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11 条记录 (耗时 0.027 秒)

    Agents for Imaging Apoptosis
    1.
    发明申请
    Agents for Imaging Apoptosis 审中-公开
    成像细胞凋亡剂

    公开(公告)号：US20090170131A1

    公开(公告)日：2009-07-02

    申请号：US12298386

    申请日：2007-05-09

    申请人： Juri Gelovani ,  William Tong ,  Amer Najjar ,  Chun Li

    发明人： Juri Gelovani ,  William Tong ,  Amer Najjar ,  Chun Li

    IPC分类号： G01N33/53

    CPC分类号： C12Q1/37 ,  A61K47/556 ,  A61K51/04 ,  G01N2333/96466 ,  G01N2510/00

    摘要： Compositions, and methods of using such compositions, having the following Formula (I) or salt, ester, or hydrate thereof, wherein R1 is Asp-Glu peotide, tert-butyloxycarbonyl, methoxyphenylacetyl, bromomethoxyphenylaceityl, fluoromethoxyphenylacetyl, (methylmethoxyphenyl)acetyl, or iodomethoxyphenylacetyl; R2 is valine with or without protecting groups), aspartale (with or without protecting groups), 1-Butyl, hydrogen, aniline, aromatic molecules, tert-butyloxycarbonyl, or fluorenyl-methoxy-carbonyl; and R3 is p-nitroaniline, 7-amino-4-methylcoumarin, fluoroethylamine, 1-amino-4-fluoromethyl-cyclohexane, 1-amino-4-fluoroethyl-cyclohexane, aniline, p-fluoroaniline, p-fluoromethylaniline, p-fluorobenzylamine, p-fluoromethylbenzylamine, 4-aminopiperidine, 4-amino-1-fluoroethylpiperidine, or 4-amino-1-fluoropropylpiperidine.

    摘要翻译： 组成和使用这种组合物的方法，其具有下式（I）或其盐，酯或水合物，其中R1是Asp-Glu磷酸酯，叔丁氧基羰基，甲氧基苯乙酰基，溴代甲氧基苯基乙基，氟甲氧基苯乙酰基，（甲基甲氧基苯基）乙酰基或碘代甲氧基苯乙酰基 ; R2是具有或不具有保护基的缬氨酸），天冬氨酸（具有或不具有保护基），1-丁基，氢，苯胺，芳族分子，叔丁氧基羰基或芴基 - 甲氧基 - 羰基; 并且R3是对硝基苯胺，7-氨基-4-甲基香豆素，氟乙胺，1-氨基-4-氟甲基 - 环己烷，1-氨基-4-氟乙基 - 环己烷，苯胺，对氟苯胺，对氟甲基苯胺，对氟苄胺 ，对氟甲基苄胺，4-氨基哌啶，4-氨基-1-氟乙基哌啶或4-氨基-1-氟丙基哌啶。

    Non-Invasive Molecular Imaging of Cellular Histone Deacetylase Substrate Using Magnetic Resonance Spectroscopy (MRS) or Positron Emission Tomography (PET)
    2.
    发明申请
    Non-Invasive Molecular Imaging of Cellular Histone Deacetylase Substrate Using Magnetic Resonance Spectroscopy (MRS) or Positron Emission Tomography (PET) 审中-公开
    使用磁共振光谱（MRS）或正电子发射断层扫描（PET）的细胞组蛋白脱乙酰酶底物的非侵入性分子成像

    公开(公告)号：US20100278730A1

    公开(公告)日：2010-11-04

    申请号：US12595281

    申请日：2008-04-08

    申请人： Sabrina Ronen ,  Juri Gelovani ,  William Tong ,  Mian Alauddin ,  Uday Mukhopadhyay ,  Madhuri Sankaranatayanapillai ,  Ashutosh Pal

    发明人： Sabrina Ronen ,  Juri Gelovani ,  William Tong ,  Mian Alauddin ,  Uday Mukhopadhyay ,  Madhuri Sankaranatayanapillai ,  Ashutosh Pal

    IPC分类号： A61K51/00 ,  A61B5/055 ,  C07C237/28

    CPC分类号： A61K49/10 ,  A61K51/04 ,  C07D249/06

    摘要： We disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one atom having a nucleus detectable by magnetic resonance spectroscopy, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by magnetic resonance spectroscopy (MRS). We also disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one positron-emission-decaying radioisotope, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by positron emission tomography (PET). We also disclose compounds useful as histone deacetylase substrates.

