发明名称 HETEROATOM CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
摘要 Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions in a method of treating cancer. The dUTPase inhibitors disclosed contain a uracil isostere in the molecule represented by a 2,6-diketopiperazine moiety. Thioanalogs of the uracil isostere where a thione replaces each of the ketone are also disclosed.
申请公布号 US2016326149(A1) 申请公布日期 2016.11.10
申请号 US201515109616 申请日期 2015.01.02
申请人 UNIVERSITY OF SOUTHERN CALIFORNIA 发明人 Ladner Robert D.;Giethlen Bruno
分类号 C07D413/06;C12Q1/68;A61K31/496;A61K31/513;C07D403/06;A61K31/5377 主分类号 C07D413/06
代理机构 代理人
主权项 1. A compound, or a tautomer thereof, including any stereoisomer, enantiomer or diastereoisomer, or a pharmaceutically acceptable salt and/or a solvate thereof of each thereof of formula (III): wherein A is each V is independently O or S, R11 is hydrogen, halo, R12 or —O—R12, wherein R12 is C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl optionally substituted with 1-3 hydroxy, fluoro, chloro, and amino substituent, r is 1, 2, or 3, Y10 is O, S, SO, SO2, NH or NR15, or L1 is joined at Y10 with Y10 being a nitrogen atom; R15 is C1-C6 alkyl optionally substituted with 1-3 C1-C6 alkoxy, hydroxy, amino, and oxo groups, L1- is Y1 is CH2, O, S, X10 is NH, NCO2R20, O, —CO—, —CO—NH—, or CH2, R20 is C1-C6 alkyl optionally substituted with 1-3 C6-C10 aryl groups, u is 0, 1, 2, 3, or 4, Rz is hydroxy or hydrogen, Rw is C1-C6 alkyl or hydrogen, and the phenylene and the heteroarylene rings are optionally substituted, Z is phenyl or a 5 or 6 member heteroaryl substituted with an R6 and an R60 groups, wherein the R6 and the R60 are positioned 1,2 with respect to each other, R6 is hydrogen, optionally substituted C1-C6 alkoxy, or halo, and R60 is —OR7 or —NHR7R70, R7 is optionally substituted C1-C10 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C5 cycloalkyl, optionally substituted C3-C10 heteroaryl, optionally substituted C3-C10 heterocyclyl, or optionally substituted phenyl, and R70 is hydrogen or R7.
地址 Los Angeles CA US