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1. 发明公开

EP1227849A2 ACTINIUM-225 COMPLEXES AND CONJUGATES FOR RADIOIMMUNOTHERAPY 审中-公开
标题翻译：锕-225情结与偶联物RADIO免疫治疗
公开(公告)号：EP1227849A2
公开(公告)日：2002-08-07
申请号：EP01922246.2
申请日：2001-02-23
申请人： Ma, Dangshe , McDevitt, Michael R. , Scheinberg, David A. , Simon, Jaime , Kiefer, Garry E. , Franck, R. Keith , Gulyas, Gyongyi
发明人： Ma, Dangshe , McDevitt, Michael R. , Scheinberg, David A. , Simon, Jaime , Kiefer, Garry E. , Franck, R. Keith , Gulyas, Gyongyi
IPC分类号： A61K51/04 , A61K51/10
CPC分类号： A61K51/1093 , A61K51/0482 , A61K51/0497 , A61K51/1027
摘要： Actinium-225 (225Ac) complexes with functionalized chelants of the formula (I) wherein: each Q is independently hydrogen or (CHR5)pCO2R; Q1 is hydrogen or (CHR5)wCO2R; each R independently is hydrogen, benzyl or C1-C4 alkyl; with the proviso that at least two of the sum of Q and Q1 must be other than hydrogen; each R5 independently is hydrogen; C¿1?-C4 alkyl or (C1-C2 alkyl)phenyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon-carbon bond; n is 0 or 1; m is an integer from 0 to 10 inclusive; p is 1 or 2; r is 0 or 1; w is 0 or 1; with the proviso that n is only 1 when X and/or Y form an additional carbon to carbon bond, and the sum of r and w is 0 or 1; L is a linker/spacer group covalently bonded to, and replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula (1) wherein s is an integer of 0 or 1; t is an integer of 0 to 20 inclusive; R?1¿ is an electrophilic or nucleophilic moiety which allows for covalent attachment to an antibody or fragment thereof, or synthetic linker which can be attached to an antibody or fragment thereof, or precursor thereof; and Cyc represents a cyclic aliphatic moiety, aromatic moiety, aliphatic heterocyclic moiety, or aromatic heterocyclic moiety, each of said moieties optionally substituted with one or more groups which do not interfere with binding to an antibody or antibody fragment; with the proviso that when s, t, m, r, and n are 0, then R1 is other than carboxyl; their pharmaceutically acceptable salts, their conjugates and the use thereof for radioimmunotherapy is disclosed.

2. 发明申请

WO2007016377A2 DIALYSIS SOLUTION INCLUDING WATER-SOLUBLE POLYELECTROLYTE OSMOTIC AGENT 审中-公开
标题翻译：透析溶液包括水溶性聚电解质电解质
公开(公告)号：WO2007016377A2
公开(公告)日：2007-02-08
申请号：PCT/US2006/029494
申请日：2006-07-27
申请人： DOW GLOBAL TECHNOLOGIES INC. , STRICKLAND, Alan, D. , SIMON, Jaime
发明人： STRICKLAND, Alan, D. , SIMON, Jaime
CPC分类号： A61K47/12 , A61K33/00 , A61K33/14 , A61K45/06 , A61K47/32
摘要： Dialysis solutions comprising aqueous solutions including physiologically acceptable salts and a polyelectrolyte osmotic agent are disclosed. The subject solutions provide an improved osmotic gradient resulting in reduced dialysis times and/or reduced volumes of required dialysis solution. Moreover, the subject osmotic agents do not significantly migrate into the patient's blood over the time period of dialysis nor are the subject osmotic agents as susceptible to forming detrimental degradation products during gamma sterilization. The subject osmotic agents are much less susceptible to microbial contamination than currently available osmotic agents used in dialysis. The use of free radical scavengers is also described along with the use of a filter to reduce the introduction of bacteria into the peritoneal cavity.
摘要翻译：公开了包含包含生理上可接受的盐和聚电解质渗透剂的水溶液的透析溶液。本发明溶液提供改善的渗透梯度，导致透析时间减少和/或减少所需透析溶液的体积。此外，在渗透期间，本发明的渗透剂不会显着迁移到患者的血液中，而且在伽马灭菌期间，受试者渗透剂也易于形成有害的降解产物。本发明的渗透剂比目前在透析中使用的渗透剂更不易受微生物污染。还描述了使用自由基清除剂以及使用过滤器以减少将细菌引入腹膜腔中。

