Compositions for targeting macrophages and other CD206 high expressing cells and methods of treating and diagnosis
Inventors
Schlesinger, Larry • Bachelder, Eric • Cope, Frederick O.
Assignees
Cardinal Health 414 LLC • Navidea Biopharmaceuticals Inc • Ohio State Innovation Foundation
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Publication Number
US-10806803-B2
Publication Date
2020-10-20
Expiration Date
Abstract
Provided are compounds and compositions for targeting macrophages and other CD206 high expressing cells.
Core Innovation
The invention relates to compounds of Formula (II) having substituents defined by X being H, L1-A, or L2-R, with L1 and L2 linkers and A comprising one selected from a therapeutic agent, a detection label, or H. The compound further includes R comprising one selected from a CD206 targeting moiety or H, with n as an integer greater than zero, and at least one X being L1-A while at least one X is L2-R.
In the defined compounds, at least one L1-A includes a hydrazone, and at least one L2-R includes a —(CH2)pS(CH2)qNH— fragment, where p and q independently are integers from 0 to 5. This structural definition combines a CD206 targeting moiety with linker chemistries that include a hydrazone on the L1 side and the specified —(CH2)pS(CH2)qNH— moiety on the L2 side.
The partial content further describes a rationale for targeting macrophage-rich disease states using CD206 and tilmanocept, including in tuberculosis and autoimmune and cancer contexts. Documented embodiments include diagnostic imaging with detectable labels and in vivo imaging-guided cancer surgery, together with therapeutic conjugates such as tilmanocept-linker constructs associated with therapeutic agents for macrophage-associated conditions.
Claims Coverage
The relevant independent claim is clm-00001, which defines a compound of Formula (II) with two linker-bearing substituent types, one associated with A (therapeutic agent or detection label) and one associated with R (CD206 targeting moiety). The independent claim includes linkers with defined structural constraints, including hydrazone-containing L1 and an —(CH2)pS(CH2)qNH— fragment in L2 for p and q within specified integer ranges.
Formula (II) compound with two linker types
A compound of Formula (II) wherein each X is independently H, L1-A, or L2-R, linkers L1 and L2 are independently linkers, A comprises one selected from a therapeutic agent, a detection label, and H, R comprises one selected from a CD206 targeting moiety and H, and n is an integer greater than zero, wherein at least one X is L1-A and at least one X is L2-R.
Hydrazone-containing L1-A substituent requirement
At least one X is L1-A wherein L1 comprises a hydrazone.
—(CH2)pS(CH2)qNH L2-R linker fragment constraint
At least one X is L2-R wherein at least one L2 comprises —(CH2)pS(CH2)qNH—, wherein p and q independently are integers from 0 to 5.
Claim clm-00001 requires a Formula (II) compound that combines a therapeutic agent or detection label (as A) via an L1 linker containing a hydrazone and a CD206 targeting moiety (as R) via an L2 linker containing a —(CH2)pS(CH2)qNH— fragment with p and q constrained to integers from 0 to 5.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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