发明名称 CYCLOPROPAHETEROCYCLES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
摘要 Compounds of Formula (I), where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C 1- C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR8)n--D-(CHR8)m-; D is -NR9-, -O-, -S-, -S(=O)- or -S(=O)2-; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl;R9 is H, C1-C3 alkyl; n and m are independently 0 , 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug esca pe mutants.
申请公布号 CA2438524(A1) 申请公布日期 2002.09.12
申请号 CA20022438524 申请日期 2002.03.04
申请人 MEDIVIR AB 发明人 ODEN, LOURDES;NAESLUND, LOTTA;WALLBERG, HANS;KALYANOV, GENAIDY;SAHLBERG, CHRISTER;LINDSTROEM, STEFAN
分类号 C07D335/06;A61K31/4155;A61K31/422;A61K31/427;A61K31/428;A61K31/44;A61K31/4433;A61K31/4436;A61K31/4709;A61K31/497;A61K31/506;A61P31/18;A61P37/04;A61P43/00;C07C43/23;C07C245/18;C07D307/93;C07D311/78;C07D311/94;C07D401/12;C07D405/12;C07D407/12;C07D409/12;C07D413/12;C07D417/12;(IPC1-7):C07D405/12;C07D487/00;C07D403/12;A61K31/35 主分类号 C07D335/06
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