3. 发明申请

WO2005049096A3 PROTEIN AND POLYMER CONJUGATES AS CHELANTS WITH ENHANCED BLOOD RETENTION 审中-公开
标题翻译：蛋白质和聚合物作为具有增强血液保持力的药物
公开(公告)号：WO2005049096A3
公开(公告)日：2005-12-29
申请号：PCT/US2004037769
申请日：2004-11-12
申请人： DOW GLOBAL TECHNOLOGIES INC , ATHEY PHILLIP S , KIEFER GARRY E , SIMON JAIME , FRANK R KEITH , ADAIR CHRISTOPHER , GULYAS GYONGYI
发明人： ATHEY PHILLIP S , KIEFER GARRY E , SIMON JAIME , FRANK R KEITH , ADAIR CHRISTOPHER , GULYAS GYONGYI
IPC分类号： A61K49/08 , A61K49/14 , A61K51/04 , A61K51/06 , A61K51/08
CPC分类号： A61K51/065 , A61K49/085 , A61K49/126 , A61K49/14 , A61K51/0497 , A61K51/088
摘要： The present invention is a pharmaceutical composition that exhibits enhanced IP blood retention, the composition comprising: a biotargeting molecule; and a chelating agent conjugated to the biotargeting molecule; wherein the composition exhibits a half-life in the bloodstream of from 15 minutes to 24 hours. The present invention is also directed to the use of functionalized chelants to modify the pharmacokinetics of radiopharmaceuticals. Compared with non-functionalized chelants, chelants functionalized with bulky and/or lipophilic groups can slow down the renal clearance and enhance the blood retention of metals complexed therewith. This enhanced blood retention leads to increased uptake of metal in target tissue.
摘要翻译：本发明是一种具有增强的IP血液保留性的药物组合物，该组合物包含：生物靶向分子; 和与生物靶向分子缀合的螯合剂; 其中所述组合物在血液中的半衰期为15分钟至24小时。本发明还涉及功能化螯合剂用于改变放射性药物的药代动力学的用途。与非官能化螯合剂相比，用大体积和/或亲脂基团官能化的螯合剂可以减慢肾清除率并增强与其结合的金属的血液保持性。这种增强的血液保留导致靶组织中金属的摄取增加。

4. 发明申请

WO0191806A3 MEASUREMENT OF THE THERAPEUTIC DOSE FOR BONE MARROW ABLATION THERAPY 审中-公开
标题翻译：用于治疗骨质疏松症治疗剂量的测量
公开(公告)号：WO0191806A3
公开(公告)日：2002-10-31
申请号：PCT/US0117608
申请日：2001-05-31
申请人： MCCULLOUGH STEVEN , WENDT RICHARD E III , SIMON JAIME
发明人： MCCULLOUGH STEVEN , WENDT RICHARD E III , SIMON JAIME
IPC分类号： A61K51/04
CPC分类号： A61K51/0478 , A61K51/0489
摘要： A method of using a surrogate, preferably Tc-MDP, for a therapeutic agent (for example, Ho-EDTMP or preferably Ho-DOTMP) to calculate the dosimetry for the therapeutic dose for bone marrow ablation therapy is disclosed. The advantages of this use of a surrogate in lieu of the therapeutic agent is lower cost, less exposure to high radiation levels, and length of the half-life, while maintaining the biodistribution in the total skeleton.
摘要翻译：使用替代物（优选99m Tc-MDP）作为治疗剂（例如，Ho-EDTMP或优选Ho-DOTMP）的方法来计算用于骨髓消融的治疗剂量的剂量测定公开了治疗。这种使用治疗剂代替替代物的优点是在保持总骨骼中的生物分布的同时降低成本，较低的暴露于高辐射水平和半衰期的长度。

5. 发明申请

WO9502086A3 PROCESS FOR REMOVING METAL IONS FROM LIQUIDS 审中-公开
标题翻译：从液体中去除金属离子的方法
公开(公告)号：WO9502086A3
公开(公告)日：1995-03-09
申请号：PCT/US9407428
申请日：1994-06-30
申请人： DOW CHEMICAL CO , MICHALOWSKI ROBERT J , CHRISTIANSEN STEVEN H , FRANK R KEITH , LITTLETON TERESA , SIMON JAIME , VAUGHN WALTER , WILSON DAVID A
发明人： MICHALOWSKI ROBERT J , CHRISTIANSEN STEVEN H , FRANK R KEITH , LITTLETON TERESA , SIMON JAIME , VAUGHN WALTER , WILSON DAVID A
IPC分类号： D21C9/00 , D21C9/10 , D21H21/06
CPC分类号： D21H21/06 , D21C9/002 , D21C9/1042
摘要： The invention is an improvement in a process for making cellulosic articles said process involving a separation of cellulosic material from a mixture containing a liquid, metal cations, and cellulosic material. The improvement involves adding to the mixture at least one retaining material which binds at least one metal cation and, in the separation, is retained with the cellulosic material. Suitable retaining agents are either organic or inorganic and include chelate-forming polymers, both synthetic and natural, colloidal suspensions of inorganic compounds, and mixed metal hydroxides. In each case, the metal cations remain in the cellulosic article, for example paper, rather going into waste water from which they would otherwise need to be removed.

