C.). The composition may also include one or more therapeutic peptides or other pharmaceutical agents. The synthetic lung surfactant may be used to treat a mammal for respiratory distress syndrome caused by an insufficiency of natural lung surfactant.
摘要翻译：一种合成肺表面活性剂组合物和用于将磷脂酰胆碱肺表面活性剂的单层沉积到哺乳动物的肺泡的方法。组合物包含磷脂酰胆碱肺表面活性剂，磷脂酰乙醇胺和胆固醇，其比例使得组合物在低于第一温度或低于第一温度的层状形式，并且在高于第一温度的第二温度下以非层状形式。用于本发明的优选的磷脂酰胆碱肺表面活性剂是二棕榈酰磷脂酰胆碱（DPPC），其已知是天然哺乳动物肺表面活性剂的主要脂质组分，优选的磷脂酰乙醇胺是二油酰磷脂酰乙醇胺（DOPE）。在具体实施方案中，组合物在约室温（25℃）下为薄片形式，并且在约30-37℃的温度范围内以非层状形式，其处于或低于正常人体温（37℃）。组合物还可以包括一种或多种治疗性肽或其它药剂。合成肺表面活性剂可用于治疗由天然肺表面活性剂不足引起的呼吸窘迫综合征的哺乳动物。

43. 发明授权

US07491409B1 Encapsulation of bioactive complexes in liposomes 失效
标题翻译：生物活性复合物在脂质体中的封装
公开(公告)号：US07491409B1
公开(公告)日：2009-02-17
申请号：US09914615
申请日：2000-03-01
申请人： Paul R. Meers , Tong Shangguan , Donna Cabral-Lilly , Patrick Ahl , Andrew S. Janoff
发明人： Paul R. Meers , Tong Shangguan , Donna Cabral-Lilly , Patrick Ahl , Andrew S. Janoff
IPC分类号： A61K9/127
CPC分类号： A61K9/1272 , A61K9/127
摘要： This invention provides a method to prepare liposome-encapsulated bioactive agents such as nucleic acids, comprising complexation of the bioactive agents in reverse micelles prior to forming liposomes, as well as methods of using the liposomes so formed and formulations to deliver nucleic acids to cells.
摘要翻译：本发明提供了一种制备脂质体包封的生物活性剂如核酸的方法，其包括在形成脂质体之前在反胶束中络合生物活性剂，以及使用如此形成的脂质体和制剂将核酸递送至细胞的方法。

44. 发明授权

US06015716A Detection of endotoxin levels in liposomes, lipid bilayers and lipid complexes 失效
标题翻译：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
申请人： Paul A. Harmon , Donna J. Cabral-Lilly , J. Craig Franklin , Robert A. Reed , Andrew S. Janoff
发明人： Paul A. Harmon , Donna J. Cabral-Lilly , J. Craig Franklin , Robert A. Reed , Andrew S. Janoff
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。

45. 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。

46. 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.

47. 发明授权

US5925375A Therapeutic use of multilamellar liposomal prostaglandin formulations 失效
标题翻译：多层脂质体前列腺素制剂的治疗用途
公开(公告)号：US5925375A
公开(公告)日：1999-07-20
申请号：US333770
申请日：1994-11-03
申请人： Robert P. Lenk , Michelle L. Tomsho , Robert L. Suddith , Robert J. Klimchak , Andrew S. Janoff , Sharma R. Minchey , Marc J. Ostro
发明人： Robert P. Lenk , Michelle L. Tomsho , Robert L. Suddith , Robert J. Klimchak , Andrew S. Janoff , Sharma R. Minchey , Marc J. Ostro
IPC分类号： A61K9/127 , A61K31/5575 , A61K9/133
CPC分类号： A61K31/5575 , A61K9/127 , A61K9/1278 , Y10S977/907 , Y10S977/915
摘要： This invention provides a multilamellar liposome containing an arachidonic acid metabolite, two or more lipid-containing bilayers and two or more aqueous compartments containing a release-inhibiting buffer. Preferred arachidonic acid metabolites are the prostaglandins, particularly PGE.sub.1. The liposomal formulations can be used to treat animals, particularly humans, for diseases, disorders or conditions which can be ameliorated by prostaglandins, e.g., disorders characterized by cellular activation and adhesion, inflammation and/or toxemia.
摘要翻译：本发明提供了含有花生四烯酸代谢物，两种或更多种含脂双层体和含有释放抑制缓冲液的两个或多个含水室的多层脂质体。优选的花生四烯酸代谢物是前列腺素，特别是PGE1。脂质体制剂可用于治疗可由前列腺素改善的疾病，病症或病症的动物，特别是人，例如以细胞活化和粘附，炎症和/或毒血症为特征的病症。

48. 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。

49. 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。

50. 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。

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