发明名称 MODIFIED NUCLEOSIDES, ANALOGS THEREOF AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM
摘要 The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
申请公布号 US2015159163(A1) 申请公布日期 2015.06.11
申请号 US201514627960 申请日期 2015.02.20
申请人 ISIS PHARMACEUTICALS, INC. 发明人 Prakash Thazha P.;Seth Punit P.;Swayze Eric E.
分类号 C12N15/113;C07H19/10 主分类号 C12N15/113
代理机构 代理人
主权项 1. A compound having Formula If:wherein: T1 is a phosphorus moiety having the formula: Ra and Rc are each, independently, protected hydroxyl, protected thiol, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy, substituted C1-C6 alkoxy, protected amino or substituted amino; Rb is O or S; M1 is H, OH or OR1; M2 is OH, OR1 or N(R1)(R2); each R1 and R2 is, independently, C1-C6 alkyl or substituted C1-C6 alkyl; r is 0 or 1; A has one of the formulas: Q1 and Q2 are each, independently, H, halogen, C1-C6 alkyl or substituted C1-C6 alkyl; Q3 is O, S, N(R5) or C(R6)(R7);each R5, R6 and R7 is, independently, H, C1-C6 alkyl, substituted C1-C6 alkyl or C1-C6 alkoxy; Bx1 is a heterocyclic base moiety; G is H, OH, halogen or O—[C(R8)(R9)]n—[(C═O)m—X1]j—Z; each R8 and R9 is, independently, H, halogen, C1-C6 alkyl or substituted C1-C6 alkyl; X1 is O, S or N(E1); Z is H, halogen, C1-C6 alkyl, substituted C1-C6 alkyl, C2-C6 alkenyl, substituted C2-C6 alkenyl, C2-C6 alkynyl, substituted C2-C6 alkynyl or N(E2)(E3); E, E2 and E3 are each, independently, H, C1-C6 alkyl or substituted C1-C6 alkyl; n is from 1 to about 6; m is 0 or 1; j is 0 or 1; each substituted group comprises one or more optionally protected substituent groups independently selected from halogen, OJ1, N(J1)(J2), =NJ1, SJ1, N3, CN, OC(═X2)J1, OC(═X2)—N(J1)(J2) and C(═X2)N(J1)(J2); X2 is O, S or NJ3; each J1, J2 and J3 is, independently, H or C1-C6 alkyl; and when j is 1 then Z is other than halogen or N(E2)(E3).
地址 Carlsbad CA US
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