IP Library Granted Patent US 11,325,943
Granted Patent B2
US 11,325,943 · App. 16/492,521 · Granted May 10, 2022

Crystalline salt forms of SBT-20

Inventor: Scott M. Duncan (Bedford, MA)
Assignee: STEALTH BIOTHERAPEUTICS INC.
C07K5/1016A61K38/00
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Quick Facts
Patent No.
US 11,325,943
App. No.
16/492,521
Granted
May 10, 2022
Kind
B2
Abstract

Disclosed are various crystalline salt forms of L-Phe-D-Arg-L-Phe-L-Lys-NH 2 .

Claims (117)

1. A crystalline form of a salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta as described in any one of Tables 32-36;

wherein the values of two theta described in Table 32 are:

4.2261

5.0243

6.6588

8.2982

8.6421

10.0369

10.9707

12.3486

16.4828

19.6073

20.1651

24.8069

29.0247

wherein the values of two theta described in Table 33 are:

4.4004

5.4676

6.7036

8.4749

8.9195

11.1651

12.2024

15.6936

16.4475

17.7995

18.5661

19.8016

24.7466

25.663

26.1011

29.1061

wherein the values of two thea described in Table 34 are:

7.2369

10.2443

18.5712

19.9056

20.5017

22.3429

25.8406

26.8697

27.6899

29.5416

wherein the values of two theta described in Table 35 are:

16.3125

17.2726

18.4711

19.0356

20.6684

21.1735

21.6748

22.0235

22.8225

23.4813

24.8323

26.1425

26.9707

28.2387

wherein the values of two theta described in Table 36 are:

4.2472

5.6124

6.005

6.5059

7.3139

8.3849

9.0331

9.3884

10.976

11.6992

12.2816

12.8483

13.6768

14.5232

15.3546

16.434

16.79

17.4904

17.9183

18.5267

19.2386

19.8404

20.5197

20.8647

21.3043

21.7736

22.1003

22.656

23.2875

23.7016

24.3712

24.9261

25.4669

25.7584

26.8617

27.8642

29.0847.

2. A crystalline form of a salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern as described in any one of FIGS. 1-5 .

3. A crystalline form of a lysine salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta (° 2θ) of: 4.2, 8.3, 12.3, 16.5, 24.8, and 29.0.

4. The crystalline form of claim 3 , wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of: 4.2, 5.0, 6.6, 8.3, 8.6, 10.0, 11.0, 12.3, 16.5, 19.6, 20.2, 24.8, and 29.0.

5. A crystalline form of a lysine salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta (° 2θ) of: 4.4, 6.7, 8.5, 8.9, 11.2, 15.7, 16.4, 19.8, and 24.7.

6. The crystalline form of claim 5 , wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of: 4.4, 5.5, 6.7, 8.5, 8.9, 11.2, 12.2, 15.7, 16.4, 17.8, 18.6, 19.8, 24.7, 25.7, 26.1, and 29.1.

7. A crystalline form of an arginine salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta (° 2θ) of: 7.2, 10.2, 18.6, 19.9, 20.5, 22.3, and 26.9.

8. The crystalline form of claim 7 , wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of: 7.2, 10.2, 18.6, 19.9, 20.5, 22.3, 25.8, 26.9, 27.7, and 29.5.

9. A crystalline form of a serine salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta (° 2θ) of: 16.3, 17.3, 19.0, 20.7, 22.8, 23.5, 24.8, and 28.2.

10. The crystalline form of claim 9 , wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of: 16.3, 17.3, 18.5, 19.0, 20.7, 21.2, 21.7, 22.0, 22.8, 23.5, 24.8, 26.1, 27.0, and 28.2.

11. A crystalline form of a tosylate salt of Compound (I),

wherein said crystalline form has characteristic peaks in its x-ray powder diffraction (XRPD) pattern at values of two theta (° 2θ) of: 4.2, 5.6, 8.4, 19.2, 19.8, 21.8, 24.4, and 24.9.

12. The crystalline form of claim 11 , wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of: 4.2, 5.6, 7.3, 8.4, 9.0, 13.7, 16.4, 16.8, 19.2, 19.8, 21.8, 22.1, 22.7, 24.4, and 24.9.

13. A composition, comprising a crystalline form of claim 1 .

14. A process for making a pharmaceutical composition comprising Compound (I),

comprising dissolving a crystalline form of claim 1 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2021
From: STEALTH BIOTHERAPEUTICS CORP
To: STEALTH BIOTHERAPEUTICS INC.
Reel/Frame 058356/0837 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 10, 2019
From: DUNCAN, SCOTT M.
To: STEALTH BIOTHERAPEUTICS CORP.
Reel/Frame 050325/0473 →
Continuity (2)
Provisional Application 62514051 · Jun 2, 2017
Related Publication 20210292361A1 · Sep 23, 2021
Cited By (1)
US 12,252,554