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    Method for determining lymphocyte distribution and trafficking in mammals using imaging
    1.
    发明授权
    Method for determining lymphocyte distribution and trafficking in mammals using imaging 失效
    使用成像确定哺乳动物淋巴细胞分布和贩运的方法

    公开(公告)号：US06146614A

    公开(公告)日：2000-11-14

    申请号：US886578

    申请日：1997-07-01

    申请人： Robert H. Rubin ,  Alan J. Fischman ,  David Baltimore

    发明人： Robert H. Rubin ,  Alan J. Fischman ,  David Baltimore

    IPC分类号： A61K49/04 ,  A61K49/18 ,  A61K51/10 ,  A61K51/12 ,  A61B5/055

    CPC分类号： A61K51/1027 ,  A61K49/04 ,  A61K49/1896 ,  A61K51/1203

    摘要： Methods for determining lymphocyte distribution and trafficking in a mammal are described. Either a labeled ligand capable of interacting specifically with the lymphocytes of the mammal is administered to the mammal so that the labeled ligand interacts in vivo with the lymphocytes, resulting in labeled lymphocytes, or, the labeled ligand is contacted with the lymphocytes in vitro so that the labeled ligand interacts with the lymphocytes resulting in labeled lymphocytes, and these labeled lymphocytes are administered to the mammal. The distribution or trafficking of the labeled lymphocytes in the mammal is determined by imaging. Methods for diagnosing the degree of progression of a disease in a mammal by determining the mammal's lymphocyte distribution or trafficking pattern, for monitoring the response to a therapy in mammal having a disease, for evaluating the ability of an agent to alter the distribution or trafficking of lymphocytes, and for identifying an agent useful for treating a mammal having a disease, are also described.

    摘要翻译： 描述了确定哺乳动物淋巴细胞分布和运输的方法。 向哺乳动物施用能够与哺乳动物的淋巴细胞相互作用的标记配体，使得标记的配体在体内与淋巴细胞相互作用，导致标记的淋巴细胞，或者标记的配体在体外与淋巴细胞接触，使得 标记的配体与淋巴细胞相互作用，导致标记的淋巴细胞，并且将这些标记的淋巴细胞施用于哺乳动物。 通过成像确定哺乳动物中标记的淋巴细胞的分布或运输。 用于通过确定哺乳动物的淋巴细胞分布或贩运模式来诊断哺乳动物疾病进展程度的方法，用于监测具有疾病的哺乳动物患有对具有疾病的哺乳动物的治疗的反应，用于评估药剂改变分布或贩运的能力 还描述了用于鉴定可用于治疗患有疾病的哺乳动物的药剂的淋巴细胞。

    Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
    4.
    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
    5.
    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。

    Catalytic radiofluorination
    9.
    发明授权
    Catalytic radiofluorination 有权
    催化放电氟化

    公开(公告)号：US08257680B1

    公开(公告)日：2012-09-04

    申请号：US11506603

    申请日：2006-08-18

    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： A61K51/00 ,  A61M36/14

    CPC分类号： A61K51/04 ,  A61B6/507 ,  A61K9/0021 ,  A61K49/0433 ,  A61K51/00 ,  A61K51/0459 ,  A61K51/0489 ,  C07B2200/05 ,  C07C209/74 ,  C07C211/64 ,  C07C381/12 ,  C07D241/04 ,  C07D295/073 ,  C07F9/5442

    摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.

    摘要翻译： 本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。 在优选的实施方案中，使用氟化钾-18。 本发明的另一方面涉及可用作成像剂的含氟-18的芳基铵化合物。 在某些实施方案中，铵化合物是四芳基铵盐。 本发明的另一方面涉及可用作成像剂的含有氟-18的芳基锍化合物。 在某些实施方案中，锍化合物是三芳基锍盐。 本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。