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1. 发明授权

US08425887B2 Amide dendrimer compositions 有权
公开(公告)号：US08425887B2
公开(公告)日：2013-04-23
申请号：US12311362
申请日：2007-09-26
申请人： Pradeep K. Dhal , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Vitaly Nivorozhkin , Bruce Shutts
发明人： Pradeep K. Dhal , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Vitaly Nivorozhkin , Bruce Shutts
IPC分类号： A61K8/72
CPC分类号： C08G69/40 , A61K8/72 , A61K31/785 , C07C235/08 , C07C237/10 , C08G83/003 , C08L101/00
摘要： Amide compounds, amide polymers, compositions including amide compounds and amide polymers may be used to bind target ions, such as phosphorous-containing compounds in the gastrointestinal tract of animals. In some cases, amide compounds and amide polymers may include a core derived from an amide polyol and an organic polyacid or ester.

2. 发明申请

US20100069500A1 AMIDE DENDRIMER COMPOSITIONS 有权
标题翻译： AMIDE DENDRIMER组合物
公开(公告)号：US20100069500A1
公开(公告)日：2010-03-18
申请号：US12311362
申请日：2007-09-26
申请人： Pradeep K. Dhal , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Vitaly Nivorozhkin , Bruce Shutts
发明人： Pradeep K. Dhal , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Vitaly Nivorozhkin , Bruce Shutts
IPC分类号： A61K31/16 , A61P13/12
CPC分类号： C08G69/40 , A61K8/72 , A61K31/785 , C07C235/08 , C07C237/10 , C08G83/003 , C08L101/00
摘要： Amide compounds, amide polymers, compositions including amide compounds and amide polymers may be used to bind target ions, such as phosphorous-containing compounds in the gastrointestinal tract of animals. In some cases, amide compounds and amide polymers may include a core derived from an amide polyol and an organic polyacid or ester.
摘要翻译：酰胺化合物，酰胺聚合物，包括酰胺化合物和酰胺聚合物的组合物可用于结合目标离子，例如动物胃肠道中的含磷化合物。在一些情况下，酰胺化合物和酰胺聚合物可以包括衍生自酰胺多元醇和有机多酸或酯的核。

3. 发明申请

US20100234309A1 Dendrimer Compositions 审中-公开
标题翻译：树枝状组合物
公开(公告)号：US20100234309A1
公开(公告)日：2010-09-16
申请号：US12310514
申请日：2007-08-31
申请人： Christopher Cooper , Pradeep K. Dhal , Rayomand H. Gimi , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Edward Lee
发明人： Christopher Cooper , Pradeep K. Dhal , Rayomand H. Gimi , David J. Harris , Stephen Randall Holmes-Farley , Chad C. Huval , Edward Lee
IPC分类号： A61K31/7004 , A61P7/00 , A61P39/00 , A61K31/13
CPC分类号： C07C217/08 , A61K31/785
摘要： Amine compounds, amine polymers, crosslinked amine polymers and pharmaceutical compositions comprising the same may include polyhydroxy-containing cores that may be substituted with amine groups and may be used to treat hyperphosphatemia or to remove ions from the gastrointestinal tract of animals, including humans.
摘要翻译：胺化合物，胺聚合物，交联胺聚合物和包含它们的药物组合物可以包括可以被胺基取代的含多羟基的核心，并且可以用于治疗高磷酸盐血症或从动物（包括人）的胃肠道中除去离子。

