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44 条记录 (耗时 0.041 秒)

    Iodine derivatives of tetrabenazine
    7.
    发明授权
    Iodine derivatives of tetrabenazine 失效
    丁苯那酸的碘衍生物

    公开(公告)号：US5278308A

    公开(公告)日：1994-01-11

    申请号：US843041

    申请日：1992-02-28

    申请人： Hank F. Kung

    发明人： Hank F. Kung

    IPC分类号： C07D455/06

    CPC分类号： C07D455/06

    摘要： Compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently selected from the group consisting of H, OH, OCH.sub.3, and Halogen or R.sub.1 and R.sub.2 can be taken together to form --O--CH.sub.2 --O--;R.sub.3 and R.sub.4 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, and ##STR2## n is an integer from 0 to 5; X and Y are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen and --R.sub.7 --CH.dbd.CHI;R.sub.5 and R.sub.6 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, --CONR.sub.8 R.sub.9 and ##STR3## X' and Y' are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen, and --R.sub.7 --CH.dbd.CHI;R.sub.7 is selected from the group consisting of a chemical bond and C.sub.1 -C.sub.10 alkyl; andR.sub.8 and R.sub.9 are independently selected from the group consisting of H and C.sub.1 -C.sub.10 alkyl;provided that there is at least one iodine atom directly attached to a phenyl moiety or as part of a --CH.dbd.CHI moiety in one or more substituents selected from the group consisting of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are disclosed as being useful as imaging agents for evaluation of the central nervous system neuronal system.

    摘要翻译： 其中R 1和R 2独立地选自H，OH，OCH 3和卤素或R 1和R 2的式的化合物可一起形成-O-CH 2 -O-; R 3和R 4独立地选自H，OH，C 1 -C 10烷基，C 1 -C 10烷氧基，C 1 -C 10链烯氧基，-R 7 -CH = CHI，且n为0至5的整数; X和Y独立地选自H，OH，OCH 3，卤素和-R 7 -CH = CHI; R 5和R 6独立地选自H，OH，C 1 -C 10烷基，C 1 -C 10烷氧基，C 1 -C 10链烯氧基，-R 7 -CH = CH 1，-CONR 8 R 9和X'和Y'独立地选自 由H，OH，OCH 3，卤素和-R 7 -CH = CHI组成的组; R7选自化学键和C1-C10烷基; 并且R 8和R 9独立地选自H和C 1 -C 10烷基; 条件是在一个或多个选自R3，R4，R5和R6的取代基中存在至少一个碘原子直接连接到苯基部分或作为-CH = CHI部分的一部分，其被公开用作成像 用于评估中枢神经系统神经元系统的药剂。

    Dopamine receptor ligands and image agents
    8.
    发明授权
    Dopamine receptor ligands and image agents 失效
    多巴胺受体配体和成像剂

    公开(公告)号：US5186921A

    公开(公告)日：1993-02-16

    申请号：US816140

    申请日：1991-12-31

    申请人： Hank F. Kung ,  Raymond Murphy

    发明人： Hank F. Kung ,  Raymond Murphy

    IPC分类号： A61K51/04 ,  C07D207/09 ,  C07D405/12

    CPC分类号： C07D405/12 ,  A61K51/0446 ,  C07D207/09 ,  A61K2123/00

    摘要： Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofuran, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.

    摘要翻译： 公开了新型CNS多巴胺D-2受体，例如化合物5-碘-7-N - [（1-乙基-2-吡咯烷基）甲基]甲酰胺-2,3-二氢苯并呋喃。 这些化合物可用作人脑中D-2受体的显像剂，并表现出良好的脑保留和体内稳定性。

    Diagnostic radiopharmaceuticals for localization in target tissues exhibiting a regional pH shift relative to surrounding tissues
    9.
    发明授权
    Diagnostic radiopharmaceuticals for localization in target tissues exhibiting a regional pH shift relative to surrounding tissues 失效
    用于在靶组织中定位的诊断性放射性药物，其显示出相对于周围组织的局部pH变化

    公开(公告)号：US4363793A

    公开(公告)日：1982-12-14

    申请号：US174491

    申请日：1980-08-08

    申请人： Monte Blau ,  Hank F. Kung

    发明人： Monte Blau ,  Hank F. Kung

    IPC分类号： A61K51/04 ,  A61K49/00 ,  A61K43/00

    CPC分类号： A61K51/041 ,  A61K51/0406 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0463 ,  A61K2123/00

    摘要： A radiopharmaceutical chemical compound comprising a radioactive isotope, other than an isotope of iodine, in chemical combination with at least one amine group. The compound has a lipophilicity sufficiently high at a pH of 7.6 to permit passage of the compound from the blood of a mammal into a target organ or tissue and sufficiently low at a pH of 6.6 to prevent rapid return of the compound from the target organ or tissue to the blood. The compound has a percent protein binding of less than ninety percent.A method for selectively depositing a radiopharmaceutical compound in at least one target tissue or organ of a mammal, which tissue or organ has a significantly different intracellular pH than the blood of the mammal, by introducing the compound of the invention into the bloodstream of the mammal.

    摘要翻译： 包含与碘同位素以外的放射性同位素与至少一个胺基化学结合的放射性药物化合物。 化合物在pH为7.6时具有足够高的亲油性，以允许化合物从哺乳动物的血液通过到目标器官或组织中，并且在6.6的pH下足够低，以防止化合物从靶器官迅速返回或 组织到血液。 该化合物的蛋白质结合百分比小于百分之九十。 通过将本发明的化合物引入哺乳动物的血液中，选择性地沉积哺乳动物的至少一种目标组织或器官中的放射性药物化合物的方法，该组织或器官的组织或器官具有与哺乳动物的血液显着不同的细胞内pH 。

    STYRYLPYRIDINE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES
    10.
    发明申请
    STYRYLPYRIDINE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES 有权
    苯乙烯吡啶衍生物及其用于结合和成像淀粉样品的用途

    公开(公告)号：US20130129624A1

    公开(公告)日：2013-05-23

    申请号：US13735609

    申请日：2013-01-07

    申请人： Hank F. Kung ,  Mei-Ping Kung

    发明人： Hank F. Kung ,  Mei-Ping Kung

    IPC分类号： C07D211/94

    CPC分类号： C07D211/94 ,  A61K51/0455 ,  C07D213/16

    摘要： This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

    摘要翻译： 本发明涉及淀粉样蛋白沉积物和苯乙烯基吡啶化合物的成像方法，以及制备用于成像淀粉样沉积物的放射性标记的苯乙烯基吡啶化合物的方法。 本发明还涉及化合物和制备用于抑制淀粉样蛋白聚集以形成淀粉样沉积物的化合物的方法，以及将治疗剂递送至淀粉样沉积物的方法。