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11. 发明申请

US20060116354A1 Antineoplastic ether lipid compounds with modifications at the sn-3 carbon 审中-公开
标题翻译：具有在sn-3碳上修饰的抗肿瘤醚脂质化合物
公开(公告)号：US20060116354A1
公开(公告)日：2006-06-01
申请号：US10541864
申请日：2004-01-09
申请人： Walter Perkins
发明人： Walter Perkins
IPC分类号： A61K31/685 , C07F9/547
CPC分类号： C07D211/24 , C07C307/02 , C07C309/14 , C07C309/19 , C07D295/088 , C07F9/10 , C07F9/4006 , C07F9/5407
摘要： Ether lipid compounds of formula (I), pharmaceutically-acceptable salts, prodrugs or isomers thereof are provided, where the variables are as defined herein. The compounds of the invention have anti-neoplastic activity, and accordingly have utility in treating cancer and related diseases. Enantiomers of these compounds, pharmaceutical compositions, and methods for treating cancer with the pharmaceutical compositions are also provided.
摘要翻译：提供式（I）的醚类脂质化合物，其药学上可接受的盐，前体药物或异构体，其中变量如本文所定义。本发明的化合物具有抗肿瘤活性，因此具有治疗癌症和相关疾病的效用。还提供了这些化合物的对映异构体，药物组合物和用药物组合物治疗癌症的方法。

12. 发明申请

US20060062839A1 Efficient liposomal encapsulation under mild conditions 审中-公开
标题翻译：在温和条件下高效的脂质体包封
公开(公告)号：US20060062839A1
公开(公告)日：2006-03-23
申请号：US10500977
申请日：2003-01-08
申请人： Alla Polozova , Xingong Li , Walter Perkins
发明人： Alla Polozova , Xingong Li , Walter Perkins
IPC分类号： A61K9/127
CPC分类号： A61K9/1277 , A61K9/1278
摘要： A method for preparing liposomes containing at least one biologically active substance encapsulated therein under mild conditions comprises the following steps: (A) providing liposomes, wherein the liposomes are prepared by a method other than the instant method; (B) mixing the product of step (A) with a water-miscible organic solvent to form a gel or a liquid containing gel particles; and thereafter (C) (a) mixing the gel or liquid containing gel particles with aqueous medium V to directly form the liposomes containing the at least one biologically active substance encapsulated therein, (b) (i) mixing the gel or liquid containing gel particles with aqueous medium V to form a curd or curdy substance; and (ii) mixing the curd or curdy substance with aqueous medium W to directly form the liposomes containing the at least one biologically active substance encapsulated therein, or (c) (i) cooling the gel or liquid containing gel particles to form a waxy substance; and (ii) mixing the waxy substance with aqueous medium W to directly form the liposomes containing the at least one biologically active substance encapsulated therein; wherein the at least one biologically active substance is added in step (A), (B) or (C), and wherein aqueous media V and W are the same or different.
摘要翻译：一种在温和条件下包含至少一种包含其中的生物活性物质的脂质体的制备方法包括以下步骤：（A）提供脂质体，其中通过本方法以外的方法制备脂质体; （B）将步骤（A）的产物与水混溶性有机溶剂混合以形成凝胶或含有凝胶颗粒的液体; 然后（C）（a）将含有凝胶颗粒的凝胶或液体与水性介质V混合以直接形成包含至少一种生物活性物质的脂质体，（b）（i）将含有凝胶颗粒的凝胶或液体与水性介质V形成凝乳或卷曲物质; 和（ii）将凝乳或卷曲物质与水性介质W混合以直接形成包含其中的至少一种生物活性物质的脂质体，或（c）（i）冷却含有凝胶颗粒的凝胶或液体以形成蜡状物质 ; 和（ii）将蜡状物质与水性介质W混合以直接形成含有其中包封的至少一种生物活性物质的脂质体; 其中所述至少一种生物活性物质在步骤（A），（B）或（C）中加入，并且其中水性介质V和W相同或不同。

