US2022112491A1PendingUtilityA1
Processes for preparing phosphorodiamidate morpholino oligomers
Est. expiryMay 24, 2036(~9.9 yrs left)· nominal 20-yr term from priority
C07F 9/65616C12N 2310/334C12N 2310/314C12N 2310/3233A61K 48/00C12N 2310/351C12N 2310/336C12N 2310/11C12N 15/113C07F 9/65583C12N 2310/333C08G 81/024A61P 21/00
61
PatentIndex Score
0
Cited by
0
References
0
Claims
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 oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.
Claims
exact text as granted — not AI-modified1 .- 22 . (canceled)
23 . A compound of Formula (A5):
or a pharmaceutically acceptable salt thereof, wherein R 1 is a support-medium, R 3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl, and
R 4 is
24 . The compound of claim 23 , wherein the support-medium comprises a material selected from the group consisting of glass, modified or functionalized glass, plastics (including acrylics, polystyrene (e.g., polystyrene with 1% crosslinked divinylbenzene), copolymers of styrene and other materials, polypropylene, polyethylene, polybutylene, polyurethanes, and TEFLON), polysaccharides, nylon or nitrocellulose, ceramics, resins, silica or silica-based materials (including silicon and modified silicon), carbon, metals, and optical fiber bundles.
25 . The compound of claim 23 , wherein the compound of Formula (A5) is of Formula (A5a):
or a pharmaceutically acceptable salt thereof, wherein:
R 1 is a support-medium,
R 3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl, and
R 4 is
26 . The compound of claim 26 , wherein the support-medium comprises a material selected from the group consisting of glass, modified or functionalized glass, plastics (including acrylics, polystyrene (e.g., polystyrene with 1% crosslinked divinylbenzene), copolymers of styrene and other materials, polypropylene, polyethylene, polybutylene, polyurethanes, and TEFLON), polysaccharides, nylon or nitrocellulose, ceramics, resins, silica or silica-based materials (including silicon and modified silicon), carbon, metals, and optical fiber bundles.
27 . A compound of Formula (A9):
or a pharmaceutically acceptable salt thereof, wherein n 22, R 1 is a support-medium, R 3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl, and R 2 is, per the oligomeric compound of Formula (C), wherein R 2 is at each position from 1 to 22 and 5′ to 3′:
Position No.
5′ to 3′
R 2
1
PC
2
PA
3
PA
4
T
5
DPG
6
PC
7
PC
8
PA
9
T
10
PC
11
PC
12
T
13
DPG
14
DPG
15
PA
16
DPG
17
T
18
T
19
PC
20
PC
21
T
22
DPG
wherein:
PC is
DPG is
T is
and PA is
28 . The compound of claim 27 , wherein the support-medium comprises a material selected from the group consisting of glass, modified or functionalized glass, plastics (including acrylics, polystyrene (e.g., polystyrene with 1% crosslinked divinylbenzene), copolymers of styrene and other materials, polypropylene, polyethylene, polybutylene, polyurethanes, and TEFLON), polysaccharides, nylon or nitrocellulose, ceramics, resins, silica or silica-based materials (including silicon and modified silicon), carbon, metals, and optical fiber bundles.
29 . The compound of claim 27 , wherein the compound of Formula (A9) is of Formula (A9a):
or a pharmaceutically acceptable salt thereof, wherein n 22, R 1 is a support-medium, R 3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl, and R 2 is, per the oligomeric compound of Formula (C), wherein R 2 is at each position from 1 to 22 and 5′ to 3′:
Position No.
5′ to 3′
R 2
1
PC
2
PA
3
PA
4
T
5
DPG
6
PC
7
PC
8
PA
9
T
10
PC
11
PC
12
T
13
DPG
14
DPG
15
PA
16
DPG
17
T
18
T
19
PC
20
PC
21
T
22
DPG
wherein:
PC is
DPG is
T is
and PA is
30 . The compound of claim 29 , wherein the support-medium comprises a material selected from the group consisting of glass, modified or functionalized glass, plastics (including acrylics, polystyrene (e.g., polystyrene with 1% crosslinked divinylbenzene), copolymers of styrene and other materials, polypropylene, polyethylene, polybutylene, polyurethanes, and TEFLON), polysaccharides, nylon or nitrocellulose, ceramics, resins, silica or silica-based materials (including silicon and modified silicon), carbon, metals, and optical fiber bundles.Cited by (0)
No later patents cite this yet.
References (0)
No backward citations on record.