N4-ethyl-N2-(5-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine | 1374826-41-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N4-ethyl-N2-(5-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine
• 英文别名: 4-N-ethyl-2-N-[5-methyl-1-(oxan-4-yl)pyrazol-4-yl]-5-(trifluoromethyl)pyrimidine-2,4-diamine
• CAS: 1374826-41-1
• 化学式: C₁₆H₂₁F₃N₆O
• 分子量: 370.378
• InChiKey: GFPAWYQBVAEYSD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  76.9
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• [EN] PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS<br/>[FR] DÉRIVÉS DE PYRAZOLE AMINOPYRIMIDINE EN TANT QUE MODULATEURS DU LRRK2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012062783A1

  公开（公告）日：2012-05-18

  Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

  化合物的结构式（I）或其药用盐，其中X，R1，R2，R3，R4和R5如本文所定义。还公开了制备这些化合物的方法，并将这些化合物用于治疗与LRRK2受体相关的疾病，如帕金森病。
• PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
  申请人：Baker-Glenn Charles

  公开号：US20120157427A1

  公开（公告）日：2012-06-21

  Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

  化合物I的公式为：或其药学上可接受的盐，其中X，R1，R2，R3，R4和R5如本文所定义。还公开了制备该化合物的方法以及使用该化合物治疗与LRRK2受体相关的疾病，如帕金森病的方法。
• ASSAYS AND BIOMARKERS FOR LRRK2
  申请人：Genentech, Inc.

  公开号：EP2646819A1

  公开（公告）日：2013-10-09
• STABLE PHARMACEUTICAL COMPOSITION OF CLOPIDOGREL FREE BASE FOR ORAL AND PARENTERAL DELIVERY
  申请人：Huang Jingjun

  公开号：US20140227360A1

  公开（公告）日：2014-08-14

  The present disclosure provides ready-to-use, oil/water emulsion compositions with mean droplet size (intensity-average, m) of 100-500 nm, wherein the oil phase comprises clopidogrel free base dispersed in pharmaceutical acceptable oil(s). The emulsion uses clopidogrel free base or premix of clopidogrel free base in oil(s) as the starting materials and may also contain one or more excipients such as surfactant and or co-surfactant, osmotic agent, pH adjustment agent, antioxidant, preservative, sweetener, and/or suspending agent, etc. The emulsion formulations and method of manufacturing significantly improves the stability of clopidogrel over other aqueous based formulations (such as cyclodextrin-based formulations and emulsion made using clopidogrel salt as the starting materials) with respect to chiral degradation, hydrolytic, and thermal degradation. Ready-to-use emulsion compositions, which can be administered orally or parentally as a single high dose with up to 300 mg of clopidogrel dose, can be prepared and stored at room temperature for at least 19 weeks or at refrigeration temperature for at least 1 year. The compositions will provide rapid therapeutic action as anti-platelet agent for patient under emergence and intense care or who cannot swallow tablet dosage form.
• US8815882B2
  申请人：——

  公开号：US8815882B2

  公开（公告）日：2014-08-26