13. 发明申请

US20060058249A1 Efficient nucleic acid encapsulation into medium sized liposomes 审中-公开
标题翻译：将有效的核酸封装到中等大小的脂质体中
公开(公告)号：US20060058249A1
公开(公告)日：2006-03-16
申请号：US10500933
申请日：2003-01-08
申请人： Shangguan Tong , Xingong Li , Paul Meers , Walter Perkins
发明人： Shangguan Tong , Xingong Li , Paul Meers , Walter Perkins
IPC分类号： A61K48/00 , A61K9/127
CPC分类号： A61K9/127 , A61K9/1277 , A61K47/36 , C12N15/88
摘要： A method for preparing liposomes containing at least one nucleic acid encapsulated therein comprising the following steps: (A) mixing a gel or a liquid containing gel particles with aqueous medium Z1 to directly form the liposomes containing the at least one nucleic acid encapsulated therein; (B)(i) mixing a gel or a liquid containing gel particles with aqueous medium Z1 to form a curd or curdy substance; and (ii) mixing the curd or curdy substance with aqueous medium Z2 to directly form the liposomes containing the at least one nucleic acid encapsulated therein; or (C)(i) cooling a gel or a liquid containing gel particles to form a waxy substance; and (ii) mixing the waxy substance with aqueous medium Z1 to directly form the liposomes containing the at least one nucleic acid encapsulated therein; wherein said gel or liquid containing gel particles comprises at least one liposome-forming lipid, at least one fusogenic lipid, a water-miscible organic solvent and the at least one nucleic acid; wherein an amount of the at least one fusogenic lipid is at least 20% by weight of a lipid content of the gel or the liquid containing gel particles; and wherein the aqueous media Z1 and Z2 are the same or different.
摘要翻译：一种制备含有至少一种包封的核酸的脂质体的方法，包括以下步骤：（A）将凝胶或含有凝胶颗粒的液体与水性介质Z1混合以直接形成包含至少一种核酸的脂质体; （B）（i）将凝胶或含有凝胶颗粒的液体与水性介质Z1混合以形成凝乳或卷曲物质; 和（ii）将凝乳或卷曲物质与水性介质Z2混合以直接形成含有其中包封的至少一种核酸的脂质体; 或（C）（i）冷却凝胶或含有凝胶颗粒的液体以形成蜡状物质; 和（ii）将蜡质物质与水性介质Z1混合以直接形成包含其中包含至少一种核酸的脂质体; 其中所述含凝胶或液体的凝胶颗粒包含至少一种形成脂质体的脂质，至少一种融合脂质，与水可混溶的有机溶剂和所述至少一种核酸; 其中所述至少一种融合脂质的量为所述凝胶或含有凝胶颗粒的液体的脂质含量的至少20重量％并且其中水性介质Z1和Z2相同或不同。

14. 发明申请

US20050249822A1 Administration of cisplatin by inhalation 审中-公开
标题翻译：通过吸入给药顺铂
公开(公告)号：US20050249822A1
公开(公告)日：2005-11-10
申请号：US11084070
申请日：2005-03-18
申请人： Frank Pilkiewicz , Walter Perkins , Beth Metzheiser
发明人： Frank Pilkiewicz , Walter Perkins , Beth Metzheiser
IPC分类号： A61K9/00 , A61K9/127 , A61K31/282 , A61K31/555 , A61K33/24
CPC分类号： A61K9/0078 , A61K9/127 , A61K31/282 , A61K31/555 , A61K33/24
摘要： Provided is a method for treating a patient having lung cancer. The method includes administering a lipid composition containing cisplatin to the patient's respiratory tract over the course of at least 2 treatment cycles. At least about 15 mg/m2 of cisplatin is administered in each treatment cycle, and there is no more than 2 weeks between treatment cycles.
摘要翻译：提供一种治疗患有肺癌的患者的方法。该方法包括在至少2个治疗周期的过程中向患者的呼吸道施用含有顺铂的脂质组合物。在每个治疗周期中施用至少约15mg / m 2顺铂，并且在治疗周期之间不超过2周。

15. 发明授权

US5766624A Liposomal defensins 失效
标题翻译：脂质体防御素
公开(公告)号：US5766624A
公开(公告)日：1998-06-16
申请号：US449598
申请日：1995-05-24
申请人： Andrew S. Janoff , Walter Perkins , Imran Ahmad
发明人： Andrew S. Janoff , Walter Perkins , Imran Ahmad
IPC分类号： A61K9/127 , A61K38/00 , A61K38/17 , A61P31/04 , A61P35/00 , A61P37/04
CPC分类号： A61K38/17 , A61K9/127
摘要： Defensins are microbicidal, tumoricidal cytotoxic protein components of animal host defense systems. They can be entrapped in liposomes containing release-inhibiting lipid such that the defensins are neutralized, and their release from the liposomes is inhibited; however, the defensins remain effective when exposed to endocytosed material in endocytic vesicles. Liposomal defensin formulations are administered to animals for the treatment or prevention of microbial infections, for the treatment of cancers and for the treatment of disorders characterized by a deficiency of protein-mediated cytotoxic activity in cytoplasmic granules.
摘要翻译：防卫素是动物宿主防御系统的杀菌，杀肿瘤细胞毒性蛋白质成分。它们可以被包裹在含有释放抑制脂质的脂质体中，使得防御素被中和，并且它们从脂质体的释放被抑制; 然而，防御素在暴露于内吞囊泡中的内吞物质时仍然有效。向动物施用脂质体防御素制剂用于治疗或预防微生物感染，用于治疗癌症和用于治疗以细胞质颗粒中蛋白质介导的细胞毒活性缺乏为特征的病症。

