Pyrrolo[1,2-c]triazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并三嗪类
• 英文名称: Pyrrolo[1,2-c]triazine
• 英文别名: pyrrolo[1,2-c]triazine
• 化学式: C₆H₅N₃
• 分子量: 119.12
• InChiKey: VCHXQLRJCRBXOD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
  申请人：Epizyme, Inc.

  公开号：US20140315961A1

  公开（公告）日：2014-10-23

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention 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药物组成物。本发明的化合物对抑制精氨酸甲基转移酶活性是有用的。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。
• [EN] SUBSTITUTED PYRROLO[1,2-α]TRIAZINES AND RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS<br/>[FR] PYRROLO[1,2-Α]TRIAZINES SUBSTITUÉES ET COMPOSÉS APPARENTÉS ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES MÉDICAUX
  申请人：LYSOSOMAL THERAPEUTICS INC

  公开号：WO2017192929A1

  公开（公告）日：2017-11-09

  The invention provides substituted pyrrolo[1,2-α]triazine compounds, related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]triazines compounds described herein include substituted 2,4-dimethyl-pyrrolo[1,2-α] [1,3,5]triazine-8-carboxamide compounds and variants thereof.

  该发明提供了替代吡咯并[1,2-α]三唑化合物，相关化合物，含有这些化合物的组合物，医疗用品包，以及使用这些化合物和组合物来治疗医学疾病的方法，例如高雪氏病、帕金森病、Lewy小体病、痴呆症或多系统萎缩症等。本文描述的示例替代吡咯并[1,2-a]三唑化合物包括替代的2,4-二甲基-吡咯并[1,2-α][1,3,5]三唑-8-羧酰胺化合物及其变体。
• PRMT1 INHIBITORS AND USES THEREOF
  申请人：Epizyme, Inc.

  公开号：US20140288140A1

  公开（公告）日：2014-09-25

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.

  本文描述了式（I）的化合物，其药用盐以及药物组成物。本文描述的化合物可用于抑制PRMT1活性。还描述了使用这些化合物治疗PRMT1介导的疾病的方法。
• [EN] 4-[[(7-AMINOPYRAZOLO[1,5-A]PYRIMIDIN-5-YL)AMINO]METHYL]PIPERIDIN-3-OL COMPOUNDS AND THEIR THERAPEUTIC USE<br/>[FR] COMPOSÉS DE 4-[[(7-AMINOPYRAZOLO[1,5-A]PYRIMIDIN-5-YL)AMINO]MÉTHYL]PIPÉRIDIN-3-OL ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：CARRICK THERAPEUTICS LTD

  公开号：WO2021122745A1

  公开（公告）日：2021-06-24

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain H-APPAMP compounds (referred to herein as "H-APPAMP compounds") that, inter alia, inhibit cyclin-dependent protein kinases (CDKs), especially CDK12 and/or CDK13, and are selective, for example, for CDK12 and/or CDK13 as compared to CDK7. In addition to selectively inhibiting CDK12 and/or CDK13, the compounds also act as selective Cyclin K degraders thereby removing the key signaling mechanism required for CDK12 and/or CDK13 activation; this confers additional cellular potency and selectivity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CDK, especially CDK12 and/or CDK13; and to treat disorders including: disorders that are associated with CDK, especially CDK12 and/or CDK13; disorders that result from an inappropriate activity of a CDK, especially CDK12 and/or CDK13; disorders that are associated with CDK mutation, especially CDK12 and/or CDK13mutation; disorders that are associated with CDK overexpression, especially CDK12 and/or CDK13 overexpression; disorders that are associated with upstream pathway activation of CDK, especially CDK12 and/or CDK13; disorders that are ameliorated by the inhibition of CDK, especially CDK12 and/or CDK13; proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischaemia; renal diseases; cardiovascular disorders (including atherosclerosis); autoimmune disorders (including rheumatoid arthritis); and disorders caused by dysfunction of translation in cells (including muscular dystrophy). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with a further active agent which is, e.g., an aromatase inhibitor, an anti estrogen, an anti-androgen, a Her2 blocker, a cytotoxic chemotherapeutic agent, an agent stimulating the immune system, a checkpoint inhibitor, a DMA repair inhibitor, etc.

  本发明一般涉及治疗化合物领域。更具体地，本发明涉及某些H-APPAMP化合物（以下简称为“H-APPAMP化合物”），其中包括抑制细胞周期依赖性蛋白激酶（CDKs），特别是CDK12和/或CDK13，并且具有选择性，例如与CDK7相比，对CDK12和/或CDK13有选择性。除了选择性地抑制CDK12和/或CDK13外，这些化合物还作为选择性的Cyclin K降解物，从而去除了CDK12和/或CDK13激活所需的关键信号机制；这赋予了额外的细胞效力和选择性。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物和组合物，无论是在体外还是在体内，来抑制CDK，特别是CDK12和/或CDK13；以及治疗包括以下疾病的疾病：与CDK有关的疾病，特别是与CDK12和/或CDK13有关的疾病；由于CDK不恰当活性导致的疾病，特别是由于CDK12和/或CDK13不恰当活性导致的疾病；与CDK突变有关的疾病，特别是与CDK12和/或CDK13突变有关的疾病；与CDK过度表达有关的疾病，特别是与CDK12和/或CDK13过度表达有关的疾病；与CDK上游途径激活有关的疾病，特别是与CDK12和/或CDK13上游途径激活有关的疾病；通过抑制CDK改善的疾病，特别是通过抑制CDK12和/或CDK13改善的疾病；增生性疾病；癌症；病毒感染（包括HIV）；神经退行性疾病（包括阿尔茨海默病和帕金森病）；缺血；肾脏疾病；心血管疾病（包括动脉粥样硬化）；自身免疫性疾病（包括类风湿性关节炎）；以及由细胞中翻译功能失调引起的疾病（包括肌肉萎缩症）的疾病。可选地，治疗进一步包括与另一活性药剂的治疗（例如同时或顺序治疗），该药剂可以是芳香化酶抑制剂、抗雌激素、抗雄激素、Her2阻断剂、细胞毒化疗药物、刺激免疫系统的药剂、检查点抑制剂、DNA修复抑制剂等。
• PRMT5 INHIBITORS AND USES THEREOF
  申请人：Epizyme, Inc.

  公开号：US20140221345A1

  公开（公告）日：2014-08-07

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-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药物组合物。本发明的化合物可用于抑制PRMT5活性。还描述了使用这些化合物治疗PRMT5介导的疾病的方法。