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US 12,214,020 B2Granted
PTH prodrugs
AssigneeAscendis Pharma Bone Diseases A/S
InventorsKennett Sprogøe, Felix Cleemann, Guillaume Maitro, Mathias Krusch, Thomas Wegge, Joachim Zettler
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Abstract
The present invention relates to PTH prodrugs, pharmaceutical compositions comprising such PTH prodrugs and their uses.
Claims9
A method of treating a patient having hypoparathyroidism comprising administering to the patient a therapeutically effective amount of a compound according to formula 31
- or a pharmaceutically acceptable salt thereof, thereby treating hypoparathyroidism in the patient,
- wherein PTH(1-34) is parathyroid hormone of the amino acid sequence SEQ ID NO:51, NαS1 is the alpha amino group of the N-terminal serine of SEQ ID NO:51 and 2×10 kDa PEG comprises a branched polyethylene glycol polymer of two arms in which each arm has a molecular weight of about 10 kDa and is a moiety of formula (b)
- wherein the dashed line indicates attachment to —S— in compound 31, and each of m and p of each moiety is independently an integer.
A method of parathyroid hormone replacement therapy, comprising administering a compound according to formula 31:
- or a pharmaceutically acceptable salt thereof to a patient in need of the therapy, thereby alleviating symptoms relating to hypocalcemia, hypercalciuria, and hyperphosphatemia, without causing hypercalcemia,
- wherein PTH(1-34) is parathyroid hormone of the amino acid sequence SEQ ID NO:51, Nαs1 is the alpha amino group of the N-terminal serine of SEQ ID NO:51 and 2×10 kDa PEG comprises a branched polyethylene glycol polymer of two arms in which each arm has a molecular weight of about 10 kDa and is a moiety of formula (b)
- wherein the dashed line indicates attachment to —S— in compound 31, and each of m and p of each moiety is independently an integer.
Dependencies are inferred from the claim text.