Mixtures of alkylated methylolated 4,5-dihydroxy-imidazolidin-2-ones
    4.
    发明授权
    Mixtures of alkylated methylolated 4,5-dihydroxy-imidazolidin-2-ones 失效
    烷基化羟甲基化的4,5-二羟基 - 咪唑烷-2-酮的混合物

    公开(公告)号:US06265589B1

    公开(公告)日:2001-07-24

    申请号:US09331583

    申请日:1999-06-30

    IPC分类号: C07D23340

    摘要: Described is a process for preparing mixtures of mixed-alkylated methylolated 4,5-dihydroxyimidazolidin-2-ones by reaction of methylolated 4,5-dihydroxyimidazolidin-2-one (DMDHEU) with a monohydric C1-5 alcohol and a polyol selected from the group consisting of ethylene glycol, diethylene glycol, 1,2-propylene glycol, 1,3-propylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, glycerol and polyethylene glycols of the formula HO(CH2CH2O)nH where 3≦n≦20, the monohydric C1-5 alcohol and the polyol each being used in an amount of from 0.1 to 2.0 mol equivalents, based on DMDHEU, and the reaction being carried out at temperatures from 20° C. to 70° C. and at a pH of from 1 to 2.5, and the pH being set to a value of from 4 to 8 after the reaction.

    摘要翻译: 描述了通过羟甲基化的4,5-二羟基咪唑烷-2-酮(DMDHEU)与一元C 1-5醇和选自以下的多元醇的反应制备混合烷基化的羟甲基化的4,5-二羟基咪唑烷-2-酮的混合物的方法: 由乙二醇,二甘醇,1,2-丙二醇,1,3-丙二醇,1,2-丁二醇,1,3-丁二醇,1,4-丁二醇,甘油和聚乙二醇组成的组 式中HO(CH 2 CH 2 O)nH其中3 <= n <= 20,一元C 1-5醇和多元醇的用量为0.1至2.0摩尔当量,基于DMDHEU,反应在温度 从20℃至70℃,pH为1〜2.5,反应后pH设定为4〜8。

    Process for producing 4,5-dihydroxy-2-imidazolidinones
    5.
    发明授权
    Process for producing 4,5-dihydroxy-2-imidazolidinones 失效
    制备4,5-二羟基-2-咪唑啉酮的方法

    公开(公告)号:US4650877A

    公开(公告)日:1987-03-17

    申请号:US664793

    申请日:1984-10-25

    CPC分类号: C07D233/40

    摘要: The invention concerns a process for producing cyclic ureas of the general formula (II): ##STR1## in which R is selected from the group comprising hydrogen atom and C.sub.1 -C.sub.4 alkyl radicals through condensation in aqueous medium at a pH of between 4 and 7 and at a temperature of between 40.degree. and 60.degree. C. of glyoxal with or without excess of a urea having the general formula (I):RNH--CO--NHR (I)in which R has the same meaning as above, said process being conducted in the presence of a catalytic amount of orthophosphoric acid.

    摘要翻译: 本发明涉及一种制备通式(II)的环脲的方法:其中R选自氢原子和C 1 -C 4烷基基团,其中R是在水介质中, 在具有或不含过量具有通式(I)的脲的乙二醛的温度为40至60℃的温度下,在其中R具有与上述相同的含义的RNH-CO-NHR(I) 所述方法在催化量的正磷酸的存在下进行。

    Substituted Dihydroimidazoles and their Use in the Treatment of Tumors
    10.
    发明申请
    Substituted Dihydroimidazoles and their Use in the Treatment of Tumors 审中-公开
    取代的二氢咪唑及其在肿瘤治疗中的应用

    公开(公告)号:US20100075966A1

    公开(公告)日:2010-03-25

    申请号:US12516414

    申请日:2007-11-26

    摘要: The invention relates to dihydroimidazoles of formula rac-(I), wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.

    摘要翻译: 本发明涉及式rac-(I)的二氢咪唑,其中基团和符号如本文所定义; 它们作为MDM2蛋白与p53样肽的相互作用的抑制剂的用途,包含所述化合物的新药物制剂,用于治疗温血动物,特别是人类的所述化合物,其用于治疗增殖性疾病 或用于制造用于治疗对MDM2蛋白与p53样肽的相互作用的调节作出反应的增殖性疾病的药物制剂,药物制剂例如 可用于治疗对MDM2蛋白与包含所述化合物的p53样肽的相互作用的调节作用的增殖性疾病的治疗,所述方法包括向温血动物施用所述化合物和/或制备方法 的所述化合物。