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51. 发明申请

US20120101055A1 METHODS AND UNIT DOSE FORMULATIONS FOR THE INHALATION ADMINISTRATION OF AMINOGLYCOSIDE ANTIBIOTICS 有权
标题翻译：氨基丁糖抗生素吸入管理的方法和单位剂量配方
公开(公告)号：US20120101055A1
公开(公告)日：2012-04-26
申请号：US13295228
申请日：2011-11-14
申请人： Robert John Speirs , Barbara Ann Schaeffler , Peter Bruce Challoner
发明人： Robert John Speirs , Barbara Ann Schaeffler , Peter Bruce Challoner
IPC分类号： A61K31/7036 , A61P31/00
CPC分类号： A61K51/0497 , A61K9/0078 , A61K31/7036 , A61K51/0491 , Y10S514/851 , Y10S514/958
摘要： A patient suffering from an endobronchial infection is treated by administering to the patient for inhalation a dose of less than about 4.0 ml of a nebulized aerosol formulation comprising from about 60 to about 200 mg/ml of an aminoglycoside antibiotic, such as tobramycin, in a physiologically acceptable carrier in a time period of less than about 10 minutes. Unit dose devices for storage and delivery of the aminoglycoside antibiotic formulations are also provided.
摘要翻译：患有支气管炎感染的患者通过向患者施用小于约4.0ml的剂量的雾化气雾剂制剂来治疗，其包含约60至约200mg / ml的氨基糖苷类抗生素例如妥布霉素，生理上可接受的载体在小于约10分钟的时间段内。还提供了用于储存和递送氨基糖苷类抗生素制剂的单位剂量装置。

52. 发明申请

US20120087857A1 GADOLINIUM EXPRESSED LIPID NANOPARTICLES FOR MAGNETIC RESONANCE IMAGING 审中-公开
标题翻译：用于磁共振成像的GADOLINIUM表达的脂质纳米颗粒
公开(公告)号：US20120087857A1
公开(公告)日：2012-04-12
申请号：US13208100
申请日：2011-08-11
申请人： Rodney J.Y. Ho , John D. Hoekman , Ken Maravilla
发明人： Rodney J.Y. Ho , John D. Hoekman , Ken Maravilla
IPC分类号： A61K51/04 , A61K47/12 , A61K47/42 , A61P35/00 , A61K47/36 , A61K47/26 , A61K49/10 , C12N13/00 , A61K47/28 , A61K47/14
CPC分类号： A61K49/1824 , A61K49/085 , A61K49/1806 , A61K49/1812 , A61K49/1881 , A61K51/0408 , A61K51/0497 , A61K51/1227 , B82Y5/00
摘要： Lipid nanoparticles expressing metal ions and methods for using the compositions for magnetic resonance imaging.
摘要翻译：表达金属离子的脂质纳米颗粒和使用该组合物进行磁共振成像的方法。

53. 发明授权

US08071134B2 Thyroid hormone analogs and methods of use 有权
标题翻译：甲状腺激素类似物和使用方法
公开(公告)号：US08071134B2
公开(公告)日：2011-12-06
申请号：US11663047
申请日：2005-09-15
申请人： Shaker A. Mousa , Faith B. Davis , Paul J. Davis
发明人： Shaker A. Mousa , Faith B. Davis , Paul J. Davis
IPC分类号： A61K9/14 , A61K9/50 , A61K3/21
CPC分类号： A61K31/192 , A61K31/195 , A61K31/4365 , A61K31/60 , A61K31/7076 , A61K31/727 , A61K38/1825 , A61K38/1866 , A61K47/58 , A61K47/593 , A61K47/60 , A61K47/61 , A61K47/64 , A61K49/0008 , A61K49/085 , A61K49/10 , A61K49/12 , A61K51/0402 , A61K51/0497 , A61K51/065 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/43 , A61L2300/606 , A61K2300/00
摘要： Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.
摘要翻译：公开了治疗具有与血管发生相关的病症的受试者的方法，包括施用有效量的甲状腺激素或其拮抗剂的聚合形式，以促进或抑制受试者的血管生成。还公开了甲状腺激素或甲状腺激素类似物的聚合形式的组合物。

54. 发明申请

US20110206604A1 NITROIMIDAZOLE-AMINO ACID HYPOXIA CONTRAST MEDIUM, PREPARATION METHOD AND USE THEREOF 审中-公开
标题翻译：硝基咪唑 - 氨基酸对羟基苯甲酸对照培养基，其制备方法及其用途
公开(公告)号：US20110206604A1
公开(公告)日：2011-08-25
申请号：US13097109
申请日：2011-04-29
申请人： Jianping Ruan
发明人： Jianping Ruan
IPC分类号： A61K49/00 , C07F13/00 , C07D233/95 , A61P43/00
CPC分类号： A61K51/0497 , A61K51/0453 , C07D233/92 , C07D233/95 , C07F13/005
摘要： A hypoxia contrast medium including nitroimidazole-amino acid chelate with a positively charged radioactive nuclide, a preparation method and use thereof. The contrast medium can be used in imaging cerebral thrombosis, tumors or other diseases such as ulceration, thrombosis, and so on.
摘要翻译：含有硝基咪唑 - 氨基酸螯合物与带正电荷的放射性核素的缺氧造影剂，其制备方法和用途。造影剂可用于成像脑血栓形成，肿瘤或其他疾病如溃疡，血栓形成等。

