发明名称 Pyrimidine compounds having phosphonate groups as antiviral nucleotide analogs
摘要 Disclosed are antiviral nucleotide analogs of formula (I) wherein: R1 is H, amino, or methylsulfanyl; R2 is H, methyl, halo, -N(R5)2, hydroxy, or protected hydroxy; R3 is independently methyl, hydroxymethyl, halomethyl, or protected hydroxymethyl; R4 is selected from alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, -CH2OH, -CH2OR5, -CH2C(O)R5, -CH2R6, ûCH2OC(O)R5, ûCH2OC(O)CH(R7)(NHR8), ûCH2NR9R10, -CH2CN, -CO2R5, ûCH2CH2OH, -CH2CH2OR5, -CH2CH2OC(O)R-5, -CH2CH2OC(O)CH(R7)(NHR8), -CH2SH, -C(O)H, -CH2CO2R9, -CH2SO3H, -CH2CH2SO3H, -CH2CH2PO3H2, -CH2CH2OCH2PO3H2, -CH2OPO3H2, -OCH2PO3H2, -OH, ûOR10, -NH2, -NR11R12, -SH, ûSR5, -SCN, -N3, -CN, ûCONR11R-12, -CH2CONR11R12, -NHOH, ûNHOR5, -NO, -NO2, ûNHNR11R12, 2-halovinyl, 3,3,3-trifluoropropenyl, 2-(alkoxycarbonyl)ethenyl, 2-carboxyethenyl, 2-cyanoethenyl, difluoromethyl, trifluoromethyl, 2,2,2-trifluoroethyl, 2-haloethyl, and -CH2N3; X independently is oxygen, sulfur, or a bond; Z independently is hydroxy, an ester or amide; and the remainder of the substituents are as described in the specification.
申请公布号 NZ543864(A) 申请公布日期 2009.10.30
申请号 NZ20040543864 申请日期 2004.06.16
申请人 K.U. LEUVEN RESEARCH & DEVELOPMENT;INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY, ACADEMY OF SCIENCES OF THE CZECH REPUBLIC 发明人 BALZARINI, JAN MARIE RENE;DE CLERCQ, ERIK DESIRE ALICE;HOCKOVA, DANA;HOLY, ANTONIN
分类号 C07F9/6512;A61K31/505;A61P31/12 主分类号 C07F9/6512
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