IP Library › Granted Patent US 12,473,326
Granted Patent B2
US 12,473,326 · App. 17/426,779 · Granted Nov 18, 2025

Crystalline forms of dexamethasone dimers and uses thereof

Inventors: Ian Charles Parrag (Mississauga, CA); Matthew Alexander John Statham (Milton, CA); Emma-Louise Elizabeth Moore (Mississauga, CA); Bahareh Khalili (Mississauga, CA); Judith Anne Williams (Toronto, CA); Elizabeth Poloz (Kitchener, CA); Boris Gorin (Oakville, CA)
Assignee: Ripple Therapeutics Corporation
C07J5/0076A61K8/00A61P19/02B29C35/02B29C49/0006B29K2105/0035C07B2200/13
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Quick Facts
Patent No.
US 12,473,326
App. No.
17/426,779
Granted
Nov 18, 2025
Kind
B2
Abstract

The disclosure features polymorphs of a prodrug dimer of dexamethasone linked at the 21-C and 21′-C carbons via a carbonate-triethylene glycol-carbonate linker. Also disclosed are pharmaceutical compositions and articles comprising said polymorphs, and the use thereof in the treatment of a disease or condition, e.g. via the extended or controlled release of dexamethasone from said articles.

Claims (15)

1 . A solid crystalline form of a compound represented by the following formula:

the solid crystalline form being characterized by an X-ray powder diffraction (XRPD) pattern comprising peaks at: 3.8°±0.2° 2θ, 7.6°±0.2° 2θ, 8.8°±0.2° 2θ, 9.72±0.2° 2θ, and 12.2°±0.2° 2θ.

2 . The solid crystalline form of claim 1 , wherein the XRPD pattern is further characterized by peaks at: 10.6°±0.2° 2θ, 13.4°±0.2° 2θ, and 14.6°±0.2° 2θ.

3 . A solid crystalline form of a compound represented by the following formula:

the solid crystalline form being characterized by an X-ray powder diffraction (XRPD) pattern comprising peaks at: 3.9°±0.2° 2θ, 7.9°±0.2° 2θ, 9.7°±0.2° 2θ, 12.0°±0.2° 2θ, and 15.9°±0.2° 2θ.

4 . The solid crystalline form of claim 3 , wherein the XRPD pattern is further characterized by peaks at: 4.8°±0.2° 2θ, 5.7°±0.2° 2θ, 6.7°±0.2° 2θ, 8.7°±0.2° 2θ, 13.5°±0.2° 2θ, 14.6°±0.2° 2θ, and 17.3°±0.2° 2θ.

5 . A solid crystalline form of a compound represented by the following formula:

the solid crystalline form being characterized by an X-ray powder diffraction XRPD pattern comprising peaks at: 8.9°±0.2° 2θ, 11.4°±0.2° 2θ, 14.1°±0.2° 2θ, 16.4°±0.2° 2θ, and 17.1°±0.2° 2θ.

6 . The solid crystalline form of claim 5 , wherein the XRPD pattern is further characterized by peaks at: 7.0°±0.2° 2θ, 17.9°±0.2° 2θ, 19.1°±0.2° 2θ, 19.8°±0.2° 2θ, and 20.3°±0.2° 2θ.

7 . An article comprising the solid crystalline form of claim 1 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

8 . An article comprising the solid crystalline form of claim 2 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

9 . An article comprising the solid crystalline form of claim 3 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

10 . An article comprising the solid crystalline form of claim 4 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

11 . An article comprising the solid crystalline form of claim 5 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

12 . An article comprising the solid crystalline form of claim 6 , wherein at least 70% weight by weight (w/w) of the article is Compound 1.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2021
From: KHALILI, BAHAREH; WILLIAMS, JUDITH ANNE; POLOZ, ELIZABETH; GORIN, BORIS
To: EUROFINS CDMO ALPHORA INC.
Reel/Frame 057027/0509 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2021
From: PARRAG, IAN CHARLES; STATHAM, MATTHEW ALEXANDER JOHN; MOORE, EMMA-LOUISE ELIZABETH
To: INTERFACE BIOLOGICS, INC.
Reel/Frame 057027/0548 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2021
From: EUROFINS CDMO ALPHORA INC.
To: INTERFACE BIOLOGICS, INC.
Reel/Frame 057027/0579 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2021
From: INTERFACE BIOLOGICS, INC.
To: RIPPLE THERAPEUTICS CORPORATION
Reel/Frame 057027/0615 →
Continuity (3)
Continuation In Part PCTCA2019050136 · Feb 1, 2019
Provisional Application 62883170 · Aug 6, 2019
Related Publication 20220089635A1 · Mar 24, 2022
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