发明名称 SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
摘要 Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus infection with one or more nucleosides, nucleotides and nucleotide analogs.
申请公布号 US2016176910(A1) 申请公布日期 2016.06.23
申请号 US201514971926 申请日期 2015.12.16
申请人 ALIOS BIOPHARMA, INC. 发明人 Wang Guangyi;Smith David Bernard;Beigelman Leonid;Jekle Christian Andreas
分类号 C07H19/06;C07H19/10 主分类号 C07H19/06
代理机构 代理人
主权项 1. A compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: B1A is an optionally substituted heterocyclic base or an optionally substituted heterocyclic base with a protected amino group; RA is hydrogen or deuterium; R1A is selected from the group consisting of hydrogen, an optionally substituted acyl, an optionally substituted O-linked amino acid, Ra1 and Ra2 are independently hydrogen or deuterium; R2A is an unsubstituted C1-4 alkyl, an unsubstituted C2-4 alkenyl, an unsubstituted C2-4 alkynyl, a C1-6 haloalkyl, a C1-6 azidoalkyl or a C1-6 aminoalkyl; R3A is selected from the group consisting of hydrogen, deuterium, halo, OH, —OC(═O)R″A and an optionally substituted O-linked amino acid; R4A is hydrogen or deuterium; R5A is hydrogen, deuterium, halogen, N3, OH, an optionally substituted C1-6 alkyl, an optionally substituted C2-6 alkenyl and an optionally substituted C2-6 alkynyl; R6A, R7A and R8A are independently selected from the group consisting of absent, hydrogen, an optionally substituted C1-24 alkyl, an optionally substituted C3-24 alkenyl, an optionally substituted C3-24 alkynyl, an optionally substituted C3-6 cycloalkyl, an optionally substituted C3-6 cycloalkenyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aryl(C1-6 alkyl), an optionally substituted *—(CR15AR16A)p—O—C1-24 alkyl, an optionally substituted *—(CR17AR18A)O—C1-24 alkenyl,or R6A isand R7A is absent or hydrogen; or R6A and R7A are taken together to form a moiety selected from the group consisting of an optionally substitutedand an optionally substitutedwherein the oxygens connected to R6A and R7A, the phosphorus and the moiety form a six-membered to ten-membered ring system; R9A is independently selected from the group consisting of an optionally substituted C1-24 alkyl, an optionally substituted C2-24 alkenyl, an optionally substituted C2-24 alkynyl, an optionally substituted C3-6 cycloalkyl, an optionally substituted C3-6 cycloalkenyl, NR31AR32A, an optionally substituted N-linked amino acid and an optionally substituted N-linked amino acid ester derivative; R10A and R11A are independently an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative; R12A and R13A are independently absent or hydrogen; R14A is O−, OH or methyl; each R15A, each R16A, each R17A and each R18A are independently hydrogen, an optionally substituted C1-24 alkyl or alkoxy; R19A, R20A, R22A and R23A are independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl and an optionally substituted aryl; R21A and R24A are independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl, an optionally substituted aryl, an optionally substituted —O—C1-24 alkyl, an optionally substituted —O-aryl an optionally substituted —O-heteroaryl, an optionally substituted —O-monocyclic heterocyclyl and R25A, R26A and R30A are independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl and an optionally substituted aryl; R27A and R28A are independently —C≡N or an optionally substituted substituent selected from the group consisting of C2-8 organylcarbonyl, C2-8 alkoxycarbonyl and C2-8 organylaminocarbonyl; R29A is selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl, an optionally substituted C2-24 alkenyl, an optionally substituted C2-24 alkynyl, an optionally substituted C3-6 cycloalkyl and an optionally substituted C3-6 cycloalkenyl; R31A and R32A are independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl, an optionally substituted C2-24 alkenyl, an optionally substituted C2-24 alkynyl, an optionally substituted C3-6 cycloalkyl, an optionally substituted C3-6 cycloalkenyl and an optionally substituted aryl(C1-4 alkyl); R″A is an optionally substituted C1-24 alkyl; m and t are independently 0 or 1; p and q are independently selected from the group consisting of 1, 2 and 3; s is 0, 1, 2 or 3; r and u are independently 1 or 2; y is 3, 4 or 5; and Z1A, Z2A, Z3A and Z4A are independently O or S.
地址 South San Francisco CA US