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Last Updated: October 22, 2019

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Claims for Patent: 9,278,995

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Summary for Patent: 9,278,995
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:13/769,744
Patent Claims: 1. A compound comprising a peptide and a conjugating group, wherein the peptide comprises an amino acid sequence having the formula X.sub.1-X.sub.2-X.sub.3-X.sub.4-X.sub.5-X.sub.6-X.sub.7 wherein X.sub.1 is D-cysteine; X.sub.2 is an amino acid selected from the group consisting of D-arginine and D-alanine; X.sub.3 is D-arginine; X.sub.4 is an amino acid selected from the group consisting of D-arginine and D-alanine; X.sub.5 is D-arginine; X.sub.6 is a non-cationic amino acid; X.sub.7 is D-arginine; wherein when X.sub.2 is D-arginine, X.sub.4 is D-alanine and when X.sub.2 is D-alanine, X.sub.4 is D-arqinine; and wherein the peptide X.sub.1 residue is linked to the conjugating group by a disulfide bond.

2. The compound of claim 1, wherein the N-terminus of the peptide is acetylated.

3. The compound of claim 2, wherein the C-terminus of the peptide is amidated.

4. The compound of claim 1, wherein the C-terminus of the peptide is amidated.

5. The compound of claim 1, wherein the conjugating group is acetylated.

6. The compound of claim 5, wherein the conjugating group is cysteine.

7. The compound of claim 1, wherein the compound is a homodimer.

8. The compound of claim 1, wherein the peptide is 8 to 15 amino acid residues in length.

9. The compound of claim 8, wherein the peptide is 8 to 11 amino acid residues in length.

10. The compound of claim 9, wherein the peptide is 8 to 9 amino acid residues in length.

11. The compound of claim 1, wherein the peptide consists of the amino acid sequence having the formula: X.sub.1-X.sub.2-X.sub.3-X.sub.4-X.sub.5-X.sub.6-X .sub.7.

12. The compound of claim 1, wherein the conjugating group is cysteine.

13. The compound of claim 12, wherein the conjugating group is L-cysteine.

14. The compound of claim 13, wherein the L-cysteine is acetylated.

15. The compound of claim 12, wherein the conjugating group is D-cysteine.

16. The compound of claim 15, wherein the D-cysteine is acetylated.

17. The compound of claim 1, wherein the conjugating group is selected from the group consisting of cysteine, homocysteine, glutathione, pegylated cysteine and a thiol-containing polypeptide.

18. The compound of claim 17, wherein the compound is a homodimer.

19. The compound of claim 17, wherein X.sub.2 is D-arginine and X.sub.4 is D-alanine.

20. The compound of claim 19, wherein the compound is a homodimer.

21. The compound of claim 19, wherein the conjugating group is cysteine.

22. The compound of claim 21, wherein the conjugating group is acetylated.

23. The compound of claim 19, wherein the N-terminus of the peptide is acetylated.

24. The compound of claim 23, wherein the C-terminus of the peptide is amidated.

25. The compound of claim 19, wherein the conjugating group is L-cysteine.

26. The compound of claim 25, wherein the conjugating group is acetylated.

27. The compound of claim 19, wherein the conjugating group is D-cysteine.

28. The compound of claim 27, wherein the conjugating group is acetylated.

29. The compound of claim 17, wherein X.sub.4 is D-arginine and X.sub.2 is D-alanine.

30. The compound of claim 29, wherein the conjugating group is cysteine.

31. The compound of claim 30, wherein the conjugating group is acetylated.

32. The compound of claim 29, wherein the N-terminus of the peptide is acetylated.

33. The compound of claim 32, wherein the C-terminus of the peptide is amidated.

34. The compound of claim 29, wherein the compound is a homodimer.

35. The compound of claim 17, wherein the conjugating group is cysteine.

36. The compound of claim 35, wherein the conjugating group is acetylated.

37. A compound comprising Ac-c(C)rrarar-NH.sub.2 (SEQ ID NO:28).

38. A compound comprising Ac-c(C)rrarar-NH.sub.2 (SEQ ID NO:28), wherein the C is acetylated.

39. A compound comprising ##STR00012##

40. A compound comprising Ac-c(C)arrrar-NH.sub.2 (SEQ ID NO:3), wherein the C is acetylated.

41. A compound comprising ##STR00013##

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