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1351 条记录 (耗时 0.054 秒)

    4-HYDROXYBENZOMORPHANS
    52.
    发明申请
    4-HYDROXYBENZOMORPHANS 有权
    4-羟基苯并恶唑

    公开(公告)号：US20140148475A1

    公开(公告)日：2014-05-29

    申请号：US14169305

    申请日：2014-01-31

    申请人： Rensselaer Polytechnic Institute

    发明人： Mark P. WENTLAND

    IPC分类号： C07D215/14

    CPC分类号： C07D221/28 ,  C07D215/14 ,  C07D215/20 ,  C07D221/26 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08

    摘要： 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. A compound of formula is disclosed, as are pharmaceutically acceptable acid addition salts, such as acetic, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric acid or p-toluenesulfonic acid salts. These compounds are useful for the treatment of pain.

    摘要翻译： 在3-位含有甲酰胺或硫代羧酰胺的4-羟基苯并呋喃可用作止痛剂，抗腹泻剂，抗惊厥药，镇咳药和抗瘾药物。 公开了式的化合物，以及药学上可接受的酸加成盐，例如乙酸，苯磺酸（苯磺酸盐），苯甲酸，樟脑磺酸，柠檬酸，乙烯磺酸，富马酸，葡糖酸，谷氨酸，氢溴酸，盐酸，羟乙磺酸， 扁桃酸，甲磺酸，粘酸，硝酸，双羟萘酸，泛酸，磷酸，琥珀酸，硫酸，酒石酸或对甲苯磺酸盐。 这些化合物可用于治疗疼痛。

    TAU IMAGING PROBE
    56.
    发明申请
    TAU IMAGING PROBE 有权
    TAU成像探索

    公开(公告)号：US20130324523A1

    公开(公告)日：2013-12-05

    申请号：US13881872

    申请日：2011-10-28

    申请人： Yukitsuka Kudo ,  Shozo Furumoto ,  Nobuyuki Okamura

    发明人： Yukitsuka Kudo ,  Shozo Furumoto ,  Nobuyuki Okamura

    IPC分类号： C07D215/12 ,  C07D215/14 ,  C07D498/04 ,  G01N33/68 ,  C07D401/04

    CPC分类号： C07D215/12 ,  A61K9/0019 ,  A61K9/08 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07B59/002 ,  C07B2200/05 ,  C07D215/14 ,  C07D215/20 ,  C07D215/233 ,  C07D215/26 ,  C07D215/38 ,  C07D215/40 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D498/04 ,  G01N33/6893 ,  G01N2800/2821

    摘要： An object of the present invention is to provide a probe for imaging a β-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity.According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.

    摘要翻译： 本发明的目的是提供一种用于成像β片结构蛋白的探针，其可用于诊断构象疾病，特别是具有诸如tau蛋白的脑内积累等基本症状的疾病（tau蛋白病），例如， 阿尔茨海默氏病。 本发明的另一个目的是提供一种对tau高度特异性并且能够令人满意的感光度的tau成像的化合物，并且还具有高的脑转换，低或未被认可的寻骨性质和低或未被认可的毒性。 根据本发明，通过提供式I化合物（其中A，R 1，R 2，R 3，R 4，R 5，R 6，R a和R b如本说明书中所定义）或其药学上可接受的 盐或其溶剂化物。