CPC A61K 47/548 (2017.08) [A61K 31/192 (2013.01); A61K 31/704 (2013.01); A61K 47/545 (2017.08); A61K 47/60 (2017.08); A61K 47/6803 (2017.08); A61K 47/6849 (2017.08); A61K 47/6851 (2017.08); A61K 47/6855 (2017.08)] | 18 Claims |
1. A composition comprising a pharmaceutically acceptable carrier and a compound having the following structure (I):
![]() or a stereoisomer, pharmaceutically acceptable salt or tautomer thereof, wherein:
M is, at each occurrence, independently a biologically active moiety selected from the group consisting of an NSAID, a kinase inhibitor, an anthracycline, an EGFR inhibitor, an alkylating agent and an anti-cancer drug or a fluorescent dye, provided at least one occurrence of M is not a fluorescent dye;
A is, at each occurrence, independently
![]() or a moiety comprising a fused aryl or heteroaryl ring system;
L is a physiologically cleavable linker cleavable at a pH ranging from 6 to 8, cleavable at a temperature ranging from 20° C. to 40° C., or cleavable by an enzyme;
L1, L2, L3 and L4 are, at each occurrence, independently absent or an alkylene, alkenylene, alkynylene, heteroalkylene, heteroalkenylene, heteroalkynylene or heteroatomic linker;
R1 is, at each occurrence, independently H, alkyl or alkoxy;
R2 and R3 are each independently H, OH, SH, alkyl, alkoxy, alkylether, —OP(═Ra)(Rb)Rc, Q or L′, wherein: Ra is O or S; Rb is OH, SH, O−, S−, ORd or SRd; Rc is OH, SH, O−, S−, ORd, SRd, OL′, alkyl, alkoxy, alkylether, alkoxyalkylether, phosphate, thiophosphate, phosphoalkyl, thiophosphoalkyl, phosphoalkylether or thiophosphoalkylether; and Rd is a counter ion;
R4 is, at each occurrence, independently OH, SH, O−, S−, ORd or SRd;
R5 is, at each occurrence, independently oxo, thioxo or absent;
Q is, at each occurrence, independently a moiety comprising a reactive group capable of forming a covalent bond with an analyte molecule, a solid support or a complementary reactive group Q′;
L′ is, at each occurrence, independently a linker covalently bonded to Q, a targeting moiety, a linker covalently bonded to a targeting moiety, a solid support or solid support residue, a linker covalently bonded to a solid support or solid support residue or a linker covalently bonded to a further compound of structure (I);
m is, at each occurrence, independently an integer of zero or greater, provided that at least one occurrence of m is an integer of one or greater; and
n is an integer of one or greater,
wherein the compound is present in the composition at a therapeutically effective amount for treating a disease or condition.
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