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公开(公告)号：EP4253402A1
公开(公告)日：2023-10-04
申请号：EP22900722.4
申请日：2022-12-09
发明人： CHEN, Xiaoyuan , XU, Pengfei , WU, Xiaoming , GUO, Zhide , YANG, Qingbao , WEN, Xuejun
IPC分类号： C07K7/64 , C07K1/04 , A61K38/08 , A61P35/00 , A61P29/00 , A61P9/10 , A61P17/02 , C07D401/12 , A61K38/00 , A61K51/04
摘要： The present disclosure relates to the fields of nuclear medicine and molecular imaging, and specifically relates to a dual-targeting compound and a preparation method and application thereof. The dual-targeting compound has the following structure shown in Formula (I). The present disclosure also provides a dual-targeting compound capable of being labeled with a radionuclide, and the compound has the following structure shown in Formula (I-1) or Formula (I-2). The dual-targeting compound of the present disclosure has high affinity for an FAP target and an integrin α v β 3 target, can realize synergistic targeting of the FAP target and the integrin α v β 3 target in tumors, and has high uptake in tumors and long retention time in tumors. The present disclosure also provides a radionuclide labeled dual-targeting compound based on the dual-targeting compound, and a preparation method and application thereof in preparation of medicines for diagnosis or therapy of diseases characterized by overexpression of FAP and/or integrin α v β 3 .
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2.发明公开
公开(公告)号：EP4227315A1
公开(公告)日：2023-08-16
申请号：EP22762458.2
申请日：2022-02-27
发明人： CHEN, Xiaoyuan , XU, Pengfei
摘要： The present disclosure provides a compound targeting prostate specific membrane antigen (PSMA), wherein the compound has the following structure shown in Formula (I); R 1 is a compound structure targeting prostate specific membrane antigen; L 1 is -(X) n -(CH 2 ) m -(Y) q -, X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH 2 may be individually substituted with -O-, -NH(CO)-, or -(CO)-NH-; L 2 is -(CH 2 ) p -, p is an integer from 0 to 30, and each CH 2 may be individually substituted with -O-, -NH(CO)-, or -(CO)-NH-; and R 2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have appropriate blood circulation time, high uptake in tumors and long retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of PSMA.
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3.发明公开
公开(公告)号：EP4227300A1
公开(公告)日：2023-08-16
申请号：EP21925385.3
申请日：2021-07-11
发明人： CHEN, Xiaoyuan , XU, Pengfei , GUO, Zhide , WU, Xiaoming , YANG, Qingbao , HE, Tian
IPC分类号： C07D401/14 , A61K31/4709 , A61P35/00 , A61K31/555 , A61K51/08 , A61K51/04 , A61K47/54 , A61K47/62 , A61K103/00 , A61K103/30 , A61K103/32
摘要： The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L 1 , L 2 , L 3 , L 4 and X. The compound has the following structure shown in Formula (I), where R 1 is a fibroblast activation protein inhibitor; L 1 is lysine, glutamic acid, or a derivative structure thereof; L 2 is -(CH 2 ) n -, n is an integer from 0 to 30, and each -CH 2 - may be individually substituted or unsubstituted with -O-, -NH-, -(CO)-, -NH(CO)-, or -(CO)-NH-; L 3 is -(CH 2 ) m -, m is an integer from 0 to 30, and each -CH 2 - may be individually substituted or unsubstituted with -O- or -(CO)-; L 4 is -(CH 2 ) p -, p is an integer from 0 to 30, and each -CH 2 - may be individually substituted or unsubstituted with -O-, -NH-, -(CO)-, -NH(CO)-, or -(CO)-NH-; X is selected from N, C, O, S, or
and R 2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-life in blood circulation, improving the uptake and enrichment in tumors and prolonging the retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of FAP.
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