1-(6-Bromopyridin-3-YL)ethanamine | 1060811-56-4

• 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-(6-Bromopyridin-3-YL)ethanamine
• CAS: 1060811-56-4
• 化学式: C₇H₉BrN₂
• 分子量: 201.06
• InChiKey: COGGCXWSBTVYEV-UHFFFAOYSA-N

物化性质

• 沸点：
  294.2±25.0 °C(Predicted)
• 密度：
  1.477±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  乙酸酐 、 1-(6-Bromopyridin-3-YL)ethanamine 生成 N-[1-(6-bromo-pyridin-3-yl)-ethyl]-acetamide
  参考文献：
  名称：

  Azetidine Derivatives

  摘要：

  以下是一种茚三烷衍生物及其在治疗肥胖症、糖尿病或血脂异常中的应用。

  公开号：

  US20130172312A1

文献信息

• BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas Operations, Inc.

  公开号：US20190300521A1

  公开（公告）日：2019-10-03

  The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，其作为SMARCA2或BRM（靶蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端结合Von Hippel-Lindau E3泛素连接酶的配体，另一端结合靶蛋白的双功能化合物，使得靶蛋白与泛素连接酶靠近以实现靶蛋白的降解（和抑制）。本公开展示了与靶蛋白降解/抑制相关的广泛药理活性。本公开的化合物和组合物用于治疗或预防由靶蛋白聚集或积累导致的疾病或紊乱。
• Azetidine Derivatives
  申请人：NOSSE Bernd

  公开号：US20130172312A1

  公开（公告）日：2013-07-04

  Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

  以下是示例性的氮杂环丙烷衍生物及其在肥胖、糖尿病或血脂异常治疗中的用途。
• [EN] SUBSTITUTED THIENYL-MERCAPTOKETONES, AND USE THEREOF FOR TREATING DISEASES ASSOCIATED WITH HISTONE DEACETYLASE ENZYMATIC ACTIVITY<br/>[FR] THIENYL-MERCAPTOKETONES SUBSTITUES, ET UTILISATION ASSOCIEE POUR LE TRAITEMENT DE MALADIES LIEES A L'ACTIVITE ENZYMATIQUE D'HISTONE DEACETYLASE
  申请人：ARGENTA DISCOVERY LTD

  公开号：WO2005075466A1

  公开（公告）日：2005-08-18

  A compound of formula: (I): in which A represents optionally substituted monocyclic heteroaryl or phenyl; B represents optionally substituted heteroaryl, aryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl, or B represents H when L represents a single bond; L represents a single bond, alkylene, (CH2)nX(CH2)m, (CH2)nX(CH2)pY(CH2)m; X represents -O-, -NR3-, -CO-, -SO2-, -NR3CO-, -NR3SO2-, -CONR3-, -SO2NR3-, -NR5CONR5a-; Y represents NR3- or -O-; R1 represents H, COR8; R2 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, CN; R3 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, or alkyl substituted by -OR4, -NR5R6, -NR6COR7, -NR6SO2R7, -CONR5R6 or -SO2NR5R6; R4 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl; R5 and R5a represent H or alkyl; R6 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl or NR5R6 represents a cyclic amine; R7 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; R8 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; n represents 0-3; m represents 0-3; p represents 1-3; and corresponding disulphides, N-oxides, pharmaceutically acceptable salts, solvates and prodrugs thereof; and use to treat a disease in which inhibition of histone deacetylase can prevent, inhibit or ameliorate the pathology and/or symptomatology of the disease.

  化合物的公式为（I）：其中A代表可选取代的单环杂芳基或苯基；B代表可选取代的杂芳基、芳基、芳基融合杂环烷基、杂芳基融合环烷基、杂芳基融合杂环烷基或芳基融合环烷基，或当L代表单键时，B代表H；L代表单键、烷基、（CH2）nX（CH2）m、（CH2）nX（CH2）pY（CH2）m；X代表-O-、-NR3-、-CO-、-SO2-、-NR3CO-、-NR3SO2-、-CONR3-、-SO2NR3-、-NR5CONR5a-；Y代表NR3-或-O-；R1代表H、COR8；R2代表卤素、烷基、卤代烷基、烷氧基、卤代烷氧基、CN；R3代表H、烷基、芳基烷基、杂芳基烷基、杂环烷基烷基、环烷基烷基或烷基取代的-OR4、-NR5R6、-NR6COR7、-NR6SO2R7、-CONR5R6或-SO2NR5R6；R4代表H、烷基、芳基烷基、杂芳基烷基、杂环烷基烷基、环烷基烷基、芳基、杂芳基、杂环烷基或环烷基；R5和R5a代表H或烷基；R6代表H、烷基、芳基烷基、杂芳基烷基、杂环烷基烷基、环烷基烷基、芳基、杂芳基、杂环烷基或环烷基，或NR5R6代表环状胺基；R7代表烷基、芳基、杂芳基、环烷基、杂环烷基、芳基烷基、杂芳基烷基、环烷基烷基或杂环烷基烷基；R8代表烷基、芳基、杂芳基、环烷基、杂环烷基、芳基烷基、杂芳基烷基、环烷基烷基或杂环烷基烷基；n代表0-3；m代表0-3；p代表1-3；以及相应的二硫化物、N-氧化物、药学上可接受的盐、溶剂化合物和前药；并用于治疗一种疾病，其中组蛋白去乙酰化酶的抑制可以预防、抑制或改善该疾病的病理学和/或症状学。
• Azaindazole Compounds As CCR1 Receptor Antagonists
  申请人：COOK Brian Nicholas

  公开号：US20100093724A1

  公开（公告）日：2010-04-15

  Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

  本发明涉及式(I)化合物，其可用于治疗多种疾病和障碍，这些疾病和障碍是通过CCR1的活性介导或维持的，包括自身免疫性疾病，如类风湿性关节炎和多发性硬化症。同时，本发明还涉及制备方法和使用方法。
• Pyridinyl Compounds Useful As Intermediates
  申请人：COOK Brian Nicholas

  公开号：US20120136158A1

  公开（公告）日：2012-05-31

  Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.

  本发明涉及一种式(I)的化合物，可用于治疗多种通过CCR1活性介导或维持的疾病和障碍，包括自身免疫性疾病，例如类风湿性关节炎和多发性硬化症。本发明还涉及其中间体，以及制备和使用它们的方法。