DESFERRITHIOCIN ANALOGS AND USES THEREOF
    81.
    发明申请
    DESFERRITHIOCIN ANALOGS AND USES THEREOF 有权
    DESFERRITHIOCIN模拟物及其用途

    公开(公告)号:US20160289223A1

    公开(公告)日:2016-10-06

    申请号:US15038188

    申请日:2014-11-21

    IPC分类号: C07D417/04

    摘要: Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).

    摘要翻译: 铁超载与氧化应激,输血铁超载,地中海贫血,原发性血色素沉着症,继发性血色素沉着症,糖尿病,肝病,心脏病,癌症,放射性损伤,神经或神经退行性疾病,弗里德里希共济失调(FRDA),黄斑变性 闭合性头部损伤,肠易激综合征和再灌注损伤。 本发明提供使用式(A)和(J)的脱铁硫代类似物用于治疗和/或预防这些病理状况的方法和药物组合物,金属(例如铁,铝,镧系元素或锕系元素(例如铀)) 过载条件和传染病(如疟疾)。

    DESAZADESFERROTHIOCIN ANALOGUES AS METAL CHELATION AGENTS
    82.
    发明申请
    DESAZADESFERROTHIOCIN ANALOGUES AS METAL CHELATION AGENTS 审中-公开
    DESAZADESFERROTHIOCIN ANALOGUES as METAL CHELATION AGENTS

    公开(公告)号:US20150259306A1

    公开(公告)日:2015-09-17

    申请号:US14722422

    申请日:2015-05-27

    摘要: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

    摘要翻译: 本文公开了新型的脱氮铁硫代聚醚(DADFT-PE)类似物的化合物,以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

    Luminescent substrate for luciferase
    83.
    发明授权
    Luminescent substrate for luciferase 有权
    荧光素酶的荧光底物

    公开(公告)号:US08962854B2

    公开(公告)日:2015-02-24

    申请号:US14240144

    申请日:2012-08-22

    摘要: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.

    摘要翻译: 本发明的目的是提供萤火虫荧光素和萤火虫萤光素类似物,其被修饰以通过荧光素酶在萤火虫生物发光系统中维持发光活性。 特别地,本发明的目的是提供一种荧光生物发光系统的发光波长比现有的发光基板移动到更长的波长的新的发光基板。 本发明提供了其中苯并噻唑环部分在7位被修饰的荧光素,其中苯环部分已经在6位被修饰的萤光素类似物和其中6-(二烷基氨基 )-2-萘基部分已经在5位修饰。

    LUMINESCENT SUBSTRATE FOR LUCIFERASE
    85.
    发明申请
    LUMINESCENT SUBSTRATE FOR LUCIFERASE 有权
    LUCIFERASE的发光基材

    公开(公告)号:US20140221665A1

    公开(公告)日:2014-08-07

    申请号:US14240144

    申请日:2012-08-22

    IPC分类号: C12Q1/66

    摘要: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.

    摘要翻译: 本发明的目的是提供萤火虫荧光素和萤火虫萤光素类似物,其被修饰以通过荧光素酶在萤火虫生物发光系统中维持发光活性。 特别地,本发明的目的是提供一种荧光生物发光系统的发光波长比现有的发光基板移动到更长的波长的新的发光基板。 本发明提供了其中苯并噻唑环部分在7位被修饰的荧光素,其中苯环部分已经在6位被修饰的萤光素类似物和其中6-(二烷基氨基 )-2-萘基部分已经在5位修饰。

    Desferrithiocin derivatives and methods of use thereof
    86.
    发明授权
    Desferrithiocin derivatives and methods of use thereof 失效
    脱铁硫代衍生物及其使用方法

    公开(公告)号:US08604216B2

    公开(公告)日:2013-12-10

    申请号:US11367042

    申请日:2006-03-02

    IPC分类号: A61K31/425 C07D277/10

    CPC分类号: C07D277/12

    摘要: Compounds represented by structural formulas such as Structural Formula (I): are highly efficient in clearing excess iron from an organism. The invention also discloses methods of treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.

    摘要翻译: 由结构式表示的化合物如结构式(I):在从生物体中清除多余的铁中是高效的。 本发明还公开了治疗诸如金属过载,氧化应激和肿瘤和肿瘤前病症的病症的方法。

    Thiazoline acid derivatives
    89.
    发明授权
    Thiazoline acid derivatives 有权
    噻唑啉酸衍生物

    公开(公告)号:US08008502B2

    公开(公告)日:2011-08-30

    申请号:US12383854

    申请日:2009-03-27

    IPC分类号: C07D277/08

    CPC分类号: A61K31/426 C07D277/12

    摘要: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.

    摘要翻译: 本发明涉及在治疗应用中用作三价金属螯合剂的新型噻唑啉酸及其衍生物。 例如,噻唑啉酸衍生物可用于诊断和治疗与人和动物中过量的三价金属相关的病理状况。