Claims for Patent: 10,501,518
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Summary for Patent: 10,501,518
Title: | Alpha-/beta-polypeptide analogs of parathyroid hormone (PTH) and method of using same |
Abstract: | Described are polypeptide analogs of parathyroid hormone (PTH) that include at least two non-adjacent .beta.-amino acid residues in place of a naturally occurring .alpha.-amino acid residues. Also described are pharmaceutical compositions useful for treating hypoparathyroidism that contain the analogs and methods of using the analogs to treat hypoparathyroidism. |
Inventor(s): | Gellman; Samuel H. (Madison, WI), Cheloha; Ross W. (Madison, WI), Gardella; Thomas J. (Needham, MA) |
Assignee: | Wisconsin Alumni Research Foundation (Madison, WI) General Hospital Corporation (Boston, MA) |
Application Number: | 14/312,012 |
Patent Litigation and PTAB cases: | See patent lawsuits and PTAB cases for patent 10,501,518 |
Patent Claims: | 1. An isolated, unnatural peptide analog comprising: PTH, a parathyroid hormone receptor (PTHR-1, PTHR-2) agonist- or inverse agonist effective fragment of PTH, a
parathyroid hormone related protein (PTHrP), a PTHR-1 or PTHR-2 agonist-, or inverse agonist-effective fragment of PTHrP, M-PTH, a PTHR-1 or PTHR-2 agonist- or inverse agonist-effective fragment of M-PTH, BA058, or a PTHR-1 or PTHR-2 agonist-, or inverse
agonist-effective fragment of BA058, in which at least five non-adjacent .alpha.-amino acid residues are replaced with .beta.-amino acid residues; and salts thereof.
2. The peptide analog of claim 1, in which the at least five .alpha.-amino acid residues are replaced with five .beta.-amino acid residues having the same side-chain as the .alpha.-amino acid residues they replace. 3. The peptide analog of claim 1, in which at least one of the at least five non-adjacent .alpha.-amino acid residues is replaced with a cyclically constrained .beta.-amino acid residue. 4. The peptide analog of claim 1, in which the at least five .beta.-amino acid residues appear in a pattern comprising .alpha..beta..alpha..beta..alpha..beta..alpha..beta..alpha..beta., .alpha..alpha..beta..alpha..alpha..beta..alpha..alpha..beta..alpha..alpha- ..beta..alpha..alpha..beta., .alpha..alpha..alpha..beta..alpha..alpha..alpha..beta..alpha..alpha..alph- a..beta..alpha..alpha..alpha..beta..alpha..alpha..alpha..beta., and .alpha..alpha..beta..alpha..alpha..alpha..beta..alpha..alpha..beta..alpha- ..alpha..alpha..beta..alpha..alpha..beta.. 5. The peptide analog of claim 1, comprising thirty four (34) N-terminal residues of a mammalian parathyroid hormone, PTH(1-34), in which at least five non-adjacent .alpha.-amino acid residues are replaced with a .beta.-amino acid residues. 6. The peptide analog of claim 5, in which the at least five .alpha.-amino acid residues are replaced with three .beta.-amino acid residues having the same side-chain as the .alpha.-amino acid residues they replace. 7. The peptide analog of claim 5, in which at least one of the at least five non-adjacent .alpha.-amino acid residues is replaced with a cyclically constrained .beta.-amino acid residue. 8. The peptide analog of claim 5, in which the at least three .beta.-amino acid residues appear in a pattern comprising .alpha..beta..alpha..beta..alpha..beta..alpha..beta..alpha..beta., .alpha..alpha..beta..alpha..alpha..beta..alpha..alpha..beta..alpha..alpha- ..beta..alpha..alpha..beta., .alpha..alpha..alpha..beta..alpha..alpha..alpha..beta..alpha..alpha..alph- a..beta..alpha..alpha..alpha..beta..alpha..alpha..alpha..beta., and .alpha..alpha..beta..alpha..alpha..alpha..beta..alpha..alpha..beta..alpha- ..alpha..alpha..beta..alpha..alpha..beta.. 9. The peptide analog of claim 1, selected from the group consisting of TABLE-US-00022 (SEQ. ID. NO: 5) A5: SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-NH.sub.2, (SEQ. ID. NO: 6) B5: SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVQNF-NH.sub.2, (SEQ. ID. NO: 7) C5: SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-NH.sub.2, (SEQ. ID. NO: 8) D5: SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-NH.sub.2, (SEQ. ID. NO: 9) D6: SVSEIQLMHNLGKWLNSMERVEWLRKKLQDVHNF-NH.sub.2, and (SEQ. ID. NO: 10) D7: SVSEIQLMHNLGKWLNSMERVEWLRKKLQDVHNF-NH.sub.2 wherein bold, underlined residues designate .beta.3 residues having a side chain of the .alpha. residue indicated by the letter, and salts thereof. 10. The peptide analog of claim 1, which is an agonist of parathyroid hormone receptor-1. 11. A pharmaceutical composition for treating hypoparathyroidism, the composition comprising a parathyroid hormone receptor agonist-effective amount of PTH, a parathyroid hormone receptor (PTHR-1, PTHR-2) agonist-effective fragment of PTH, a parathyroid hormone related protein (PTHrP), a PTHR-1 or PTHR-2 agonist-effective fragment of PTHrP, M-PTH, a PTHR-1 or PTHR-2 agonist-effective fragment of M-PTH, BA058, or a PTHR-1 or PTHR-2 agonist-effective fragment of BA058, in which at least five non-adjacent .alpha.-amino acid residues are replaced with .beta.-amino acid residues, in combination with a pharmaceutically suitable carrier. 12. A method of treating hypoparathyroidism in a mammalian subject, including a human subject, the method comprising administering to the subject a parathyroid hormone receptor agonist-effective amount of a pharmaceutical composition as recited in claim 11. |
Details for Patent 10,501,518
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Nps Pharmaceuticals, Inc. | NATPARA | parathyroid hormone | For Injection | 125511 | 01/23/2015 | ⤷ Try a Trial | 2033-06-23 |
>Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
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