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11. 发明授权

US07700612B2 Di-ester prodrugs of camptothecin, process for their preparation and their therapeutical applications 失效
标题翻译：喜树碱的二酯前药，其制备方法及其治疗应用
公开(公告)号：US07700612B2
公开(公告)日：2010-04-20
申请号：US10583803
申请日：2004-12-23
申请人： Patrick Soon-Shiong , Neil P. Desai , Chunlin Tao , Cheng Zhi Yu
发明人： Patrick Soon-Shiong , Neil P. Desai , Chunlin Tao , Cheng Zhi Yu
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： C07D491/22 , C07D498/14
摘要： The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced toxicity, while maintaining anti-cancer activity.
摘要翻译：本发明涉及喜树碱的10,20-二-O-酯衍生物及其药物制剂。本发明的化合物和药物制剂在保持抗癌活性的同时具有增加的生物寿命和生物利用度和降低的毒性。

12. 发明申请

US20100035800A1 NOVEL FORMULATIONS OF PHARMACOLOGICAL AGENTS, METHODS FOR THE PREPARATION THEREOF AND METHODS FOR THE USE THEREOF 审中-公开
标题翻译：药物代谢产品的新配方，其制备方法及其使用方法
公开(公告)号：US20100035800A1
公开(公告)日：2010-02-11
申请号：US12474218
申请日：2009-05-28
申请人： Neil P. DESAI , Patrick SOON-SHIONG
发明人： Neil P. DESAI , Patrick SOON-SHIONG
IPC分类号： A61K38/13
CPC分类号： A61K9/1623 , A61K9/0019 , A61K9/0075 , A61K9/146 , A61K9/1658 , A61K9/19 , A61K9/5052 , A61K9/5169 , A61K31/195 , A61K31/337 , A61K31/43 , A61K38/00 , A61K2039/55555
摘要： In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.
摘要翻译：根据本发明，提供了用于体内递送基本上不溶于水的药理学活性剂（例如抗癌药物紫杉醇）的组合物和方法，其中药理活性剂以包被的蛋白质（其作为稳定剂）。特别地，生物相容性分散介质中的蛋白质和药理学活性剂在没有任何常规表面活性剂的情况下进行高剪切，并且在没有用于颗粒的任何聚合物芯材料的情况下进行。该方法产生直径小于约1微米的颗粒。使用特定的组成和制备条件（例如，向有机相中加入极性溶剂）以及仔细选择合适的有机相和相分数使得能够可重复地生产直径小于200nm的异常小的纳米颗粒，其中可以无菌过滤。根据本发明制备的颗粒系统可以转化成可再分散的干粉，其包含用蛋白质包被的水不溶性药物的纳米颗粒，以及结合有药理学分子的游离蛋白质。这导致独特的递送系统，其中药理活性剂的一部分容易生物利用（以与蛋白质结合的分子的形式），并且部分药剂存在于颗粒内，而其中没有任何聚合物基质。

13. 发明申请

US20090304805A1 COMBINATIONS AND MODES OF ADMINISTRATION OF THERAPEUTIC AGENTS AND COMBINATION THERAPY 有权
标题翻译：治疗药物和组合治疗的组合和模式
公开(公告)号：US20090304805A1
公开(公告)日：2009-12-10
申请号：US12436697
申请日：2009-05-06
申请人： Neil P. Desai , Patrick Soon-Shiong
发明人： Neil P. Desai , Patrick Soon-Shiong
IPC分类号： A61K9/14 , A61K39/395 , A61P35/00
CPC分类号： A61K47/6845 , A61K9/0019 , A61K9/5169 , A61K31/282 , A61K31/337 , A61K31/7072 , A61K33/24 , A61K39/395 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents (such as an anti-VEGF antibody), or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.
摘要翻译：本发明提供了治疗增殖性疾病（例如癌症）的组合治疗方法，其包括第一疗法，其包括向个体施用有效量的纳米颗粒组合物中的紫杉烷，以及第二疗法，其可包括例如放射，外科手术，化疗剂（如抗VEGF抗体）的施用，或其组合。还提供了基于节律剂给药方案向个体施用纳米颗粒组合物中的药物紫杉烷的方法。

