IP Library Granted Patent US 11,241,439
Granted Patent B2
US 11,241,439 · App. 16/800,979 · Granted Feb 8, 2022

Salts and solid forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and compositions comprising and methods of using the same

Inventors: Benjamin M. Cohen (Cranford, NJ); John F. Traverse (Lebanon, NJ); Jean Xu (Warren, NJ); Ying Li (Millburn, NJ)
Assignee: Celgene Corporation
A61K31/5377C07D401/04A61K31/4035A61K31/4412
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Quick Facts
Patent No.
US 11,241,439
App. No.
16/800,979
Granted
Feb 8, 2022
Kind
B2
Abstract

Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.

Claims (14)

1. A process for preparing Form A of HCl salt of Compound (I-S):

comprising slurrying a hydrate of HCl salt of Compound (I-S) in 2-propanol, wherein Form A of HCl salt of Compound (I-S) is characterized by an XRPD pattern comprising peaks at approximately 15.09, 15.94, and 22.30 degrees 2θ.

2. The process of claim 1 , wherein the hydrate of HCl salt of Compound (I-S) is Form D of HCl salt of Compound (I-S) characterized by an XRPD pattern comprising peaks at approximately 13.52, 14.16, and 25.00 degrees 2θ.

3. The process of claim 1 , wherein the hydrate of HCl salt of Compound (I-S) is Form E of HCl salt of Compound (I-S) characterized by an XRPD pattern comprising peaks at approximately 9.82, 17.06, and 17.73 degrees 2θ.

4. The process of claim 1 , wherein the hydrate of HCl salt of Compound (I-S) is Form F of HCl salt of Compound (I-S) characterized by an XRPD pattern comprising peaks at approximately 13.71, 14.22, and 20.87 degrees 2θ.

5. A process for preparing Form A of HCl salt of Compound (I-S):

comprising slurrying Form F of HCl salt of Compound (I-S) in a solvent, wherein the solvent is water, MeOAc saturated with water, or a mixture of 2-propanol and water, wherein Form A of HCl salt of Compound (I-S) is characterized by an XRPD pattern comprising peaks at approximately 15.09, 15.94, and 22.30 degrees 2θ, and wherein Form F of HCl salt of Compound (I-S) is characterized by an XRPD pattern comprising peaks at approximately 13.71, 14.22, and 20.87 degrees 2θ.

6. The process of claim 5 , wherein the solvent is water.

7. The process of claim 5 , wherein the solvent is MeOAc saturated with water.

8. The process of claim 5 , wherein the solvent is a mixture of 2-propanol and water.

9. The process of claim 8 , wherein the solvent is a 50/50 mixture of 2-propanol and water.

10. The process of claim 8 , wherein the solvent is a 65/35 mixture of 2-propanol and water.

11. The process of claim 8 , wherein the solvent is a 80/20 mixture of 2-propanol and water.

12. The process of claim 8 , wherein the solvent is a 95/5 mixture of 2-propanol and water.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2020
From: COHEN, BENJAMIN M.; TRAVERSE, JOHN F.; XU, JEAN; LI, YING
To: CELGENE CORPORATION
Reel/Frame 053449/0818 →
Continuity (7)
Continuation 16443161 · Jun 17, 2019
Continuation 15856845 · Dec 28, 2017
Continuation 15445070 · Feb 28, 2017
Continuation 14945147 · Nov 18, 2015
Continuation 13962745 · Aug 8, 2013
Provisional Application 61681484 · Aug 9, 2012
Related Publication 20200360395A1 · Nov 19, 2020