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1. 发明申请

WO2011150022A2 POLYMER-CONJUGATED METAP2 INHIBITORS, AND THERAPEUTIC METHODS OF USE THEREOF 审中-公开
标题翻译：聚合物连接的METAP2抑制剂及其使用的治疗方法
公开(公告)号：WO2011150022A2
公开(公告)日：2011-12-01
申请号：PCT/US2011/037857
申请日：2011-05-25
申请人： SYNDEVRX, INC. , PETERSEN, John, S.
发明人： PETERSEN, John, S.
IPC分类号： C08F20/56 , C07D407/04 , C07D405/14 , C07K7/06 , A61K47/48 , A61P35/00
CPC分类号： A61K31/785 , A61K31/336 , A61K47/58 , C07D303/18 , C07D405/14 , C07D407/04 , C07D473/34 , C07K7/06 , C08F220/58
摘要： One aspect of the invention provides polymer conjugated MetAP2 inhibitors. While not being bound by any particular theory, it is believed that coupling the MetAP2 inhibitory core via the linkers described herein provides compounds with superior efficacy to the parent small molecules and superior pharmacokinetic profiles. In one aspect of the invention, the polymer conjugated MetAP2 inhibitors are useful in methods of treating disease, comprising administering to a subject in need thereof a therapeutically effective amount of a polymer conjugated MetAP2 inhibitor.
摘要翻译：本发明的一个方面提供了聚合物缀合的MetAP2抑制剂。虽然不受任何特定理论的约束，但是认为通过本文所述的接头偶联MetAP2抑制性核提供对母体小分子具有优异功效的化合物和优异的药代动力学特征。在本发明的一个方面，缀合有共轭的MetAP2抑制剂可用于治疗疾病的方法，包括向有需要的受试者施用治疗有效量的聚合物缀合的MetAP2抑制剂。

2. 发明申请

WO2008042404A2 ELECTROKINETIC SYSTEM AND METHOD FOR DELIVERING METHOTREXATE 审中-公开
标题翻译：用于输送甲基磺酸酯的电动系统和方法
公开(公告)号：WO2008042404A2
公开(公告)日：2008-04-10
申请号：PCT/US2007/021226
申请日：2007-10-03
申请人： TRANSPORT PHARMACEUTICALS, INC. , ETHEREDGE, Robert, W, III , GOLDBERG, Dennis, I. , FRIDEN, Phillip, M. , PETERSEN, John, S.
发明人： ETHEREDGE, Robert, W, III , GOLDBERG, Dennis, I. , FRIDEN, Phillip, M. , PETERSEN, John, S.
IPC分类号： A61N1/30
CPC分类号： A61B17/205 , A61M37/0015 , A61M2037/0061
摘要： The electrokinetic methotrexate delivery system includes at least one applicator having a multiplicity of non-conductive micro-needles carried on a non-conductive surface of the applicator. The opposite surface is formed of electrically conductive material for contact with an active electrode. The applicator includes a matrix containing a medicament, e.g., methotrexate, or a carrier therefor between the opposite surfaces. When the applicator is applied to the individual's skin with the micro-needles penetrating the skin, an electrical current is completed through the power source, the active electrode, methotrexate, or electrically conductive carrier therefor, the targeted treatment site, the individual's body, a ground electrode and the power supply, thereby electokinetically driving the medicament through the non-conductive micro-needles into the targeted treatment site.
摘要翻译：电动甲氨喋呤递送系统包括至少一个涂药器，其具有承载在涂药器的非导电表面上的多个不导电微针。相对表面由导电材料形成以用于与有源电极接触。涂药器包括含有药物的基质，例如甲氨蝶呤或其相对表面之间的载体。当使用微针穿透皮肤将施用器施用到个体的皮肤上时，通过电源，活性电极，甲氨蝶呤或其导电载体，靶向治疗部位，个体身体，a 接地电极和电源，从而通过不导电的微针将药物电动驱动到目标治疗部位。

3. 发明申请

WO2011150088A1 OPTIMIZED DRUG CONJUGATES 审中-公开
标题翻译：优化药物联合
公开(公告)号：WO2011150088A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/037946
申请日：2011-05-25
申请人： SYNDEVRX , PETERSEN, John, S.
发明人： PETERSEN, John, S.
IPC分类号： A61K47/00
CPC分类号： A61K47/48176 , A61K31/336 , A61K38/00 , A61K47/58 , A61K47/65
摘要： Optimized drug conjugates, wherein the active moiety is modified and attached to a cleavable linker, and wherein the conjugate exhibits enhanced bioavailability in part due to decreased efflux out of the target tissue are disclosed.
摘要翻译：优化的药物偶联物，其中活性部分被修饰并连接到可切割的接头，并且其中缀合物显示增强的生物利用度部分是由于目标组织外出的减少。

