| 摘要 |
The present invention provides compounds of formula (I), wherein x is zero, 1 or 2; R<1> and R<6> are each independently hydrogen, C1-4alkyl or CH2C1-3alkyl where the C1-3alkyl portion is substituted by OH; R<2>, R<3>, R<4> and R<5> are each independently hydrogen, methyl, ethyl, CH2OH,CH2NH2 or COOH when x is zero, or R<2>, R<3>, R<4> and R<5> are each independently hydrogen, methyl or CH2OH when x is 1 or 2; R<7> and R<9> are each independently hydrogen, C1-10alkyl, C3-8cycloalkyl, ArC1-4alkyl, HetC1-4alkyl, COAr, COHet, COCH2R<13>, COCH(OH)Ar, COCH(OH)Het, COCH=CHPh, COR<14>, CO2CH2Ar, CO2CH2Het, SO2Ar, SO2Het,SO2CH2R<15>, SO2CH=CHPh or SO2R<16>[where R<13> and R<15> each independently represent hydrogen, C1-6alkyl, aryl, heteroaryl, ArC1-4alkyl, HetC1-4alkyl, aryloxy, heteroaryloxy, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, (CH2)nCO2R<17> (where n is zero or 1 and R<17> is hydrogen or C1-6alkyl), (CH2)mNR<18>R<19> (where m is zero, 1, 2, 3, 4 or 5 and R<19> are each independently hydrogen or C1-4alkyl or together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group), and R<14> and R<16> each independently represent C3-8cycloalkyl substituted by phenyl]; R<8> and R<10> are each independently hydrogen, C1-6alkyl, COOR<20> (where R<20> is hydrogen, C1-6alkyl or ArC1-4alkyl) or CONR<21>R<22>[where R<21> is hydrogen or C1-4alkyl and R<22> is hydrogen, OH, aryl, heteroaryl, ArC1-4alkyl (wherein the C1-4alkyl portion is optionally substituted by hydroxymethyl), HetC1-4alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, (CH2pR<23> (where p is zero or 1 and R<23> is CF3 or CO2R<24> where R<24> is hydrogen or C1-6alkyl), (CH2)qNR<25>R<26> (where q is zero, 1, 2, 3, 4, or 5 and R<25> and R<26> are each independently hydrogen, C1-4alkyl or aryl or together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group), CHArCO2R<27>, CHHet CO2R<28> (where R<27> and R<28> are each independently hydrogen or C1-6alkyl) or C1-6alkyl optionally substituted by OH, or R<21> and R<22> together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group]; R<11> and R<12> are each independently hydrogen, hydroxy or acetoxy; and physiologically acceptable salts and solvates thereof. Also described are the use of the compounds as antiviral agents, pharmaceutical compositions containing them and methods for their preparation. |
