YM8XB3LD56 | 2470433-96-4

• 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: YM8XB3LD56
• 英文别名: N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]formamide
• CAS: 2470433-96-4
• 化学式: C₁₄H₁₈F₃N₃O
• 分子量: 301.31
• InChiKey: ZRWQQOCHKAAIFC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  35.6
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] ISOQUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES<br/>[FR] DÉRIVÉS D'ISOQUINOLINE ET COMPOSITIONS PHARMACEUTIQUES ASSOCIÉES POUR LE TRAITEMENT DE MALADIES
  申请人：GALAPAGOS NV

  公开号：WO2022008383A1

  公开（公告）日：2022-01-13

  The present invention discloses compounds according to Formula (I) wherein R1, R2, R3, L1, L2, and L3 are as defined herein. The present invention relates to compounds inhibiting discoidin domain receptors (DDRs), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering a compound of the invention.

  本发明揭示了根据式（I）中R1、R2、R3、L1、L2和L3的定义的化合物。本发明涉及抑制盘状结构域受体（DDRs）的化合物，其生产方法，包含相同化合物的药物组合物，以及使用相同化合物进行预防和/或治疗纤维化疾病、炎症性疾病、呼吸系统疾病、自身免疫疾病、代谢性疾病、心血管疾病和/或增殖性疾病的方法，通过给予本发明的化合物。
• SUBSTITUTED PENTA- AND HEXA-HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, DRUG COMBINATION AND USE THEREOF
  申请人：Xiamen University

  公开号：EP3663293A1

  公开（公告）日：2020-06-10

  A type of substituted penta- fused hexa-heterocyclic compounds having selective inhibition for PIKfyve kinase, a pharmaceutically acceptable salt and pharmaceutically acceptable solvate thereof, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with PIKfyve in vivo, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

  一种对PIKfyve激酶具有选择性抑制作用的取代五融合六杂环化合物、其药学上可接受的盐和药学上可接受的溶液、其制备方法、包含这些化合物的药物组合物，以及这些化合物在制造预防或治疗体内PIKfyve相关疾病的药物中的用途，特别是在制造预防或治疗肿瘤生长和转移的药物中的用途。
• CLASS OF PYRIMIDINE DERIVATIVE KINASE INHIBITORS
  申请人：Hefei Institutes of Physical Science, Chinese Academy of Sciences

  公开号：EP3730483A1

  公开（公告）日：2020-10-28

  The present invention relates to a kinase inhibitor, comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. The present invention also relates to a pharmaceutical composition comprising the kinase inhibitor, and to uses and methods for using these compounds and compositions to inhibit the activity of wild-type FLT3, mutant FLT3-ITD, PDGFRα and/or PDGFRβ kinase in a cell or a subject, as well as uses and methods of these compounds and compositions to preventing or treating kinase-associated conditions in a subject.

  本发明涉及一种激酶抑制剂，包括式I化合物或其药学上可接受的盐、溶液剂、酯、酸、代谢物或原药。本发明还涉及一种包含激酶抑制剂的药物组合物，以及使用这些化合物和组合物抑制细胞或受试者体内野生型FLT3、突变型FLT3-ITD、PDGFRα和/或PDGFRβ激酶活性的用途和方法，以及这些化合物和组合物预防或治疗受试者体内激酶相关疾病的用途和方法。