6. 发明申请

WO1993011802A1 BICYCLOAZAMACROCYCLOPHOSPHONIC ACID, CONJUGATES, CONTRAST AGENTS AND PREPARATION 审中-公开
标题翻译： BICYCLOAZAMACROCYCLOPHOSPHONIC ACID，CONJUGATES，对比剂和制剂
公开(公告)号：WO1993011802A1
公开(公告)日：1993-06-24
申请号：PCT/US1992010668
申请日：1992-12-10
申请人： THE DOW CHEMICAL COMPANY , KIEFER, Garry, E. , SIMON, Jaime , GARLICH, Joseph, R.
发明人： THE DOW CHEMICAL COMPANY
IPC分类号： A61K49/04
CPC分类号： C07F9/6561 , A61K49/06 , A61K51/0497 , C07F9/6524
摘要： Bicyclopolyazamacrocyclophosphonic acid compounds are disclosed which may form inert complexes with Gd, Mn or Fe ions. The overall charge of the complex can be varied to alter the in vivo biolocalization. Such complexes can be covalently attached to an antibody, antibody fragment or other biologically active molecule to form conjugates. The complexes and conjugates are useful as contrast agents for diagnostic purposes. Processes for the preparation of the ligand, complex and conjugate are also disclosed.
摘要翻译：公开了可与Gd，Mn或Fe离子形成惰性络合物的双环多氮杂泛膦酸化合物。可以改变复合物的总电荷以改变体内生物定位。这样的复合物可以共价连接到抗体，抗体片段或其他生物活性分子上以形成缀合物。复合物和缀合物可用作诊断目的的造影剂。还公开了制备配体，复合物和缀合物的方法。

7. 发明申请

WO2010093738A1 PREPARATION OF ANNEXIN DERIVATIVES 审中-公开
标题翻译：安瓿衍生物的制备
公开(公告)号：WO2010093738A1
公开(公告)日：2010-08-19
申请号：PCT/US2010/023813
申请日：2010-02-11
申请人： CLEAR VASCULAR, INC. , SIMON, Jaime
发明人： SIMON, Jaime
IPC分类号： A61K38/00
CPC分类号： A61K51/088 , A61K47/544 , A61K51/087
摘要： Labeled annexin is formed by reacting annexin or a modified annexin with a phosphatidylserine group or an analogue of phosphatidylserine. This phosphatidylserine annexin conjugate is then reacted with an appropriate label to form a labeled annexin and the annexin is separated from the phosphatidylserine group. The reaction between the phosphatidylserine group and the annexin is calcium ion concentration dependent. Therefore, the reaction can be promoted by having a high calcium ion concentration and the separation of the phosphatidyl group from the annexin group is facilitated by reducing the calcium ion concentration preferably by addition of an appropriate calcium chelating agent.
摘要翻译：标记的膜联蛋白通过膜联蛋白或修饰的膜联蛋白与磷脂酰丝氨酸基团或磷脂酰丝氨酸的类似物反应而形成。然后将该磷脂酰丝氨酸膜联蛋白缀合物与合适的标记反应以形成标记的膜联蛋白，并将膜联蛋白与磷脂酰丝氨酸基团分离。磷脂酰丝氨酸与膜联蛋白之间的反应是钙离子浓度依赖性。因此，通过优选通过加入适当的钙螯合剂来降低钙离子浓度，可以通过具有高钙离子浓度促进磷脂酰丝氨酸与膜联蛋白基团的分离来促进反应。

8. 发明申请

WO2008060393A3 THE USE OF MATERIALS AND EXTERNAL STIMULI FOR SYNOVECTOMY 审中-公开
标题翻译：用于SYNOVECTOMY的材料和外部刺激的使用
公开(公告)号：WO2008060393A3
公开(公告)日：2008-10-16
申请号：PCT/US2007022536
申请日：2007-10-24
申请人： ISO THERAPEUTICS GROUP LLC , FRANK R KEITH , MCMILLAN KENNETH , SIMON JAIME , STRICKLAND ALAN D
发明人： FRANK R KEITH , MCMILLAN KENNETH , SIMON JAIME , STRICKLAND ALAN D
IPC分类号： A61K9/14
CPC分类号： A61K51/1244 , A61K41/0052 , A61K47/6849
摘要： This invention has as one of its aspects a method to provide a safe an effective treatment for synovectomy. The method involves the administration a material to the affected joint, allowing the material to localize in the synovial membrane, and then applying an external stimulus that interacts with the material to provide therapy. The materials of this invention are preferably particles, which are either magnetic or contain a heavy element. The external stimuli of this invention includes an alternating magnetic field to heat magnetic particles, infrared laser to heat heavy elements, or electromagnetic ionizing radiation (X- or gamma-radiation) that interacts with heavy elements to produce a localized radiation dose.
摘要翻译：本发明的一个方面是为滑膜切除术提供安全有效的治疗方法。该方法涉及向受影响的关节施用材料，允许材料定位在滑膜中，然后施加与材料相互作用以提供治疗的外部刺激。本发明的材料优选是磁性的或含有重元素的颗粒。本发明的外部刺激包括加热磁性颗粒的交变磁场，加热重元素的红外激光或与重元素相互作用产生局部辐射剂量的电磁电离辐射（X或γ辐射）。

