US10093646, Example 8 | 1801747-12-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: US10093646, Example 8
• 英文别名: 6-[4-(aminomethyl)-4-methylpiperidin-1-yl]-3-(2,3-dichlorophenyl)pyrazin-2-amine
• CAS: 1801747-12-5
• 化学式: C₁₇H₂₁Cl₂N₅
• 分子量: 366.3
• InChiKey: ZAMNYDQBNJFTSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  81.1
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] 1 -PYRIDAZIN-/TRIAZIN-3-YL-PIPER(-AZINE)/IDINE/PYROLIDINE DERIVATIVES AND AND COMPOSITIONS THEREOF FOR INHIBITING THE ACTIVITY OF SHP2<br/>[FR] DÉRIVÉS DE 1-PYRIDAZIN-/TRIAZIN-3-YL-PIPER(-AZINE)/IDINE/PYROLIDINE ET COMPOSITIONS LES CONTENANT POUR L'INHIBITION DE L'ACTIVITÉ DE SHP2
  申请人：NOVARTIS AG

  公开号：WO2015107493A1

  公开（公告）日：2015-07-23

  The present invention relates to compounds of formula (I): in which m, p,Y1 Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R4a and R5b are defined in the claims; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

  本发明涉及式(I)的化合物：其中m、p、Y1、Y2、Y3、R1、R2a、R2b、R3a、R3b、R4a、R4b、R4a和R5b在权利要求中定义；能够抑制SHP2活性。该发明还提供了一种制备该类化合物的方法，包括含有这类化合物的药物制剂以及在管理与SHP2异常活性相关的疾病或疾病中使用这类化合物和组合物的方法。
• 1-PYRIDAZIN-/TRIAZIN-3-YL-PIPER(-AZINE)/IDINE/PYROLIDINE DERIVATIVES AND COMPOSITIONS THEREOF FOR INHIBITING THE ACTIVITY OF SHP2
  申请人：CHEN Christine Hiu-tung

  公开号：US20170204080A1

  公开（公告）日：2017-07-20

  The present invention relates to compounds of formula I: in which m, Y 1 , Y 2 , Y 3 , R 1 , R 2a , R 2b , R 3a , R 3b , R 4a , R 4b , R 5a and R 5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

  本发明涉及式I的化合物： 其中m，Y1，Y2，Y3，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a和R5b在本发明概要中有定义；能够抑制SHP2活性。本发明还提供了一种制备本发明化合物的方法，包括含有这种化合物的药物制剂以及在管理与SHP2异常活性相关的疾病或紊乱的方法中使用这种化合物和组合物。
• [EN] PHARMACEUTICAL COMBINATION COMPRISING AN ALK INHIBITOR AND A SHP2 INHIBITOR<br/>[FR] COMBINAISON PHARMACEUTIQUE COMPRENANT UN INHIBITEUR D'ALK ET UN INHIBITEUR DE SHP2
  申请人：NOVARTIS AG

  公开号：WO2018130928A1

  公开（公告）日：2018-07-19

  A pharmaceutical combination comprising an ALK inhibitor, in free form or a pharmaceutically acceptable salt thereof, and a SHP2 inhibitor, in free form or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, for simultaneous or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

  一种药物组合物，包括自由形式或其药学上可接受的盐形式的ALK抑制剂和SHP2抑制剂，以及可选的药学上可接受的载体，用于同时或顺序给药；该组合物在治疗增生性疾病中的用途；以及治疗患有增生性疾病的受试者的方法，包括给予该组合物的治疗有效量。
• 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
  申请人：Chen Christine Hiu-Tung

  公开号：US10774065B2

  公开（公告）日：2020-09-15

  The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

  本发明涉及式 I 的化合物： 其中m、Y1、Y2、Y3、R1、R2a、R2b、R3a、R3b、R4a、R4b、R5a和R5b在发明概述中定义；能够抑制SHP2的活性。本发明进一步提供了制备本发明化合物的工艺、包含此类化合物的药物制剂以及使用此类化合物和组合物治疗与SHP2活性异常有关的疾病或紊乱的方法。
• SHP2 INHIBITORS AND METHODS OF USE THEREOF
  申请人：Research Development Foundation

  公开号：US20190231805A1

  公开（公告）日：2019-08-01

  Provided are methods for the treatment of insulin resistance and insulin receptor diseases with SHP2 inhibitors, such as allosteric inhibitors of SHP2 and RNAi or siRNA that target SHP2 expression. Compositions and methods for delivery of SHP2 inhibitors, such as liver-targeting liposomes or nanoparticles, are also provided.