US 9,808,452 B2
Polysubunit opioid prodrugs resistant to overdose and abuse
Thomas E. Jenkins, Half Moon Bay, CA (US)
Assigned to Elysium Therapeutics, Inc., San Ramon, CA (US)
Filed by Elysium Therapeutics, Inc., San Ramon, CA (US)
Filed on Oct. 3, 2016, as Appl. No. 15/284,269.
Claims priority of provisional application 62/236,048, filed on Oct. 1, 2015.
Prior Publication US 2017/0100390 A1, Apr. 13, 2017
Int. Cl. A61K 31/485 (2006.01)
CPC A61K 31/485 (2013.01) 35 Claims
 
1. A compound represented by the structure of Formula (I):

OG Complex Work Unit Drawing
or a salt thereof, wherein:
Q is independently selected from optionally substituted heteroalkyl and optionally substituted alkyl;
L1 is independently at each occurrence absent or a cleavable or non-cleavable linker;
L2 is independently at each occurrence absent or a cleavable or non-cleavable linker;
R1 is independently selected at each occurrence from a GI enzyme substrate, a GI enzyme inhibitor, and an opioid antagonist;
R2 is an opioid agonist covalently bound to a GI enzyme substrate; and
m and n are independently selected at each occurrence from 1 to 1,000,000.