(5-Bromo-thiazol-2-yl)-pyridin-2-yl-amine | 54670-78-9

• 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: (5-Bromo-thiazol-2-yl)-pyridin-2-yl-amine
• 英文别名: 5-bromo-N-(pyridin-2-yl)thiazol-2-amine；N-(5-Bromothiazol-2-yl)-2-pyridinamine；5-bromo-N-(pyridine-2-yl)thiazol-2-amine；2--5-bromthiazol；2-(2-Pyridylamino)-5-bromthiazol；5-bromo-N-pyridin-2-yl-1,3-thiazol-2-amine
• CAS: 54670-78-9
• 化学式: C₈H₆BrN₃S
• mdl: MFCD27925209
• 分子量: 256.126
• InChiKey: WZNOXZQMWMMJMJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  66
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (5-Bromo-thiazol-2-yl)-pyridin-2-yl-amine 在 N-羟基-7-氮杂苯并三氮唑 、 sodium methylate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 1-(4-(2-Hydroxy-5-(2-(pyridin-2-ylamino)thiazol-5-ylthio)benzoyl)piperazin-1-yl)ethanone
  参考文献：
  名称：

  Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors

  摘要：

  A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 3 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.04.060
• 作为产物：
  描述：

  1-苯甲酰-3-(2-吡啶基)-2-硫脲 在 水 、 溴 、 溶剂黄146 、 sodium hydroxide 作用下， 以 乙醇 为溶剂， 反应 7.33h， 生成 (5-Bromo-thiazol-2-yl)-pyridin-2-yl-amine
  参考文献：
  名称：

  [EN] COMPOUNDS AND METHODS FOR MODULATING INTERLEUKIN-2-INDUCIBLE T-CELL KINASE
  [FR] COMPOSÉS ET MÉTHODES DE MODULATION DE KINASE DE LYMPHOCYTES T INDUCTIBLE PAR L'INTERLEUKINE 2

  摘要：

  公开号：

  WO2018089261A3

文献信息

• Thiazolyl inhibitors of Tec family tyrosine kinases
  申请人：——

  公开号：US20030069238A1

  公开（公告）日：2003-04-10

  Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.

  新型噻唑基化合物及其盐，含有这种化合物的药物组合物，以及在治疗 Tec 家族酪氨酸激酶相关疾病（如癌症、免疫性疾病和过敏性疾病）中使用这种化合物的方法。
• THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS
  申请人：Marinier Anne

  公开号：US20100048581A1

  公开（公告）日：2010-02-25

  The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

  这项发明提供了化合物I的公式[插入化学结构在这里]（I）及其药学上可接受的盐。公式I的噻唑基化合物抑制酪氨酸激酶活性，因此可用作抗癌剂以及治疗阿尔茨海默病。
• Tyrosine kinase inhibitors
  申请人：Merck & Co., Inc.

  公开号：US20020147203A1

  公开（公告）日：2002-10-10

  The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

  本发明涉及抑制、调节和/或调控酪氨酸激酶信号传导的化合物，包含这些化合物的组合物，以及使用它们来治疗依赖酪氨酸激酶的疾病和状况的方法，如在哺乳动物中的血管生成、癌症、肿瘤生长、动脉粥样硬化、老年性黄斑变性、糖尿病性视网膜病变、炎症性疾病等。
• 5-Substituted Thiazol-2-Yl Amino Compounds and Compositions as Protein Kinase Inhibitors
  申请人：Wan Yongqin

  公开号：US20080227783A1

  公开（公告）日：2008-09-18

  The invention provides 5-substituted thiazol-2-yl amino compounds of Formula (I): pharmaceutical compositions comprising such compounds and the use of such compounds for the treatment or prevention of diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Ab 1, Aurora-A, Ber-Ab1, Bmx, CDKI/cyclinB, CHK2, Fes, FGFR3, Flt3, GSK3β, JNK1α1, Lck, MKK4 and TrkB kinases.

  本发明提供了式(I)的5-取代噻唑-2-基氨基化合物，以及包含这种化合物的制药组合物，并将这种化合物用于治疗或预防与异常或失调的激酶活性相关的疾病或障碍，特别是涉及Ab 1、Aurora-A、Ber-Ab1、Bmx、CDKI/cyclinB、CHK2、Fes、FGFR3、Flt3、GSK3β、JNK1α1、Lck、MKK4和TrkB激酶异常激活的疾病或障碍。
• Thiazolyl compounds useful as kinase inhibitors
  申请人：Bristol-Myers Squibb Company

  公开号：US08148400B2

  公开（公告）日：2012-04-03

  The invention provides compounds of formula II: and pharmaceutically acceptable salts thereof. The formula II thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

  该发明提供了II式化合物及其药学上可接受的盐。II式噻唑基化合物抑制酪氨酸激酶活性，因此可用作抗癌剂和治疗阿尔茨海默病的药物。