发明名称 Bicyclic cyclohexose nucleic acid analogs
摘要 The present invention provides bicyclic cyclohexose nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
申请公布号 US9012421(B2) 申请公布日期 2015.04.21
申请号 US201013388115 申请日期 2010.08.05
申请人 Isis Pharmaceuticals, Inc. 发明人 Migawa Michael T.;Seth Punit P.;Swayze Eric E.;Ross Bruce S.;Song Quanlai;Han Mingming
分类号 A61K31/712;C07H19/06;C07H21/00;C12N5/071;C07H19/16 主分类号 A61K31/712
代理机构 Isis Pharmaceuticals, Inc. Patent Dept. 代理人 Isis Pharmaceuticals, Inc. Patent Dept. ;Jones, S.C. Casimir
主权项 1. A bicyclic nucleoside analog of Formula I:wherein: Bx is a heterocyclic base moiety; Z is O; Q is 5′-CR3R4—O-2′, 5′-(CR3R4)2-2′, 5′-CR3═CR4-2′, 5′-CR3R4—O—N(R5)-2′ or 5′-CR3R4—N(R5)—O-2; each R3 and R4 is, independently, H, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy, substituted C1-C6 alkoxy or halogen; R5 is H, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy or substituted C1-C6 alkoxy; L1 and L2 are each H or one of L1 and L2 is H and the other of L1 and L2 is CH3 or OCH3; one of E1, E2, E3 and E4 is O-T2, two of E1, E2, E3 and E4 are H and the remaining one of E1, E2, E3 and E4 is H, halogen, C1-C6 alkyl or substituted C1-C6 alkyl; one of T1 and T2 is H, a hydroxyl protecting group or a phosphorus moiety and the other of T1 and T2 is H, a hydroxyl protecting group or a reactive phosphorus group; each substituted group comprises one or more optionally protected substituent groups independently selected from halogen, OJ5, N(J5)(J6), ═NJ5, SJ5, N3, CN, OC(=L)J5, OC(=L)N(J5)(J6) and C(=L)N(J5)(J6); L is O, S or NJ7; and each J5, J6 and J7 is, independently, H, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C5-C20 aryl or C1-C12 aminoalkyl.
地址 Carlsbad CA US