초록 ▼

The present invention is directed to nucleoside monomers wherein the 3′-O atom is replaced with a methylene group. The present invention also provides oligomers comprising a plurality of such monomers which are linked by methylene phosphonate linkages. Further, methods of preparing monomers and olig

The present invention is directed to nucleoside monomers wherein the 3′-O atom is replaced with a methylene group. The present invention also provides oligomers comprising a plurality of such monomers which are linked by methylene phosphonate linkages. Further, methods of preparing monomers and oligomers according to the present invention are provided.

대표청구항 ▼

1. An oligomer of formula II: wherein:Bx is a protected or unprotected heterocyclic base moiety; T1 is an oligonucleotide, oligonucleoside, nucleoside, nucleotide, H or a hydroxyl protecting group; each X1 and X3 is, independently, O, S or NH; each X2 is, independantly, OH, SH or NH2; each L is, ind

1. An oligomer of formula II: wherein:Bx is a protected or unprotected heterocyclic base moiety; T1 is an oligonucleotide, oligonucleoside, nucleoside, nucleotide, H or a hydroxyl protecting group; each X1 and X3 is, independently, O, S or NH; each X2 is, independantly, OH, SH or NH2; each L is, independantly, C(Y1)(Y2) or O, provided that at least one L is C(Y1)(Y2); each R1, independently, has one of formulas: wherein:Z0 is, independently, O, S or NH; E2 is N(Q1)(Q2) or N?C(Q1)(Q2); E2 is C1-C10 alkyl; each Q1 and Q2 is, independently, H, C1-C10 alkyl, substituted alkyl, dialkylaminoalkyl, a nitrogen protecting group, a tethered or untethered conjugate group, a linker to a solid support; or Q1 and Q2, together, are joined in a nitrogen protecting group or a ring structure that can include at least one additional heteroatom selected from N and O; each q1 is, independently, from 1 to 10; q2 is from 1 to 10; q3 q4 is zero, 1 or 2; q5 each M1 is, independently, H, C1-C8 alkyl, C1-C8 haloalkyl, C(?NH)N(H)M2, C(?O)N(H)M2 or OC(?O)N(H)M2; M2 is H or C1-C8 alkyl; Z1, Z2 and Z3 comprise a ring system having from about 4 to about 7 carbon atoms or having from about 3 to about 6 carbon atoms and 1 or 2 heteroatoms wherein said heteroatoms are selected from oxygen, nitrogen and sulfur and wherein said ring system is aliphatic, unsaturated aliphatic, aromatic, or saturated or unsaturated heterocyclic; and Z4 is OM1, SM1, or N(M1)2; Z5 is alkyl or haloalkyl having 1 to about 10 carbon atoms, alkenyl having 2 to about 10 carbon atoms, alkynyl having 2 to about 10 carbon atoms, aryl having 6 to about 14 carbon atoms, N(Q1)(Q2), OQ1, halo, SQ1 or CN; p is 0 or an integer from 1 to 50; and each of Y1 and Y2 is, independently, H, alkyl, substituted alkyl, aryl, substituted aryl, heterocyclyl, cyano, carboxyl, ester or a cyclic moiety; wherein said substituted alkyl groups are substituted with one or more of alkyl, alkenyl, alkynyl, aryl, hydroxyl, alkoxy, alcohol, benzyl, phenyl, nitro, thiol, thioalkoxy, thioalkyl, trifluoromethyl, halo, nitrile, trifluoromethoxy or azido, and said substituted aryl groups are substituted with one or more of hydroxyl, alkoxy, alcohol, benzyl, phenyl, nitro, thiol, thioalkoxy, halogen, alkyl, aryl, alkenyl, or alkynyl. 2. The oligomer of claim 1 wherein at least one L is a methylene group.3. The oligomer of claim 1 wherein said hydroxyl protecting group is trityl, monomethoxytrityl, dimethoxytrityl, trimethoxytrityl, 9-phenylxanthin-9-yl, t-butyldiphenylsilyl or t-butyldimethylsilyl.4. The oligomer of claim 1 wherein at least one R1 is OCH2CH2OCH3.