4. 发明申请

US20090155368A1 Pharmaceutical compositions 审中-公开
标题翻译：药物组合物
公开(公告)号：US20090155368A1
公开(公告)日：2009-06-18
申请号：US12314554
申请日：2008-12-12
申请人： Stephen Randall Holmes-Farley , David J. Harris , Steven C. Polomoscanik , Adnan Salameh , Bruce Shutts , Richard Silva , Pradeep K. Dhal , Lynne Sole
发明人： Stephen Randall Holmes-Farley , David J. Harris , Steven C. Polomoscanik , Adnan Salameh , Bruce Shutts , Richard Silva , Pradeep K. Dhal , Lynne Sole
IPC分类号： A61K9/14 , A61K31/785 , A61P1/00
CPC分类号： A61K31/785 , A61K9/146 , A61K9/16 , A61K9/1688 , A61K9/20 , A61K9/2031 , A61K9/2077 , A61K9/2095 , A61K9/282 , A61K9/284 , A61K9/2853 , B01J41/14 , Y10T428/2982
摘要： The present invention relates to crosslinked polyamine particles and/or pharmaceutical compositions comprising, at least in part, crosslinked polyamine particles and aggregates of such particles (including cured aggregates of crosslinked polyamine particles). The compositions may be in the form of tablets comprising, for example, particles larger than 500 μm, and used for treating patients, for example, patients with hyperphosphatemia.
摘要翻译：本发明涉及交联的多胺颗粒和/或药物组合物，其至少部分地包含交联的多胺颗粒和这种颗粒的聚集体（包括交联的聚胺颗粒的固化聚集体）。组合物可以是包含例如大于500μm的颗粒的片剂的形式，并且用于治疗患者，例如高磷酸盐血症的患者。

5. 发明申请

US20110142952A1 Pharmaceutical Compositions 审中-公开
标题翻译：药物组合物
公开(公告)号：US20110142952A1
公开(公告)日：2011-06-16
申请号：US13000114
申请日：2009-06-17
申请人： David J. Harris , Stephen Randall Holmes-Farley , Steven C. Polomoscanlk , Adnan Salameh , Bruce Shutts , Richard Silva
发明人： David J. Harris , Stephen Randall Holmes-Farley , Steven C. Polomoscanlk , Adnan Salameh , Bruce Shutts , Richard Silva
IPC分类号： A61K9/16 , A61K31/785 , A61K31/132 , C08G73/02 , C07C217/42 , B32B5/16
CPC分类号： A61K9/1641 , Y10T428/2982
摘要： This invention relates to crosslinked amine-containing polymers for binding compounds or ions, and more specifically relates to pharmaceutically acceptable compositions for binding compounds or ions that include crosslinked amine-containing polymers. The pharmaceutically acceptable composition includes, for example, crosslinked polyamine particles, or pharmaceutically acceptable salts thereof, having a particle size distribution wherein greater than 10 vol. % of the particles have a particle size greater than 500 μm.
摘要翻译：本发明涉及用于结合化合物或离子的交联的含胺聚合物，更具体地涉及用于结合包含交联的含胺聚合物的化合物或离子的药学上可接受的组合物。药学上可接受的组合物包括例如交联的多胺颗粒或其药学上可接受的盐，其具有大于10体积％颗粒的％具有大于500μm的粒度。

6. 发明申请

US20120322786A1 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 有权
标题翻译： 2-乙酰氨基酚类型葡萄糖苷合成酶抑制剂
公开(公告)号：US20120322786A1
公开(公告)日：2012-12-20
申请号：US13595251
申请日：2012-08-27
申请人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
发明人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
IPC分类号： A61K31/4025 , A61K31/4439 , A61K31/397 , A61K31/428 , A61K31/5377 , A61K31/40 , A61K31/422
CPC分类号： A61K31/4025 , C07C271/12 , C07D207/12 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/16 , C07D407/06 , C07D407/12 , C07D409/04 , C07D413/04 , C07D417/12
摘要： A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：用于治疗多囊肾病的化合物由结构式（I）表示：或其药学上可接受的盐。药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。分别在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。