55. 发明申请

US20110189086A1 Diagnostic Method for Atherosclerosis 有权
标题翻译：动脉粥样硬化的诊断方法
公开(公告)号：US20110189086A1
公开(公告)日：2011-08-04
申请号：US13083121
申请日：2011-04-08
申请人： Philip Stewart Low
发明人： Philip Stewart Low
IPC分类号： A61K49/00 , A61K51/04 , A61K51/10
CPC分类号： A61K49/0043 , A61K49/0041 , A61K49/0052 , A61K49/006 , A61K51/0474 , A61K51/0497 , G01N33/5061 , G01N33/92 , G01N2800/323
摘要： The invention relates to a method of identifying/monitoring active atherosclerotic plaques associated with blood vessel walls wherein the plaques comprise activated macrophages having accessible binding sites for a ligand. The method comprises the steps of administering to a patient being evaluated for atherosclerosis an effective amount of a composition comprising a conjugate of a ligand and a chromophore capable of emitting light under predetermined conditions, allowing sufficient time for the ligand conjugate to bind to the activated macrophages, subjecting the blood vessels to the predetermined conditions using a catheter-based device, and identifying active plaques by detecting light emitted by the chromophore using a catheter-based device or by using an external imaging technique. The invention also relates to a similar method wherein a chemical moiety capable of emitting radiation is conjugated to the ligand.
摘要翻译：本发明涉及鉴定/监测与血管壁相关的活动性动脉粥样硬化斑块的方法，其中斑块包含具有可配位结合位点的活化巨噬细胞。该方法包括以下步骤：向被评估动脉粥样硬化的患者施用有效量的包含配体和能够在预定条件下发光的发色团的缀合物的组合物，允许配体缀合物足够的时间结合活化的巨噬细胞使用基于导管的装置对血管进行预定条件，并且使用基于导管的装置或通过使用外部成像技术检测由发色团发出的光来识别活性斑块。本发明还涉及一种类似的方法，其中能够发射辐射的化学部分与配体缀合。

56. 发明申请

US20110060138A1 Compounds and Compositions for the Detection and Treatment of Alzheimer's Disease and Related Disorders 有权
标题翻译：用于检测和治疗阿尔茨海默病和相关疾病的化合物和组合物
公开(公告)号：US20110060138A1
公开(公告)日：2011-03-10
申请号：US12933139
申请日：2009-03-23
申请人： David R. Elmaleh , Timothy M. Shoup , Hongning Fu
发明人： David R. Elmaleh , Timothy M. Shoup , Hongning Fu
IPC分类号： C07H17/02 , C07D471/10 , C07C35/16 , C07C43/196 , C07H13/02
CPC分类号： A61K51/0497 , C07C43/192 , C07C43/196 , C07C43/253 , C07D471/10 , C07H13/02 , C07H13/10 , C07H15/26
摘要： One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.
摘要翻译：本发明的一个方面涉及用于诊断和/或治疗患有淀粉样变性相关病理状况的受试者的化合物，组合物和方法。在某些实施方案中，本发明的成像和/或治疗剂可以施用于受试者以鉴定和/或治疗淀粉样沉积物。具体的成像方法通过对受试者施用成像剂并检测试剂的空间分布来检测淀粉样蛋白沉积物。药剂的差异积累是AD或淀粉样变性相关病理状态的指示，并且可以通过使用PET或SPECT照相机进行监测。

57. 发明授权

US07893266B2 Detection of cancer cells in vitro using sigma-2 receptor ligands as radiotracers 有权
标题翻译：使用σ-2受体配体作为放射性示踪剂检测体外癌细胞
公开(公告)号：US07893266B2
公开(公告)日：2011-02-22
申请号：US12550220
申请日：2009-08-28
申请人： Robert H. Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
发明人： Robert H. Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
IPC分类号： C07D491/00
CPC分类号： C07D295/13 , A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02
摘要： Methods for detection of cancer cells and for determining the proliferative status of cells in a tissue sample in vitro are disclosed. These methods comprise contacting a tissue sample with a radiolabeled compound or salt thereof of Formula wherein at least one of X, Y, and Z comprises a radioisotope, n is an integer from 2 to about 10; and each of A and A1 is a C1-C4 alkoxyl, a C1-C4 fluoroalkyl or a C1-C4 fluoroalkoxyl. The methods further comprise detecting the distribution of the radioisotope in the tissue sample, whereby a cell having a high density of the radioisotope compared to quiescent cells is diagnostic for a cancer cell.
摘要翻译：公开了用于检测癌细胞并用于测定体外组织样品中细胞增殖状态的方法。这些方法包括使组织样品与其中X，Y和Z中的至少一个包含放射性同位素的放射性标记的化合物或其盐接触，n为2至约10的整数; A和A1各自为C1-C4烷氧基，C1-C4氟烷基或C1-C4氟烷氧基。所述方法还包括检测组织样品中放射性同位素的分布，由此与静止细胞相比具有高密度放射性同位素的细胞是癌细胞的诊断。

