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    Imaging agents for early detection and monitoring of cardiovascular plaque
    2.
    发明授权
    Imaging agents for early detection and monitoring of cardiovascular plaque 失效
    用于早期检测和监测心血管斑块的成像剂

    公开(公告)号：US07060251B1

    公开(公告)日：2006-06-13

    申请号：US09530818

    申请日：1998-09-08

    申请人： David R. Elmaleh ,  Alan J. Fischman ,  John W. Babich

    发明人： David R. Elmaleh ,  Alan J. Fischman ,  John W. Babich

    IPC分类号： A61K49/04

    CPC分类号： A61K51/088

    摘要： The invention provides imaging agents comprising a label in association with a plaque specific targeting molecule. Methods for using the imaging agents to diagnose or monitor plaque formation and growth and kits containing the cardiovascular agents or components suitable for production of the imaging agents are also provided.

    摘要翻译： 本发明提供包含与斑块特异性靶向分子相关联的标记物的成像剂。 还提供了使用成像剂诊断或监测斑块形成和生长的方法以及含有适合于生产成像剂的心血管药剂或成分的试剂盒。

    Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
    5.
    发明授权
    Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process 有权
    诊断和治疗烷基哌啶/哌嗪化合物和方法

    公开(公告)号：US08114379B2

    公开(公告)日：2012-02-14

    申请号：US12100067

    申请日：2008-04-09

    申请人： David R. Elmaleh ,  Choi Sungwoon ,  Alan J. Fischman

    发明人： David R. Elmaleh ,  Choi Sungwoon ,  Alan J. Fischman

    IPC分类号： A61K51/04 ,  A61K49/22 ,  A61K31/4965 ,  A61K31/497

    CPC分类号： C07D295/205 ,  C07D211/26 ,  C07D211/58 ,  C07D213/74 ,  C07D241/06 ,  C07D241/08 ,  C07D295/088 ,  C07D295/096 ,  C07D295/135 ,  C07D295/192 ,  C07D295/21 ,  C07D295/26

    摘要： Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: wherein: n is an integer of 1 to 6; X, Y, Z1 and Z2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6) alkoxy, N-alkyl, (C2-C6) acyloxy, N-alkylene, —SH, —SR, wherein R is from the same group as R1 and R2 and can be the same or different than R1 and R2, amino, nitro, cyano, hydroxy, C(═O)OR6, —C(═O)NR5R4, NR3R2, or S(═O)kR1 wherein k is 1 or 2, and R1 to R6 are independently hydrogen or (C1-C6) alkyl; R1, and R2 can be the same or different and are hydrogen, (C1-C6) alkyl, hydroxyalkyl or mercaptoalkyl, —C(═O)OR1, cyano, (C1-C6) alkenyl, (C2-C6) alkynyl, or 1,2,4-oxadiazol-5-yl optionally substituted at the 3-position by Z4 wherein any (C1-C6) alky, (C1-C6) alkanoyl, (C2-C6) alkenyl or (C2-C6) alkynyl can optionally be substituted by 1, 2 or 3 Z; R7 can be hydrogen, O or phenyl R8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl Z4 is (C1-C6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z1 W is O or S T is amino or C1-C6 aminoalkyl A is N or C T is C1-C6 alklyl or sulfonyl and V is alkyl (C0-C6), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R1 or R2 as indicated above and φ is phenyl, naphthyl, thienyl or pyridinyl.

    摘要翻译： 提供了可用于治疗特征在于缺乏多巴胺神经元活性或成像多巴胺神经元的神经变性疾病的哌啶或哌嗪化合物。 该化合物的特征在于下式：其中：n为1至6的整数; X，Y，Z 1和Z 2可以相同或不同，为氢，卤素，卤代烷基，烷基，芳基，（C1-C6）烷氧基，N-烷基，（C2-C6）酰氧基，N-亚烷基， -SR，其中R是与R1和R2相同的基团，并且可以相同或不同于R1和R2，氨基，硝基，氰基，羟基，C（= O）OR6，-C（= O）NR5R4，NR3R2 或S（= O）kR1其中k为1或2，并且R 1至R 6独立地为氢或（C 1 -C 6）烷基; R 1和R 2可以相同或不同，为氢，（C 1 -C 6）烷基，羟烷基或巯基烷基，-C（= O）OR 1，氰基，（C 1 -C 6）烯基，（C 2 -C 6）炔基或 其中任何（C 1 -C 6）烷基，（C 1 -C 6）烷酰基，（C 2 -C 6）烯基或（C 2 -C 6）炔基可以在3位上被Z 4任意取代在3位上的1,2,4-恶二唑-5-基， 任选被1,2或3个Z取代; R7可以是氢，O或苯基R8可以是氢，苯基，卤代苯基，硝基苯基，吡啶基，胡椒基或磺基亚硝基苯基Z4是（C1-C6）烷基或苯基，任选被1,2或3取代，Z1是O或ST是 氨基或C 1 -C 6氨基烷基A为N或CT为C 1 -C 6烷基或磺酰基，V为烷基（C 0 -C 6），链烯基，炔基，卤代芳基，烷基苯酚，烷基卤代苯基和如上所述的R 1或R 2， 是苯基，萘基，噻吩基或吡啶基。

    Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid
    6.
    发明申请
    Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权
    用放射性标记的链烷酸监测组织中血流和代谢摄取的方法

    公开(公告)号：US20080206135A1

    公开(公告)日：2008-08-28

    申请号：US11974139

    申请日：2007-10-11

    申请人： David R. Elmaleh ,  Alan J. Fischman ,  Timothy M. Shoup

    发明人： David R. Elmaleh ,  Alan J. Fischman ,  Timothy M. Shoup

    IPC分类号： A61K51/04

    CPC分类号： A61K51/0402

    摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.

    摘要翻译： 本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换在2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。 这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

    Polybiotin compounds of magnetic resonance imaging and drug delivery
    9.
    发明授权
    Polybiotin compounds of magnetic resonance imaging and drug delivery 有权
    用于磁共振成像和药物递送的多生物素化合物

    公开(公告)号：US08092782B2

    公开(公告)日：2012-01-10

    申请号：US12208025

    申请日：2008-09-10

    申请人： David R. Elmaleh ,  Timothy M. Shoup ,  Alan J. Fischman

    发明人： David R. Elmaleh ,  Timothy M. Shoup ,  Alan J. Fischman

    IPC分类号： A61B5/055 ,  A61B5/05 ,  C07F5/00 ,  C07D255/02 ,  C07D235/02

    CPC分类号： C07D519/00 ,  A61B5/0059 ,  A61B5/055 ,  A61B5/412 ,  A61B5/4839 ,  A61K47/557 ,  A61K49/085 ,  A61K49/10 ,  A61K49/106 ,  A61K49/124 ,  A61K51/0446 ,  A61K51/0497 ,  G01R33/5601

    摘要： The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.

    摘要翻译： 本发明一般涉及可用作成像剂和药物递送剂的含生物素的化合物。 本发明的另一方面涉及上述与金属原子螯合的化合物。 在优选的实施方案中，金属原子是钆。 本发明的另一方面涉及包含三个生物素部分和共价结合到杂环核心的药剂的化合物。 在某些实施方案中，药剂是抗生素，抗病毒剂或放射性核素。 本发明的另一方面涉及一种治疗涉及将哺乳动物施用本发明化合物的疾病的方法。 本发明的另一方面涉及使用本发明化合物获得磁共振图像的方法。

    Aryl Bidentate Isonitriles and Their Uses
    10.
    发明申请
    Aryl Bidentate Isonitriles and Their Uses 审中-公开
    芳基二异丁腈及其用途

    公开(公告)号：US20110236308A1

    公开(公告)日：2011-09-29

    申请号：US12297513

    申请日：2007-04-17

    申请人： David R. Elmaleh ,  Timothy M. Shoup ,  Alan J. Fischman ,  Bhaskar C. Das

    发明人： David R. Elmaleh ,  Timothy M. Shoup ,  Alan J. Fischman ,  Bhaskar C. Das

    IPC分类号： A61K51/04 ,  C07C255/33 ,  C07C255/51 ,  C07F13/00 ,  A61K47/48 ,  A61P43/00

    CPC分类号： A61K51/0478 ,  A61K49/0002 ,  A61K49/0019

    摘要： The present invention relates generally to chelation compounds, radionuclide metal chelate compounds, i.e., complexes, and radiolabeled targeting moieties, i.e., conjugates, formed therefrom, and methods of using these compounds, complexes and conjugates for diagnostic and therapeutic purposes. This invention is more particularly related to aryl bidentate isonitrile metal complexes generated by a chemical interaction of a metal salt oxide or weak complex of the metal with aryl isonitrile bidentate ligands.

    摘要翻译： 本发明一般涉及螯合化合物，即放射性核素金属螯合物，即络合物和放射性标记的靶向部分，即由其形成的缀合物，以及用于诊断和治疗目的的这些化合物，复合物和缀合物的使用方法。 本发明更特别涉及通过金属盐氧化物或金属与芳基异腈二齿配体的弱络合物的化学相互作用产生的芳基二齿异腈金属络合物。