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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：EP4310504A3
公开(公告)日：2024-05-01
申请号：EP23207737.0
申请日：2017-12-23
CPC分类号： C12Q1/37 , G01N33/574 , G01N33/68 , G01N2333/94820130101 , A61K49/0032 , A61K49/0052
摘要： The present invention relates to a compound for use in labeling a protease having the formula (II):
wherein D comprises a benzoindole dye; L1 is a linker; AA1 is an amino acid side chain; U is O, NH, or S; R1 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, or a protecting group, and is optionally substituted with 1 to 3 A groups; each A is independently alkyl, alkenyl, alkynyl, alkoxy, alkanoyl, alkylamino, aryl, aryloxy, arylamino, aralkyl, aralkoxy, aralkanoyl, aralkamino, heteroaryl, heteroaryloxy, heteroarylamino, heteroaralkyl, heteroaralkoxy, heteroaralkanoyl, heteroaralkamino, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkoxy, cycloalkanoyl, cycloalkamino, heterocyclyl, heterocyclyloxy, heterocyclylamino, heterocyclylalkyl, heterocyclylalkoxy, heterocyclylalkanoyl, heterocyclylalkamino, hydroxyl, thio, amino, alkanoylamino, aroylamino, aralkanoylamino, alkylcarboxy, carbonate, carbamate, guanidinyl, urea, halo, trihalomethyl, cyano, nitro, phosphoryl, sulfonyl, sulfonamido, or azido, L3 is a linker; and Q comprises a quencher, and wherein the benzoindole dye has the structure:
wherein o is an integer from 1 to 4; R2 is a C2-C8 alkyl group, optionally substituted with a sulfonate or carbonate; each R3 is independently a C1-C6 alkyl group; and L4 is an optionally substituted alkyl linker, wherein each carbon atom is optionally replaced with a heteroatom.-
公开(公告)号：EP2971065A2
公开(公告)日：2016-01-20
申请号：EP14764975.0
申请日：2014-03-15
IPC分类号： C12Q1/37 , C07D401/00 , A61B5/00
CPC分类号： C07D401/14 , A61K49/0032 , A61K49/0034 , A61K49/0041
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：EP4310504A2
公开(公告)日：2024-01-24
申请号：EP23207737.0
申请日：2017-12-23
IPC分类号： G01N33/68
摘要： The present invention relates to a compound for use in labeling a protease having the formula (II):
wherein D comprises a benzoindole dye; L 1 is a linker; AA 1 is an amino acid side chain; U is O, NH, or S; R 1 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, or a protecting group, and is optionally substituted with 1 to 3 A groups; each A is independently alkyl, alkenyl, alkynyl, alkoxy, alkanoyl, alkylamino, aryl, aryloxy, arylamino, aralkyl, aralkoxy, aralkanoyl, aralkamino, heteroaryl, heteroaryloxy, heteroarylamino, heteroaralkyl, heteroaralkoxy, heteroaralkanoyl, heteroaralkamino, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkoxy, cycloalkanoyl, cycloalkamino, heterocyclyl, heterocyclyloxy, heterocyclylamino, heterocyclylalkyl, heterocyclylalkoxy, heterocyclylalkanoyl, heterocyclylalkamino, hydroxyl, thio, amino, alkanoylamino, aroylamino, aralkanoylamino, alkylcarboxy, carbonate, carbamate, guanidinyl, urea, halo, trihalomethyl, cyano, nitro, phosphoryl, sulfonyl, sulfonamido, or azido, L 3 is a linker; and Q comprises a quencher, and wherein the benzoindole dye has the structure:
wherein o is an integer from 1 to 4; R 2 is a C 2 -C 8 alkyl group, optionally substituted with a sulfonate or carbonate; each R 3 is independently a C 1 -C 6 alkyl group; and L 4 is an optionally substituted alkyl linker, wherein each carbon atom is optionally replaced with a heteroatom.-
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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