DITHIOAMINE REDUCING AGENTS
    73.
    发明公开
    DITHIOAMINE REDUCING AGENTS 审中-公开
    二硫代氨酸还原剂

    公开(公告)号:EP2814472A1

    公开(公告)日:2014-12-24

    申请号:EP13749206.2

    申请日:2013-02-15

    IPC分类号: A61K31/095

    摘要: Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention can be employed to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents of this invention can prevent inactivation of a given protein or enhance activation of a given protein or other biological molecule in vitro and/or in vivo. Reducing agents of this invention can prevent or reduce oxidation of cysteine residues in proteins and prevent the formation of reduced activity protein dimers (or other oligomers). Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents.

    摘要翻译: 用于还原二硫键的二硫代胺还原剂。 例如,本发明的还原剂可用于减少二硫键,特别是在蛋白质中,或防止形成二硫键,特别是在蛋白质和其他生物分子中。 本发明的还原剂可用于调节巯基与生物活性相关的蛋白质功能。 本发明的还原剂可防止给定蛋白质的失活或在体外和/或体内增强给定蛋白质或其他生物分子的活化。 本发明的还原剂可防止或减少蛋白质中半胱氨酸残基的氧化,并防止还原活性蛋白质二聚体(或其他寡聚体)的形成。 本发明的还原剂适用于各种生物应用,特别是作为研究和合成试剂。

    2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES
    75.
    发明公开
    2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES 有权
    2-甲基 - 维生素D-ANALOGE IN IHRE VERWENDUNGEN

    公开(公告)号:EP2768804A1

    公开(公告)日:2014-08-27

    申请号:EP12781531.4

    申请日:2012-10-11

    IPC分类号: C07C401/00

    摘要: This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-1α,25 -dihydroxy-2-methylene-vitamin D3 as well as (5E)-(20S)-1α,25-dihydroxy-2 -methylene-vitamin D3 and (20R)-1α,25-dihydroxy-2-methylene-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.

    摘要翻译: 本发明公开了2-亚甲基维生素D类似物,特别是(20S)-1α,25-二羟基-2-亚甲基维生素D3以及(5E) - (20S)-1α,25-二羟基-2-亚甲基 - 维生素D3和(20R)-1α,25-二羟基-2-亚甲基维生素D3,以及其用途。 这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出相对高的结合活性和显着的活性,从而证明其用作抗癌剂,特别是用于治疗或预防骨肉瘤,白血病,结肠癌,乳腺癌, 皮肤癌或前列腺癌。 这些化合物还具有相对较高的钙血活性,其用于治疗骨疾病。

    2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES
    76.
    发明公开
    2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES 有权
    2-甲基维生素D-ANALOGE UND DEREN VERWENDUNGEN

    公开(公告)号:EP2768803A1

    公开(公告)日:2014-08-27

    申请号:EP12778892.5

    申请日:2012-10-09

    IPC分类号: C07C401/00 A61K31/59

    摘要: This invention discloses 2-methylene- vitamin D analogs of formula ( I) (wherein R and X are as defined in claim 1 ), and specifically (20S)-25- hydroxy-2-methylene- vitamin D3 and (20R)-25-hydroxy-2-mcthylene-vitamin D3, as well as pharmaceutical uses therefor, These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti¬ cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing USC in the treatment of bone diseases. Formula (I).

    摘要翻译: 本发明公开了2-亚甲基 - 维生素D类似物,特别是(20S)-25-羟基-2-亚甲基维生素D3和(20R)-25-羟基-2-亚甲基维生素D3及其药物用途。 这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出相对高的结合活性和显着的活性,从而证明其用作抗癌剂,特别是用于治疗或预防骨肉瘤,白血病,结肠癌,乳腺癌, 皮肤癌或前列腺癌。 这些化合物还具有相对较高的钙血活性,其用于治疗骨疾病。

    Crystallization of 1alpha-hydroxy-2-methylene- 18,19-dinor-homopregnacalciferol
    77.
    发明公开
    Crystallization of 1alpha-hydroxy-2-methylene- 18,19-dinor-homopregnacalciferol 审中-公开
    Kristallisierung von 1alpha-羟基-2-亚甲基-18,19-二 - 均孕孕甾醇

    公开(公告)号:EP2746252A1

    公开(公告)日:2014-06-25

    申请号:EP12199224.2

    申请日:2012-12-21

    IPC分类号: C07C401/00

    摘要: A method of purifying 1α-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol to obtain 1α-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol in crystalline form using precipitation with hexane from ethyl acetate. A method of preparing 1α-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol crystals acceptable for X-ray experiment using precipitation with hexane from benzene by diffusive exchange of the solvents is also described.

    摘要翻译: 一种纯化1± - 羟基-2-亚甲基-18,19-二氢 - 孕代孕甾醇的方法,用己烷从乙酸乙酯沉淀得到结晶形式的1± - 羟基-2-亚甲基-18,19-二氢 - 孕代孕酸钙。 还描述了通过溶剂的扩散交换制备用苯与己烷一起沉淀的X射线实验可接受的1± - 羟基-2-亚甲基-18,19-二氢 - 均二孕烯雌酚晶体的方法。