Functional biopolymer modification reagents and uses thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07F-009/02
A61K-047/48
C04B-035/632
C07D-207/46
C07D-207/452
C07D-213/82
C07D-401/12
C07F-007/18
C07F-009/24
C07F-009/58
C07H-021/00
출원번호
US-0491563
(2012-06-07)
등록번호
US-RE46171
(2016-10-04)
발명자
/ 주소
Schwartz, David A.
Hogrefe, Richard I.
출원인 / 주소
SOLULINK, INCORPORATED
인용정보
피인용 횟수 :
0인용 특허 :
84
초록▼
Hydrazino, oxyamino and carbonyl-based reagents and methods for incorporation into oligonucleotides during their solid phase synthesis are provided. Modified oligonucleotides are provided that incorporate the reagents provided herein. Immobilized oligonucleotides and oligonucleotide conjugates that
Hydrazino, oxyamino and carbonyl-based reagents and methods for incorporation into oligonucleotides during their solid phase synthesis are provided. Modified oligonucleotides are provided that incorporate the reagents provided herein. Immobilized oligonucleotides and oligonucleotide conjugates that contain covalent hydrazone or oxime linkages are provided. Methods for preparation of surface bound oligonucleotides are provided. Methods for the preparation of oligonucleotide conjugates are also provided.
대표청구항▼
1. A compound that has formula (I): P1-M-X wherein: P1 is a phosphorous based coupling group selected from the group consisting of phosphoramidite, H-phosphonate and phosphotriester;X is selected from the group consisting of: —NHNH—R4, —NHN═C(CH3)2, —(C═O)CH3, —(C═O)H and —ONHR4 wherein R4 is a pro
1. A compound that has formula (I): P1-M-X wherein: P1 is a phosphorous based coupling group selected from the group consisting of phosphoramidite, H-phosphonate and phosphotriester;X is selected from the group consisting of: —NHNH—R4, —NHN═C(CH3)2, —(C═O)CH3, —(C═O)H and —ONHR4 wherein R4 is a protecting group; and M is a divalent group of the formula —(CH2)n—NH—(C═R1)—R2— wherein R1 is S or O; R2 is pyrimidinyl group, a quinolinyl group or a pyrrolyl group; and n is 2, 3, 4, 5, 6, 7, 8, 9, or 10. 2. The compound of claim 1, wherein R4 is a protecting group selected from the group consisting of monomethoxytrityl (MMT), dimethoxytrityl (DMT), 9-fluorenylmethoxycarbonyl (FMOC) and trifluoroacetyl (TEA). 3. The compound of claim 1 wherein X is —NHNH—R4. 4. The compound of claim 1 wherein X is —NHN═C(CH3)2. 5. The compound of claim 1 wherein X is —(C═O)CH3. 6. The compound of claim 1 wherein X is —(C═O)H. 7. The compound of claim 1 wherein X is —ONR4. 8. The compound of claim 1 wherein R4 is MMT. 9. The compound of claim 1 wherein R4 DMT. 10. The compound of claim 1 wherein R4 FMOC. 11. The compound of claim 1 wherein R4 is TFA. 12. A compound that has formula (I): P1-M-Xwherein:P1 is a phosphorous based coupling group selected from the group consisting of phosphoramidite, H-phosphonate and phosphotriester;X is selected from the group consisting of:—NHNH—R4, —NHN═C(CH3)2, —(C═O)CH3, —(C═O)H and —ONHR4 wherein R4 is a protecting group; andM is a divalent group of the formula —(CH2)n—NH—(C═R1)—R2— wherein R1 is S or O; R2 is pyrimidinyl group, a quinolinyl group or a pyrrolyl group; and n is 2, 3, 4, 5, 6, 7, 8, 9, or 10. 13. The compound of claim 12, wherein R4 is a protecting group selected from the group consisting of monomethoxytrityl (MMT), dimethoxytrityl (DMT), 9-fluorenylmethoxycarbonyl (FMOC) and trifluoroacetyl (TEA). 14. The compound of claim 12 wherein X is —NHNH—R4. 15. The compound of claim 12 wherein X is —NHN═C(CH3)2. 16. The compound of claim 12 wherein X is —(C═O)CH3. 17. The compound of claim 12 wherein X is —(C═O)H. 18. The compound of claim 12 wherein X is —ONR4. 19. The compound of claim 12 wherein R4 is MMT. 20. The compound of claim 12 wherein R4 is DMT. 21. The compound of claim 12 wherein R4 is FMOC. 22. The compound of claim 12 wherein R4 is TFA. 23. A compound that has formula (I): P1-M-Xwherein:P1 is a phosphoramidite;X is selected from the group consisting of:—NHNH—R4, —NHN═C(CH3)2, —(C═O)CH3, —(C═O)H and —ONHR4 wherein R4 is a protecting group; andM is selected from a pyrimidinyl group, a quinolinyl group or a pyrrolyl group.
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이 특허에 인용된 특허 (84)
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