US 12,433,883 B2
Covalent modification and controlled delivery of mu opioid receptor antagonists
Saadyah Averick, Pittsburgh, PA (US); and Andrew Kassick, Wexford, PA (US)
Assigned to Allegheny Singer Research Institute, Pittsburgh, PA (US)
Appl. No. 17/598,691
Filed by Allegheny Singer Research Institute, Pittsburgh, PA (US)
PCT Filed Mar. 27, 2020, PCT No. PCT/US2020/025266
§ 371(c)(1), (2) Date Sep. 27, 2021,
PCT Pub. No. WO2020/205537, PCT Pub. Date Oct. 8, 2020.
Claims priority of provisional application 62/826,438, filed on Mar. 29, 2019.
Prior Publication US 2022/0152017 A1, May 19, 2022
Int. Cl. A61K 31/485 (2006.01); A61K 47/69 (2017.01); A61P 25/36 (2006.01)
CPC A61K 31/485 (2013.01) [A61K 47/6937 (2017.08); A61P 25/36 (2018.01)] 24 Claims
 
1. A polymer conjugate comprising: a hydrophobic biodegradable polymer covalently attached to a mu opioid receptor (MOR) antagonist through a linkage consisting of an ester, wherein the ester is prepared from a phenolic hydroxy of the MOR antagonist by ring-opening polymerization, wherein the MOR antagonist is selected from the group consisting of naloxone, naltrexone, and nalmefene, and wherein the polymer consists of polylactic acid.