Claims for Patent: 10,793,596

Summary for Patent: 10,793,596

Title:	Synthetic peptide amides
Abstract:	The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P.sub.450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: ##STR00001## These compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.
Inventor(s):	Schteingart; Claudio D. (San Diego, CA), Menzaghi; Frederique (Rye, NY), Jiang; Guangcheng (San Diego, CA), Alexander; Roberta Vezza (San Diego, CA), Sueiras-Diaz; Javier (La Jolla, CA), Spencer; Robert H. (New Hope, PA), Chalmers; Derek T. (Riverside, CT), Luo; Robert Zhiyong (New City, NY)
Assignee:	Cara Therapeutics, Inc. (Stamford, CT)
Application Number:	16/199,308
Patent Claims:	1. A synthetic peptide amide having the formula: ##STR00049## D-Phe-D-Phe-D-Leu-D-Lys-[.omega.(4-aminopiperidine-4-carboxylic acid)]-OH or a pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof. 2. The synthetic peptide amide or pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof according to claim 1, wherein the pharmaceutically acceptable salt or acid salt hydrate comprises HCl. 3. The synthetic peptide amide or pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof according to claim 1, wherein the pharmaceutically acceptable salt or acid salt hydrate comprises acetic acid. 4. The synthetic peptide amide or pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof according to claim 1, which is a solid composition. 5. The synthetic peptide amide or pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof according to claim 4, herein the solid composition is a lyophilized solid composition. 6. A pharmaceutical composition comprising the synthetic peptide amide having the formula: ##STR00050## D-Phe-D-Phe-D-Leu-D-Lys-[.omega.(4-aminopiperidine-4-carboxylic acid)]-OH or a pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof and a pharmaceutically acceptable excipient or carrier. 7. The pharmaceutical composition according to claim 6, wherein the pharmaceutical composition comprising the pharmaceutically acceptable excipient or carrier is an aqueous solution. 8. The pharmaceutical composition aqueous solution according to claim 7, wherein the aqueous solution is an isotonic solution. 9. The pharmaceutical composition which is an aqueous solution according to claim 7, wherein the aqueous solution is a buffered solution. 10. A method for the treatment of a kappa opioid receptor-associated disease or condition in a patient, wherein the kappa opioid receptor-associated disease or condition is pruritus, the method comprising administering to the patient a composition comprising an effective amount of a synthetic peptide amide having the formula: ##STR00051## D-Phe-D-Phe-D-Leu-D-Lys-[.omega.(4-aminopiperidine-4-carboxylic acid)]-OH or a pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof. 11. The method according to claim 10, wherein the pruritus is associated with chronic kidney disease. 12. The method according to claim 11, wherein the pruritus is associated with chronic kidney disease in a patient undergoing hemodialysis. 13. The method according to claim 11, wherein the chronic kidney disease is end-stage renal disease. 14. The method according to claim 10, wherein the pruritus is associated with a disease or condition selected from the group consisting of primary biliary cholangitis, primary biliary cirrhosis and chronic cholestatic liver disease. 15. The method according to claim 14, wherein the pruritus is associated chronic cholestatic liver disease. 16. The method according to claim 10, wherein the pruritus is associated with atopic dermatitis. 17. The method according to claim 10, wherein the pruritus is associated with contact dermatitis. 18. The method according to claim 10, wherein the pruritus is associated with psoriasis.