N2-(4-methoxy-6-(thiazol-5-yl)pyridin-3-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine | 1440963-64-3

• 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: N2-(4-methoxy-6-(thiazol-5-yl)pyridin-3-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
• 英文别名: N2-(4-Methoxy-6-(thiazol-5-yl)pyridin-3-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine；2-N-[4-methoxy-6-(1,3-thiazol-5-yl)pyridin-3-yl]-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
• CAS: 1440963-64-3
• 化学式: C₁₅H₁₃F₃N₆OS
• 分子量: 382.369
• InChiKey: UDDBPMAJONZIOE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  6-氯-4-甲氧基-3-吡啶胺 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 对甲苯磺酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 19.17h， 生成 N2-(4-methoxy-6-(thiazol-5-yl)pyridin-3-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
  参考文献：
  名称：

  [EN] 2-(PHENYL OR PYRID-3-YL) AMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE
  [FR] DÉRIVÉS 2-(PHÉNYL OU PYRID-3-YL)AMINOPYRIMIDINES EN TANT QUE MODULATEURS DE LA KINASE LRRK2 POUR LE TRAITEMENT DE LA MALADIE DE PARKINSON

  摘要：

  化合物的结构式（I），或其药用盐，其中m、n、X、R1、R2、R3、R4和R5的定义如本文所述。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。

  公开号：

  WO2013079495A1

文献信息

• AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
  申请人：Genentech, Inc.

  公开号：US20130158057A1

  公开（公告）日：2013-06-20

  Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. 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.

  公式I的化合物或其药学上可接受的盐，其中m，n，X，R1，R2，R3，R4和R5的定义如本文所述。还揭示了制备这些化合物的方法以及使用这些化合物治疗与LRRK2受体相关的疾病，如帕金森病。
• Aminopyrimidine derivatives as LRRK2 modulators
  申请人：Genentech, Inc.

  公开号：US08791130B2

  公开（公告）日：2014-07-29

  Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. 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.

  式I的化合物，或其药学上可接受的盐，其中m、n、X、R1、R2、R3、R4和R5的定义如本文所述。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。
• 2-(PHENYL OR PYRID-3-YL)AMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE
  申请人：F.Hoffmann-La Roche AG

  公开号：EP2785711B1

  公开（公告）日：2016-08-03
• 2-(PHENYL OR PYRID-3-YL) AMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE
  申请人：F.Hoffmann-La Roche AG

  公开号：EP2785711A1

  公开（公告）日：2014-10-08
• PHOSPHO-RAB ANTIBODIES, ASSAYS AND METHODS OF USE THEREOF
  申请人：Denali Therapeutics Inc.

  公开号：US20210147573A1

  公开（公告）日：2021-05-20

  In one aspect, antibodies that specifically bind to a phosphorylated Rab protein are provided. In some embodiments, the antibody is a monoclonal antibody that specifically binds to a phosphorylated human Rab10 protein and recognizes an epitope within or comprising the sequence AGQERFH(pT)ITTSYYR. In some embodiments, the antibody is a monoclonal antibody that specifically binds to a phosphorylated human Rab8a protein and recognizes an epitope within or comprising the sequence QERFR(pT)ITTAY. Methods and materials for detecting LRRK2 and Rab protein are also provided.