IP Library › Granted Patent US 12,509,469
Granted Patent B2
US 12,509,469 · App. 17/633,072 · Granted Dec 30, 2025

Compositions and methods for the treatment of pain and dependence disorders

Inventors: Ian Charles Parrag (Toronto, CA); Wendy Alison Naimark (Toronto, CA); Matthew Alexander John Statham (Milton, CA); Georgios Rizis (Toronto, CA); Kyle Giovanni Battiston (Toronto, CA)
Assignee: Ripple Therapeutics Corporation
C07D489/02A61K9/0024A61K47/542A61K47/545A61K47/55A61K47/552C07D489/08
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Quick Facts
Patent No.
US 12,509,469
App. No.
17/633,072
Granted
Dec 30, 2025
Kind
B2
Abstract

Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders.

Claims (25)

1 . A compound having a structure represented by Formula (IID):

wherein:

R 1 and R 1 ′ are each independently unsaturated alkyl; or R 1 and R 1 ′ are each independently cycloalkyl;

R a and R a ′ are each independently H or —OH;

L d is selected from the group consisting of —(CR 2 ) y —, —O(CR 2 ) y O—, —O(CR 2 ) y —, —(CR 2 ) y O—, and —O(CH 2 CH 2 O) y —, wherein y is 1-10 and each R is independently selected from the group consisting of H, hydroxyl, halogen, alkyl, or is taken together with another R to form an optionally substituted cycloalkyl; and

X and X′ are each independently O or CH 2 , or

a pharmaceutically salt thereof.

2 . A compound having a structure represented by:

3 . The compound of claim 1 , wherein R 1 and R 1 ′ are each independently unsaturated alkyl.

4 . The compound of claim 1 , wherein R 1 and R 1 ′ are each independently cycloalkyl.

5 . The compound of claim 1 , wherein R a and R a ′ are each H.

6 . The compound of claim 1 , wherein R a and R a ′ are each —OH.

7 . The compound of claim 1 , wherein X and X′ are each O.

8 . The compound of claim 1 , wherein X and X′ are each CH 2 .

9 . The compound of claim 1 , wherein L d is —(CR 2 ) y — or —O(CR 2 ) y O—, wherein y is 1-10 and each R is independently selected from the group consisting of H, hydroxyl, halogen, alkyl, or is taken together with another R to form an optionally substituted cycloalkyl.

10 . A pharmaceutical implant or article comprising a compound having a structure represented by Formula (IID):

wherein:

R 1 and R 1 ′ are each independently unsaturated alkyl or cycloalkyl;

R a and R a ′ are each independently H or —OH;

L d is selected from the group consisting of —(CR 2 ) y —, —O(CR 2 ) y O—, —O(CR 2 ) y —, —(CR 2 ) y O—, and —O(CH 2 CH 2 O) y —, wherein y is 1-10 and each R is independently selected from the group consisting of H, hydroxyl, halogen, alkyl, or is taken together with another R to form an optionally substituted cycloalkyl; and

X and X′ are each independently O or CH 2 , or

a pharmaceutically salt thereof.

11 . The pharmaceutical implant or article of claim 10 , wherein the implant or article comprises at least 50 wt. % of the compound and/or pharmaceutically acceptable salt thereof.

12 . A pharmaceutical implant or article comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

13 . The pharmaceutical implant or article of claim 12 , wherein the implant or article comprises at least 50 wt. % of the compound and/or pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 28, 2022
From: PARRAG, IAN CHARLES; NAIMARK, WENDY ALISON; STATHAM, MATTHEW ALEXANDER JOHN; RIZIS, GEORGIOS; BATTISTON, KYLE GIOVANNI
To: RIPPLE THERAPEUTICS CORPORATION
Reel/Frame 059122/0221 →
Continuity (3)
Provisional Application 62883987 · Aug 7, 2019
Provisional Application 63019181 · May 1, 2020
Related Publication 20220274999A1 · Sep 1, 2022
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