1-(4-nitrobenzyl)-5-phenyl-1H-imidazole | 1185760-56-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(4-nitrobenzyl)-5-phenyl-1H-imidazole
• 英文别名: 1-[(4-Nitrophenyl)methyl]-5-phenylimidazole
• CAS: 1185760-56-8
• 化学式: C₁₆H₁₃N₃O₂
• 分子量: 279.298
• InChiKey: CHOAUJWZAOEZCR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  63.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• N-benzyl imidazole derivatives and their use as aldosterone synthase inhibitors
  申请人：Maastricht University

  公开号：EP2095819A1

  公开（公告）日：2009-09-02

  The invention relates to the use of a N-benzyl 5-substituted imidazole derivative having the general formula I wherein R is (C1-3)alkyl, (C1-3)alkyloxy, halogen, nitro or cyano; R1 is (C1-6)alkyl, optionally substituted with OH, (C1-3)alkyloxy, (C1-3)alkylcarbonyloxy, (C1-3)alkyloxycarbonyl or halogen, or (C1-3)alkyloxycarbonyl; or R1 is phenyl, optionally substituted with 1-3 substituents independently selected from (C1-3)alkyl, (C1-3)alkyloxy, hydroxylmethyl and halogen; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of a disorder or disease in a subject mediated by aldosterone synthase or responsive to inhibition of aldosterone synthase.

  该发明涉及使用具有通式I的N-苄基5-取代咪唑衍生物，其中R为(C1-3)烷基，(C1-3)烷氧基，卤素，硝基或氰基；R1为(C1-6)烷基，可选择地取代为羟基，(C1-3)烷氧基，(C1-3)烷基羰氧基，(C1-3)烷氧羰基或卤素，或(C1-3)烷氧羰基；或R1为苯基，可选择地取代为1-3个独立选择自(C1-3)烷基，(C1-3)烷氧基，羟甲基和卤素的取代基；或其药学上可接受的盐，用于制备一种药物，用于治疗由醛固酮合酶介导或对醛固酮合酶抑制响应的受体引起的主体的紊乱或疾病。
• IDO Inhibitors
  申请人：Mautino Mario R.

  公开号：US20110136796A1

  公开（公告）日：2011-06-09

  Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R 1 , R 4 , and R 5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

  目前提供了按照公式(I)或(II)定义的化合物以及含有这些化合物的药物组合物，其中R1、R4和R5的定义在此处。这些化合物和组合物对于调节吲哚胺2,3-二氧化酶的活性；治疗吲哚胺2,3-二氧化酶(IDO)介导的免疫抑制；治疗从抑制吲哚胺-2,3-二氧化酶的酶活性中获益的医疗状况；增强包括给予抗癌剂的抗癌治疗的有效性；治疗与癌症相关的肿瘤特异性免疫抑制；以及治疗与传染性疾病相关的免疫抑制具有用处。
• US8748469B2
  申请人：——

  公开号：US8748469B2

  公开（公告）日：2014-06-10
• US9174942B2
  申请人：——

  公开号：US9174942B2

  公开（公告）日：2015-11-03
• [EN] N-BENZYL IMIDAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS DE N-BENZYL-IMIDAZOLE
  申请人：MAASTRICHT UNIVERSITY

  公开号：WO2009106640A2

  公开（公告）日：2009-09-03

  The invention relates to the use of a N-benzyl 5-substituted imidazole derivative having the general formula (I) wherein R is (C1-3)alkyl, (C1-3)alkyloxy, halogen, nitro or cyano; R1 is formyl, (C1-6)alkyl, optionally substituted with OH, (C1-3)alkyloxy, (C1-3)alkylcarbonyloxy, (C1-3)alkyloxy- carbonyl or halogen, or (C1-3)alkyloxycarbonyl; or R1 is phenyl, optionally substituted with 1 -3 substituents independently selected from (C1-3)alkyl, (C1-3)alkyloxy, hydroxylmethyl and halogen; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of a disorder or disease in a subject mediated by aldosterone synthase or responsive to inhibition of aldosterone synthase.