Granted Patent
B2
US 12,258,362 · App. 17/169,611 · Granted Mar 25, 2025
Processes for preparing phosphorodiamidate morpholino oligomers
Inventors:
Baozhong Cai (Cambridge, MA); Mitchell Martini (Cambridge, MA); Ross Shimabuku (Cambridge, MA); Katie Thomas (Cambridge, MA)
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Abstract
Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomersynthesis while maintaining overall yield and purity of a synthesized oligomer.
Claims (216)
1. A compound of Formula (A9):
or a pharmaceutically acceptable salt thereof, wherein:
n is an integer from 10 to 40;
R 1 is a support-medium;
R 3 is selected from the group consisting of hydrogen, trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl; and
R 4 is, independently at each occurrence, selected from the group consisting of:
2. The compound of claim 1 , wherein the compound of Formula (A9) is a compound of Formula (A9a):
wherein:
n is an integer from 10 to 40,
R 1 is a support-medium
R 3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl, and
R 4 is, independently for each occurrence, selected from the group consisting of:
3. The compound of claim 1 , wherein the compound of Formula (A9) is a compound of Formula (IX):
or a pharmaceutically acceptable salt thereof, wherein:
R 1 is a support-medium, and
R 2 is, independently at each occurrence, selected from the group consisting of:
and
wherein R 2 is at each position from 1 to 30 and 5′ to 3′:
Position No. 5′ to 3′
R 2
1
PC
2
T
3
PC
4
PC
5
PA
6
PA
7
PC
8
PA
9
T
10
PC
11
PA
12
PA
13
DPG
14
DPG
15
PA
16
PA
17
DPG
18
PA
19
T
20
DPG
21
DPG
22
PC
23
PA
24
T
25
T
26
T
27
PC
28
T
29
PA
30
DPG.
4. The compound of claim 3 , wherein the compound of Formula (IX) is a compound of Formula (IXa):
or a pharmaceutically acceptable salt thereof, wherein
R 1 is a support-medium, and
R 2 is, independently at each occurrence, selected from the group consisting of:
and
wherein R 2 is at each position from 1 to 30 and 5′ to 3′:
Position No. 5′ to 3′
R 2
1
PC
2
T
3
PC
4
PC
5
PA
6
PA
7
PC
8
PA
9
T
10
PC
11
PA
12
PA
13
DPG
14
DPG
15
PA
16
PA
17
DPG
18
PA
19
T
20
DPG
21
DPG
22
PC
23
PA
24
T
25
T
26
T
27
PC
28
T
29
PA
30
DPG.
5. The compound of claim 1 , wherein the compound of Formula (A9) is a compound of Formula (Xa):
or a pharmaceutically acceptable salt thereof, wherein
R 1 is a support-medium, and
R 2 is, independently at each occurrence, selected from the group consisting of:
and
wherein R 2 is at each position from 1 to 30 and 5′ to 3′:
Position No. 5′ to 3′
R 2
1
PC
2
T
3
PC
4
PC
5
PA
6
PA
7
PC
8
PA
9
T
10
PC
11
PA
12
PA
13
DPG
14
DPG
15
PA
16
PA
17
DPG
18
PA
19
T
20
DPG
21
DPG
22
PC
23
PA
24
T
25
T
26
T
27
PC
28
T
29
PA
30
DPG.
Assignments (2)
SECURITY INTEREST
Recorded May 7, 2025
From: SAREPTA THERAPEUTICS, INC.
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 071218/0445 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded May 26, 2021
From: CAI, BAOZHONG; MARTINI, MITCHELL; SHIMABUKU, ROSS; THOMAS, KATIE
To: SAREPTA THERAPEUTICS, INC.
Reel/Frame 056355/0521 →
Continuity (4)
Continuation
16302443
Provisional Application
62357134
· Jun 30, 2016
Provisional Application
62340953
· May 24, 2016
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