Pan-selectin inhibitor with enhanced pharmacokinetic activity
US-2015051164-A1 · Feb 19, 2015 · US
US9109002B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9109002-B2 |
| Application number | US-201214367561-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 21, 2012 |
| Priority date | Dec 22, 2011 |
| Publication date | Aug 18, 2015 |
| Grant date | Aug 18, 2015 |
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Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
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We claim the following: 1. A compound having the formula (I): or a pharmaceutically acceptable salt, isomer, tautomer, hydrate or solvate thereof, wherein: R 1 is C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, C 1 -C 8 haloalkyl, C 2 -C 8 haloalkenyl or C 2 -C 8 haloalkynyl; R 2 is a linker-non-glycomimetic moiety, wherein the non-glycomimetic moiety compr…
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