7. 发明授权

US5948767A Cationic amphiphile/DNA complexes 失效
标题翻译：阳离子两亲物/ DNA复合物
公开(公告)号：US5948767A
公开(公告)日：1999-09-07
申请号：US679514
申请日：1996-07-12
申请人： Ronald K. Scheule , Rebecca G. Bagley , Simon J. Eastman , Seng H. Cheng , John Marshall , Nelson S. Yew , David J. Harris , Edward R. Lee , Craig S. Siegel , Chau-Dung Chang , S. Catherine Hubbard
发明人： Ronald K. Scheule , Rebecca G. Bagley , Simon J. Eastman , Seng H. Cheng , John Marshall , Nelson S. Yew , David J. Harris , Edward R. Lee , Craig S. Siegel , Chau-Dung Chang , S. Catherine Hubbard
IPC分类号： A61K47/18 , A61K9/127 , A61K31/7105 , A61K31/711 , A61K38/00 , A61K38/22 , A61K47/28 , A61K47/48 , A61K48/00 , A61P7/00 , A61P9/00 , A61P11/00 , A61P21/00 , A61P25/00 , A61P35/00 , C07J41/00 , C07J43/00 , C12N15/88
CPC分类号： A61K9/1272 , A61K47/48023 , A61K47/48038 , A61K47/48046 , A61K47/48123 , A61K48/00 , C07J41/0005 , C07J41/0055 , C07J41/0061 , C07J43/003 , C12N15/88
摘要： Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.Novel and highly effective plasmid constructs are also disclosed, including those that are particularly effective at providing gene therapy for clinical conditions complicated by inflammation. Additionally, targeting of organs for gene therapy by intravenous administration of therapeutic compositions is described.
摘要翻译：提供了新的阳离子两亲物，其促进生物活性（治疗性）分子进入细胞。两亲物含有衍生自类固醇的单亲或二烷基胺或烷基或酰基的亲脂基团; 和在生理pH下可质子化的阳离子基团，衍生自胺，烷基胺或多烷基胺。还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。根据本发明的实践可以递送到细胞中的治疗分子包括DNA，RNA和多肽。本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。关于基因治疗的治疗组合物，通常以与阳离子两亲物络合的质粒的形式提供DNA。还公开了新型和高效的质粒构建体，包括在为炎症复杂的临床病症提供基因治疗方面特别有效的质粒构建体。另外，描述了通过静脉内施用治疗组合物靶向用于基因治疗的器官。

8. 发明授权

US5783565A Cationic amphiphiles containing spermine or spermidine cationic group for intracellular delivery of therapeutic molecules 失效
标题翻译：含有精胺或亚精胺阳离子基团的阳离子两亲物用于细胞内递送治疗分子
公开(公告)号：US5783565A
公开(公告)日：1998-07-21
申请号：US595375
申请日：1996-02-01
申请人： Edward R. Lee , David J. Harris , Craig S. Siegel , Seng H. Cheng , Simon J. Eastman , John Marshall , Ronald K. Scheule
发明人： Edward R. Lee , David J. Harris , Craig S. Siegel , Seng H. Cheng , Simon J. Eastman , John Marshall , Ronald K. Scheule
IPC分类号： A61K9/127 , A61K47/48 , A61K48/00 , C07J41/00 , C07J43/00 , C12N15/88 , B01F17/16 , C12N15/00
CPC分类号： B82Y5/00 , A61K47/48023 , A61K47/48038 , A61K47/48046 , A61K47/48123 , A61K48/00 , A61K9/1272 , C07J41/0005 , C07J41/0055 , C07J41/0061 , C07J43/003 , C12N15/88 , Y10S516/07
摘要： Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile. Novel and highly effective plasmid constructs are also disclosed, including those that are particularly effective at providing gene therapy for clinical conditions complicated by inflammation. Additionally, targeting of organs for gene therapy by intravenous administration of therapeutic compositions is described.
摘要翻译：提供了新的阳离子两亲物，其促进生物活性（治疗性）分子进入细胞。两亲物含有衍生自类固醇的单亲或二烷基胺或烷基或酰基的亲脂基团; 和在生理pH下可质子化的阳离子基团，衍生自胺，烷基胺或多烷基胺。还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。根据本发明的实践可以递送到细胞中的治疗分子包括DNA，RNA和多肽。本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。关于基因治疗的治疗组合物，通常以与阳离子两亲物络合的质粒的形式提供DNA。还公开了新型和高效的质粒构建体，包括在为炎症复杂的临床病症提供基因治疗方面特别有效的质粒构建体。另外，描述了通过静脉内施用治疗组合物靶向用于基因治疗的器官。

