Claims for Patent: 9,701,712
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Summary for Patent: 9,701,712
|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)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 9,701,712|
1. A pharmaceutically acceptable salt of a peptide, wherein the peptide is 8 to 11 amino acids in length and comprises the amino acid sequence
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 L-cysteine or D-cysteine, X.sub.2 is D-alanine or D-arginine X.sub.3 is D-arginine, X.sub.4 is D-alanine or D-arginine X.sub.5 is D-arginine, X.sub.6 is D-alanine, and
X.sub.7 is D-arginine.
2. The salt of claim 1, wherein the N-terminus of the peptide is acetylated.
3. The salt of claim 1, wherein the C-terminus of the peptide is amidated.
4. The salt of claim 1, wherein the N-terminus of the peptide is acetylated and the C-terminus of the peptide is amidated.
5. The salt of claim 1, wherein X.sub.1 is conjugated to L-cysteine via a disulfide bond.
6. The salt of claim 1, wherein X.sub.1 is conjugated to D-cysteine via a disulfide bond.
7. The salt of claim 1, wherein the N-terminus of the peptide is acetylated.
8. A pharmaceutically acceptable salt of a peptide comprising Ac-c(C)arrrar-NH.sub.2 (SEQ ID NO:3).
9. The salt of claim 8, wherein the salt is an HCI salt.
10. A pharmaceutical composition comprising the salt of claim 8.
11. The salt of claim 1, wherein the salt is an HCI salt.
12. A method of treating secondary hyperparathyroiclism (SHPT) in a subject, comprising administering to the subject a therapeutically effective amount of the salt of claim 1.
13. The method of claim 12, wherein the subject is suffering from chronic kidney disease.
14. The method of claim 12, wherein the administering is intravenous.
15. A method of treating secondary hyperparathyroidism (SHPT) in a subject, comprising administering to the subject a therapeutically effective amount of the salt of claim 8.
16. The method of claim 15, wherein the subject is suffering from chronic kidney disease.
17. The method of claim 15, wherein the administering is intravenous.
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