    摘要翻译： 我们公开了通过向哺乳动物施用包含至少一个具有可通过磁共振光谱法检测的核的原子的化合物，其中所述化合物是组蛋白脱乙酰酶的底物，来检测哺乳动物组蛋白脱乙酰酶活性的方法; 并通过磁共振光谱法（MRS）观察哺乳动物体内至少一部分的化合物或其裂解产物。 我们还公开了通过向哺乳动物施用包含至少一种正电子发射衰减放射性同位素的化合物来检测哺乳动物中组蛋白脱乙酰酶活性的方法，其中该化合物是组蛋白脱乙酰酶的底物; 并通过正电子发射断层摄影（PET）观察哺乳动物身体的至少一部分中的化合物或其裂解产物。 我们还公开了可用作组蛋白脱乙酰酶底物的化合物。

    Dichloroacetate Analogs as Imaging Agents
    3.
    发明申请
    Dichloroacetate Analogs as Imaging Agents 审中-公开
    二氯乙酸酯类似物作为成像剂

    公开(公告)号：US20090028791A1

    公开(公告)日：2009-01-29

    申请号：US12178826

    申请日：2008-07-24

    申请人： Julius A. Balatoni ,  Louis R. DePalatis ,  William Tong ,  Juri Gelovani

    发明人： Julius A. Balatoni ,  Louis R. DePalatis ,  William Tong ,  Juri Gelovani

    IPC分类号： A61K51/04 ,  C07C69/63 ,  A61K31/22 ,  A61P35/00

    CPC分类号： A61K51/04 ,  A61K49/10 ,  A61K51/0402 ,  C07B59/001 ,  C07B2200/05 ,  C07C53/16 ,  C07C53/18 ,  C07C69/63

    摘要： A compound having structure I: wherein xC is selected from the group consisting of 11C, 12C, and 13C; R is selected from the group consisting of —OH, —O−R4+ wherein R4 is selected from the group consisting of Na and K, —OR3 wherein R3 is selected from the group consisting of C1-8 alkyl and C1-8 alkenyl, —NH2, and NHR3; R′ is selected from the group consisting of —H, —Cl, —F, —Br, and —I; R″ is selected from the group consisting of —H, —Cl, —F, —Br, and —I; and R′″ is selected from the group consisting of —H, —Cl, —F, —Br, —I, 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I; provided, when xC is 12C, R′″ is selected from the group consisting of 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I. Also, a method of imaging in a mammal a medical condition, such as a cancer, lactic acidosis, or cardiac or cardiovascular function by administering to the mammal a composition comprising a compound having structure I and observing the distribution of the compound in the mammal by an imaging modality selected from the group consisting of positron emission tomography (PET) imaging, single photon emission computed tomography (SPECT), gamma camera devices, magnetic resonance imaging (MRI), and hand-held radiation detection probes. In addition, a method of treating a cancer in a mammal by administering to the mammal a composition comprising a compound having structure I.

    摘要翻译： 具有结构I的化合物：其中xC选自11C，12C和13C; R选自-OH，-O-R 4 +，其中R 4选自Na和K，-OR 3，其中R 3选自C 1-8烷基和C 1-8链烯基， NH2和NHR3; R'选自-H，-Cl，-F，-Br和-I; R“选自-H，-Cl，-F，-Br和-I; 并且R“'选自-H，-Cl，-F，-Br，-I，18F，19F，75Br，76Br，77Br，123I，124I和131I; 条件是当xC为12℃时，R“'选自18F，19F，75Br，76Br，77Br，123I，124I和131I。 另外，通过向哺乳动物施用包含具有结构I的化合物的组合物并通过以下方式观察哺乳动物中化合物的分布来观察哺乳动物中化合物的分布，在哺乳动物体内成像哺乳动物的医学病症例如癌症，乳酸性酸中毒或心脏或心血管功能的方法 选自正电子发射断层摄影（PET）成像，单光子发射计算机断层摄影（SPECT），伽马相机装置，磁共振成像（MRI）和手持放射检测探针的成像模式。 另外，通过向哺乳动物施用包含具有结构I的化合物的组合物来治疗哺乳动物的癌症的方法。