5-furan-3-yl-2H-pyrazol-3-ylamine | 1028843-02-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 5-furan-3-yl-2H-pyrazol-3-ylamine
• 英文别名: 5-(Furan-3-yl)-2H-pyrazol-3-ylamine；5-(furan-3-yl)-1H-pyrazol-3-amine
• CAS: 1028843-02-8
• 化学式: C₇H₇N₃O
• 分子量: 149.152
• InChiKey: KPRVRQADAMFPLR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.8
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-furan-3-yl-2H-pyrazol-3-ylamine 在 水 、 potassium carbonate 、 溶剂黄146 、 N,N-二异丙基乙胺 、 sodium hydroxide 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 35.17h， 生成 N-(1-adamantyl)-2-(furan-3-yl)-7-oxo-4-pentylpyrazolo[1,5-a]pyrimidine-6-carboxamide
  参考文献：
  名称：

  Discovery of 7-Oxopyrazolo[1,5-a]pyrimidine-6-carboxamides as Potent and Selective CB₂ Cannabinoid Receptor Inverse Agonists

  摘要：

  We recently described the medicinal chemistry of a new series of heteroaryl-4-oxopyridine/7-oxopyrimidines as CB2 receptor partial agonists, showing that the functionality of these ligands is controlled by the nature of the heteroaryl function condensed with the pyridine ring. We describe herein the design and synthesis of the 7-oxopyrazolo[1,5-a]pyrimidine-6-carboxamides, structural isomers of our previously reported pyrazolo[3,4-Hpyridines. All of the new compounds showed high affinity and selectivity for the CB2 receptor in the nanomolar range. In 3,5-cyclic adenosine monophosphate (cAMP) assays, the novel series shows stimulatory effects on forskolin-induced cAMP production acting as inverse agonists.

  DOI：

  10.1021/jm400182t

文献信息

• FUSED PYRIMIDINE COMPOUND OR SALT THEREOF
  申请人：TAIHO PHARMACEUTICAL CO., LTD.

  公开号：US20180009817A1

  公开（公告）日：2018-01-11

  The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R 1 to R 3 , X, and n are as defined in the specification.

  本发明提供了一种新型RET抑制剂，其包括作为活性成分的化合物或其盐，这些化合物以前并未因其RET抑制活性而为人所知，并且还提供了一种用于预防或治疗疾病（例如恶性肿瘤）的药剂，该疾病可通过RET抑制活性预防或治疗。该RET抑制剂包括作为活性成分的由下式（I）表示的化合物或其盐：其中A、R1至R3、X和n如规范中所定义。
• CXCR2 INHIBITORS
  申请人：Hunt Peter

  公开号：US20100152205A1

  公开（公告）日：2010-06-17

  The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.

  本发明涉及式（I）的化合物以及将这些化合物用作药物的用途，例如在预防或治疗CXCR2受体介导的疾病或疾病中。
• Tissue non-specific alkaline phosphatase inhibitors and uses thereof for treating vascular calcification
  申请人：Burnham Institute for Medical Research

  公开号：EP2433496A1

  公开（公告）日：2012-03-28

  Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.

  本文公开的化合物是组织非特异性碱性磷酸酶抑制剂。所公开的化合物可用于治疗、预防或减轻血管钙化、动脉钙化和其他心血管疾病。
• CONDENSED PYRIMIDINE COMPOUND OR SALT THEREOF
  申请人：Taiho Pharmaceutical Co., Ltd.

  公开号：EP3260454A1

  公开（公告）日：2017-12-27

  The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.

  本发明提供了一种新型 RET 抑制剂，其活性成分包括一种尚未发现具有 RET 抑制活性的化合物或其盐，本发明还提供了一种用于预防或治疗可通过 RET 抑制活性预防或治疗的疾病（如恶性肿瘤）的制剂。作为活性成分，RET 抑制剂包括下式 (I) 所代表的化合物或其盐类： 其中 A、R1 至 R3、X 和 n 如说明书中所定义。
• Fused pyrimidine compound or salt thereof
  申请人：TAIHO PHARMACEUTICAL CO., LTD.

  公开号：US10233189B2

  公开（公告）日：2019-03-19

  The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.

  本发明提供了一种新型 RET 抑制剂，其活性成分包括一种尚未发现具有 RET 抑制活性的化合物或其盐，本发明还提供了一种用于预防或治疗可通过 RET 抑制活性预防或治疗的疾病（如恶性肿瘤）的制剂。作为活性成分，RET 抑制剂包括下式 (I) 所代表的化合物或其盐类： 其中 A、R1 至 R3、X 和 n 如说明书中所定义。