9. 发明授权

US4646114A Integrated circuit Zener diode 失效
标题翻译：集成电路齐纳二极管
公开(公告)号：US4646114A
公开(公告)日：1987-02-24
申请号：US687894
申请日：1984-12-31
申请人： Charles L. Vinn , David J. Harris
发明人： Charles L. Vinn , David J. Harris
IPC分类号： H01L29/861 , H01L29/866 , H01L29/90
CPC分类号： H01L29/866
摘要： A subsurface Zener diode is provided wherein a semiconductor has formed thereon spaced apart anode and cathode regions of opposite type conductivity, such regions having opposing surface portions, and disposed beneath a surface of such semiconductor a buried region of conductivity type the same as one of such regions, such buried region extending laterally through the spaced apart regions, one of the spaced apart regions having an opposing surface portion thereof formed with a portion which protrudes towards the opposing surface portion of the other one of the spaced apart regions. With such arrangement, an electric field produced between the spaced apart regions becomes concentrated at the protrusion with the result that Zener breakdown occurs repeatedly at the same point in the semiconductor thereby reducing long term drift. Also, a Kelvin buried Zener diode is provided by forming a second laterally spaced anode region with the cathode region disposed between the pair of anode regions. One of the pair of anodes provides the force anode and the other the sense anode. The buried region extends laterally through the pair of anodes and the cathode region. The cathode region is provided with the portion which protrudes towards the force anode of the pair of anode regions and such cathode is elongated along an axis which passes between the pair of force and sense anode regions. The elongated cathode thus improves isolation between the force and sense anodes.
摘要翻译：提供了一个次表面的齐纳二极管，其中半导体已经在其上形成了具有相反导电性的间隔开的阳极和阴极区域，这些区域具有相对的表面部分，并且在这种半导体的表面下方设置与其中之一相同的导电类型的掩埋区域区域，这样的掩埋区域横向延伸穿过间隔开的区域，其中一个间隔开的区域具有相对的表面部分，其形成有朝向另一个间隔开的区域的相对表面部分突出的部分。通过这样的布置，在间隔开的区域之间产生的电场在突起处变得集中，结果是在半导体的同一点处重新产生齐纳击穿从而减少长期漂移。此外，通过形成第二横向间隔开的阳极区域，其中阴极区域设置在一对阳极区域之间，提供开尔文掩埋齐纳二极管。一对阳极中的一个提供了力阳极和另一个阳极。埋入区域横向延伸穿过一对阳极和阴极区域。阴极区域设置有朝向一对阳极区域的力阳极突出的部分，并且该阴极沿着在一对力和感测阳极区域之间通过的轴线延伸。因此，细长的阴极改善了力和感应阳极之间的隔离。

10. 发明授权

US4492954A Digital-to-analog converter 失效
标题翻译：数模转换器
公开(公告)号：US4492954A
公开(公告)日：1985-01-08
申请号：US608928
申请日：1984-05-11
申请人： David J. Harris , Charles L. Vinn
发明人： David J. Harris , Charles L. Vinn
IPC分类号： H03M1/00 , H03K13/05
CPC分类号： H03M1/747
摘要： A digital-to-analog conversion circuitry is provided wherein a switching network is adapted to couple, or decouple, a selected one, or ones, of a plurality of identical current sources to, or from, an output bus selectively in accordance with the digital word being converted to produce an output current through an output bus having a level related to such digital word. The switching network includes: a logic network for selectively combining the plurality of bits of the digital word to produce a plurality of control signals, at least one thereof being related to a plurality of the bits of the digital word; and, a plurality of switching transistors, each one thereof having: a control (or base) electrode coupled to a corresponding one of the plurality of control signals; a first (or emitter) electrode coupled to a corresponding one of the plurality of identical current sources; and a second (or collector) electrode coupled to the output bus, such current source being coupled to, or decoupled from, such output bus selectively in accordance with the control signal fed to the control electrode of the transistor coupled to such current source, the logic network produces the plurality of control signals with substantially equal switching level variations.
摘要翻译：提供了一种数模转换电路，其中交换网络适于将多个相同电流源中的一个或多个选择的一个或多个耦合或去耦合到输出总线或从输出总线选择性地根据数字字被转换以通过具有与这种数字字相关的电平的输出总线产生输出电流。交换网络包括：逻辑网络，用于选择性地组合数字字的多个位以产生多个控制信号，其至少一个与数字字的多个位相关; 以及多个开关晶体管，其中的每一个具有：耦合到所述多个控制信号中的相应一个控制信号的控制（或基极）电极; 耦合到所述多个相同电流源中的相应一个的第一（或发射极）电极; 以及耦合到输出总线的第二（或集电极）电极，这样的电流源根据馈送到耦合到这种电流源的晶体管的控制电极的控制信号选择性地耦合到这种输出总线或从该输出总线去耦，逻辑网络产生具有基本相等的开关电平变化的多个控制信号。

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