Jeffrey, B.,Джефри Б.,Colleen, B.,Коллин Б.,William, B.,Вильям Б.
申请号：
EA200970261
公开号：
EA016830B1
申请日:
2007.09.11
申请国别(地区):
EA
年份:
2012
代理人:
摘要：
The invention provides azole nucleosides represented by the formulae (I) and (II) wherein A=C or N B=C or N X=H, C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br and I, OH, NH2, NH-(C1-C6 alkyl, cycloalkyl, aryl, or heterocyclo) Z=H, C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I, OH, NH2, NH-(C1-C6alkyl, cycloalkyl, aryl, or heterocyclo) E=(CH2)nONHR1 n is an integer from 0-6 and more typically 0-3 R1=aryl or heterocyclo each of W, Y, R is individually selected from the group consisting of H, C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, and I, O, OH, O-alkyl, O-aryl, NH2, NH-(C1-C6alkyl, cycloalkyl, aryl, or heterocyclo) provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be =O and each D individually is OH, O-alkyl, O-aryl, Fl and H pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided. Compounds of this disclosure are useful as inhibitors of viral RNA and DNA polymerases such as, but not limited to, Influenza, Hantaan Virus, Crimean Congo hemorrhagic fever virus, hepatitis B, hepatitis C, Polio, Coxsackie A and B, Rhino, Echo, orthopoxvirus (small pox), HIV, Ebola, and West Nile virus polymerases and especially orthopoxvirus, HIV, and hepatitis B.Изобретение обеспечивает азольные нуклеозиды, представленные формулами (I) и (II), где А = С или N В = С или N X = Н С1-С6алкил, циклоалкил, алкенил, циклоалкенил, алкинил, арил гетероцикло, галоген, в частности F, Cl, Br и I ОН, NH2, NH-(С1-С6алкил, циклоалкил, арил или гетероцикло), Z = Н, С1-С6алкил, циклоалкил, алкенил, циклоалкенил, алкинил, арил, гетероцикло, галоген, в частности F, Cl, Br и I ОН, NH2, NH-(С1-С6алкил, циклоалкил, арил или гетероцикло) Е = (CH2)nONHR1, n - целое число от 0 до 6, более типично 0-3 R1 = арил или гетероцикло каждый из W, Y, R отдельно вы
