发明名称 SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
摘要 Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
申请公布号 US2015005251(A1) 申请公布日期 2015.01.01
申请号 US201414312990 申请日期 2014.06.24
申请人 Alios BioPharma, Inc. 发明人 Dyatkina Natalia;Wang Guangyi;Beigelman Leonid;Rajwanshi Vivek Kumar
分类号 C07H19/20;C07H19/16;A61K45/06;A61K31/7072;A61K31/7068;A61K31/708;C07H19/06;C07H19/10 主分类号 C07H19/20
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 a C1-6 azidoalkyl or a C1-6 aminoalkyl; R3A is selected from the group consisting of OH, —OC(═O)R″A and an optionally substituted O-linked amino acid; R4A is halogen; R5A is hydrogen or halogen; 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)q—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, NR30AR31A, 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, R13A and R14A are independently absent or hydrogen; 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 and R29A are independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl and an optionally substituted aryl; R26A and R27A 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; R28A 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; R30A and R31A 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 and an optionally substituted C3-6 cycloalkenyl; 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; r is 1 or 2; s is 0, 1, 2 or 3; u is 1 or 2; and Z1A, Z2A, Z3A and Z4A are independently O or S.
地址 South San Francisco CA US