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1. 发明授权

US07169819B2 Pharmaceutical compositions of fenretinide having increased bioavailability and methods of using the same 有权
标题翻译：具有增加的生物利用度的芬维A胺的药物组合物及其使用方法
公开(公告)号：US07169819B2
公开(公告)日：2007-01-30
申请号：US10010914
申请日：2001-12-05
申请人： Shanker Gupta , Barry J. Maurer , C. Patrick Reynolds , B. Rao Vishnuvajjala
发明人： Shanker Gupta , Barry J. Maurer , C. Patrick Reynolds , B. Rao Vishnuvajjala
IPC分类号： A61K31/07 , A61K47/00 , A61P35/00
CPC分类号： A61K31/16 , A61K9/107 , A61K9/1075 , A61K31/164 , A61K31/167 , A61K47/10 , A61K47/44 , Y10S514/937 , Y10S514/938 , Y10S514/975
摘要： A pharmaceutical composition for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent capable of dispersing or solubilizing the retinide. The solvent comprises an alcohol, such as ethanol, in combination with an alkoxylated castor oil, such as CREMOPHOR® EL, or comprising a retinide, such as fenretinide, in an emulsion composed of a lipoid dispersed in an aqueous phase, a stabilizing amount of a non-ionic surfactant, optionally a solvent, and optionally an isotonic agent. In addition, a method of use in the treatment of hyperproliferative disorders, such as cancers is described.
摘要翻译：一种用于胃肠外递送的药物组合物，其包含视网膜如芬维A胺与能够分散或溶解视黄酸盐的溶剂的组合。溶剂包括醇，如乙醇，与烷氧基化蓖麻油（如ELEM）组合，或在分散在水相中的脂质组成的乳液中包含视黄酸盐，如芬维A胺，稳定剂非离子表面活性剂，任选的溶剂和任选的等渗剂的量。此外，描述了用于治疗过度增殖性疾病如癌症的方法。

2. 发明授权

US07476692B2 Pharmaceutical compositions of safingol and methods of using the same 有权
标题翻译：安息香的药物组合物及其使用方法
公开(公告)号：US07476692B2
公开(公告)日：2009-01-13
申请号：US10782459
申请日：2004-02-19
申请人： Shanker Gupta , C. Patrick Reynolds , Barry J. Maurer , B. Rao Vishnuvajjala
发明人： Shanker Gupta , C. Patrick Reynolds , Barry J. Maurer , B. Rao Vishnuvajjala
IPC分类号： A61K31/19 , A61K31/13
CPC分类号： A61K31/133 , A61K9/0019 , A61K9/08 , A61K9/107 , A61K9/19 , A61K31/19 , A61K31/685 , A61K31/739 , A61K47/10 , A61K47/12 , A61K47/26
摘要： The present invention provides stable aqueous solutions consisting essentially of: (a) a sphingolipid; (b) lactic acid; and (c) optionally a stabilizing agent; wherein the solution has a molar ratio of lactic acid to sphingolipid of 1:1 to 10:1. The present invention further provides an emulsion formulation consisting essentially of: (a) lactic acid; (b) a sphingolipid, wherein the sphingolipid is present in an amount of about 0.1 to about 30 mg/ml of emulsion; (b) optionally an isotonic agent; and (c) a phospholipid present in an amount of about 0.2 to about 200 mg/ml of emulsion. Methods of making and using the compositions are also provided.
摘要翻译：本发明提供基本上由以下组成的稳定的水溶液：（a）鞘脂; （b）乳酸; 和（c）任选的稳定剂; 其中所述溶液的乳酸与鞘脂的摩尔比为1:1至10:1。本发明还提供一种乳液制剂，其主要由以下物质组成：（a）乳酸; （b）鞘脂，其中所述神经鞘脂以约0.1至约30mg / ml的乳剂的量存在; （b）任选的等渗剂; 和（c）以约0.2至约200mg / ml的乳液的量存在的磷脂。还提供了制备和使用组合物的方法。

3. 发明授权

US06368831B1 Treatment of hyperproliferative disorders 有权
标题翻译：治疗过度增生性疾病
公开(公告)号：US06368831B1
公开(公告)日：2002-04-09
申请号：US09471944
申请日：1999-12-23
申请人： Barry J. Maurer , C. Patrick Reynolds
发明人： Barry J. Maurer , C. Patrick Reynolds
IPC分类号： C12N1509
CPC分类号： A61K31/165 , A61K31/07 , A61K31/535 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors and/or 1-acylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.
摘要翻译：一种治疗需要这种治疗的受试者的过度增殖性疾病的方法，包括给所述受试者组合施用治疗有效量的：（a）产生神经酰胺的类视黄醇例如芬维A胺或其药学上可接受的盐; 和（b）至少一种（以及在某些实施方案中为至少两种）神经酰胺降解抑制剂，例如选自（i）葡萄糖神经酰胺合成抑制剂和/或1-酰基神经酰胺合成抑制剂的化合物，（ii）鞘氨醇-1 磷酸盐合成抑制剂，和（iii）蛋白激酶C抑制剂。优选的葡糖基神经酰胺合成抑制剂是1-苯基-2-棕榈酰氨基-3-吗啉代-1-丙醇。优选的鞘氨醇-1-磷酸合成抑制剂是D-赤式-N，N-二甲基鞘氨醇。优选的蛋白激酶C抑制剂是L-苏式 - 二氢鞘氨醇。

