N~1~-({5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N~1~,N~2~-dimethylethane-1,2-diamine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N~1~-({5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N~1~,N~2~-dimethylethane-1,2-diamine
• 英文别名: N'-[[5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N,N'-dimethylethane-1,2-diamine
• 化学式: C₂₀H₃₈N₄O₂
• 分子量: 366.5
• InChiKey: SPEGERVLTUWZPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  26
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  62.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS D'ARGININE MÉTHYLTRANSFÉRASE ET LEURS UTILISATIONS
  申请人：EPIZYME INC

  公开号：WO2016044626A1

  公开（公告）日：2016-03-24

  Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

  本文描述了式（S-I）的化合物，其药用盐以及药物组合物。本文描述的化合物对抑制精氨酸甲基转移酶活性有用。还描述了利用这些化合物治疗精氨酸甲基转移酶介导的疾病的方法。
• ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
  申请人：EPIZYME, INC.

  公开号：US20160024016A1

  公开（公告）日：2016-01-28

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

  本文描述了式(I)的化合物，其药学上可接受的盐以及其制药组合物。所述化合物可用于抑制精氨酸甲基转移酶活性。本文还描述了使用这些化合物治疗精氨酸甲基转移酶介导的疾病的方法。
• Arginine methyltransferase inhibitors and uses thereof
  申请人：Epizyme, Inc.

  公开号：US10800743B2

  公开（公告）日：2020-10-13

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

  本文描述了式（I）化合物、其药学上可接受的盐及其药物组合物。本文所述化合物可用于抑制精氨酸甲基转移酶活性。还描述了使用这些化合物治疗精氨酸甲基转移酶介导的疾病的方法。
• Combination therapy
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US11197857B2

  公开（公告）日：2021-12-14

  The present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a Type II protein arginine methyltransferase (Type II PRMT) inhibitor. The present invention also provides methods for treating cancer in a human in need thereof, the methods comprising administering to the human a combination of a Type I PRMT inhibitor and a Type II PRMT inhibitor, together with at least one of: a pharmaceutically acceptable carrier and a pharmaceutically acceptable diluent, thereby treating the cancer in the human. The present invention further provide a pharmaceutical composition comprising a therapeutically effective amount of a Type I PRMT inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of a Type II PRMT inhibitor.

  本发明提供了 I 型蛋白精氨酸甲基转移酶（I 型 PRMT）抑制剂和 II 型蛋白精氨酸甲基转移酶（II 型 PRMT）抑制剂的组合。本发明还提供了治疗有需要的人的癌症的方法，该方法包括向该人施用 I 型 PRMT 抑制剂和 II 型 PRMT 抑制剂的组合，以及以下至少一种：药学上可接受的载体和药学上可接受的稀释剂，从而治疗该人的癌症。本发明进一步提供一种药物组合物，包含治疗有效量的 I 型 PRMT 抑制剂和第二种药物组合物，包含治疗有效量的 II 型 PRMT 抑制剂。
• COMBINATION THERAPY
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US20190343803A1

  公开（公告）日：2019-11-14

  In one embodiment, the present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and an immuno-modulatory agent selected from: an anti-PD-1 antibody or antigen binding fragment thereof, an anti-PDL1 antibody or antigen binding fragment thereof, and an anti-OX40 antibody or antigen binding fragment thereof. In another embodiment, the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of an immuno-modulatory agent selected from: an anti-PD-1 antibody or antigen binding fragment thereof, an anti-PDL1 antibody or antigen binding fragment thereof, and an anti-OX40 antibody or antigen binding fragment thereof. In another embodiment, methods for treating cancer in a human in need thereof are provided, the methods comprising administering to the human the combinations or pharmaceutical compositions provided herein.