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Last Updated: October 22, 2019

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Claims for Patent: 8,999,932

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Summary for Patent: 8,999,932
Title:Therapeutic agents for reducing parathyroid hormone levels
Abstract: Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X.sub.1-X.sub.2-X.sub.3-X.sub.4-X.sub.5-X.sub.6-X.sub.7, wherein the X.sub.1 subunit comprises a thiol-containing moiety and the distribution of charge on the X.sub.2-X.sub.7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
Inventor(s): Karim; Felix (Walnut Creek, CA), Baruch; Amos (San Francisco, CA), Maclean; Derek (Los Altos, CA), Das; Kanad (San Francisco, CA), Yin; Qun (Palo Alto, CA)
Assignee: KAI Pharmaceuticals, Inc. (South San Francisco, CA)
Application Number:12/846,724
Patent Claims: 1. A conjugate, comprising a peptide and a conjugating group, wherein the peptide comprises the amino acid sequence carrrar (SEQ ID NO:2), and wherein the peptide is linked to the conjugating group by a disulfide bond.

2. The conjugate of claim 1, wherein the peptide is chemically modified at the N-terminus, the C-terminus, or both.

3. The conjugate of claim 1, wherein the N-terminus of the peptide is chemically modified by acetylation and the C-terminus of the peptide is chemically modified by amidation.

4. The conjugate of claim 1, wherein the conjugating group is L-Cys.

5. The conjugate of claim 1, wherein the conjugating group is D-Cys.

6. A pharmaceutical composition comprising the conjugate according to claim 1 and a pharmaceutically acceptable excipient.

7. The pharmaceutical composition of claim 6, wherein the conjugating group is L-Cys.

8. The pharmaceutical composition of claim 6, wherein the conjugating group is D-Cys.

9. The pharmaceutical composition of claim 6, wherein the peptide is chemically modified at the N-terminus, the C-terminus, or both.

10. The pharmaceutical composition of claim 6, wherein the N-terminus of the peptide is chemically modified by acetylation and the C-terminus of the peptide is chemically modified by amidation.

11. A method of treating secondary hyperparathyroidism (SHPT) in a subject, comprising administering to the subject a therapeutically effective amount of a conjugate comprising a peptide and a conjugating group, wherein the peptide comprises the amino acid sequence carrrar (SEQ ID NO:2), and wherein the peptide is linked to the conjugating group by a disulfide bond.

12. The method of claim 11, wherein said administering comprises administering intravenously.

13. The method of claim 11, wherein said administering comprises administering transdermally.

14. The method of claim 11, wherein the conjugating group is L-Cys.

15. The method of claim 11, wherein the conjugating group is D-Cys.

16. The method of claim 11, wherein the peptide is chemically modified at the N-terminus, the C-terminus, or both.

17. The method of claim 11, wherein the N-terminus of the peptide is chemically modified by acetylation and the C-terminus of the peptide is chemically modified by amidation.

18. A method of decreasing parathyroid hormone levels in a subject, comprising administering to the subject an amount of a conjugate comprising a peptide and a conjugating group, wherein the peptide comprises the amino acid sequence carrrar (SEQ ID NO:2), and wherein the peptide is linked to the conjugating group by a disulfide bond.

19. The method of claim 18, wherein said administering comprises administering intravenously.

20. The method of claim 18, wherein said administering comprises administering transdermally.

21. The method of claim 18, wherein the conjugating group is L-Cys.

22. The method of claim 18, wherein the conjugating group is O-Cys.

23. The method of claim 18, wherein the peptide is chemically modified at the N-terminus, the C-terminus, or both.

24. The method of claim 18, wherein the N-terminus of the peptide is chemically modified by acetylation and the C-terminus of the peptide is chemically modified by amidation.

25. A method for treating a subject, comprising administering to the subject (i) a conjugate comprising a peptide and a conjugating group, wherein the peptide comprises the amino acid sequence carrrar (SEQ ID NO:2), and wherein the peptide is linked to the conjugating group by a disulfide bond and (ii) a second therapeutic agent.

26. The method of claim 25, wherein the second therapeutic agent is vitamin D, a vitamin D analog or cinacalcet hydrochloride.

27. The method of claim 25, wherein the conjugating group is L-Cys.

28. The method of claim 25, wherein the conjugating group is D-Cys.

29. The method of claim 25, wherein the peptide is chemically modified at the N-terminus, the C-terminus, or both.

30. The method of claim 25, wherein the N-terminus of the peptide is chemically modified by acetylation and the C-terminus of the peptide is chemically modified by amidation.

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