N-(3,4-dimethylphenyl)-3-(trifluoromethyl)benzamide

• 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-(3,4-dimethylphenyl)-3-(trifluoromethyl)benzamide
• 化学式: C₁₆H₁₄F₃NO
• 分子量: 293.28
• InChiKey: QCOLMNZWCBFLJX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER
  申请人：Rajapakse Hemaka A.

  公开号：US20100113415A1

  公开（公告）日：2010-05-06

  The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.

  本发明涉及一般式(I)的化合物，它们是ephrin A4的抑制剂。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物和组合物治疗由EphA4 RTK信号调节的疾病，如神经系统和神经退行性疾病以及癌症。
• Compounds for use in inhibiting HIV capsid assembly
  申请人：Ruprecht-Karls-Universität Heidelberg

  公开号：EP2769722A1

  公开（公告）日：2014-08-27

  The present invention relates a compound or a pharmaceutically acceptable salt or solvate thereof for use in inhibiting HIV capsid assembly, wherein the compound is a pyrimidine being at least substituted in two positions, preferably in 2 and 4 position or in 4 and 6 position, more preferably in 2 and 4 position.

  本发明涉及一种用于抑制 HIV 荚膜组装的化合物或其药学上可接受的盐或溶液，其中该化合物是至少在两个位置被取代的嘧啶，优选在 2 和 4 位置或 4 和 6 位置，更优选在 2 和 4 位置。
• HETEROARYL AMIDE COMPOUNDS, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITIONS THEREOF, AND APPLICATIONS THEREOF
  申请人：Rui Jin Hospital Affiliated To Shanghai Jiao Tong University School of Medicine

  公开号：EP3705481A1

  公开（公告）日：2020-09-09

  The present invention relates to heteroaryl amide compounds, a preparation method therefor, pharmaceutical compositions thereof and applications thereof, and specifically, relates to a type of compounds having broad-spectrum tumor resistant activity, a preparation method therefor, pharmaceutical compositions containing the compounds, and uses of the compounds in the preparation of drugs for treating tumors.

  本发明涉及杂芳基酰胺化合物、其制备方法、药物组合物及其应用，特别是涉及一种具有广谱抗肿瘤活性的化合物、其制备方法、含有该化合物的药物组合物以及该化合物在制备治疗肿瘤药物中的用途。
• Bicyclic urea kinase inhibitors and uses thereof
  申请人：The Broad Institute, Inc.

  公开号：US10954242B2

  公开（公告）日：2021-03-23

  The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

  本公开提供了式(I)、(II)和(III)化合物。所提供的化合物能够结合蛋白激酶（如 SIK），可用于调节（如抑制）受试者或细胞中蛋白激酶（如 SIK、（如 SIK1、SIK2 或 SIK3））的活性。所提供的化合物可用于治疗或预防有需要的受试者的疾病（如增殖性疾病、肌肉骨骼疾病、遗传性疾病、血液病、神经性疾病、疼痛性疾病、精神疾病或代谢性疾病）。还提供了包括或涉及本文所述化合物的药物组合物、试剂盒、方法和用途。
• 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。