17-02-2022 дата публикации
Номер: US20220047725A1
Принадлежит:
The present invention provides dioxetane-based chemiluminescence probes, more specifically fluorophore-tethered dioxetane-based chemiluminescence probes and compositions thereof. The chemiluminescence probes disclosed are useful for both diagnostics and in vivo imaging. 3. The conjugate of claim 2 , wherein Rand Rtogether with the carbon atom to which they are attached form adamantyl.4. The conjugate of claim 2 , wherein Xis —(CH)-para-phenylene; and Xis —C(O)—.5. The conjugate of claim 1 , wherein:{'sup': '1', 'sub': 1', '8, 'Ris a linear or branched (C-C)alkyl;'}{'sup': 2', '3, 'Rand Rtogether with the carbon atom to which they are attached form a fused, spiro or bridged polycyclic ring;'}{'sup': 7', '8', '9', '7', '8', '9, 'sub': '2', 'at least one of R, Rand Ris H, and the other of R, Rand Reach independently is an electron acceptor group selected from the group consisting of halogen, —NOand —CN; and'}{'sub': 1', '2', '1', '1', '18', '6', '14', '1', '18', '6', '14', '2', '2', '2', '2', '2', '3', '6', '10', '1', '4', '6', '10', '1', '4', '1', '18', '1', '8', '6', '10', '6', '10', '2, 'X is a linker of the formula —X—X—, wherein Xis (C-C)alkylene, (C-C)arylene-diyl, or (C-C)alkylene-(C-C)arylene-diyl, optionally substituted by one or more groups each independently selected from the group consisting of halogen, —COH, —COOH, —OCOOH, —OCONH, —CN, —NO, —SH, —OH, —NH, —CONH, —SOH, —SOH, —S(═O)H, (C-C)aryl, (C-C)alkylene-(C-C)aryl, heteroaryl, and (C-C)alkylene-heteroaryl, and said (C-C)alkylene being further optionally interrupted by one or more identical or different heteroatoms selected from the group consisting of S, O and N, and/or at least one group each independently selected from the group consisting of —NH—CO—, —CO—NH—, —N(C-Calkyl)-, —N(C-Caryl)-, (C-C)arylene-diyl, and heteroarylenediyl; and Xis —C(O)—.'}6. The conjugate of claim 5 , wherein Ris methyl; Rand Rtogether with the carbon atom to which they are attached form adamantly; Xis —(CH)-para-phenylene; ...
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