1-(5-fluoro-pyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid | 1373147-31-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-(5-fluoro-pyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid
• 英文别名: 1-(5-Fluoropyridin-2-yl)-5-methylpyrazole-4-carboxylic acid
• CAS: 1373147-31-9
• 化学式: C₁₀H₈FN₃O₂
• 分子量: 221.191
• InChiKey: OFPOOVTWQOYIEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  68
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-(5-fluoro-pyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid 、 4-cyclobutyl-5-[2-(piperidin-1-yl)ethyl]-1,3-thiazol-2-amine 在 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 、 盐酸 作用下， 以 N-甲基吡咯烷酮 、 1,4-二氧六环 为溶剂， 反应 24.0h， 以60%的产率得到N-{4-cyclobutyl-5-[2-(piperidin-1-yl)ethyl]-1,3-thiazol-2-yl}-1-(5-fluoropyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxamide dihydrochloride
  参考文献：
  名称：

  Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit

  摘要：

  DOI：

  10.1016/j.bmc.2019.05.041

文献信息

• AMIDE DERIVATIVE AND USE THEREOF
  申请人：Ushio Hiroyuki

  公开号：US20130211075A1

  公开（公告）日：2013-08-15

  The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.

  本发明涉及一种新型酰胺衍生物。更具体地说，本发明提供了一种药用剂，可用作依赖于T细胞产生细胞因子的疾病的预防或治疗剂，该药用剂包括酰胺衍生物或其药理学上可接受的盐或该衍生物或药理学上可接受的盐的溶剂的溶剂作为活性成分。提供的是由通式(I)所表示的酰胺衍生物[其中每个符号如描述中所定义]或其药理学上可接受的盐，或该衍生物或药理学上可接受的盐的溶剂。
• AMIDOPYRIDINE DERIVATIVE AND USE THEREOF
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：US20150065715A1

  公开（公告）日：2015-03-05

  The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.

  本发明涉及新型的酰胺吡啶衍生物。更具体地说，本发明提供了一种药物剂，其作为预防或治疗基于T细胞产生细胞因子的疾病的药物剂，包括酰胺吡啶衍生物或其药理学上可接受的盐作为活性成分。提供了以下一般式（I）的酰胺吡啶衍生物，其中每个符号具有与描述中定义的相同含义，或其药理学上可接受的盐。
• AMIDOPYRIDINE DERIVATIVE, AND USE THEREOF
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP2837627A1

  公开（公告）日：2015-02-18

  The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.

  本发明涉及新型氨基吡啶衍生物。更具体地说，本发明提供了一种可作为预防或治疗基于 T 细胞产生细胞因子的疾病的药物，其活性成分包括脒基吡啶衍生物或其药理学上可接受的盐。本发明提供了以下通式(I)的脒基吡啶衍生物： 其中各符号的含义与描述中所定义的相同，或其药理学上可接受的盐。
• US9150555B2
  申请人：——

  公开号：US9150555B2

  公开（公告）日：2015-10-06
• US9527859B2
  申请人：——

  公开号：US9527859B2

  公开（公告）日：2016-12-27