发明名称 NUCLEOSIDE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C
摘要 Use of compounds of formula (I), wherein R<1> is hydrogen, hydroxy, alkyl, hydroxyalkyl, alkoxy, halogen, cyano, isocyano or azido; R<2> is hydrogen, hydroxy, alkoxy, chlorine, bromine or iodine; R<3> is hydrogen; or R<2> and R<3> together represent =CH2; or R<2> and R<3> represent fluorine; X is O, s or CH2; a, b, c, d denoting asymmetric carbon atoms each of which is substituted with 4 different substituents; and B signifies a purine base B1 which is connected through the 9-nitrogen of formula (B1), wherein R<4> is hydrogen, hydroxyl, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR<7>R<8>, halogen or SH; R<5> is hydrogen, hydroxy, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR<7>R<8>, NHOR<9>, NHNR<7>R<8> or SH; R<6> is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR<7>R<8>, halogen, SH or cyano; R<7> and R<8> are independently of each other hydrogen, alkyl, aryl, hydroxyalkyl, alkenylalkyl, alkynylalkyl, cycloalkyl or acyl; R<9> is hydrogen, alkyl or aryl; or B signifies an oxidised purine base B2 which is connected through the 9-nitrogen of formula (B2), wherein R<4>, R<5> and R<6> are as defined above; or B signifies a purine base B3 which is connected through the 9-nitrogen of formula (B3), wherein R<4> and R<6> are as defined above; R<10> is hydrogen, alkyl or aryl; Y is O, S or NR<11>; R<11> is hydrogen, hydroxy, alkyl, OR<9>, heterocyclyl or NR<7>R<8>; R<7>, R<8> and R<9> are as defined above; or B signifies a pyrimidine base B4 which is connected through the 1-nitrogen of formula (B4), wherein Z is O or S; R<12> is hydrogen, hydroxy, alkyl, alkoxy, haloalkyl, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR<7>R<8>, NHOR<9>, NHNR<7>R<8> or SH; R<13> is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl or halogen; R<7>, R<8> and R<9> are as defined above; or B signifies a pyrimidine base B5 which is connected through the 1-nitrogen of formula (B5), wherein Y, Z, R<10> are as defined above for the treatment of diseases mediated by the Hepatitis C Virus (HIV) or for the preparation of a medicament for such treatment. The invention is concerned with novel and known purine and pyrimidine nucleoside derivatives, their use as inhibitors of subgenomic Hepatitis C Virus (HCV) RNA replication and pharmaceutical compositions of such compounds.
申请公布号 WO0218404(A3) 申请公布日期 2002.11.14
申请号 WO2001EP09633 申请日期 2001.08.21
申请人 F. HOFFMANN-LA ROCHE AG 发明人 DEVOS, RENE;DYMOCK, BRIAN, WILLIAM;HOBBS, CHRISTOPHER, JOHN;JIANG, WEN-RONG;MARTIN, JOSEPH, ARMSTRONG;MERRETT, JOHN, HERBERT;NAJERA, ISABEL;SHIMMA, NOBUO;TSUKUDA, TAKUO
分类号 C07H19/067;A61K31/7064;A61K31/7076;A61K31/708;A61P1/16;A61P9/10;A61P9/14;A61P29/00;A61P31/04;A61P31/12;A61P31/14;A61P35/00;A61P37/04;A61P43/00;C07H19/06;C07H19/073;C07H19/09;C07H19/16;C07H19/167;C07H19/173 主分类号 C07H19/067
代理机构 代理人
主权项
地址