5-cyclopentylthiazole-2-amine | 851233-57-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-cyclopentylthiazole-2-amine
• 英文别名: 5-Cyclopentyl-1,3-thiazol-2-amine
• CAS: 851233-57-3
• 化学式: C₈H₁₂N₂S
• 分子量: 168.263
• InChiKey: IRFQAEMTMPWQPW-UHFFFAOYSA-N

物化性质

• 沸点：
  317.9±11.0 °C(Predicted)
• 密度：
  1.220±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  苯乙酸 、 5-cyclopentylthiazole-2-amine 在 propylphosphonic anhydride 、 三乙胺 作用下， 以 乙酸乙酯 为溶剂， 生成 N-(5-Cyclopentyl-thiazol-2-yl)-2-phenyl-acetamide
  参考文献：
  名称：

  Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease

  摘要：

  High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.09.006
• 作为产物：
  描述：

  1-(2-Amino-1,3-thiazol-5-yl)cyclopentan-1-ol 在 三乙基硅烷 、 三氟乙酸 作用下， 生成 5-cyclopentylthiazole-2-amine
  参考文献：
  名称：

  Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease

  摘要：

  High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.09.006

文献信息

• NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR SALT THEREOF
  申请人：FUJIFILM Corporation

  公开号：US20150322063A1

  公开（公告）日：2015-11-12

  A compound represented by Formula [1] (in the formula, Z 1 represents N, CH, or the like; X 1 represents NH or the like; R 1 represents a heteroaryl group or the like; each of R 2 , R 3 , and R 4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R 5 represents a heteroaryl group or the like) or salt thereof.

  由式[1]表示的化合物（在该式中，Z表示N、CH或类似物；X表示NH或类似物；R表示杂环烷基或类似物；R2、R3和R4中的每一个表示氢原子、卤原子、烷氧基或类似物；R5表示杂环烷基或类似物）或其盐。
• [EN] PHARMACEUTICAL COMPOSITION COMPRISING PYRIDONE DERIVATIVES<br/>[FR] COMPOSITION PHARMACEUTIQUE COMPRENANT DES DÉRIVÉS DE PYRIDONE
  申请人：SK BIOPHARMACEUTICALS CO LTD

  公开号：WO2012102583A1

  公开（公告）日：2012-08-02

  A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.

  一种吡啶酮衍生物化合物及其药用盐、异构体、溶剂化合物或水合物，以及用于认知障碍的预防或治疗的药用组合物，包括该吡啶酮衍生物化合物或其药用盐、异构体、溶剂化合物或水合物。
• PHARMACEUTICAL COMPOSITION COMPRISING PYRIDONE DERIVATIVES
  申请人：SK BIOBPHARMACEUTICALS CO., LTD.

  公开号：US20150111901A1

  公开（公告）日：2015-04-23

  A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.

  一种吡啶酮衍生物化合物及其药学上可接受的盐、异构体、溶剂或水合物，以及预防或治疗认知障碍的药物组合物，其中包括该吡啶酮衍生物化合物或其药学上可接受的盐、异构体、溶剂或水合物。
• NITROGEN-CONTAINING HETEROCYLIC COMPOUND OR SALT THEREOF
  申请人：FUJIFILM Corporation

  公开号：EP2944637A1

  公开（公告）日：2015-11-18

  A compound represented by Formula [1] (in the formula, Z1 represents N, CH, or the like; X1 represents NH or the like; R1 represents a heteroaryl group or the like; each of R2, R3, and R4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R5 represents a heteroaryl group or the like) or salt thereof.

  式 [1] 所代表的化合物（式中，Z1 代表 N、CH 或类似物；X1 代表 NH 或类似物；R1 代表杂芳基或类似物；R2、R3 和 R4 各代表氢原子、卤素原子、烷氧基或类似物；R5 代表杂芳基或类似物）或其盐。
• Pharmaceutical composition comprising pyridone derivatives
  申请人：SK BIOPHARMACEUTICALS CO., LTD.

  公开号：US10456385B2

  公开（公告）日：2019-10-29

  A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.

  一种吡啶酮衍生物化合物及其药学上可接受的盐、异构体、溶液或水合物，以及一种用于认知障碍的预防或治疗药物组合物，其中包括吡啶酮衍生物化合物或其药学上可接受的盐、异构体、溶液或水合物。