5-amino-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid methyl ester | 361369-87-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 5-amino-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid methyl ester
• 英文别名: Methyl 5-amino-5,6,7,8-tetrahydronaphthalene-2-carboxylate
• CAS: 361369-87-1
• 化学式: C₁₂H₁₅NO₂
• 分子量: 205.257
• InChiKey: PBMWFDPFLABNFP-UHFFFAOYSA-N

物化性质

• 沸点：
  345.4±42.0 °C(Predicted)
• 密度：
  1.129±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
  申请人：Blackburn Christopher

  公开号：US20120015943A1

  公开（公告）日：2012-01-19

  This invention provides compounds of formula (I): wherein R 1 , R 1b , R 2a , R 2b , R 2c , and R 2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

  本发明提供了公式(I)的化合物： 其中R1、R1b、R2a、R2b、R2c和R2d的值如说明书中所述，可用作HDAC6的抑制剂。本发明还提供了包含本发明化合物的药物组合物，以及使用这些组合物治疗增殖性、炎症性、感染性、神经性或心血管疾病或失调的方法。
• Amide compounds and use thereof
  申请人：——

  公开号：US20030158413A1

  公开（公告）日：2003-08-21

  The present invention relates to an amide compound of the formula 1 wherein R 1 is a hydrogen and the like, R 2 is a hydrogen and the like, X is SO 2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

  本发明涉及一种式1的酰胺化合物，其中R1为氢等，R2为氢等，X为SO2等，Y为式（III）等，a为2，其异构体或其药学上可接受的盐。本发明的化合物显示出显著且选择性的Rho激酶抑制作用，不具有有毒性问题，显示出良好的口服吸收和药物动力学（药物的吸收、分布、代谢、排泄等），并且显示出优越的特性（例如稳定性等）作为一种化合物。因此，它可以作为治疗涉及Rho激酶的各种疾病的治疗药物。
• SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF
  申请人：Blackburn Christopher

  公开号：US20140243335A1

  公开（公告）日：2014-08-28

  This invention provides compounds of formula (I): wherein R 1 , R 1b , R 2a , R 2b , R 2c , and R 2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

  本发明提供了式（I）的化合物：其中R1、R1b、R2a、R2b、R2c和R2d的值如说明书中所述，可用作HDAC6的抑制剂。本发明还提供了包含本发明化合物的药物组合物以及使用该组合物治疗增生性、炎症性、感染性、神经系统或心血管疾病或疾患的方法。
• AMIDE COMPOUNDS
  申请人：Nozawa Eisuke

  公开号：US20110028463A1

  公开（公告）日：2011-02-03

  [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

  【问题】提供一种可用作治疗慢性肾功能不全或糖尿病肾病的药物化合物。 【解决问题的方法】本发明者对具有EP4受体拮抗作用的化合物进行了广泛的研究，结果发现具有羧酸基或其等效物的各种酰胺衍生物表现出优异的EP4受体拮抗作用，从而完成了本发明。由于本发明的化合物具有优异的EP4受体拮抗作用，因此可用作预防和/或治疗慢性肾功能不全或糖尿病肾病的药物。
• AMIDE COMPOUNDS AND USE THEREOF
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1270570A1

  公开（公告）日：2003-01-02

  The present invention relates to an amide compound of the formula wherein R1 is a hydrogen and the like, R2 is a hydrogen and the like, X is SO2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

  本发明涉及一种如下式的酰胺化合物 其中 R1 为氢等，R2 为氢等，X 为 SO2 等，Y 为式（III）等，a 为 2、其异构体或其药学上可接受的盐。本发明的化合物具有显著和选择性的 Rho 激酶抑制作用，无毒性问题，口服吸收和药物动力学（药物的吸收、分布、代谢、排泄等）良好，并显示出作为化合物的优越性能（如稳定性等）。因此，它可以作为一种治疗药物，用于治疗 Rho 激酶参与的各种疾病。