PF-670462 free base | 950980-98-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: PF-670462 free base
• 英文别名: 4-[3-cyclohexyl-5-(4-fluorophenyl)imidazol-4-yl]pyrimidin-2-amine
• CAS: 950980-98-0
• 化学式: C₁₉H₂₀FN₅
• 分子量: 337.4
• InChiKey: WUDBUIUHVNECTM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  69.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] 4—(1H— IMIDAZOL— 5— YL) -1H-PYRROLO [2, 3-B] PYRIDINES FOR USE IN THE TREATMENT OF LEUKAEMIAS, LYMPHOMAS AND SOLID TUMORS<br/>[FR] 4-(1H-IMIDAZOL-5-YL)-1H-PYRROLO [2,3-B] PYRIDINES DESTINÉES À ÊTRE UTILISÉES DANS LE TRAITEMENT DE LEUCÉMIES, DE LYMPHOMES ET DE TUMEURS SOLIDES
  申请人：UNIV MASARYKOVA

  公开号：WO2019185631A1

  公开（公告）日：2019-10-03

  The present invention relates to novel 4-(1H-imidazol-5-yl)-1H-pyrrolo[2,3-b]pyridine compounds which are useful in the treatment of lymphomas, leukaemias, and solid tumors.

  本发明涉及一种新型的4-(1H-咪唑-5-基)-1H-吡咯[2,3-b]吡啶化合物，可用于治疗淋巴瘤、白血病和实体肿瘤。
• INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1E
  申请人：Okamoto Masako

  公开号：US20130137730A1

  公开（公告）日：2013-05-30

  There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).

  提供了一种新型的噁唑酮衍生物，具有对酪蛋白激酶1δ和酪蛋白激酶1ε的抑制活性。此外，该抑制剂还能抑制酪蛋白激酶1δ和酪蛋白激酶1ε，因此还提供了一种用于治疗和/或预防与酪蛋白激酶1δ或酪蛋白激酶1ε的激活机制相关的疾病的药物剂。此外，还提供了一种用于治疗尤其是昼夜节律紊乱（包括睡眠障碍）、中枢神经退行性疾病和癌症的药物剂。一种酪蛋白激酶1δ和酪蛋白激酶1ε的抑制剂，包括作为活性成分的噁唑酮衍生物，其表示如下通用式（1），其盐、溶剂或水合物：其中X代表卤素原子（可以是氟原子、氯原子、溴原子或碘原子中的任意一种）。
• INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1EPSILON
  申请人：Okamoto Masako

  公开号：US20110294857A1

  公开（公告）日：2011-12-01

  There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R 1 and R 2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]

  提供了一种抑制剂，可抑制酪蛋白激酶1δ和酪蛋白激酶1ε，因此还提供了一种用于治疗和/或预防疾病的药物，该疾病的病理条件与酪蛋白激酶1δ或酪蛋白激酶1ε的激活机制相关。特别地，上述描述的抑制剂用于提供一种用于治疗昼夜节律紊乱（包括睡眠障碍）、中枢神经退行性疾病和癌症的药物。一种酪蛋白激酶1δ和酪蛋白激酶1ε的抑制剂，包括以下一般式（1）所表示的噁唑酮衍生物作为活性成分，其盐、溶剂化合物或水合物：[在式（1）中，R1和R2中的每一个独立地表示取代或未取代的6元或5元杂环基，可选择具有缩合环的取代或未取代的芳香烃基，以及取代或未取代的芳香烃基低烷基基团或芳香烃基低烯基基团，可选择具有缩合环。]
• INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1EPSILON
  申请人：Pharmadesign, Inc.

  公开号：EP2397481A1

  公开（公告）日：2011-12-21

  There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]

  本发明提供了一种抑制酪蛋白激酶1δ和酪蛋白激酶1ε的抑制剂，因此还提供了一种用于治疗和/或预防疾病的药剂，该疾病的病理条件与酪蛋白激酶1δ或酪蛋白激酶1ε的激活机制有关。特别是，上述抑制剂可用于提供治疗昼夜节律紊乱（包括睡眠障碍）、中枢神经退行性疾病和癌症的药物制剂。 一种酪蛋白激酶1δ和酪蛋白激酶1ε的抑制剂，其活性成分包括由下通式(1)代表的噁唑酮衍生物、其盐、其溶液或其水合物： [其中，在式 (1) 中，R1 和 R2 各自独立地代表任选具有缩合环的取代或未取代的 6 元或 5 元杂环基团、任选具有缩合环的取代或未取代的芳香烃基团和任选具有缩合环的取代或未取代的芳香烃低级烷基或芳香烃低级烯基中的任一种。］
• INHIBITOR OF CASEIN KINASE 1 AND CASEIN KINASE 1
  申请人：Pharmadesign, Inc.

  公开号：EP2604606A1

  公开（公告）日：2013-06-19

  There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of, particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).

  本发明提供了一种对酪蛋白激酶 1δ 和酪蛋白激酶 1ε 具有抑制活性的新型噁唑酮衍生物。此外，本发明的抑制剂可抑制酪蛋白激酶 1δ 和酪蛋白激酶 1ε，因此还提供了一种用于治疗和/或预防与酪蛋白激酶 1δ 或酪蛋白激酶 1ε 的活化机制相关的病理条件的疾病的药物。还提供了一种可用于治疗昼夜节律紊乱（包括睡眠紊乱）、中枢神经退行性疾病和癌症的药剂。 一种酪蛋白激酶1δ和酪蛋白激酶1ε的抑制剂，其活性成分包括由下通式(1)代表的噁唑酮衍生物、其盐、其溶液或其水合物： 其中 X 代表卤原子（可以是氟原子、氯原子、溴原子和碘原子中的任一种）。