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US 2020/0369723 A1Published application
Llp2a-bisphosphonate conjugates for osteoporosis treatment
AssigneeThe Regents of the University of California
InventorsKit S. Lam, Ruiwu Liu, Wei Yao, Nancy Lane
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Abstract
The present invention provides compounds and pharmaceutical compositions of a peptidomimetic ligand, e.g. LLP2A, conjugated with a bisphosphonate drug, e.g. Alendronate. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of osteoporosis and for the promotion of bone growth due to their specificity for the α4β1 integrin on mesenchymal stem cells and for the surface of bone.
Claims20
A compound of Formula I:
- wherein
- each R1 and R2 is independently selected from the group consisting of H, halogen, C1-6 alkyl, C1-6 alkoxy, and C1-6 haloalkyl;
- R3 is selected from the group consisting of H, C1-6 alkyl and C3-8 cycloalkyl;
- X is selected from the group consisting of O, S and NH;
- Y is selected from the group consisting of O and NH;
- alternatively, le or le is combined with Y and the atoms to which they are attached to form a 5-membered heteroaryl ring;
- Z is a peptide having 3-20 independently selected amino acids, wherein at least one amino acid is selected from the group consisting of an unnatural amino acid and a D-amino acid;
- L is a linker;
- D is a bisphosphonate drug;
- subscripts m, n and q are each independently from 0 to 2;
- and salts and isomers thereof.
8 more elements
Dependencies are inferred from the claim text.