IP Library › Granted Patent US 11,279,729
Granted Patent B2
US 11,279,729 · App. 17/350,888 · Granted Mar 22, 2022

Heterodimer compositions and methods for the treatment of ocular disorders

Inventors: Ian Charles Parrag (Mississauga, 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
C07J7/008A61K9/0024
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Quick Facts
Patent No.
US 11,279,729
App. No.
17/350,888
Granted
Mar 22, 2022
Kind
B2
Abstract

Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.

Claims (22)

1. A compound of a structure represented by Formula (VI-C):

or a pharmaceutically acceptable salt thereof,

wherein,

L is a linker; and

PG is a prostaglandin radical.

2. The compound of claim 1 , wherein PG is represented by a structure of Formula (IIA):

wherein:

is a single bond or a double bond;

R 1 and R 3 are OH;

R 2 is hydrogen;

R 4 is alkyl substituted with oxo, —C(═O)OC 1 -C 3 alkyl, —COOH, —CONH 2 , or —CONHC 1 -C 3 alkyl;

R 5 is —O-aryl or arylalkyl; and

R 6 and R 6′ are each independently hydrogen, halogen, or OH.

3. The compound of claim 1 , wherein L is a bond.

4. The compound of claim 1 , wherein L comprises one or more linker group, each linker group being independently selected from the group consisting of alkyl, cycloalkyl, heteroalkyl, and alkoxy, wherein the alkyl, cycloalkyl, heteroalkyl, or alkoxy is optionally substituted.

5. The compound of claim 1 , of the structure:

6. The compound of claim 1 , of the structure:

7. The compound of claim 1 , of the structure:

8. The compound of claim 1 , of the structure:

9. The compound of claim 1 , of the structure:

10. The compound of claim 1 , having of the structure:

11. A pharmaceutical implant comprising at least 50 wt. % of the compound of claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2021
From: PARRAG, IAN CHARLES; NAIMARK, WENDY ALISON; STATHAM, MATTHEW ALEXANDER JOHN; RIZIS, GEORGIOS; BATTISTON, KYLE GIOVANNI
To: RIPPLE THERAPEUTICS CORPORATION
Reel/Frame 056823/0866 →
Continuity (3)
Continuation PCTIB2021000332 · Apr 29, 2021
Provisional Application 63019182 · May 1, 2020
Related Publication 20210347809A1 · Nov 11, 2021
Cited By (1)
US 12,509,469