9. 发明申请

WO2006130920A1 SCATTERING ELONGATE PHOTOVOLTAIC CELL 审中-公开
标题翻译：散射最近光照细胞
公开(公告)号：WO2006130920A1
公开(公告)日：2006-12-14
申请号：PCT/AU2006/000795
申请日：2006-06-08
申请人： MONASH UNIVERSITY , SPICCIA, Leone , THOMPSON, Simon, Jaime , CHENG, Yi-Bing , MENZIES, David, Brian , SIMON, George, Philip
发明人： SPICCIA, Leone , THOMPSON, Simon, Jaime , CHENG, Yi-Bing , MENZIES, David, Brian , SIMON, George, Philip
IPC分类号： H01L31/0352 , H01G9/20 , H01L31/042
CPC分类号： H01G9/20 , H01G9/2068 , Y02E10/542
摘要： This invention relates to a photovoltaic cell (60) comprising a light incident surface and at least one elongated light transmitting fibre comprising a longitudinally extending core (62) having an end for receiving light from the light incident surface, said fibre extending away from the light incident surface to guide light received therefrom within the core and comprising a counter electrode (62a) surrounding the core and a dye-sensitive semiconductor (63) extending about the core and an electrolyte (64) and wherein light passing longitudinally through the core from the light incident surface is scattered laterally onto the dye nanoparticles (63) by bubbles, defects, particles etc.
摘要翻译：本发明涉及包括光入射表面的光伏电池（60）和至少一个细长的光传输光纤，其包括纵向延伸的芯（62），其具有用于接收来自光入射表面的光的端部，所述光纤远离光以引导在芯内从其接收的光并且包括围绕芯的对电极（62a）和围绕芯延伸的染料敏感半导体（63）和电解质（64），并且其中从所述芯的纵向穿过所述芯的光光入射表面通过气泡，缺陷，颗粒等横向散射到染料纳米颗粒（63）上。

10. 发明申请

WO2005049096A2 CHELANTS WITH ENHANCED BLOOD RETENTION 审中-公开
标题翻译：具有增强血液保留的化痰
公开(公告)号：WO2005049096A2
公开(公告)日：2005-06-02
申请号：PCT/US2004/037769
申请日：2004-11-12
申请人： DOW GLOBAL TECHNOLOGIES INC. , ATHEY, Phillip, S. , KIEFER, Garry, E. , SIMON, Jaime , FRANK, R. Keith , ADAIR, Christopher , GULYAS, Gyongyi
发明人： ATHEY, Phillip, S. , KIEFER, Garry, E. , SIMON, Jaime , FRANK, R. Keith , ADAIR, Christopher , GULYAS, Gyongyi
IPC分类号： A61K51/06
CPC分类号： A61K51/065 , A61K49/085 , A61K49/126 , A61K49/14 , A61K51/0497 , A61K51/088
摘要： The present invention is a pharmaceutical composition that exhibits enhanced IP blood retention, the composition comprising: a biotargeting molecule; and a chelating agent conjugated to the biotargeting molecule; wherein the composition exhibits a half-life in the bloodstream of from 15 minutes to 24 hours. The present invention is also directed to the use of functionalized chelants to modify the pharmacokinetics of radiopharmaceuticals. Compared with non-functionalized chelants, chelants functionalized with bulky and/or lipophilic groups can slow down the renal clearance and enhance the blood retention of metals complexed therewith. This enhanced blood retention leads to increased uptake of metal in target tissue.
摘要翻译：本发明是一种具有增强的IP血液保留性的药物组合物，该组合物包含：生物靶向分子; 和与生物靶向分子缀合的螯合剂; 其中所述组合物在血液中的半衰期为15分钟至24小时。本发明还涉及功能化螯合剂用于改变放射性药物的药代动力学的用途。与非官能化螯合剂相比，用大体积和/或亲脂基团官能化的螯合剂可以减慢肾清除率并增强与其结合的金属的血液保持性。这种增强的血液保留导致靶组织中金属的摄取增加。

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