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    .alpha.-substituted hydrazides having calpain inhibitory activity
    1.
    发明授权
    .alpha.-substituted hydrazides having calpain inhibitory activity 失效
    具有钙蛋白酶抑制活性的α-取代酰肼

    公开(公告)号：US5679680A

    公开(公告)日：1997-10-21

    申请号：US389525

    申请日：1995-02-16

    申请人： Kevin Ka-Wang Wang ,  Po-Wai Yuen

    发明人： Kevin Ka-Wang Wang ,  Po-Wai Yuen

    IPC分类号： A61K31/495 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/18 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  C07D241/44 ,  C07D241/54

    CPC分类号： C07D241/44

    摘要： The invention covers a novel series of .alpha.-substituted hydrazides that inhibit both calpain I and calpain II. They are non-peptide irreversible active site inhibitors of calpain. The compounds are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders, brain injury, spinal cord, and peripheral nerve injury, cardiac infarction, cataracts, inflammation, restenosis, muscular dystrophy, and platelet aggregation. Pharmaceutical compositions, methods of using processes for preparing and novel intermediates useful in the processes are also disclosed.

    摘要翻译： 本发明涵盖了抑制钙蛋白酶I和钙蛋白酶II两者的新一代α-取代酰肼。 它们是钙肽酶的非肽不可逆活性位点抑制剂。 该化合物可用于治疗神经变性障碍，包括脑血管障碍，脑损伤，脊髓和周围神经损伤，心肌梗死，白内障，炎症，再狭窄，肌营养不良和血小板聚集。 还公开了药物组合物，使用制备方法的方法和用于该方法的新型中间体。

    Imaging of Neural and Organ Injury or Damage
    6.
    发明申请
    Imaging of Neural and Organ Injury or Damage 审中-公开
    神经和器官损伤或损伤的成像

    公开(公告)号：US20080311036A1

    公开(公告)日：2008-12-18

    申请号：US11914003

    申请日：2006-05-11

    申请人： Kevin Ka-Wang Wang ,  Ronald L. Hayes ,  Lewis R. Baxter, JR. ,  Laszlo Prokai

    发明人： Kevin Ka-Wang Wang ,  Ronald L. Hayes ,  Lewis R. Baxter, JR. ,  Laszlo Prokai

    IPC分类号： A61K51/08 ,  A61K51/04

    CPC分类号： A61K51/04 ,  A61K51/08 ,  A61K51/088

    摘要： In vivo determination of regional damage with neural and organ injury specific imaging agents. Rapid, and non-invasive imaging compositions and methods for assessment of the extent of neurotoxic cell loss or nervous system damage resulting from nervous system injury due to ischemia, stroke, trauma, chemical or electrical insult, acute drug overdose or exposure to substance abuse (such as “recreational drugs”) infection or other insults. The same or similar rapid, and non-invasive imaging compositions and methods for assessment of the extent of the organ injury comprises any damage, injury or infection, functional failure to specific organs such as liver, kidney, prostate, lung, skeletal muscle, heart, pancreas, stomach, small and large intestine, bladder and the reproductive system as well as damage, injury or infection, functional failure to multi-organs, trauma-hemorrhagic shock and sepsis. In particular, neural and organ damage is detected via protease inhibitor-based radionuclide-labeled imaging ligand binding to overactivated proteases (calpains, caspases, cathepsins, proteasome, metalloproteases, granzyme B or other proteases) that are specific to neural or organ injury or damage.

    摘要翻译： 用神经和器官损伤特异性成像剂进行体内区域损伤测定。 用于评估由于缺血，中风，创伤，化学或电气侮辱，急性药物过量或暴露于药物滥用引起的神经系统损伤引起的神经毒性细胞损失或神经系统损伤的程度的快速和非侵入性成像组合物和方法（ 如“娱乐性药物”）感染或其他侮辱。 用于评估器官损伤程度的相同或相似的快速和非侵入性成像组合物和方法包括任何损伤，损伤或感染，对特定器官如肝，肾，前列腺，肺，骨骼肌，心脏的功能衰竭 ，胰腺，胃，小肠和大肠，膀胱和生殖系统以及损伤，损伤或感染，多器官功能衰竭，创伤性出血性休克和败血症。 特别地，通过基于蛋白酶抑制剂的放射性核素标记的成像配体结合到对神经或器官损伤或损伤特异性的过度活化的蛋白酶（钙蛋白酶，胱天蛋白酶，组织蛋白酶，蛋白酶体，金属蛋白酶，粒酶B或其他蛋白酶）来检测神经和器官损伤 。