IPC분류정보
국가/구분 |
United States(US) Patent
등록
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국제특허분류(IPC7판) |
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출원번호 |
US-0329416
(1999-06-10)
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발명자
/ 주소 |
- Manoharan, Muthiah
- Guzaev, Andrei
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출원인 / 주소 |
- ISIS Pharmaceuticals, Inc.
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대리인 / 주소 |
Isis Patent Department Woodcock Washburn LLP
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인용정보 |
피인용 횟수 :
1 인용 특허 :
16 |
초록
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Methods for the preparation of oligonucleotides having bioreversible phosphate blocking groups are disclosed. In one aspect, the present invention provides compounds comprising a sequence of nucleotide units that includes a first segment having at least one internucleoside linkage of formula:3′-O?P(
Methods for the preparation of oligonucleotides having bioreversible phosphate blocking groups are disclosed. In one aspect, the present invention provides compounds comprising a sequence of nucleotide units that includes a first segment having at least one internucleoside linkage of formula:3′-O?P(X)(O?)?O-5′and a second segment having at least one internucleoside linkage of formula:3′-O?P(X)(Y1?(CH2)q?Y2?Y3?Z)?O-5′wherein each of X, Y1, and Y2 is, independently, O or S; q is 2 to about 4; Y3 is C(?O) or S; and Z is aryl having 6 to about 14 carbon atoms or alkyl having from one to about six carbon atoms.
대표청구항
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1. A compound having the formula: wherein:each B is, independently, a naturally occurring or non-naturally occurring nucleobase; each R1 is, independently, H, OH, F, or a group of formula R7?(R8)n; each R7 is, independently, a diradical of C3-C20 alkyl C4-C20 alky, C2-C20 alkynyl, C1-C20 alkoxy, C2-
1. A compound having the formula: wherein:each B is, independently, a naturally occurring or non-naturally occurring nucleobase; each R1 is, independently, H, OH, F, or a group of formula R7?(R8)n; each R7 is, independently, a diradical of C3-C20 alkyl C4-C20 alky, C2-C20 alkynyl, C1-C20 alkoxy, C2-C20 alkenyloxy, or C2-C20 alkynyloxy; each R8 is, independently, hydrogen, amino, protected amino, halogen, hydroxyl, thiol, keto, carboxyl, nitro, nitroso, trifluoromethyl, trifluoromethoxy, O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aryl, S-aryl, NH-aryl, O-aralkyl, S-aralkyl, NH-aralkyl, N-phthalimido, azido, hydrazino, hydroxylamino, isocyanato, aryl, a radical derived from imidazole, polyamide, polyalkylene glycol, polyether, or a group of formula (?O?X3)p1, where p1 is 2 to about 10 and X3 is alkylene having from one to about 10 carbons or alkyl having form one to about 10 carbons; each X is, independently, O or S; Rz is a divalent aromatic radical having about 5 to about 8 carbon atoms or has formula (CH2)x3; z is 0 or 1; x1, x2, and x3 are, independently, 1 to about 5; RL is ?OH or ?N(RN1)(RN2); RN1 is H or alkyl having 1 to about 10 carbon atoms; RN2 is a solid support; and R3 is hydrogen, a hydroxyl protecting group, or group of the formula: wherein:each X is, independently, O or S; Z1 is H or a hydroxyl protecting group; n is 1 to about 100; m is 1 to about 100; and Rn and Rm are selected such that: each Rn is, independently, O? or O?(CH2)p2?E and each Rm is ?Y1?(CH2)q?Y2?Y3?Z; or each Rn is ?Y1?(CH2)q?Y2?Y3?Z and each Rm is, independently, O? or O?(CH2)p2?E; wherein: p2 is 1 to about 5; E is ?CN; each Y1 is O; each q is, independently, 2 to about 4; each Y2 is, independently O or S; each Y3 is, independently, C(?O) or S; and each Z is, independently, aryl having 6 to about 14 carbon atoms or alkyl having from one to about six carbon atoms; provided that at least one of x1 and x2 is not 1 when R3 is hydrogen or a hydroxyl protecting group and z is 0, and provided that at least one nucleoside is a β-nucleoside and bound at its 3′ position to a linking group of formula ?O?P(X)(Rn)?O? or ?O?P(X)(Rm)?O? where Rn or Rm is O? or ?O?(CH2)p2?E.2. The compound of claim 1 wherein each X is O.3. The compound of claim 1 wherein x1 and x3 are 1 or 2, and z is 0.4. The compound of claim 1 wherein RL is ?N(RN1)(RN2).5. The compound of claim 1 wherein:Y2 is O and Y3 is C(?O); or Y2 is S and Y3 is C(?O). 6. The compound of claim 5 wherein q is 2 and Z is alkyl having 1 to about 6 carbon atoms.7. The compound of claim 5 wherein Z is methyl, phenyl, or t-butyl.8. The compound of claim 1 wherein p1 is 2.9. The compound of claim 1 wherein n and m are each about 2 to about 25.
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