6-Fluor-picolinsaeure-hydrazid | 701-41-7

• 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: 6-Fluor-picolinsaeure-hydrazid
• 英文别名: 6-fluoro-pyridine-2-carboxylic acid hydrazide；6-fluoro-2-pyridinecarbohydrazide；6-Fluoropyridine-2-carbohydrazide
• CAS: 701-41-7
• 化学式: C₆H₆FN₃O
• 分子量: 155.132
• InChiKey: ZWWGWPLNTDADAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-Fluor-picolinsaeure-hydrazid 在 potassium carbonate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 3-[[5-[5-(difluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridyl]methyl]-5-(6-fluoro-2-pyridyl)-1,3,4-oxadiazol-2-one
  参考文献：
  名称：

  히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이의 용도

  摘要：

  本发明涉及一种具有组蛋白去乙酰化酶6 (Histone deacetylase 6, HDAC6)抑制活性的新化合物、其制备方法及其用途。根据本发明的新化合物、其立体异构体或其药学上可接受的盐具有HDAC6抑制活性，并且在预防或治疗与HDAC6相关的疾病（包括癌症、炎症性疾病、自身免疫性疾病、神经学疾病或退行性神经疾病）方面有效。

  公开号：

  KR20240035172A
• 作为产物：
  描述：

  1,1-dimethylethyl 2-[(6-fluoro-2-pyridinyl)carbonyl]hydrazinecarboxylate 在 盐酸 、 氨 作用下， 以 1,4-二氧六环 、 甲醇 为溶剂， 生成 6-Fluor-picolinsaeure-hydrazid
  参考文献：
  名称：

  [EN] 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
  [FR] DÉRIVÉS DE 5,6,7,8-TÉTRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZINE COMME MODULATEURS DE P2X7

  摘要：

  本发明提供了一种式(I)化合物或其药学上可接受的盐，其中A为氢、C1-4烷基、C3-6环烷基、C1-3烷氧基、C1-3烷氧基C1-4烷基、C1-2氟烷基、卤素、NR6 R7、任选取代的杂芳基(Het)或任选取代的苯基，且R1、R2、R3、R4、R5、R6和R7如说明书中所定义。这些化合物或盐被认为能够调节P2X7受体功能，并能拮抗ATP在P2X7受体上的作用。本发明还提供了该化合物或盐在治疗或预防例如炎症性疼痛、神经性疼痛、内脏疼痛、类风湿性关节炎、骨关节炎或神经退行性疾病中的用途。

  公开号：

  WO2010125102A1

文献信息

• Chemical Compounds
  申请人：Turnbull Philip Stewart

  公开号：US20090170907A1

  公开（公告）日：2009-07-02

  This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.

  这项发明涉及非甾体化合物，它们是雄激素、糖皮质激素、矿质皮质激素和孕激素受体的调节剂，以及这些化合物的制备和使用方法。
• 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
  申请人：Dean David Kenneth

  公开号：US20120157436A1

  公开（公告）日：2012-06-21

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 1-3 alkoxy, C 1-3 alkoxy C 1-4 alkyl, C 1-2 -fluoroalkyl, halogen, NR 6 R 7 , optionally substituted heteroaryl, or optionally substituted phenyl, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

  本发明提供了式（I）的化合物或其药学上可接受的盐： 其中，A为氢、C1-4烷基、C3-6环烷基、C1-3烷氧基、C1-3烷氧基C1-4烷基、C1-2氟代烷基、卤素、NR6R7、可选取代杂环芳基或可选取代苯基；R1、R2、R3、R4、R5、R6和R7如描述中所定义。 这些化合物或盐被认为可以调节P2X7受体功能，并能够拮抗P2X7受体上ATP的作用。本发明还提供了该化合物或盐在治疗或预防炎症性疼痛、神经病理性疼痛、内脏疼痛、类风湿性关节炎、骨关节炎或神经退行性疾病中的应用。
• 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators
  申请人：Dean David Kenneth

  公开号：US08501946B2

  公开（公告）日：2013-08-06

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

  本发明提供了一个式（I）的化合物或其药学上可接受的盐：其中A为氢、C1-4烷基、C3-6环烷基、C1-3烷氧基、C1-3烷氧基C1-4烷基、C1-2氟代烷基、卤素、NR6R7、可选取代的杂环芳基（Het）或可选取代的苯基，而R1、R2、R3、R4、R5、R6和R7如描述中所定义。这些化合物或盐被认为可以调节P2X7受体功能，并且能够拮抗P2X7受体上ATP的作用。本发明还提供了该化合物或盐在治疗或预防例如炎症性疼痛、神经病理性疼痛、内脏疼痛、类风湿性关节炎、骨关节炎或神经退行性疾病中的用途。
• Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists
  作者：Dale A. Rudolph、Jesus Alcazar、Michael K. Ameriks、Ana Belen Anton、Hong Ao、Pascal Bonaventure、Nicholas I. Carruthers、Christa C. Chrovian、Meri De Angelis、Brian Lord、Jason C. Rech、Qi Wang、Anindya Bhattacharya、Jose Ignacio Andres、Michael A. Letavic

  DOI：10.1016/j.bmcl.2015.06.004

  日期：2015.8

  The optimization efforts that led to a novel series of methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of compounds with good drug-like properties that are capable of high P2X7 receptor occupancy in rat following oral administration, including compounds 7n (P2X7 IC50 = 7.7 nM) and 7u (P2X7 IC50 = 7.7 nM). These compounds are expected to be useful tools for characterizing the effects of P2X7 antagonism in models of depression and epilepsy, and several of the compounds prepared are candidates for effective P2X7 PET tracers. (C) 2015 Elsevier Ltd. All rights reserved.
• Synthesis and anti-prion aggregation activity of acylthiosemicarbazide analogues
  作者：Dong Hwan Kim、Jaehyeon Kim、Hakmin Lee、Dongyun Lee、So Myoung Im、Ye Eun Kim、Miryeong Yoo、Yong-Pil Cheon、Jason C. Bartz、Young-Jin Son、Eun-Kyoung Choi、Yong-Sun Kim、Jae-Ho Jeon、Hyo Shin Kim、Sungeun Lee、Chongsuk Ryou、Tae-gyu Nam

  DOI：10.1080/14756366.2023.2191164

  日期：2023.12.31