14. 发明授权

US07586008B2 Propofol analogs, process for their preparation, and methods of use 有权
标题翻译：丙泊酚类似物，其制备方法和使用方法
公开(公告)号：US07586008B2
公开(公告)日：2009-09-08
申请号：US12170314
申请日：2008-07-09
申请人： Chunlin Tao , Cheng Zhi Yu , Neil P. Desai , Vuong Trieu
发明人： Chunlin Tao , Cheng Zhi Yu , Neil P. Desai , Vuong Trieu
IPC分类号： C07C49/00 , C07C325/00 , C07F9/02 , A61K31/12 , A61K31/125
CPC分类号： C07C205/45 , A61K31/05 , A61K31/095 , A61K31/12 , A61K31/15 , C07C39/367 , C07C39/373 , C07C45/46 , C07C49/83 , C07C49/84 , C07C69/78 , C07C225/22 , C07C235/84 , C07C251/48 , C07C255/56 , C07C309/87 , C07C311/29 , C07C317/24 , C07C325/02 , C07D317/54 , C07D317/56 , C07D317/58
摘要： The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.
摘要翻译：本发明提供异丙酚的对位取代的二烷基酚衍生物。本发明进一步提供包含此类类似物的药物组合物，制备此类类似物的方法，以及使用此类类似物诱发患者全身麻醉，镇静和/或催眠或睡眠效应的方法。

15. 发明申请

US20080255035A1 SPARC AND METHODS OF USE THEREOF 审中-公开
标题翻译： SPARC及其使用方法
公开(公告)号：US20080255035A1
公开(公告)日：2008-10-16
申请号：US12102383
申请日：2008-04-14
申请人： Vuong Trieu , Neil P. Desai
发明人： Vuong Trieu , Neil P. Desai
IPC分类号： A61K38/17 , A61P35/00
CPC分类号： A61K38/17 , A61K31/337 , A61K38/39 , A61K45/06 , A61K2300/00
摘要： The invention provides methods of treating a mammalian tumors comprising combination therapy with SPARC polypeptides, an angiogenesis inhibitor and paclitaxel. The invention provides also methods of treating a mammalian tumors comprising combination therapy with SPARC polypeptides and paclitaxel. Further, the invention produces kits and methods to predict therapy responses.
摘要翻译：本发明提供了治疗哺乳动物肿瘤的方法，其包括与SPARC多肽，血管发生抑制剂和紫杉醇的联合治疗。本发明还提供了治疗包含SPARC多肽和紫杉醇的组合疗法的哺乳动物肿瘤的方法。此外，本发明产生预测治疗反应的试剂盒和方法。

16. 发明申请

US20080182258A1 Q3 SPARC DELETION MUTANT AND USES THEREOF 审中-公开
标题翻译： Q3 SPARC删除错误及其使用
公开(公告)号：US20080182258A1
公开(公告)日：2008-07-31
申请号：US11964390
申请日：2007-12-26
申请人： Vuong Trieu , Neil P. Desai , Patrick Soon-Shiong
发明人： Vuong Trieu , Neil P. Desai , Patrick Soon-Shiong
IPC分类号： C12Q1/68 , C12Q1/00
CPC分类号： C07K16/18 , A61K38/191 , C07K14/47 , C07K14/4747 , C07K14/51 , C07K14/82 , G01N2800/52
摘要： The invention provides for SPARC polypeptides with a mutation corresponding to a deletion of the third glutamine in the mature form of the human SPARC protein, nucleic acids encoding such polypeptides, antibodies against such polypeptides, and methods of the use of such polypeptides, nucleic acids, and antibodies.
摘要翻译：本发明提供具有对应于成熟形式的人SPARC蛋白中的第三种谷氨酰胺的缺失的突变的SPARC多肽，编码这种多肽的核酸，针对这种多肽的抗体，以及使用这种多肽，核酸，和抗体。

17. 发明申请

US20080171687A1 Compositions And Methods For The Preparation And Administration Of Poorly Water Soluble Drugs 审中-公开
标题翻译：用于制备和施用不良水溶性药物的组合物和方法
公开(公告)号：US20080171687A1
公开(公告)日：2008-07-17
申请号：US11575031
申请日：2005-09-16
申请人： Neil P. Desai , Chunlin Tao , Andrew Yang , Bridget Beal-Grim , Tapas De , Patrick Soon-Shiong
发明人： Neil P. Desai , Chunlin Tao , Andrew Yang , Bridget Beal-Grim , Tapas De , Patrick Soon-Shiong
IPC分类号： A61K38/02 , A61K31/351 , A61K31/222 , A61K31/427
CPC分类号： A61K9/0019 , A61K31/00 , A61K47/26
摘要： Sterile, stable pharmaceutical formulations of poorly water-soluble drugs dissolved in dimethyl isosorbide, a water-miscible solvent, as well as methods for their preparation and administration.
摘要翻译：溶于二甲基异山梨醇，水溶性溶剂的水溶性差的药物的无菌，稳定的药物制剂，以及其制备和给药方法。

