OESTERGAARD, Michael,PRAKASH, Thazha,SETH, Punit,SWAYZE, Eric
申请号：
ES12751399
公开号：
ES2651514T3
申请日:
2012.08.08
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
An oligomeric compound with gaps comprising a contiguous sequence of joined monomeric subunits having an interstitial region located between a 5 'region and a 3' region in which regions 5 'and 3' each independently have 2 to 8 RNA-like contiguous nucleosides that are modified furanosyl nucleosides that adopt a 3'-endo shaped geometry when placed in an oligomeric compound and the hollow region has 6 to 14 contiguous monomer subunits selected from ß-D- 2'- 5'-substituted deoxyribonucleosides and 5'-substituted β-D-2'-deoxyribonucleosides having Formula I: ** Formula ** where independently for each 5'-substituted β-D-2'-deoxyribonucleoside having Formula I : T1 and T2 are each, independently, an internucleoside binding group that binds the 5'-substituted β-D-2'-deoxyribonucleoside having Formula I with the remainder of the separated oligomeric compound； Bx is a heterocyclic base moiety； R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C2-C6 alkenyl, substituted C2-C6 alkenyl, C2-C6 alkynyl or substituted C2-C6 alkynyl； Each substituted group comprises one or more optionally protected substituent groups independently selected from halogen, OJ1, NJ1J2,>； = NJ1, SJ1, N3, CN, OC (>； = L) J1, OC (>； = L) NJ1J2 and NJ3C (>； = L ) NJ1J2, wherein each J1, J2 and J3 is, independently, H, C1-C6 alkyl or a protecting group, and L is O, S or NJ1； and wherein said interstitium region comprises at least one 5'-substituted β-D-2'-deoxyribonucleoside having Formula I and a plurality of β-D-2'-deoxyribonucleosides； said separate oligomeric compound having a 5'-substituted β-D-2'-deoxyribonucleoside of Formula I, or having two 5'-substituted β-D-2'-deoxyribonucleosides of Formula I, or having three β-D -2'- 5-substituted deoxyribonucleosides of Formula I.Un compuesto oligomérico con huecos que comprende una secuencia contigua de subunidades monoméricas unidas que tiene una región de intersticio situada entre una región 5' y una región 3' en la que las regiones 5' y 3' cada una, indep
