US 11,986,509 B2
Oligosaccharide formulations of kappa opioid receptor agonists
Bryan R. Wilson, Brewster, NY (US); and Stephen J. O'Connor, Guilford, CT (US)
Assigned to Cara Therapeutics, Inc., Stamford, CT (US)
Filed by CARA THERAPEUTICS, INC., Stamford, CT (US)
Filed on Mar. 18, 2021, as Appl. No. 17/204,986.
Claims priority of provisional application 62/991,560, filed on Mar. 18, 2020.
Prior Publication US 2021/0290723 A1, Sep. 23, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/07 (2006.01); A61K 9/16 (2006.01); A61K 9/48 (2006.01); A61K 9/50 (2006.01); A61K 31/40 (2006.01); A61K 31/485 (2006.01)
CPC A61K 38/07 (2013.01) [A61K 9/1617 (2013.01); A61K 9/1623 (2013.01); A61K 9/1694 (2013.01); A61K 9/4808 (2013.01); A61K 9/5089 (2013.01); A61K 31/40 (2013.01); A61K 31/485 (2013.01)] 11 Claims
 
1. A formulation for oral delivery of a kappa opioid receptor agonist, the formulation comprising,
particles including a kappa opioid receptor agonist and an oligosaccharide, wherein the kappa opioid receptor agonist is CR845 having the formula:

OG Complex Work Unit Chemistry
D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopiperidine-4-carboxylic acid)]-OH or a hydrate, salt, acid salt or acid salt hydrate thereof;
wherein the oligosaccharide is trehalose and wherein the CR845 is stable for at least a year at 25° C.