N-[4-[(1S,2R)-2-(cyclopropylmethylamino)cyclopropyl]phenyl]-1-methylpyrazole-4-carboxamide | 1422620-34-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[4-[(1S,2R)-2-(cyclopropylmethylamino)cyclopropyl]phenyl]-1-methylpyrazole-4-carboxamide
• CAS: 1422620-34-5
• 化学式: C₁₈H₂₂N₄O
• 分子量: 310.4
• InChiKey: NTRMVYTYDOLCRU-DLBZAZTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  59
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• GFI1 inhibitors for the treatment of hyperglycemia
  申请人：INSERM (Institut National de la Santé et de la Recherche Médicale)

  公开号：US10980779B2

  公开（公告）日：2021-04-20

  The present invention relates to methods and pharmaceutical compositions useful for the treatment of hyperglycemia. Thorough multiple analyses, inventors demonstrated that Gfi1 is expressed in pancreatic acinar cells, starting from the first stages of pancreatic embryonic development. Furthermore, they observed that Gfi1 mRNA levels remain steady throughout embryonic development, while they significantly increase during the first days of life. They challenged conditional mutant mice with high fat diet for 5 months and monitored their weight and glycemia weekly. All the animals displayed a rapid increase in body mass as expected. While control mice rapidly developed a massive hyperglycemia, mutant mice remained normoglycemic throughout the entire experiment. A similar protection from induced diabetes was observed upon treatment with a high dose of Streptozotocin. Accordingly, the present invention relates to a method of treating hyperglycemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an inhibitor of Gfi1.

  本发明涉及治疗高血糖的方法和药物组合物。通过多种分析，发明者证明，从胰腺胚胎发育的最初阶段开始，Gfi1 就在胰腺尖突细胞中表达。此外，他们还观察到，Gfi1 mRNA 水平在整个胚胎发育过程中保持稳定，而在生命的最初几天则显著增加。他们对条件突变小鼠进行了为期5个月的高脂饮食挑战，并每周监测它们的体重和血糖。所有动物的体重都如预期般迅速增加。对照组小鼠迅速出现大量高血糖，而突变体小鼠在整个实验过程中血糖保持正常。在使用大剂量链脲佐菌素治疗时，也观察到了类似的保护作用，使其免于诱发糖尿病。因此，本发明涉及一种治疗有需要的受试者高血糖症的方法，包括向受试者施用治疗有效量的 Gfi1 抑制剂。
• CYCLOPROPANEAMINE COMPOUND
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2743256B1

  公开（公告）日：2018-06-27
• ENHANCING T-CELL FUNCTION AND TREATING A T-CELL DYSFUNCTIONAL DISORDER WITH A COMBINATION OF AN LSD INHIBITOR AND A PD1 BINDING ANTAGONIST
  申请人：Epiaxis Therapeutics Pty Ltd

  公开号：EP3716963A1

  公开（公告）日：2020-10-07
• Compositions for Modulating Cancer Stem Cells and Uses Therefor
  申请人：University of Canberra

  公开号：US20170266140A1

  公开（公告）日：2017-09-21

  Disclosed are compositions and methods for modulating cancer stem cells. More particularly, the present invention discloses the use of lysine demethylase (LSD) inhibitors and protein kinase C theta inhibitors (PKC-θ) for inhibiting the growth of LSD- and/or PKC-θ-overexpressing cells including cancer stem cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells, for treating cancer, including non-metastatic and metastatic cancer and/or for preventing cancer recurrence.
• GFI1 INHIBITORS FOR THE TREATMENT OF HYPERGLYCEMIA
  申请人：INSERM (Institut National de la Sante et de la Recherche Medicale)

  公开号：US20200030292A1

  公开（公告）日：2020-01-30

  The present invention relates to methods and pharmaceutical compositions useful for the treatment of hyperglycemia. Thorough multiple analyses, inventors demonstrated that Gfi1 is expressed in pancreatic acinar cells, starting from the first stages of pancreatic embryonic development. Furthermore, they observed that Gfi1 mRNA levels remain steady throughout embryonic development, while they significantly increase during the first days of life. They challenged conditional mutant mice with high fat diet for 5 months and monitored their weight and glycemia weekly. All the animals displayed a rapid increase in body mass as expected. While control mice rapidly developed a massive hyperglycemia, mutant mice remained normoglycemic throughout the entire experiment. A similar protection from induced diabetes was observed upon treatment with a high dose of Streptozotocin. Accordingly, the present invention relates to a method of treating hyperglycemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an inhibitor of Gfi1.