4. 发明申请

WO2009029824A1 RESOLUTION ENHANCEMENT TECHNIQUES COMBINING INTERFERENCE-ASSISTED LITHOGRAPHY WITH OTHER PHOTOLITHOGRAPHY TECHNIQUES 审中-公开
标题翻译：与其他光刻技术相结合的干扰辅助光刻技术的分辨率增强技术
公开(公告)号：WO2009029824A1
公开(公告)日：2009-03-05
申请号：PCT/US2008/074840
申请日：2008-08-29
申请人： APPLIED MATERIALS, INC. , HENDEL, Rudolf , RAO, Zhilong , LIU, Kuo-Shih , MACK, Chris, A. , PETERSEN, John, S. , PALMER, Shane
发明人： HENDEL, Rudolf , RAO, Zhilong , LIU, Kuo-Shih , MACK, Chris, A. , PETERSEN, John, S. , PALMER, Shane
IPC分类号： G06F15/18 , G06N1/00
CPC分类号： G03F7/7045 , G03F7/203 , G03F7/70408 , G03F7/70558 , G03F7/70991
摘要： Methods and systems are disclosed that provide multiple lithography exposures on a wafer, for example, using interference lithography and optical photolithography. Various embodiments may balance the dosage and exposure rates between the multiple lithography exposures to provide the needed exposure on the wafer. Other embodiments provide for assist features and/or may apply resolution enhancement to various exposures. In a specific embodiment, a wafer is first exposed using optical photolithography and then exposed using interference lithography.
摘要翻译：公开了在晶片上提供多次光刻曝光的方法和系统，例如使用干涉光刻和光学光刻。各种实施方案可平衡多次光刻曝光之间的剂量和曝光速率，以在晶片上提供所需的曝光。其他实施例提供辅助特征和/或可以对各种曝光应用分辨率增强。在具体实施例中，首先使用光学光刻曝光晶片，然后使用干涉光刻曝光。

5. 发明申请

WO2008042404A3 ELECTROKINETIC SYSTEM AND METHOD FOR DELIVERING METHOTREXATE 审中-公开
标题翻译：电动系统及其输送方法
公开(公告)号：WO2008042404A3
公开(公告)日：2008-08-07
申请号：PCT/US2007021226
申请日：2007-10-03
申请人： TRANSPORT PHARMACEUTICALS INC , ETHEREDGE ROBERT W III , GOLDBERG DENNIS I , FRIDEN PHILLIP M , PETERSEN JOHN S
发明人： ETHEREDGE ROBERT W III , GOLDBERG DENNIS I , FRIDEN PHILLIP M , PETERSEN JOHN S
IPC分类号： A61N1/30
CPC分类号： A61B17/205 , A61M37/0015 , A61M2037/0061
摘要： The electrokinetic methotrexate delivery system includes at least one applicator having a multiplicity of non-conductive micro-needles carried on a non-conductive surface of the applicator. The opposite surface is formed of electrically conductive material for contact with an active electrode. The applicator includes a matrix containing a medicament, e.g., methotrexate, or a carrier therefor between the opposite surfaces. When the applicator is applied to the individual's skin with the micro-needles penetrating the skin, an electrical current is completed through the power source, the active electrode, methotrexate, or electrically conductive carrier therefor, the targeted treatment site, the individual's body, a ground electrode and the power supply, thereby electokinetically driving the medicament through the non-conductive micro-needles into the targeted treatment site.
摘要翻译：电动氨甲蝶呤递送系统包括至少一个施用器，其具有承载在施用器的非导电表面上的多个非导电微针。相对表面由用于与有源电极接触的导电材料形成。施用器包括在相对表面之间包含药物，例如甲氨蝶呤或其载体的基质。当施用器被微针穿透皮肤施加到个体的皮肤上时，通过电源，有效电极，甲氨蝶呤或导电载体，目标治疗部位，个体的身体，接地电极和电源，从而通过非导电微针将药物电动驱动到目标治疗部位。

