IP Library Granted Patent US 10,596,180
Granted Patent B2
US 10,596,180 · App. 16/443,161 · Granted Mar 24, 2020

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 10,596,180
App. No.
16/443,161
Granted
Mar 24, 2020
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 (17)

1. A method of treating cancer, an immune-related disease or disorder, an inflammatory disease or disorder, or a symptom thereof in a subject, comprising administering to the subject a therapeutically effective amount of a solid form comprising a racemic Compound (I):

or a hydrate or anhydrate thereof, wherein the solid form is crystalline, wherein the solid form comprises a HCl salt of racemic Compound (I) and water, having an XRPD pattern comprising peaks at approximately 13.88, 14.30, and 15.36 degrees 2θ; or

comprises a HCl salt of racemic Compound (I) and methanol, having an XRPD pattern comprising peaks at approximately 12.38, 14.54, and 26.10 degrees 2θ;

wherein the cancer, immune-related disease or disorder, or inflammatory disease or disorder is lupus, scleroderma, Sjögren syndrome, ANCA-induced vasculitis, anti-phospholipid syndrome, myasthenia gravis, or multiple myeloma.

2. The method of claim 1 , wherein the solid form comprises a HCl salt of racemic Compound (I) and water, having an XRPD pattern comprising peaks at approximately 13.88, 14.30, and 15.36 degrees 2θ.

3. The method of claim 2 , wherein the XRPD pattern further comprises peaks at approximately 9.84, 16.42, and 19.82 degrees 2θ.

4. The method of claim 2 , wherein the XRPD pattern matches the XRPD pattern presented in FIG. 101 .

5. The method of claim 1 , wherein the solid form comprises a HCl salt of racemic Compound (I) and methanol, having an XRPD pattern comprising peaks at approximately 12.38, 14.54, and 26.10 degrees 2θ.

6. The method of claim 5 , wherein the XRPD pattern further comprises peaks at approximately 15.06, 20.00, and 26.86 degrees 2θ.

7. The method of claim 5 , wherein the XRPD pattern matches the XRPD pattern presented in FIG. 104 .

8. The method of claim 1 , wherein the immune-related or inflammatory disease or disorder is lupus, scleroderma, Sjögren syndrome, ANCA-induced vasculitis, anti-phospholipid syndrome, or myasthenia gravis.

9. The method of claim 1 , wherein the immune-related or inflammatory disease or disorder is scleroderma.

10. The method of claim 1 , wherein the immune-related or inflammatory disease or disorder is systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE), discoid lupus erythematosus (DLE), or drug-induced lupus.

11. The method of claim 10 , wherein the immune-related or inflammatory disease or disorder is systemic lupus erythematosus (SLE).

12. The method of claim 10 , wherein the immune-related or inflammatory disease or disorder is cutaneous lupus erythematosus (CLE).

13. The method of claim 1 , wherein the cancer is multiple myeloma.

14. The method of claim 1 , wherein the lupus is systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE), discoid lupus erythematosus (DLE), or drug-induced lupus.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2019
From: COHEN, BENJAMIN M.; TRAVERSE, JOHN F.; XU, JEAN; LI, YING
To: CELGENE CORPORATION
Reel/Frame 050154/0253 →
Continuity (6)
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 20190365772A1 · Dec 5, 2019