16. 发明授权

US5415867A High ratio active agent: lipid complex 失效
标题翻译：高比例活性剂：脂质复合物
公开(公告)号：US5415867A
公开(公告)日：1995-05-16
申请号：US105764
申请日：1993-08-11
申请人： Sharma R. Minchey , Christine E. Swenson , Andrew S. Janoff , Lawrence Boni , Kathy A. Stewart , Walter Perkins
发明人： Sharma R. Minchey , Christine E. Swenson , Andrew S. Janoff , Lawrence Boni , Kathy A. Stewart , Walter Perkins
IPC分类号： A61K9/127 , A61K31/545 , A61K49/04
CPC分类号： A61K49/0466 , A61K31/545 , A61K47/48053 , A61K9/127
摘要： High ratio active agent:lipid complexes, their preparation and use are disclosed. Particular reference is made to cephalosporin:lipid complex and iodinated contrast agent:lipid complex. Use of high ratio cephalosporin:lipid complex in bacterial prophylaxis, and particularly bacteremia prophylaxis, including a method of preventing bacterial infection in an animal over an extended period comprising the step of administering to said animal a high ratio cephalosporin:lipid complex is further disclosed as is the use of high ratio iodinated contrast agent:lipid complex in X-ray applications.
摘要翻译：高比例的活性剂：脂质复合物，其制备和用途被公开。特别提到头孢菌素：脂质复合物和碘化造影剂：脂质复合物。在细菌预防中使用高比例头孢菌素：脂质复合物，特别是菌血症预防，包括在长时间内预防动物细菌感染的方法，包括向所述动物施用高比例头孢菌素：脂质复合物的步骤进一步公开为是使用高比例碘化造影剂：X射线应用中的脂质复合物。

17. 发明申请

US20070190180A1 Methods of treating cancer with high potency lipid-based platinum compound formulations administered intravenously 审中-公开
标题翻译：用静脉内施用的高效脂质类铂化合物制剂治疗癌症的方法
公开(公告)号：US20070190180A1
公开(公告)日：2007-08-16
申请号：US11592714
申请日：2006-11-03
申请人： Frank Pilkiewicz , Roman Perez-Soler , Walter Perkins , Yiyu Zou , Mary Neville , Jin Lee
发明人： Frank Pilkiewicz , Roman Perez-Soler , Walter Perkins , Yiyu Zou , Mary Neville , Jin Lee
IPC分类号： A61K33/24 , A61K31/555 , A61K31/282
CPC分类号： A61K31/555 , A61K9/0019 , A61K9/127 , A61K31/282 , A61K33/24
摘要： In one aspect, the present invention relates to methods of treating cancer in a patient comprising administering intravenously to a patient in need thereof a cancer treating effective amount of a lipid-based platinum compound formulation wherein the concentration of the platinum compound of the lipid-based platinum compound formulation is greater than about 1.2 mg/ml.
摘要翻译：一方面，本发明涉及在患者中治疗癌症的方法，包括向有需要的患者静脉内施用治疗有效量的基于脂质的铂化合物制剂的癌症，其中所述脂质基铂化合物的铂化合物的浓度铂化合物制剂大于约1.2mg / ml。

18. 发明申请

US20060122153A1 Antineoplastic ether lipid compounds with modifications at the sn-2 carbon 审中-公开
标题翻译：在sn-2碳上具有修饰的抗肿瘤醚类脂质化合物
公开(公告)号：US20060122153A1
公开(公告)日：2006-06-08
申请号：US10541862
申请日：2004-01-09
申请人： Walter Perkins
发明人： Walter Perkins
IPC分类号： A61K31/685 , C07F9/6533 , C07F9/59 , C07F9/06
CPC分类号： C07F9/10 , C07F9/59
摘要： Ether lipid compounds of formula (I), Pharmaceutically-acceptable salts, prodrugs or isomers thereof are provided, where the variables are as defined herein. The compounds of the invention have antineoplastic activity, and accordingly have utility in treating cancer and related diseases. Enantiomers of these compounds, pharmaceutical compositions, and methods for treating cancer with the pharmaceutical compositions are also provided.
摘要翻译：提供式（I）的醚类脂质化合物，其药学上可接受的盐，前药或异构体，其中变量如本文所定义。本发明的化合物具有抗肿瘤活性，因此具有治疗癌症和相关疾病的效用。还提供了这些化合物的对映异构体，药物组合物和用药物组合物治疗癌症的方法。

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