58. 发明授权

US07875612B2 Folate mimetics and folate-receptor binding conjugates thereof 有权
标题翻译：叶酸模拟物和叶酸受体结合结合物
公开(公告)号：US07875612B2
公开(公告)日：2011-01-25
申请号：US10475876
申请日：2002-04-24
申请人： Mark A. Green , Chun-Yen Ke , Christopher P. Leamon
发明人： Mark A. Green , Chun-Yen Ke , Christopher P. Leamon
IPC分类号： A01N43/64 , A01N43/58 , A01N43/60 , A01N43/90 , A61K31/53 , A61K31/50 , A61K31/495 , A61K31/519 , C07D253/08 , C07D487/00 , C07D475/00
CPC分类号： C07D475/04 , A61K31/519 , A61K51/0497
摘要： A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.
摘要翻译：表达叶酸受体的细胞群体选择性地用非肽叶酸类似物靶向。非肽叶酸类似物与诊断或治疗剂缀合以使得药剂能够选择性递送至靶细胞群体。

59. 发明申请

US20110008253A1 PROCESS FOR PRODUCTION OF HETERODIMERS OF GLUTAMIC ACID 有权
标题翻译：制备葡萄糖酸酐的方法
公开(公告)号：US20110008253A1
公开(公告)日：2011-01-13
申请号：US12815637
申请日：2010-06-15
申请人： John W. Babich , Craig Zimmerman , Kevin P. Maresca
发明人： John W. Babich , Craig Zimmerman , Kevin P. Maresca
IPC分类号： A61K51/04 , C07C273/18 , C07F7/22 , A61P43/00
CPC分类号： A61K51/0497 , C07B59/001 , C07B2200/05 , C07C273/1854 , C07C303/40 , C07F7/2208 , C07C311/19 , C07C275/16 , C07C275/24 , C07C275/30
摘要： A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; R′ is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.
摘要翻译：用于制备放射性标记的式（I）化合物的制备方法包括在酸性条件下，在氧化剂存在下使式（II）化合物与卤素的准氮化物源反应，其中：* I为123 I，124 I，125 I 或131I; R是低级烷基，任选被一个或多个氟原子取代; Q是C（O），O，NR'，S，S（O）2，C（O）2，（CH 2）p; Y是C（O），O，NR'，S，S（O）2，C（O）2，（CH 2）p; R'是H，C（O），S（O）2，C（O）2; Z是H，C 1 -C 4烷基，苄基，取代的苄基或三烷基甲硅烷基; m为0,1,2,3,4或5; n为0，1，2，3，4，5或6; p为0,1,2,3,4,5或6。

60. 发明申请

US20110008252A9 STABALISED 99MTC COMPOSITIONS 有权
标题翻译： STABALISED 99MTC组合物
公开(公告)号：US20110008252A9
公开(公告)日：2011-01-13
申请号：US11721064
申请日：2005-10-14
申请人： Ole Kristian Hjelstuen , Grethe Karin Martinussen , Gry Stensrud
发明人： Ole Kristian Hjelstuen , Grethe Karin Martinussen , Gry Stensrud
IPC分类号： A61K51/00 , A61P43/00
CPC分类号： A61K51/0497
摘要： The present invention relates to stabilised 99mTc radiopharmaceutical compositions of the ligand tetrofosmin, which include an ascorbic acid or ascorbate radioprotectant, in the absence of an antimicrobial preservative. The invention also provides lyophilised kits suitable for the bulk preparation of multiple unit patient doses of 99mTc-tetrofosmin metal complexes. Also disclosed are unit doses of 99mTc-tetrofosmin, together with processes for preparing such unit doses from the lyophilised bulk vial.
摘要翻译：本发明涉及在不存在抗微生物防腐剂的情况下，包括抗坏血酸或抗坏血酸盐放射防护剂的配体四氟吗啉的稳定化99mTc放射性药物组合物。本发明还提供了适用于批量制备多单位患者剂量的99mTc-四替吗啉金属络合物的冻干试剂盒。还公开了99mTc-四唑磷的单位剂量，以及从冻干的散装小瓶中制备这种单位剂量的方法。

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