4. 发明授权

US06352844B1 Treatment of hyperproliferative disorders 有权
标题翻译：治疗过度增生性疾病
公开(公告)号：US06352844B1
公开(公告)日：2002-03-05
申请号：US09342019
申请日：1999-06-28
申请人： Barry J. Maurer , Myles Cabot , C. Patrick Reynolds
发明人： Barry J. Maurer , Myles Cabot , C. Patrick Reynolds
IPC分类号： C12N1509
CPC分类号： A61K45/06 , A61K31/07 , A61K31/165 , A61K31/535 , A61K31/70 , Y10S424/15 , A61K2300/00
摘要： A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.
摘要翻译：一种治疗需要这种治疗的受试者的过度增殖性疾病的方法，包括给所述受试者组合施用治疗有效量的：（a）产生神经酰胺的类视黄醇例如芬维A胺或其药学上可接受的盐; 和（b）至少一种（和在某些实施方案中至少两种）神经酰胺降解抑制剂，例如选自（i）葡糖基神经酰胺合成抑制剂，（ii）鞘氨醇-1-磷酸合成抑制剂和（iii））蛋白激酶C抑制剂。优选的葡糖基神经酰胺合成抑制剂是1-苯基-2-棕榈酰氨基-3-吗啉代-1-丙醇。优选的鞘氨醇-1-磷酸合成抑制剂是D-赤式-N，N-二甲基鞘氨醇。优选的蛋白激酶C抑制剂是L-苏式 - 二氢鞘氨醇。

5. 发明授权

US07785621B2 Oral compositions of fenretinide having increased bioavailability and methods of using the same 有权
标题翻译：具有增加的生物利用度的芬维A胺的口服组合物及其使用方法
公开(公告)号：US07785621B2
公开(公告)日：2010-08-31
申请号：US10767352
申请日：2004-01-30
申请人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
发明人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
IPC分类号： A61K47/00 , A61K31/16 , A23L1/308
CPC分类号： A61K9/0095 , A23L33/10 , A23V2002/00 , A61K9/1617 , A61K9/1664 , A61K31/167 , A23V2250/30 , A23V2250/186 , A23V2250/192 , A23V2250/1846
摘要： The present invention provides an edible composition for oral delivery of an active agent such as a retinide. The composition comprises, in the form of a dry flowable powder: (a) an active agent such as a retinide; (b) lipid matrix composition; (c) optionally sweetener; (d) flour. Compositions of the invention may be administered per se or mixed with a solid or liquid food carrier, for direct oral consumption by a subject or administration through a feeding tube.
摘要翻译：本发明提供了用于口服递送活性剂如视黄酸盐的可食用组合物。组合物包含干燥可流动粉末的形式：（a）活性剂如视黄酸盐; （b）脂质基质组成; （c）任选的甜味剂; （d）面粉。本发明的组合物本身可以施用或与固体或液体食品载体混合，由受试者或给药通过饲管直接口服消费。

6. 发明申请

US20050271707A1 Oral compositions having increased bioavailability and methods of using the same 审中-公开
标题翻译：具有增加的生物利用度的口服组合物及其使用方法
公开(公告)号：US20050271707A1
公开(公告)日：2005-12-08
申请号：US11170371
申请日：2005-06-29
申请人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
发明人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
IPC分类号： A23L1/30 , A61K9/00 , A61K31/167 , A61K47/00 , A61K31/337
CPC分类号： A61K9/0095 , A23L33/10 , A23V2002/00 , A61K9/1617 , A61K9/1664 , A61K31/167 , A23V2250/30 , A23V2250/186 , A23V2250/192 , A23V2250/1846
摘要： The present invention provides an edible composition for oral delivery of an active agent such as paclitaxel or a retinide. The composition comprises, in the form of a dry flowable powder: (a) an active agent such as a retinide; (b) lipid matrix composition; (c) optionally sweetener; (d) flour. Compositions of the invention may be administered per se or mixed with a solid or liquid food carrier, for direct oral consumption by a subject or administration through a feeding tube.
摘要翻译：本发明提供了用于口服递送活性剂如紫杉醇或视黄酸盐的可食用组合物。组合物包含干燥可流动粉末的形式：（a）活性剂如视黄酸盐; （b）脂质基质组成; （c）任选的甜味剂; （d）面粉。本发明的组合物本身可以施用或与固体或液体食品载体混合，由受试者或给药通过饲管直接口服消费。

7. 发明授权

US07780978B2 Oral pharmaceutical compositions and methods of using the same 有权
标题翻译：口服药物组合物及其使用方法
公开(公告)号：US07780978B2
公开(公告)日：2010-08-24
申请号：US11170561
申请日：2005-06-29
申请人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
发明人： Barry J. Maurer , Charles Patrick Reynolds , David W. Yesair , Robert Travis McKee , Stephen W. Burgess , Walter A. Shaw
IPC分类号： A61K47/00 , A61K31/16 , A23L1/308
CPC分类号： A61K9/0095 , A23L33/10 , A23V2002/00 , A61K9/1617 , A61K9/1664 , A61K31/167 , A23V2250/30 , A23V2250/186 , A23V2250/192 , A23V2250/1846
摘要： The present invention provides an edible composition for oral delivery of an active agent such as paclitaxel or a retinide. The composition comprises, in the form of a dry flowable powder: (a) an active agent such as a retinide; (b) lipid matrix composition; (c) optionally sweetener; (d) flour. Compositions of the invention may be administered per se or mixed with a solid or liquid food carrier, for direct oral consumption by a subject or administration through a feeding tube.
摘要翻译：本发明提供了用于口服递送活性剂如紫杉醇或视黄酸盐的可食用组合物。组合物包含干燥可流动粉末的形式：（a）活性剂如视黄酸盐; （b）脂质基质组成; （c）任选的甜味剂; （d）面粉。本发明的组合物本身可以施用或与固体或液体食品载体混合，由受试者或给药通过饲管直接口服消费。

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