2-bromomethyl-3-methylbenzofuran | 58863-50-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 2-bromomethyl-3-methylbenzofuran
• 英文别名: 2-(Bromomethyl)-3-methyl-1-benzofuran
• CAS: 58863-50-6
• 化学式: C₁₀H₉BrO
• 分子量: 225.085
• InChiKey: YABPWQOZFNSTAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  13.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  cis-1-[4-(tert-butyl-dimethyl-silanyloxy)-cyclohexyl]-pyrrolidin-2-one 、 2-bromomethyl-3-methylbenzofuran 以afford the title compound as a tan powder (295 mg, 54%)的产率得到1-(4-hydroxycyclohexyl)-3-(3-methyl-benzofuran-2-ylmethyl)-pyrrolidin-2-one
  参考文献：
  名称：

  Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

  摘要：

  本发明提供了一种公式I的化合物，其可用作11-β羟基类固醇脱氢酶1的有效且选择性的抑制剂。本发明还提供了一种药物组合物，其包括公式I的化合物或其药物盐，以及药学上可接受的载体、稀释剂或赋形剂。此外，本发明还提供了含有公式I的化合物的组合物，用于治疗代谢综合症、糖尿病、高血糖、肥胖症、高血压、高脂血症、与高血糖相关的其他症状和相关疾病。其中，公式（I）中，R0是（II）或（III），G1是亚甲基或乙烯基；L是从-（C1-C4）烷基，-S-，-CH（OH）-或-O-中选择的二价连接基；A是亚甲基，-S-，-O-或-NH-；其他取代基如权利要求所定义。

  公开号：

  US07834194B2

文献信息

• Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
  申请人：Aicher Thomas Daniel

  公开号：US20080207691A1

  公开（公告）日：2008-08-28

  The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru 0 is (II), or (III) G 1 is methylene or ethylene; L is a divalent linking group selected from —(C 1 -C 4 ) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.

  本发明提供了式I的化合物，其作为11-β羟基类固醇脱氢酶1的有效和选择性抑制剂。本发明进一步提供了一种药物组合物，其包括式I的化合物或其药用盐，以及药用可接受的载体、稀释剂或赋形剂。此外，本发明还提供了包含式I化合物的组合物，用于治疗代谢综合征、糖尿病、高血糖、肥胖症、高血压、高脂血症、与高血糖相关的其他症状和相关疾病。其中，式（I）中，Ru0是（II）或（III），G1是亚甲基或乙烯基；L是选择自—（C1-C4）烷基-、—S—、—CH（OH）—或—O—的二价连接基；A是亚甲基、—S—、—O—或—NH—；其他取代基如权利要求所定义。
• SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS
  申请人：Aurigene Discovery Technologies Limited

  公开号：US20140336153A1

  公开（公告）日：2014-11-13

  The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式（I）的取代吡啶衍生物，其可作为抗菌剂，更特别地是FabI抑制剂，具有治疗上的用途。式（I）中，R1至R5和L具有规范中所给出的含义，以及其药学上可接受的盐，在特定的疾病或疾病预防治疗中有用，特别是在有优势的抗菌剂，更特别地是FabI抑制剂的疾病或疾病预防治疗中的使用。本发明还提供了合成和给予FabI抑制剂化合物的方法。本发明还提供了包含至少一种FabI抑制剂化合物的药物配方，以及与其药学上可接受的载体、稀释剂或赋形剂一起使用的药物配方。
• Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors
  作者：Jason S. Xiang、Yonghan Hu、Thomas S. Rush、Jennifer R. Thomason、Manus Ipek、Phaik-Eng Sum、Leila Abrous、Joshua J. Sabatini、Katy Georgiadis、Erica Reifenberg、Manas Majumdar、Elisabeth A. Morris、Steve Tam

  DOI：10.1016/j.bmcl.2005.10.001

  日期：2006.1

  Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of biphenylsulfonamidocarboxylic acid inhibitors of aggrecanase-1 are reported. Compound 24 demonstrated 89% inhibition of proteoglycan degradation at 10 mu g/mL and has an oral bioavailability in rat of 35%. (c) 2005 Elsevier Ltd. All rights reserved.
• CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
  申请人：ELI LILLY AND COMPANY

  公开号：EP1830840A1

  公开（公告）日：2007-09-12
• US7834194B2
  申请人：——

  公开号：US7834194B2

  公开（公告）日：2010-11-16