Crystalline bis- and tris-hydrochloride salt of elamipretide

Patent metadata

Field	Value
Publication number	US-10676506-B2
Application number	US-201916259575-A
Country	US
Kind code	B2
Filing date	Jan 28, 2019
Priority date	Jan 26, 2018
Publication date	Jun 9, 2020
Grant date	Jun 9, 2020

Abstract

Disclosed are crystalline forms of the bis- and tris-(hydrochloride) salts of D-Arg-Tyr(2,6-DiMe)-Lys-Phe-NH2, which is also known as MTP-131.

First claim

What is claimed is:

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

wherein said crystalline form has peaks in its XRPD pattern at values of two theta as listed in Table 2A:

TABLE 2A

d spacing
Height
Relative intensity

2θ (°)
(A°)
(cps)
(%)

6.40
13.79726
1343
28

6.98
12.65711
406
9

7.88
11.20719
160
3

9.05
9.76484
112
2

9.84
8.97904
1550
33

10.18
8.67918
186
4

11.65
7.58843
340
7

13.06
6.77213
4732
100

16.88
5.24746
715
15

19.09
4.64608
790
17

20.61
4.30611
289
6

24.21
3.67305
113
2

24.84
3.58126
433
9

26.33
3.38163
298
6

27.44
3.24777
327
7

28.59
3.11934
158
3

29.73
3.00251
480
10.

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

wherein said crystalline form has peaks in its XRPD pattern as shown in FIG. 2 .

3. A crystalline form of a bis-(hydrochloride) salt of Compound (I),

wherein said crystalline form has peaks in its XRPD pattern at values of two theta (° 2) of: 6.4, 9.8, 13.1, 16.9, 19.1, and 29.7.

4. The crystalline form of claim 3 , wherein said crystalline form has peaks in its XRPD pattern at values of two theta (° 2) of: 6.4, 7.0, 7.9, 9.1, 9.8, 10.2, 11.7, 13.1, 16.9, 19.1, 20.6, 24.2, 24.8, 26.3, 27.4, 28.6, and 29.7.

5. A crystalline form of a tris-(hydrochloride) salt of Compound (I),

wherein said crystalline form has peaks in its XRPD pattern at values of two theta as listed in Table 10A:

TABLE 10A

Pos.
d-spacing
Height
Rel. Int.

[°2θ]
[Å]
[cts]
[%]

5.6826
15.55252
48.89
5.06

6.669
13.25428
16.7
1.73

8.1507
10.84783
650.66
67.29

9.2697
9.54072
154.41
15.97

9.8231
9.00438
277.37
28.68

11.0495
8.00758
264.45
27.35

11.4729
7.713
393.18
40.66

12.3925
7.14266
360.31
37.26

12.8405
6.89444
63.27
6.54

13.6472
6.48865
237.2
24.53

14.3699
6.16392
107.3
11.1

14.8755
5.95554
245.56
25.39

15.5909
5.68384
369.87
38.25

15.8566
5.58918
690.32
71.39

Assignees

• Stealth Biotherapeutics Corp

Inventors

• Duncan Scott M

Classifications

• C07K5/1019 Primary

  with the first amino acid being basic · CPC title

• C07K1/14

  Extraction; Separation; Purification · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title