6. 发明申请

WO2007064723A1 COMBINATION CARTRIDGE AND DEVICE FOR ELECTROKINETIC DELIVERY OF MEDICAMENT TO A TREATMENT SITE 审中-公开
标题翻译：组合式药盒和用于向治疗场地进行药物输送的装置
公开(公告)号：WO2007064723A1
公开(公告)日：2007-06-07
申请号：PCT/US2006/045720
申请日：2006-11-30
申请人： TRANSPORT PHARMACEUTICALS, INC. , GLAXOSMITHKLINE UK LIMITED , PETERSEN, John, S. , GOLDBERG, Dennis, I. , KELLAND, James W. , RAND, Paul, K. , JONES, Anthony, Patrick Charles , ETHEREDGE, Robert, W.
发明人： PETERSEN, John, S. , GOLDBERG, Dennis, I. , KELLAND, James W. , RAND, Paul, K. , JONES, Anthony, Patrick Charles , ETHEREDGE, Robert, W.
IPC分类号： A61N1/30
CPC分类号： A61N1/303
摘要： A device for electrokinetic delivery of medicament to a treatment site includes a cartridge having an active electrode and a membrane overlying the active electrode and a medicament or a medicament and an electrically conductive carrier therefor, carried by the membrane in electrical contact with the electrode. The electrode opens through a surface of the cartridge remote from the membrane for connection with an electrical connector carried by the device. An locking element releasably couples the cartridge to the housing.
摘要翻译：用于将药物电动递送到治疗部位的装置包括具有活性电极和覆盖有源电极的膜的药筒以及与电极电接触的膜携带的药物或药物及其导电载体。电极通过远离膜的盒的表面打开，以与由装置承载的电连接器连接。锁定元件可释放地将盒连接到壳体。

7. 发明申请

WO9829107A3 POLY(DIALLYLAMINE)-BASED BILE ACID SEQUESTRANTS 审中-公开
标题翻译：聚（氨基甲酸） - 双酯酸序列
公开(公告)号：WO9829107A3
公开(公告)日：2001-03-01
申请号：PCT/US9723899
申请日：1997-12-29
申请人： GELTEX PHARMA INC , HOLMES FARLEY STEPHEN RANDALL , DHAL PRADEEP K , PETERSEN JOHN S
发明人： HOLMES-FARLEY STEPHEN RANDALL , DHAL PRADEEP K , PETERSEN JOHN S
IPC分类号： A61K31/785 , A61K31/787 , A61K31/795 , A61K47/48 , A61P3/06 , A61P9/10 , A61P43/00 , C08F26/04 , C08G61/12 , A61K31/14
CPC分类号： B82Y5/00 , A61K31/785 , A61K31/787 , A61K31/795 , A61K47/6949 , C08G61/12 , Y10S514/824
摘要： The present invention relates to a method for removing bile acids from a patient and certain polymers of use in the method. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer composition which includes a poly(diallylamine) polymer which is substituted with hydrophobic groups. The hydrophobic groups can be a substituted or unsubstituted, straight chain or branched C3-C24-alkyl group, an aralkyl group or an aryl group.
摘要翻译：本发明涉及一种从患者中除去胆汁酸的方法以及在该方法中使用的某些聚合物。该方法包括向患者施用治疗有效量的聚合物组合物的步骤，所述聚合物组合物包括被疏水基团取代的聚（二烯丙基胺）聚合物。疏水基团可以是取代或未取代的直链或支链C 3 -C 24 - 烷基，芳烷基或芳基。

8. 发明申请

WO1998029107A2 POLY(DIALLYLAMINE)-BASED BILE ACID SEQUESTRANTS 审中-公开
标题翻译：多（氨基甲酸） - 双酯酸序列
公开(公告)号：WO1998029107A2
公开(公告)日：1998-07-09
申请号：PCT/US1997023899
申请日：1997-12-29
申请人： GELTEX PHARMACEUTICALS, INC. , HOLMES-FARLEY, Stephen, Randall , DHAL, Pradeep, K. , PETERSEN, John, S.
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： A61K31/00
CPC分类号： B82Y5/00 , A61K31/785 , A61K31/787 , A61K31/795 , A61K47/6949 , C08G61/12 , Y10S514/824
摘要： The present invention relates to a method for removing bile acids from a patient and certain polymers of use in the method. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer composition which includes a poly(diallylamine) polymer which is substituted with hydrophobic groups. The hydrophobic groups can be a substituted or unsubstituted, straight chain or branched C3-C24-alkyl group, an aralkyl group or an aryl group.
摘要翻译：本发明涉及一种从患者中除去胆汁酸的方法和本方法中使用的某些聚合物。该方法包括向患者施用治疗有效量的包含被疏水基团取代的聚（二烯丙基胺）聚合物的聚合物组合物的步骤。疏水基团可以是取代或未取代的直链或支链C 3 -C 24 - 烷基，芳烷基或芳基。

