Backfunctionalized imidazolinium salts and NHC carbene-metal complexes

    公开(公告)号:US10538494B2

    公开(公告)日:2020-01-21

    申请号:US16103267

    申请日:2018-08-14

    IPC分类号: C07D233/28 C07F15/00

    摘要: Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each selected from the group consisting of a C1-C20 alkyl group, C1-C20 partially fluorinated alkyl group, an aryl group, an aryl group with para CF3 functionality, an aryl group having C1-C20 partially fluorinated alkyl groups or partially fluorinated alkoxy groups, and a C1-C20 partially fluorinated aliphatic group, and a C1-C20 aryl group; and X is an anion. The method comprises cyclization of a halogenated acrylate with a formamidine with Hünig's base in a solvent.

    BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES

    公开(公告)号:US20180370920A1

    公开(公告)日:2018-12-27

    申请号:US16103267

    申请日:2018-08-14

    IPC分类号: C07D233/28 C07F15/00

    摘要: Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each selected from the group consisting of a C1-C20 alkyl group, C1-C20 partially fluorinated alkyl group, an aryl group, an aryl group with para CF3 functionality, an aryl group having C1-C20 partially fluorinated alkyl groups or partially fluorinated alkoxy groups, and a C1-C20 partially fluorinated aliphatic group, and a C1-C20 aryl group; and X is an anion. The method comprises cyclization of a halogenated acrylate with a formamidine with Hünig's base in a solvent.

    SUBSTITUTED HETEROCYCLES AS THERAPEUTIC AGENTS FOR TREATING CANCER
    7.
    发明申请
    SUBSTITUTED HETEROCYCLES AS THERAPEUTIC AGENTS FOR TREATING CANCER 审中-公开
    作为治疗癌症的治疗药物的替代治疗剂

    公开(公告)号:US20130211079A1

    公开(公告)日:2013-08-15

    申请号:US13841648

    申请日:2013-03-15

    摘要: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.

    摘要翻译: MDM2和MDM4蛋白通过负调节转录因子p53阻止癌细胞的凋亡。 根据式I的化合物是MDM2和MDM4蛋白的选择性拮抗剂,破坏p53 / MDM2和p53 / MDM4复合物。 因此,这些化合物是用于治疗癌症以及其它细胞增殖性疾病状态的候选治疗剂。

    Pharmaceutical composition
    10.
    发明授权
    Pharmaceutical composition 有权
    药物组成

    公开(公告)号:US08202898B1

    公开(公告)日:2012-06-19

    申请号:US13365785

    申请日:2012-02-03

    摘要: To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

    摘要翻译: 提供含有在水性载体中具有高溶解度和高稳定性的2-硝基咪唑衍生物的药物组合物。 该药物组合物的特征在于含有1-(1-羟甲基-2,3-二羟丙基)氧甲基-2-硝基咪唑和肌酸酐,相对于1质量份的1-(1 - 羟基甲基-2,3-二羟丙基)氧基甲基-2-硝基咪唑。