Cambridge id 5472671

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: Cambridge id 5472671
• 英文别名: 4-[2-(2,4,6-trimethylphenoxy)ethyl]morpholine
• 化学式: C₁₅H₂₃NO₂
• 分子量: 249.35
• InChiKey: BMCNSNITRUYHLG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] USES OF SATL-INDUCIBLE KINASE (SIK) INHIBITORS FOR TREATING OSTEOPOROSIS<br/>[FR] UTILISATIONS D'INHIBITEURS DE KINASE INDUCTIBLE PAR UN SEL (SIK) POUR TRAITER L'OSTÉOPOROSE
  申请人：MASSACHUSETTS GEN HOSPITAL

  公开号：WO2018053373A1

  公开（公告）日：2018-03-22

  The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI).

  本公开提供了使用盐诱导激酶（SIK）抑制剂治疗和/或预防骨质疏松症的方法。还提供了使用SIK抑制剂增加成骨细胞功能、增加成骨细胞数量、增加成骨细胞活性、抑制骨骼吸收、减少破骨细胞数量、抑制破骨细胞活性、增加骨骼质量、下调SOST基因表达和/或抑制硬化蛋白活性的方法。SIK抑制剂可以与Src抑制剂或CSF I R抑制剂结合使用。典型的SIK抑制剂包括公式：（I）、（II）、（III）、（IV）、（V）或（VI）的化合物。
• USES OF SALT-INDUCIBLE KINASE (SIK) INHIBITORS
  申请人：Dana Farber Cancer Institute, Inc.

  公开号：EP3536323A1

  公开（公告）日：2019-09-11

  The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inhibitors of Formula (II), and urea and carbamate SIK inhibitors of Formula (III-A) (e.g., urea and carbamate SIK inhibitors of Formula (III)).

  本公开提供了使用盐诱导激酶(SIK)抑制剂，如式(I)的大环SIK抑制剂、式(II)的咪唑基SIK抑制剂和式(III-A)的脲和氨基甲酸酯SIK抑制剂(例如，式(III)的脲和氨基甲酸酯SIK抑制剂)治疗和/或预防炎症性肠病(IBD)和移植物抗宿主病(GVHD)的方法。
• Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
  申请人：The General Hospital Corporation

  公开号：US11241435B2

  公开（公告）日：2022-02-08

  The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI).

  本公开提供了使用盐诱导激酶（SIK）抑制剂治疗和/或预防骨质疏松症的方法。还提供了使用 SIK 抑制剂增加骨细胞功能、增加成骨细胞数量、增加成骨细胞活性、抑制骨吸收、减少破骨细胞数量、抑制破骨细胞活性、增加骨质量、下调 SOST 基因表达和/或抑制硬骨素活性的方法。SIK 抑制剂可与 Src 抑制剂或 CSF I R 抑制剂结合使用。示例性 SIK 抑制剂包括式中的化合物：(I)、(II)、(III)、(IV)、(V)或(VI)式的化合物。
• USES OF SALT-INDUCIBLE KINASE (SIK) INHIBITORS FOR TREATING OSTEOPOROSIS
  申请人：The General Hospital Corporation

  公开号：US20200179387A1

  公开（公告）日：2020-06-11

  The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI).