4-[(3,5-difluorobenzyl)amino]-6-[(4-morpholinophenyl)amino]pyridine-3-carboxyamide | 1227482-95-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-[(3,5-difluorobenzyl)amino]-6-[(4-morpholinophenyl)amino]pyridine-3-carboxyamide
• 英文别名: 4-[(3,5-Difluorophenyl)methylamino]-6-(4-morpholin-4-ylanilino)pyridine-3-carboxamide
• CAS: 1227482-95-2
• 化学式: C₂₃H₂₃F₂N₅O₂
• 分子量: 439.465
• InChiKey: IATYMOMRBMSOAE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  92.5
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• PYRIDINE-3-CARBOXYAMIDE DERIVATIVE
  申请人：Kitamura Takahiro

  公开号：US20110237590A1

  公开（公告）日：2011-09-29

  To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.

  提供一种新型JAK3抑制剂，可用作器官移植中的预防和/或治疗剂，以及风湿性关节炎、多发性硬化、系统性红斑狼疮、干燥综合征、贝赫切特病、I型糖尿病、自身免疫性甲状腺炎、特发性血小板减少性紫癜、溃疡性结肠炎、克罗恩病、哮喘、过敏性鼻炎、特应性皮炎、接触性皮炎、荨麻疹、湿疹、牛皮癣、过敏性结膜炎、葡萄膜炎、白血病等疾病的预防和治疗。通式（1）所代表的吡啶-3-羧酰胺衍生物： 或其盐或溶剂化合物。
• 4,6-DIAMINONICOTINAMIDE COMPOUND
  申请人：Shirakami Shohei

  公开号：US20110230467A1

  公开（公告）日：2011-09-22

  [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.

  [问题] 本发明提供了一种4,6-二氨基烟酰胺化合物，该化合物可用作制药组合物的活性成分，特别是用于治疗由不良和/或异常的细胞因子信号传导引起的疾病的制药组合物。 [解决方法] 本发明人广泛研究了具有JAK3抑制作用的化合物，结果发现本发明的4,6-二氨基烟酰胺化合物具有出色的JAK3抑制作用，并且可用作预防或治疗由不良和/或异常的细胞因子信号传导引起的疾病的药剂，从而完成了本发明。
• US8575153B2
  申请人：——

  公开号：US8575153B2

  公开（公告）日：2013-11-05