2-(5H-imidazo[5,1-α]isoindol-5-yl)-1-(piperidin-4-yl)ethanol | 1402836-85-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-(5H-imidazo[5,1-α]isoindol-5-yl)-1-(piperidin-4-yl)ethanol
• 英文别名: US10233190, Example 1370；2-(5H-imidazo[5,1-a]isoindol-5-yl)-1-piperidin-4-ylethanol
• CAS: 1402836-85-4
• 化学式: C₁₇H₂₁N₃O
• 分子量: 283.373
• InChiKey: XRBKUEHFWMLWQX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  50.1
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Fused Imidazole Derivatives Useful as IDO Inhibitors
  申请人：NewLink Genetics Corporation

  公开号：US20140066625A1

  公开（公告）日：2014-03-06

  Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleanine 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IDO抑制剂及其制药组合物，用于调节吲哚胺2,3-双加氧酶的活性；治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制；治疗受益于抑制吲哚胺-2,3-双加氧酶酶活性的医疗状况；增强包括给予抗癌药物在内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；以及治疗与传染病相关的免疫抑制。
• COMPOSITIONS COMPRISING FUSED IMIDAZOLE DERIVATIVES USEFUL AS IDO INHIBITORS
  申请人：Newlink Genetics Corporation

  公开号：EP3348558A1

  公开（公告）日：2018-07-18

  Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated inimunosuppression; 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 immunosuppression associated with an infectious disease.

  目前提供的IDO抑制剂及其药物组合物可用于调节吲哚胺-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-2,3-二氧化酶酶活性中获益的病症；提高抗癌治疗的有效性，包括施用抗癌剂；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。
• FUSED IMIDAZOLE COMPOUND HAVING INDOLEAMINE 2,3-DIOXYGENASE INHIBITORY ACTIVITY
  申请人：Shenzhen Chipscreen Biosciences Co., Ltd.

  公开号：EP3560928A1

  公开（公告）日：2019-10-30

  The invention discloses a type of fused imidazole compound, preparation method and application thereof. The structure of the compound is shown in general formula I. The definition of each group therein is as described in the specification. These compounds are capable of selectively inhibiting indoleamine 2,3-dioxygenase (IDO). The compounds can act as an IDO inhibitor for treating and/or preventing a disease having a pathological feature with IDO-mediated tryptophan metabolic pathways, for example, cancer, eye disease, autoimmune disease, psychological disorder, depression symptom, anxiety disorder and other diseases.

  本发明公开了一种融合咪唑化合物及其制备方法和应用。该化合物的结构如通式 I 所示。其中各基团的定义如说明书所述。这些化合物能够选择性地抑制吲哚胺 2,3-二氧化酶（IDO）。这些化合物可作为 IDO 抑制剂，用于治疗和/或预防具有 IDO 介导的色氨酸代谢途径病理特征的疾病，例如癌症、眼病、自身免疫性疾病、心理障碍、抑郁症状、焦虑症和其他疾病。
• IDO inhibitors
  申请人：NewLink Genetics Corporation

  公开号：US10233190B2

  公开（公告）日：2019-03-19

  Presently provided are IDO inhibitors and pharmaceutical compositions thereof, 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.

  目前提供的 IDO 抑制剂及其药物组合物可用于调节吲哚胺-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 化酶酶活性中获益的病症；提高抗癌治疗的有效性，包括施用抗癌剂；治疗与癌症相关的肿瘤特异性免疫抑制；以及治疗与传染病相关的免疫抑制。
• Heterocycles useful as IDO and TDO inhibitors
  申请人：Hangzhou Innogate Pharma Co., Ltd.

  公开号：US10358451B2

  公开（公告）日：2019-07-23

  Provided are compounds of Formula (I) shown below using for treatment of diseases or disorders mediated by IDO and/or TDO, pharmaceutical compositions and methods of preparation thereof.

  本发明提供了用于治疗 IDO 和/或 TDO 介导的疾病或紊乱的下式（I）化合物、药物组合物及其制备方法。