3-(2,4-difluorobenzyl)-2-methyl-N-(1-methyl-1H-imidazol-4-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine | 1555422-17-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 3-(2,4-difluorobenzyl)-2-methyl-N-(1-methyl-1H-imidazol-4-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine
• 英文别名: 3-[(2,4-difluorophenyl)methyl]-2-methyl-N-(1-methylimidazol-4-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine
• CAS: 1555422-17-7
• 化学式: C₂₃H₂₅F₂N₇O
• 分子量: 453.495
• InChiKey: YXKQAFRBQBJIRA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  72.5
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] IMIDAZO[1,2-B]PYRIDAZIN-6-AMINE DERIVATIVES AS KINASE JAK-2 INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-B]PYRIDAZIN-6-AMINE UTILISABLES EN TANT QU'INHIBITEURS DE LA KINASE JAK2
  申请人：CELON PHARMA SA

  公开号：WO2014020531A1

  公开（公告）日：2014-02-06

  A compound represented by the general formula (I) wherein R1represents H or C1-C4 alkyl; R2 represents phenyl substituted with one or two substituents selected from the group consisting of halogen atom and OC1-C4 alkyl;R3 represents phenyl or 5 to 10-membered monocyclic or bicyclic heteroaryl having from 1 to 4 ring heteroatoms selected from the group consisting of N, S, and O, which can be unsubstituted or substituted with a substituent selected from halogen atom, C1-C4-alkyl, and -C(O)O-C1-C4 -alkyl; and X represents –CH2-group or carbonyl-C(O)-group;and their acid addition salts;with the exclusion of 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)-imidazo[1,2-b]pyridazine-6-amine and its salts. The compounds are JAK2 inhibitors and are useful as medicaments, especially for treating proliferative disorders and cancer diseases

  通用式（I）所代表的化合物，其中R1代表H或C1-C4烷基；R2代表苯基，其上取代基可为卤原子和OC1-C4烷基中选择的一个或两个取代基；R3代表苯基或含有1至4个来自N、S和O的环异原子的5至10元杂环或双环杂环，可以未取代或取代为卤原子、C1-C4-烷基和-C（O）O-C1-C4-烷基中选择的取代基；X代表-CH2-基团或羰基-C（O）-基团；以及它们的酸盐；不包括3-（4-氯-2-氟苄基）-2-甲基-N-（5-甲基-1H-吡唑-3-基）-8-（吗啉甲基）-咪唑并[1,2-b]吡啶并[1,2-b]吡啶-6-胺及其盐。这些化合物是JAK2抑制剂，可用作药物，特别用于治疗增殖性疾病和癌症。