发明名称 THIOUREA COMPOUNDS AND THEIR USE AS INHIBITORS OF SIRT2 OR SIRT5
摘要 A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.;
申请公布号 US2016130246(A1) 申请公布日期 2016.05.12
申请号 US201414896057 申请日期 2014.06.06
申请人 CORNELL UNIVERSITY 发明人 LIN Hening
分类号 C07D335/06;C07C335/08 主分类号 C07D335/06
代理机构 代理人
主权项 1. A compound useful as a Sirt2 or Sirt5 inhibitor having the formula: wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group optionally includes one heteroatom group selected from —O—, —NR5—, and —S— that interrupts a carbon-carbon bond of said hydrocarbon group, and wherein one or more hydrogen atoms in said hydrocarbon group are optionally replaced with fluoro atoms, and wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, amino acids, dipeptides, tripeptides, oligopeptides, proteins, nucleobases, nucleotides, dinucleotides, trinucleotides, oligonucleotides, monosaccharides, disaccharides, oligosaccharides, and protecting groups, wherein R4 may optionally be selected from OR5, N(R5)2, and SR5; and R5 is independently selected from hydrogen atom and hydrocarbon groups.
地址 Ithaca NY US