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公开(公告)号：EP3247802A1
公开(公告)日：2017-11-29
申请号：EP16740869.9
申请日：2016-01-22
IPC分类号： C12Q1/37 , C07D401/14
CPC分类号： C07K5/06086 , A61K49/0032 , A61K49/0056 , A61K51/08 , A61K51/088 , C07D401/14 , C07D403/08 , C07D405/06
摘要： Compounds useful as contrast agents in image-guided surgery are provided. The compounds comprise a latent cationic lysosomotropic fragment that is detectable upon cleavage by lysosomal proteases within treated tissues, particularly within tumors and other diseased tissues. Also provided are compositions comprising the compounds and methods for using the compounds, for example in dynamically monitoring protease activity in vivo during image-guided tumor resection surgery.
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公开(公告)号：EP2029135A2
公开(公告)日：2009-03-04
申请号：EP07863360.9
申请日：2007-06-13
IPC分类号： A61K31/335 , A01N43/20 , A01N43/24
CPC分类号： C07D401/12 , C07D303/48
摘要： Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
摘要翻译： 本文提供了半胱氨酸蛋白酶的新型环氧化物抑制剂，包含环氧化物抑制剂的组合物和包装的药物。 还提供了抑制木瓜蛋白酶家族半胱氨酸蛋白酶的方法和通过施用含有本发明的环氧化物抑制剂的组合物来治疗或预防疾病的方法。 组合物可以与另一种治疗剂联合给药。
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公开(公告)号：EP4218829A3
公开(公告)日：2023-08-16
申请号：EP22213062.7
申请日：2014-03-15
IPC分类号： A61K49/00 , C07D401/14
摘要： Activity-based probe compounds for use in labeling a cysteine protease are provided. The compounds are targeted to the protease through a specific targeting element. The compounds additionally include a detectable element, such as a fluorescent label, a radiolabel, or a chelator. In some cases, the compounds additionally include a quenching element that is released upon reaction with the protease. Also provided are compositions comprising the compounds and methods for using the compounds, for example in labeling a protease in an animal and in visualizing a tumor in an animal.
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公开(公告)号：EP4218829A2
公开(公告)日：2023-08-02
申请号：EP22213062.7
申请日：2014-03-15
IPC分类号： A61K49/00 , C12Q1/37 , C07D401/14
摘要： Activity-based probe compounds for use in labeling a cysteine protease are provided. The compounds are targeted to the protease through a specific targeting element. The compounds additionally include a detectable element, such as a fluorescent label, a radiolabel, or a chelator. In some cases, the compounds additionally include a quenching element that is released upon reaction with the protease. Also provided are compositions comprising the compounds and methods for using the compounds, for example in labeling a protease in an animal and in visualizing a tumor in an animal.
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公开(公告)号：EP3601261A1
公开(公告)日：2020-02-05
申请号：EP18777788.3
申请日：2018-03-30
IPC分类号： C07D401/14 , C12Q1/37
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公开(公告)号：EP3510380A1
公开(公告)日：2019-07-17
申请号：EP17883805.8
申请日：2017-12-23
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