18. 发明申请

US20080166389A1 Compositions and methods for treatment of hyperplasia 审中-公开
标题翻译：用于治疗增生的组合物和方法
公开(公告)号：US20080166389A1
公开(公告)日：2008-07-10
申请号：US11890603
申请日：2007-08-06
申请人： Neil P. Desai , Patrick Soon-Shiong
发明人： Neil P. Desai , Patrick Soon-Shiong
IPC分类号： A61F2/04 , A61K47/42 , A61K9/10
CPC分类号： A61K47/42 , A61K9/0019 , A61K9/1658 , A61K9/5169 , A61K31/335 , A61K31/337 , A61K31/427 , A61K31/436 , A61K31/495 , A61K38/13 , A61K45/06 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61L2300/624 , B82Y5/00 , A61K2300/00 , C08L89/00
摘要： In accordance with the present invention, there are provided methods for treating hyperplasia in a subject in need thereof. In another aspect of the invention, there are provided methods for reducing neointimal hyperplasia associated with vascular interventional procedures. Formulations contemplated for use herein comprise proteins and at least one pharmaceutically active agent.
摘要翻译：根据本发明，提供了在有需要的受试者中治疗增生的方法。在本发明的另一方面，提供了减少与血管介入程序相关的新内膜增生的方法。预期用于本文的制剂包含蛋白质和至少一种药物活性剂。

19. 发明申请

US20080160095A1 Novel formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof 审中-公开
公开(公告)号：US20080160095A1
公开(公告)日：2008-07-03
申请号：US11890599
申请日：2007-08-06
申请人： Neil P. Desai , Patrick Soon-Shiong
发明人： Neil P. Desai , Patrick Soon-Shiong
IPC分类号： A61K9/14 , A61K31/337
CPC分类号： A61K9/5169 , A61K9/5192
摘要： In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.

20. 发明授权

US06306922B1 Photopolymerizable biodegradable hydrogels as tissue contacting materials and controlled-release carriers 失效
标题翻译：可光聚合的可生物降解的水凝胶作为组织接触材料和控制释放载体
公开(公告)号：US06306922B1
公开(公告)日：2001-10-23
申请号：US09492011
申请日：2000-01-26
申请人： Jeffrey A. Hubbell , Chandrashekhar P. Pathak , Amarpreet S. Sawhney , Neil P. Desai , Jennifer L. Hill
发明人： Jeffrey A. Hubbell , Chandrashekhar P. Pathak , Amarpreet S. Sawhney , Neil P. Desai , Jennifer L. Hill
IPC分类号： C08G6308
CPC分类号： A61K9/0024 , A61K9/1635 , A61K9/1647 , A61K38/47 , A61K38/49 , A61K47/32 , A61K2035/128 , A61L24/0031 , A61L24/0042 , A61L24/046 , A61L26/0019 , A61L27/34 , A61L27/36 , A61L27/38 , A61L27/3839 , A61L27/52 , A61L29/085 , A61L31/10 , A61L31/145 , A61L31/148 , A61L31/16 , A61L2300/424 , A61L2300/602 , C08F290/00 , C08F290/06 , C08F291/00 , C09D153/00 , C09J153/00 , C12N5/0012 , C12N5/0677 , C12N11/04 , C12N2533/30 , C12N2533/32 , C12N2533/40 , C12N2533/74 , C12Y302/01017 , C12Y304/21068 , Y10T428/29 , Y10T428/2913 , Y10T428/2967 , Y10T428/31786 , C08L71/02
摘要： Hydrogels of polymerized and crosslinked macromers comprising hydrophilic oligomers having biodegradable monomeric or oligomeric extensions, which biodegradable extensions are terminated on free ends with end cap monomers or oligomers capable of polymerization and cross linking are described. The hydrophilic core itself may be degradable, thus combining the core and extension functions. Macromers are polymerized using free radical initiators under the influence of long wavelength ultraviolet light, visible light excitation or thermal energy. Biodegradation occurs at the linkages within the extension oligomers and results in fragments which are non-toxic and easily removed from the body. Preferred applications for the hydrogels include prevention of adhesion formation after surgical procedures, controlled release of drugs and other bioactive species, temporary protection or separation of tissue surfaces, adhering of sealing tissues together, and preventing the attachment of cells to tissue surfaces.
摘要翻译：描述了聚合和交联的大分子单体的水凝胶，其包含具有可生物降解的单体或低聚延伸的亲水性低聚物，其生物可降解的延伸部分在端基单体或能够聚合和交联的低聚物的自由端上终止。亲水核心本身可以是可降解的，因此结合核心和延伸功能。大分子单体在长波长紫外光，可见光激发或热能的影响下，使用自由基引发剂聚合。生物降解发生在延伸低聚物内的连接处，并导致无毒且容易从体内去除的碎片。水凝胶的优选应用包括防止外科手术后的粘连形成，药物和其他生物活性物质的控制释放，临时保护或组织表面分离，将密封组织粘附在一起，以及防止细胞附着到组织表面。

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