9. 发明申请

WO1995008529A1 CHIRAL SURFACTANTS AND METHODS FOR THEIR USE IN CHIRAL SEPARATIONS 审中-公开
标题翻译： CHIRAL表面活性剂及其在CHIRAL分离中使用的方法
公开(公告)号：WO1995008529A1
公开(公告)日：1995-03-30
申请号：PCT/US1994010655
申请日：1994-09-20
申请人： WATERS CORPORATION , MAZZEO, Jeffrey, R. , GROVER, Edward, R. , SCHWARTZ, Michael, E. , MERION, Michael , PETERSEN, John, S.
发明人： WATERS CORPORATION
IPC分类号： C07C233/47
CPC分类号： C07C237/06 , B01F17/00 , C07B57/00 , C07C233/18 , C07C233/47 , C07C235/06 , C07C271/16 , C07C271/22 , C07C271/34 , C07C275/10 , C07C275/16 , C07C305/06 , C07C309/18 , C07C311/06 , C07C2601/14 , C07D207/16 , C07J41/0055
摘要： Chiral surfactants, methods for their synthesis and use, and apparatus designed to facilitate chiral separations using micellar capillary electrophoresis is disclosed. A chiral surfactant having general formula (I) is described. R1 is the hydrophobic tail, Y-A-X is the linker, the brackets define a chiral center, and the hydrophilic head group is Z. All the various components may potentiate the enantioselectivity of the chiral surfactant. The capillary electrophoresis (CE) system includes a narrow diameter capillary, a high voltage power supply, an electrolyte reservoir at each end of the capillary, a means for injecting a sample, and a detector. Chiral surfactants are dissolved in the electrolyte above their critical micelle concentration (cmc), resulting in the formation of chiral micelles. The elecrolyte reservoirs and capillary tube are filled with the electrolyte. A sample containing a mixture of enantiomers is then injected into the capillary, and a high voltage potential is applied across the capillary. The sample components migrate through the capillary due to the influence of the applied electric field. An example separation of the four stereoisomers of aspartame is shown.
摘要翻译：公开了手性表面活性剂，它们的合成和使用方法，以及设计用于促进使用胶束毛细管电泳的手性分离的装置。描述了具有通式（I）的手性表面活性剂。 R1是疏水尾，Y-A-X是接头，支架定义手性中心，亲水性头基为Z。所有各种成分均可加强手性表面活性剂的对映体选择性。毛细管电泳（CE）系统包括窄直径毛细管，高压电源，毛细管两端的电解质储存器，注射样品的装置和检测器。手性表面活性剂溶解在电解质中高于其临界胶束浓度（cmc），导致手性胶束的形成。电解液储存器和毛细管充满电解液。然后将含有对映异构体混合物的样品注入毛细管中，并在毛细管上施加高电压电位。由于施加的电场的影响，样品组分迁移通过毛细管。示出了阿斯巴甜的四种立体异构体的实例分离。

10. 发明申请

WO2011150022A3 POLYMER-CONJUGATED METAP2 INHIBITORS, AND THERAPEUTIC METHODS OF USE THEREOF 审中-公开
标题翻译：聚合物连接的METAP2抑制剂及其使用的治疗方法
公开(公告)号：WO2011150022A3
公开(公告)日：2012-04-12
申请号：PCT/US2011037857
申请日：2011-05-25
申请人： SYNDEVRX INC , PETERSEN JOHN S
发明人： PETERSEN JOHN S
IPC分类号： C08F20/56 , A61K47/48 , A61P35/00 , C07D405/14 , C07D407/04 , C07K7/06
CPC分类号： A61K31/785 , A61K31/336 , A61K47/58 , C07D303/18 , C07D405/14 , C07D407/04 , C07D473/34 , C07K7/06 , C08F220/58
摘要： One aspect of the invention provides polymer conjugated MetAP2 inhibitors. While not being bound by any particular theory, it is believed that coupling the MetAP2 inhibitory core via the linkers described herein provides compounds with superior efficacy to the parent small molecules and superior pharmacokinetic profiles. In one aspect of the invention, the polymer conjugated MetAP2 inhibitors are useful in methods of treating disease, comprising administering to a subject in need thereof a therapeutically effective amount of a polymer conjugated MetAP2 inhibitor.
摘要翻译：本发明的一个方面提供了聚合物缀合的MetAP2抑制剂。虽然不受任何特定理论的约束，但是认为通过本文所述的接头偶联MetAP2抑制性核心提供对母体小分子具有优异功效的化合物和优异的药代动力学特征。在本发明的一个方面，所述聚合物缀合的MetAP2抑制剂可用于治疗疾病的方法，包括向有需要的受试者施用治疗有效量的聚合物缀合的MetAP2抑制剂。

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