6-(4-cyclopropylpiperazin-1-yl)pyridin-3-amine | 1180133-30-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 6-(4-cyclopropylpiperazin-1-yl)pyridin-3-amine
• 英文别名: 6-(4-cyclopropyl-piperazin-1-yl)-pyridin-3-ylamine
• CAS: 1180133-30-5
• 化学式: C₁₂H₁₈N₄
• 分子量: 218.302
• InChiKey: AGLIGQPGUGTVRW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  45.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-环丙基-4-(5-硝基-吡啶-2-基)-哌嗪 在 palladium on activated charcoal 、 氢气 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 20.0 ℃ 、241.32 kPa 条件下， 反应 3.0h， 以175 mg的产率得到6-(4-cyclopropylpiperazin-1-yl)pyridin-3-amine
  参考文献：
  名称：

  [EN] INDOLINONE COMPOUNDS FOR USE AS MAP4K1 INHIBITORS
  [FR] COMPOSÉS D'INDOLINONE SERVANT D'INHIBITEURS DE MAP4K1

  摘要：

  本公开涉及式(I)的化合物及其药用盐，其中环A、环C、X1、X2、L1、R1、R2、R3、R4、R5、R6、R7、m和n如本文所定义，这些化合物可用作MAP4K1抑制剂，其制备方法，包含这些化合物的药物组合物，以及这些化合物或组合物在治疗或预防由MAP4K1介导的各种疾病、症状和/或紊乱中的用途。

  公开号：

  WO2020070331A1

文献信息

• [EN] PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES<br/>[FR] DÉRIVÉS DE PYRIMIDINE CAPABLES D'INHIBER UNE OU PLUSIEURS KINASES
  申请人：MEDICAL RES COUNCIL

  公开号：WO2009122180A1

  公开（公告）日：2009-10-08

  A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.

  本发明的第一个方面涉及式(I)的化合物，或其药学上可接受的盐或酯，式(I)如下：其中：R1为C3-8环烷基；X为O、NR7或C3-6杂环烷基；R2为芳基、杂芳基、融合或未融合的芳基-C3-6杂环烷基或融合或未融合的杂芳基-C3-6杂环烷基，每个基可选择地由来自芳基、杂芳基、C1-6烷基、C3-7环烷基和A基的一个或多个取代基取代，其中所述C1-6烷基基可选择地由来自芳基、杂芳基、R10和A基的一个或多个取代基取代，所述杂芳基可选择地由一个或多个R10基取代；以及所述C3-6杂环烷基基可选择地包含一个或多个来自氧、硫、氮和CO的基；R3为C1-6烷基，可选择地由一个或多个来自芳基、杂芳基、-NR4R5、-OR6、-NR7(CO)R6、-NR7(CO)NR4R5、-NR7SO2R6、-NR7COOR7、-CONR4R5、C3-6杂环烷基和式(a, b, c)的取代基取代；其中R4-7和A如权利要求中所定义。进一步方面涉及所述化合物在治疗各种治疗性疾病中的使用，特别是作为一个或多个激酶的抑制剂。
• HETEROCYCLIC COMPOUNDS
  申请人：GAUL Christoph

  公开号：US20090203688A1

  公开（公告）日：2009-08-13

  The invention relates to compounds of formula I and salts thereof wherein the substituents are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

  该发明涉及公式I的化合物及其盐，其中取代基如规范中定义，以及其制备方法；含有这种化合物的药物，特别用于在一个或多个蛋白酪氨酸激酶介导的疾病中使用。
• Compound
  申请人：Mciver Edward Giles

  公开号：US20100056524A1

  公开（公告）日：2010-03-04

  A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R 1 is C 3-8 -cycloalkyl; X is O, NR 7 or C 3-6 -heterocycloalkyl; R 2 is aryl, heteroaryl, fused or unfused aryl-C 3-6 -heterocycloalkyl or fused or unfused heteroaryl-C 3-6 -heterocycloalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C 1-6 -alkyl, C 3-7 -cycloalkyl and a group A, wherein said C 1-6 -alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R 10 and a group A, said heteroaryl group is optionally substituted by one or more R 10 groups; and wherein said C 3-6 -heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R 3 is C 1-6 -alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, —NR 4 R 5 , —OR 6 , —NR 7 (CO)R 6 , —NR 7 (CO)NR 4 R 5 , —NR 7 SO 2 R 6 , —NR 7 COOR 7 , —CONR 4 R 5 , C 3-6 -heterocycloalkyl and wherein R 4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.

  本发明的第一方面涉及化合物(I)的公式，或其药学上可接受的盐或酯，其中： R1是C3-8环烷基；X是O，NR7或C3-6杂环烷基；R2是芳基、杂芳基、融合或未融合的芳基-C3-6杂环烷基或融合或未融合的杂芳基-C3-6杂环烷基，其中每个基团可选地由一个或多个取代基选自芳基、杂芳基、C1-6烷基、C3-7环烷基和A组成，其中所述的C1-6烷基可选地由一个或多个取代基选自芳基、杂芳基、R10和A组成，所述的杂芳基可选地由一个或多个R10基团取代；其中所述的C3-6杂环烷基可选地包含一个或多个选自氧、硫、氮和CO的基团；R3是C1-6烷基，可选地被一个或多个取代基选自芳基、杂芳基、-NR4R5、-OR6、-NR7(CO)R6、-NR7(CO)NR4R5、-NR7SO2R6、-NR7COOR7、-CONR4R5、C3-6杂环烷基和其中R4-7和A如权利要求所定义。 进一步的方面涉及所述化合物在治疗各种治疗性疾病中的应用，特别是作为一个或多个激酶的抑制剂。
• PYRROLO [2, 3-D]PYRIDINES AND USE THEREOF AS TYROSINE KINASE INHIBITORS
  申请人：Novartis AG

  公开号：EP2247591A1

  公开（公告）日：2010-11-10
• INDOLINONE COMPOUNDS FOR USE AS MAP4K1 INHIBITORS
  申请人：ICHNOS SCIENCES S.A.

  公开号：EP3860976A1

  公开（公告）日：2021-08-11