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US 8,895,734 B2Granted
Peptide nucleic acid derivatives with good cell penetration and strong affinity for nucleic acid
AssigneeOliPass Corporation
InventorsShin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
Life of this patent
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Abstract
The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
Claims2
A compound of Formula VIII:
- wherein,
- R9 is hydrido, N-succinyl, or substituted or non-substituted alkyl radical;
- P1 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, and substituted or non-substituted arylsulfonyl radical;
- P2 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, substituted alkyloxycarbonyl, substituted or non-substituted alkyl, amidinyl, 1,3-bis(t-butoxy-carbonyl)amidinyl, 1,3-bis-(benzyl-oxycarbonyl)amidinyl radical;
- and,
- L3 is a linker represented by Formula V:
- wherein,
- Q1 and Qm are substituted or non-substituted methylene radical, and Qm is directly linked to the amino radical;
- Q2, Q3, . . . , and Qm-1 are independently selected from substituted or non-substituted methylene, oxygen, sulfur, and substituted or non-substituted amino radical;
- and,
- m is an integer from 2 to 15.
8 more elements
A compound of Formula XI:
- wherein,
- R12 is hydroxy, substituted or non-substituted alkyloxy, or substituted or non-substituted amino radical;
- P2 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, substituted alkyloxycarbonyl, substituted or non-substituted alkyl, amidinyl, 1,3-bis(t-butoxy-carbonyl)amidinyl, 1,3-bis-(benzyl-oxycarbonyl)amidinyl radical;
- and,
- L3 is a linker represented by Formula V:
- wherein,
- Q1 and Qm are substituted or non-substituted methylene radical, and Qm is directly linked to the amino radical;
- Q2, Q3, . . . , and Qm-1 are independently selected from substituted or non-substituted methylene, oxygen, sulfur, and substituted or non-substituted amino radical;
- and,
- m is an integer from 2 to 15.
7 more elements
Dependencies are inferred from the claim text.