5-[[[trans-1-methyl-2-phenylcyclopropyl]amino]methyl]-1,3,4-oxadiazol-2-amine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 5-[[[trans-1-methyl-2-phenylcyclopropyl]amino]methyl]-1,3,4-oxadiazol-2-amine
• 英文别名: 5-[[(1-Methyl-2-phenylcyclopropyl)amino]methyl]-1,3,4-oxadiazol-2-amine；5-[[(1-methyl-2-phenylcyclopropyl)amino]methyl]-1,3,4-oxadiazol-2-amine
• 化学式: C₁₃H₁₆N₄O
• 分子量: 244.296
• InChiKey: NNVMCQRRXNZZQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  77
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 以77%的产率得到5-[[[trans-1-methyl-2-phenylcyclopropyl]amino]methyl]-1,3,4-oxadiazol-2-amine
  参考文献：
  名称：

  [EN] CYCLOPROPYLAMINE DERIVATIVES USEFUL AS INHIBITORS OF HISTONE DEMETHYLASES KDM1A
  [FR] DÉRIVÉS DE CYCLOPROPYLAMINE UTILES EN TANT QU'INHIBITEURS DE HISTONE DÉMÉTHYLASES KDM1A

  摘要：

  本发明涉及一般式(I)的环丙基衍生物，其中A、R1和R2如规范中定义。本申请还涉及含有这类化合物的药物组合物以及它们在治疗中的应用。

  公开号：

  WO2014086790A1

文献信息

• CYCLOPROPYLAMINE DERIVATIVES USEFUL AS INHIBITORS OF HISTONE DEMETHYLASES KDM1A
  申请人：INSTITUTO EUROPEO DI ONCOLOGIA S.R.L.

  公开号：US20150315126A1

  公开（公告）日：2015-11-05

  The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R 1 , and R 2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

  本发明涉及一般式(I)的环丙基衍生物，其中A、R1和R2如规范中所定义。本申请还涉及含有这种化合物的药物组合物以及它们在治疗中的使用。
• USE OF A COMBINATIONAL THERAPY OF LSD1 INHIBITORS WITH CDK2 INHIBITORS IN THE TREATMENT OF CANCER
  申请人：Rasna Therapeutics Limited

  公开号：US20180311245A1

  公开（公告）日：2018-11-01

  The present disclosure relates to methods of treating cancer and pharmaceutical compositions for use in the treatment of cancer, including LSD1-inhibitor-resistant cancers, comprising administering to a subject an effective amount of a CDK2 inhibitor and an effective amount of a LSD1 inhibitor.
• USE OF A COMBINATIONAL THERAPY OF LSD1 INHIBITORS WITH P21 ACTIVATORS IN THE TREATMENT OF CANCER
  申请人：Istituto Europeo di Oncologia S.r.l.

  公开号：US20210100800A1

  公开（公告）日：2021-04-08

  The present disclosure relates to methods of treating cancer and pharmaceutical compositions for use in the treatment of cancer, including LSD1-inhibitor-resistant cancers, comprising administering to a subject an effective amount of a cell cycle inhibitor, such as a CDK4/6 inhibitor or a p21 enhancer, and an effective amount of a LSD1 inhibitor.
• US9944589B2
  申请人：——

  公开号：US9944589B2

  公开（公告）日：2018-04-17
• [EN] COMBINATION OF CALORIC RESTRICTION (CR) OR IGF1/INSULIN RECEPTOR INHIBITOR WITH LSD1 INHIBITOR<br/>[FR] COMBINAISON D'UNE RESTRICTION CALORIQUE OU D'UN INHIBITEUR DES RÉCEPTEURS À L'IGF1/INSULINE AVEC UN INHIBITEUR DE LSD1
  申请人：ST EUROPEO DI ONCOLOGIA

  公开号：WO2017097865A1

  公开（公告）日：2017-06-15

  The present application relates to the use of an LSD1 inhibitor in combination with a caloric restricted diet, a calorie restriction mimetic and/or an IGF1/Insulin receptor inhibitor for the treatment of cancer, e.g., a leukemia, such as acute myeloid leukemia, acute promyelocytic leukemia.