发明名称 Nucleoside cyclicphosphates
摘要 Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:;
申请公布号 US8759510(B2) 申请公布日期 2014.06.24
申请号 US201213439991 申请日期 2012.04.05
申请人 Gilead Pharmasset LLC 发明人 Du Jinfa;Nagarathnam Dhanapalan;Pamulapati Ganapati Reddy;Ross Bruce S.;Sofia Michael Joseph
分类号 A01N43/04;A61K31/70;C07H19/00;C07H19/04;C07H19/20 主分类号 A01N43/04
代理机构 Sheppard Mullin Richter & Hampton LLP 代理人 Sheppard Mullin Richter & Hampton LLP
主权项 1. A compound of formula I:or a stereoisomer, salt, hydrate, solvate, deuterated analogue, or crystalline form thereof, wherein R1 is n-alkyl, branched alkyl, cycloalkyl, alkaryl, phenyl or naphthyl, where the phenyl or naphthyl is optionally substituted with at least one of F, Cl, Br, I, OH, OR′, SH, SR′, NH2, NHR′, NR′2, NHR′2+, NR′3+, C1-C6 alkyl, halogenated C1-C6 alkyl, halogenated C2-C6 alkenyl, C2-C6 alkynyl, halogenated C2-C6 alkynyl, C1-C6 alkoxy, halogenated C1-C6 alkoxy, CO2H, CO2R′, CONH2, CONHR′, CONR′2, CH═CHCO2H, or CH═CHCO2R′; R2 is of H, optionally substituted alkyl, cyano, CH3, vinyl, O-alkyl, O—(C1-C6 alkyl), hydroxyl C1-C6 alkyl, fluoromethyl, azido, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, optionally substituted ethynyl alkyne, or halogen; R3 is CH3, CH2F, CHF2, CF3, F, or CN; X is F, OCH3, halogen, NH2, or N3; Base is of formula b: wherein R4 and R5 are independently H, F, CI, Br, I, OH, OR′, SH, SR′, NH2, NHR′, NR′2, NHR′2+, NR′3+, heterocycle, C1-C6 alkyl, halogenated C1-C6 alkyl, C2-C6 alkenyl, halogenated C2-C6 alkenyl, C2-C6 alkynyl, halogenated C2-C6 alkynyl, C1-C6 alkoxy, halogenated C1-C6 alkoxy, CO2H, CO2R′, CONH2, CONHR′, CONR′2, CH═CHCO2H, or CH═CHCO2R′; and wherein R′ is an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted alkynyl, an optionally substituted alkenyl, an optionally substituted acyl, or an optionally substituted alkoxyalkyl, where for the instance of NR′2 or NHR′2+, each R′ is independent of one another or both R′ are joined to form a heterocycle comprising at least two carbon atoms, and where for the instance of NR′3+, each R′ is independent of one another or at least two R′ are joined to form a heterocycle comprising at least two carbon atom.
地址 Foster City CA US
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