发明名称 Optical sensor conjugates for detecting reactive oxygen and/or reactive nitrogen species in vivo
摘要 The present invention provides methods and compositions based on optical sensor conjugates that are useful for detecting reactive oxygen, reactive nitrogen, or both species that are a direct result of inflammation caused by tissue damage.
申请公布号 US9636423(B2) 申请公布日期 2017.05.02
申请号 US201113700255 申请日期 2011.06.02
申请人 The General Hospital Corporation 发明人 Hilderbrand Scott A.;Weissleder Ralph;Panizzi Peter;McCarthy Jason R.
分类号 A61K49/00 主分类号 A61K49/00
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A method of imaging reactive oxygen species, reactive nitrogen species, or both in a subject, the method comprising: administering to the subject an optical sensor conjugate comprising a fluorogenic small molecule, a particle or polymer, and a linker that connects the small molecule to the particle or polymer, for a time sufficient for the small molecule to react with the reactive oxygen or reactive nitrogen, or both, thereby releasing the small molecule from the optical sensor conjugate and becoming fluorescent; and obtaining a fluorescence image of the small molecule in the subject, thereby imaging the subject, wherein the small molecule with the linker comprises a compound of Formula I:wherein: Z is the linker and comprises C3-20 alkyl, wherein any of the carbons in C3-20 alkyl can be replaced with —C(O)—, C(O)O—, —C(O)NRA—, —C(NH)—, oxygen, sulfur, —SO2—, —NRASO2— —NRA—; X is selected from  N3, C(O)Cl, and C(O)ORA; Y is selected from O, S, Se, Te, N(RA), and C(Me)2; R1 is selected from H, C1-6 alkyl, ORA, and NRCRD, wherein said C1-6 alkyl is optionally substituted by ORA or NRCRD; or 2 or 3 R1 adjacent to each other and together with the C atoms to which they are attached form 1or 2 heterocycloalkyl, optionally substituted by 1, 2, 3, or 4 substituents independently selected from H, OH, C1-6 alkyl, ORA, C(O)RB, C(O)NRCRD, and C(O)ORA; RA, RB, RC and RD are independently selected from H, C1-6 alkyl, and succinimidyl; and m is 1, 2, 3, or 4.
地址 Boston MA US
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