6-溴-2-氟吡啶-3-胺 | 850220-97-2

• 物质功能分类: 有机原料 - 氨基化合物
• 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
• 中文名称: 6-溴-2-氟吡啶-3-胺
• 英文名称: 6-bromo-2-fluoropyridin-3-amine
• 英文别名: 6-bromo-2-fluoropyridin-3-ylamine
• CAS: 850220-97-2
• 化学式: C₅H₄BrFN₂
• 分子量: 191.003
• InChiKey: QYJIKULJTMICLA-UHFFFAOYSA-N

物化性质

• 沸点：
  282.6±35.0 °C(Predicted)
• 密度：
  1.813±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  6-溴-2-氟吡啶-3-胺 在 三丁基膦 、 palladium diacetate 、 sodium cyanoborohydride 、 caesium carbonate 、 溶剂黄146 、 copper(I) bromide 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 9.0h， 生成 2-fluoro-6-(6-methoxybenzo[d]thiazol-2-yl)-N-methylpyridin-3-amine
  参考文献：
  名称：

  Synthesis and evaluation of pyridylbenzofuran, pyridylbenzothiazole and pyridylbenzoxazole derivatives as 18F-PET imaging agents for β-amyloid plaques

  摘要：

  The synthesis and SAR of new beta-amyloid binding agents are reported. Evaluation of important properties for achieving good signal-to-background ratio is described. Compounds 27, 33, and 36 displayed desirable lipophilic and pharmacokinetic properties. Compound 27 was further evaluated with autoradiographic studies in vitro on human brain tissue and in vivo in Tg2576 mice. Compound 27 showed an increased signal-to-background ratio compared to flutemetamol 4, indicating its suitability as PET ligand for b-amyloid deposits in AD patients. The preparation of the corresponding F-18-labeled PET radioligand of compound 27 is presented. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.05.011
• 作为产物：
  描述：

  3-氨基-2-氟吡啶 在 溴 、 sodium acetate 、 溶剂黄146 、 sodium hydroxide 作用下， 以 水 为溶剂， 反应 1.0h， 生成 6-溴-2-氟吡啶-3-胺
  参考文献：
  名称：

  Novel 2-Heteroaryl Substituted Benzothiophenes and Benzofuranes 709

  摘要：

  本发明涉及新型2-杂环芳基取代苯并噻吩和苯并呋喃衍生物，其前体以及这些化合物的治疗用途，具有如下结构式(Ia)： 以及它们的药用盐、组合物和使用方法。此外，本发明涉及适用于在活体患者中成像淀粉样沉积物的新型2-杂环芳基取代苯并噻吩和苯并呋喃衍生物，它们的组合物、使用方法以及制备这类化合物的过程。更具体地，本发明涉及一种在体内成像脑部淀粉样沉积物的方法，以允许在死前诊断阿尔茨海默病，并测量阿尔茨海默病治疗药物的临床疗效。

  公开号：

  US20080221149A1

文献信息

• [EN] FUSED LACTAM COMPOUNDS<br/>[FR] COMPOSES DE LACTAME CONDENSE
  申请人：PFIZER JAPAN INC

  公开号：WO2005035523A1

  公开（公告）日：2005-04-21

  This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or substituted and said ary is substituted by at least one substituer,t selected from the group consisting of substituents a; said substituents a are selected from the group 10 consisting of halogen ate ms, alkyl groups having from 1 to 6 carbon atoms etc.; or a pharmaceutically ac eptable ester of such compound, or a pharmaceutically ac eptable salt thereof. These compou ds are useful for the treatment of disease conditions caused 15 by overactivation of N DA NR2B receptor such of pain, stroke, traumatic brain injury, Parkinson's disease, Alzheimer's disease, depression, anxiety, migraine, or the like in mammalian, especially humans. This invention also provides a pharmaceutical composi ion comprising the above compound.

  本发明提供了一种具有公式(I)的化合物，其中R1代表一个具有6到10个环碳原子的芳基团等；R2代表一个氢原子等，n代表0、1或2；所说的杂芳基团未取代或取代，所说的芳基至少被一个从由取代基a组成的组中选择的取代基t所取代；所说的取代基a是从由卤素原子、具有1到6个碳原子的烷基团等组成的组中选择的；或者该化合物的药物可接受的酯，或者其药物可接受的盐。这些化合物用于治疗由NDA NR2B受体过度激活引起的疾病状况，如疼痛、中风、创伤性脑损伤、帕金森病、阿尔茨海默病、抑郁症、焦虑症、偏头痛或类似疾病，特别是在哺乳动物中，特别是人类。本发明还提供了一种包含上述化合物的药物组合物。
• Novel 2-Heteroaryl Substituted Benzothiophenes and Benzofuranes 709
  申请人：Arzel Erwan

  公开号：US20080221149A1

  公开（公告）日：2008-09-11

  The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

  本发明涉及新型2-杂环芳基取代苯并噻吩和苯并呋喃衍生物，其前体以及这些化合物的治疗用途，具有如下结构式(Ia)： 以及它们的药用盐、组合物和使用方法。此外，本发明涉及适用于在活体患者中成像淀粉样沉积物的新型2-杂环芳基取代苯并噻吩和苯并呋喃衍生物，它们的组合物、使用方法以及制备这类化合物的过程。更具体地，本发明涉及一种在体内成像脑部淀粉样沉积物的方法，以允许在死前诊断阿尔茨海默病，并测量阿尔茨海默病治疗药物的临床疗效。
• NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
  申请人：MENET Christel Jeanne Marie

  公开号：US20150203455A1

  公开（公告）日：2015-07-23

  The present invention discloses compounds according to Formula I: wherein Cy, R 1 , L 1 , R 3 , R 4 , R 5 , L a , and R a are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

  本发明公开了根据以下公式I的化合物：其中Cy、R1、L1、R3、R4、R5、La和Ra如本文所定义。根据公式I的新型苯并咪唑，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括但不限于过敏性疾病、炎症性疾病、自身免疫性疾病、增殖性疾病、移植排斥反应、涉及软骨周转障碍的疾病、先天性软骨畸形以及与IL6过度分泌或干扰素过度分泌相关的疾病。
• Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
  申请人：GALAPAGOS NV

  公开号：US09440929B2

  公开（公告）日：2016-09-13

  The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

  本发明公开了根据式I的化合物：其中Cy、R1、L1、R3、R4、R5、La和Ra如本文所定义。根据式I公开了新的苯并咪唑，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗哺乳动物包括人类的各种疾病，包括但不限于过敏性疾病、炎症性疾病、自身免疫性疾病、增殖性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形以及与IL6过度分泌或干扰素过度分泌有关的疾病。
• [EN] BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] DÉRIVÉS DE BENZIMIDAZOLE ET COMPOSITIONS PHARMACEUTIQUES DE CEUX-CI POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2015110378A1

  公开（公告）日：2015-07-30

  The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

  本发明公开了根据式(I)的化合物，其中Cy、R1、L1、R3、R4、R5、La和Ra如本文所定义。公开了根据式(I)的能够抑制JAK的新型苯并咪唑类化合物，这些化合物可以制备成药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括但不限于过敏性疾病、炎症性疾病、自身免疫性疾病、增生性疾病、移植排斥、涉及软骨代谢障碍的疾病、先天性软骨畸形以及与IL6或干扰素过度分泌相关的疾病。