RO5068760 | 947182-25-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: RO5068760
• 英文别名: (2S,3S)-2-{(R)-4-[4-((R)-2,3-dihydroxy-propoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl}-N-(2-fluoro-4-iodo-phenyl)-3-phenyl-butyramide；Unii-M58joz0T53；(2S,3S)-2-[(4R)-4-[4-[(2R)-2,3-dihydroxypropoxy]phenyl]-2,5-dioxoimidazolidin-1-yl]-N-(2-fluoro-4-iodophenyl)-3-phenylbutanamide
• CAS: 947182-25-4
• 化学式: C₂₈H₂₇FIN₃O₆
• 分子量: 647.442
• InChiKey: MEPDJWRMAAUPBM-VGUPLNMOSA-N

物化性质

• 密度：
  1.607±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  39
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  128
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  RO5068760 在 二氧化碳 、 甲醇 、 乙腈 作用下， 以 甲醇 为溶剂， 25.0~50.0 ℃ 、1333.22 MPa 条件下， 反应 54.0h， 以to obtain (2S,3S)-2-{(S)-4-[4-((R)-2,3-dihydroxy-propoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl}-N-(2-fluoro-4-iodo-phenyl)-3-phenyl-butyramide as a colorless solid (35 mg, 44%)的产率得到(2S,3S)-2-{(S)-4-[4-((R)-2,3-dihydroxy-propoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl}-N-(2-fluoro-4-iodo-phenyl)-3-phenyl-butyramide
  参考文献：
  名称：

  METHOD FOR INHIBITING PROLIFERATION OF TUMOR CELLS

  摘要：

  本发明揭示了一种通过将MEK抑制剂化合物和厄洛替尼与肿瘤细胞接触来协同抑制肿瘤细胞增殖的方法，无论是顺序还是同时进行。本发明还揭示了一种通过向人体内逐步或同时给予厄洛替尼和MEK抑制剂化合物的有效量来抑制人体内肿瘤细胞增殖的方法，这些量在组合时对协同抑制人体内肿瘤细胞增殖有效。

  公开号：

  US20080207563A1

文献信息

• Substituted hydantoins
  申请人：Chen Shaoqing

  公开号：US20070197617A1

  公开（公告）日：2007-08-23

  The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.

  本发明涉及公式化合物的方法，其制备方法以及它们的使用方法。这些化合物在治疗由MEK高活性特征的疾病中很有用。因此，这些化合物在治疗癌症、认知和中枢神经系统疾病以及炎症/自身免疫疾病等疾病中很有用。
• HYDANTOIN BASED KINASE INHIBITORS
  申请人：F.HOFFMANN-LA ROCHE AG

  公开号：EP1989186A1

  公开（公告）日：2008-11-12
• COMPOUNDS AND METHODS FOR THE TREATMENT OF ITCH
  申请人：Westfälische Wilhelms-Universität Münster

  公开号：EP3169365A2

  公开（公告）日：2017-05-24
• USE OF NEUROKININ-1 ANTAGONISTS TO TREAT A VARIETY OF PRURITIC CONDITIONS
  申请人：MENLO THERAPEUTICS INC.

  公开号：US20190216779A1

  公开（公告）日：2019-07-18

  The disclosure relates to the use of neurokinin-1 (NK-1) antagonists, such as serlopitant, in treating acute or chronic pruritus associated with a variety of medical conditions, including dermatitis/eczema, psoriasis, prurigo, urticaria, cutaneous T-cell lymphoma, epidermolysis bullosa, bums and hepato-biliary diseases, or/and treating the medical conditions themselves. One or more additional antipruritic or therapeutic agents can optionally be used in combination with an NK-1 antagonist to treat acute or chronic pruritus associated with a medical condition or/and the medical condition itself.
• COMBINATION THERAPIES
  申请人：Mirati Therapeutics, Inc.

  公开号：US20220395507A1

  公开（公告）日：2022-12-15

  The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a SOS1 inhibitor and a KRas G12C inhibitor, pharmaceutical compositions comprising a such compositions, kits comprising such compositions and methods of use therefor.