4-(1-phenylcyclopropylamino)-6-(4-(4-propionylpiperazin-1-yl)phenylamino)nicotinamide | 1374211-57-0

• 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: 4-(1-phenylcyclopropylamino)-6-(4-(4-propionylpiperazin-1-yl)phenylamino)nicotinamide
• 英文别名: 4-[(1-phenylcyclopropyl)amino]-6-[4-(4-propanoylpiperazin-1-yl)anilino]pyridine-3-carboxamide
• CAS: 1374211-57-0
• 化学式: C₂₈H₃₂N₆O₂
• 分子量: 484.601
• InChiKey: LMENZUNITRTKNP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  104
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-苯基环丙胺 在 palladium diacetate caesium carbonate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 乙腈 为溶剂， 反应 63.0h， 生成 4-(1-phenylcyclopropylamino)-6-(4-(4-propionylpiperazin-1-yl)phenylamino)nicotinamide
  参考文献：
  名称：

  NICOTINAMIDES AS JAK KINASE MODULATORS

  摘要：

  本发明涉及具有公式I的化合物及其药用可接受的盐、酯和前药，这些化合物是JAK激酶的抑制剂。本发明还涉及用于制备这类化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由JAK激酶活性介导的多种疾病条件的方法，例如不良血栓形成和非霍奇金淋巴瘤。

  公开号：

  US20120108566A1

文献信息

• Nicotinamides as JAK kinase modulators
  申请人：Bauer Shawn M.

  公开号：US09102625B2

  公开（公告）日：2015-08-11

  The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及化合物I的制备及其药物可接受的盐、酯和前药，这些化合物是JAK激酶的抑制剂。本发明还涉及用于制备这些化合物的中间体，制备这种化合物的方法，含有这种化合物的制药组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗由JAK激酶活性至少部分介导的多种情况，如不良血栓形成和非霍奇金淋巴瘤的方法。
• US9102625B2
  申请人：——

  公开号：US9102625B2

  公开（公告）日：2015-08-11
• [EN] NICOTINAMIDES AS JAK KINASE MODULATORS<br/>[FR] NICOTINAMIDES EN TANT QUE MODULATEURS DES JAK KINASES
  申请人：PORTOLA PHARM INC

  公开号：WO2012061428A2

  公开（公告）日：2012-05-10

  The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods ofinhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
• NICOTINAMIDES AS JAK KINASE MODULATORS
  申请人：Bauer Shawn M.

  公开号：US20120108566A1

  公开（公告）日：2012-05-03

  The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及具有公式I的化合物及其药用可接受的盐、酯和前药，这些化合物是JAK激酶的抑制剂。本发明还涉及用于制备这类化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由JAK激酶活性介导的多种疾病条件的方法，例如不良血栓形成和非霍奇金淋巴瘤。