OESTERGAARD, Michael,PRAKASH, Thazha P.,SETH, Punit P.,SWAYZ, Eric E.
申请号：
ES12748812
公开号：
ES2635866T3
申请日:
2012.08.08
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
An oligomeric compound with gaps comprising a contiguous sequence of monomeric subunits with bonds that have a gap region located between a 5 'region and a 3' region in which regions 5 'and 3' each independently have 2 to 8 contiguous furanosyl RNA-modified nucleosides that adopt a conformational 3'-endo geometry when placed in an oligomeric compound and the hollow region has 6 to 14 contiguous monomeric subunits selected from β-D-2'-deoxyribonucleosides and modified nucleosides that are DNAs that adopt a conformational 2'-endo geometry when placed in an oligomeric compound and wherein at least one of the internucleoside binding groups in the hollow region or the hollow region and the 5 'region or the 3 'region has the formula I: ** Formula ** where independently for each internucleoside linking group having the Formula I: X is O or S； Q is C1-C6 alkyl, substituted C1-C6 alkyl, C2-C6 alkenyl, substituted C2-C6 alkenyl, C2-C6 alkynyl, substituted C2-C6 alkynyl, -C (>； = O) OH or CH2C (>； = O) OH； each substituted group comprises one or more optionally protected substituent groups independently selected from halogen, OJ1, SJ1 and OC (>； = O) J1； and each J1 is, independently, H or C1-C6 alkyl； said oligomeric hollow compound having only one internucleoside bonding group of formula I in the hollow region, or having only two internucleoside linking groups of formula I in the hollow region, or having only three internucleoside bonding groups of formula I in the hollow region.Un compuesto oligomérico con huecos que comprende una secuencia contigua de subunidades monoméricas con enlaces que tienen una región de hueco situada entre una región 5' y una región 3'en la que las regiones 5' y 3' cada una, independientemente, tienen de 2 a 8 nucleósidos modificados de tipo ARN de furanosilo contiguos que adoptan una geometría 3'-endo conformacional cuando se ponen en un compuesto oligomérico y la región de hueco tiene de 6 a 14 subunidades monoméricas contiguas seleccionada
