5-(溴甲基)-2-甲基嘧啶 | 802559-38-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 5-(溴甲基)-2-甲基嘧啶
• 英文名称: 2-Methyl-5-brommethylpyrimidin
• 英文别名: 5-(Bromomethyl)-2-methylpyrimidine；5-(bromomethyl)-2-methylpyrimidine
• CAS: 802559-38-2
• 化学式: C₆H₇BrN₂
• 分子量: 187.039
• InChiKey: RKNJOWSXQZGAMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] PYRROLIDINE AND BICYCLOHETEROARYL CONTAINING OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA CONTENANT DE LA PYRROLIDINE ET DE LA BICYCLOHÉTÉROARYLE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021094312A1

  公开（公告）日：2021-05-20

  The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations; or alpha synucleinopathies, in particular Parkinson's disease, dementia due to Parkinson's (or neurocognitive disorder due to Parkinson's disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher's disease.

  本发明涉及O-GIcNAc水解酶（OGA）抑制剂。该发明还涉及包含这类化合物的药物组合物，制备这类化合物和组合物的方法，以及利用这类化合物和组合物预防和治疗抑制OGA有益的疾病，如tau病变，特别是阿尔茨海默病或进行性上行性麻痹；以及伴有tau病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩侧索硬化或额颞叶痴呆；或α-突触核蛋白病，特别是帕金森病，由帕金森病引起的痴呆（或由帕金森病引起的神经认知障碍），具有Lewy小体的痴呆，多系统萎缩，或由高雪氏病引起的α-突触核蛋白病。
• [EN] OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2019243530A1

  公开（公告）日：2019-12-26

  The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).

  本发明涉及具有式(I)所示结构的O-GIcNAc水解酶（OGA）抑制剂。该发明还涉及包含这种化合物的药物组合物、制备这种化合物和组合物的方法，以及利用这种化合物和组合物预防和治疗抑制OGA有益的疾病，如tau病变，特别是阿尔茨海默病或进行性上核性麻痹；以及伴有tau病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩侧索硬化或额颞叶痴呆症。其中RB是从（b-1）到（b-6）组成的芳香杂双环基团。
• KINASE INHIBITOR AND USE THEREOF
  申请人：Xuanzhu Pharma Co., Ltd.

  公开号：EP3091008A1

  公开（公告）日：2016-11-09

  The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.

  本发明涉及一种CDK4/6激酶抑制剂，或其药学上可接受的盐、酯或溶液剂，或其异构体；包含所述CDK4/6激酶抑制剂，或其药学上可接受的盐、酯或溶液剂，或其异构体的药物制剂、药物组合物和试剂盒，以及所述CDK4/6激酶抑制剂，或其药学上可接受的盐、酯或溶液剂，或其异构体的用途。例如，本发明的化合物可用于降低或抑制细胞中CDK4/6激酶的活性，和/或治疗和/或预防由CDK4/6激酶介导的癌症相关疾病。
• PIPERIDINES OR PIPERIDONES SUBSTITUTED WITH UREA AND HETEROARYL
  申请人：Grünenthal GmbH

  公开号：EP3789378A1

  公开（公告）日：2021-03-10

  The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.

  本发明涉及一种符合通式 (I) 的化合物 它作为 FPR2 的调节剂，可用于治疗和/或预防至少部分由 FPR2 介导的疾病。
• OGA INHIBITOR COMPOUNDS
  申请人：Janssen Pharmaceutica NV

  公开号：EP3810612A1

  公开（公告）日：2021-04-28