2-((3-(1H-1,2,3-triazol-2-yl)phenyl)amino)-6-(((1R,2S)-2-aminocyclohexyl)amino)-5-fluoronicotinamide | 1374969-26-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-((3-(1H-1,2,3-triazol-2-yl)phenyl)amino)-6-(((1R,2S)-2-aminocyclohexyl)amino)-5-fluoronicotinamide
• 英文别名: 2-(3-(1H-1,2,4-triazol-1-yl)phenylamino)-6-((1R,2S)-2-aminocyclohexylamino)-5-fluoronicotinamide；6-[[(1R,2S)-2-aminocyclohexyl]amino]-5-fluoro-2-[3-(triazol-1-yl)anilino]pyridine-3-carboxamide
• CAS: 1374969-26-2
• 化学式: C₂₀H₂₃FN₈O
• 分子量: 410.454
• InChiKey: CPRKKBPLHFSZEJ-DLBZAZTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  137
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
  申请人：FUJIFILM Corporation

  公开号：US20140309225A1

  公开（公告）日：2014-10-16

  The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R 1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R 3 , R 4 , R 5 , n, and X 1 have the same definitions as those described in the specification), and R 2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

  本发明的目的是提供一种具有优异的Syk抑制活性的化合物和药物组合物。根据本发明，提供了由以下式（I）表示的烟酰胺衍生物或其盐， 其中 R 1 是由以下式（II-1）、（III-1）或（IV-1）表示的取代基 （其中R 3 、R 4 、R 5 、n和X 1 的定义与说明书中描述的相同），而R 2 是吡啶基、吲唑基、苯基、吡唑吡啶基、苯并异噁唑基、嘧啶基或喹啉基，每种基可选择地具有至少一个取代基。
• BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS
  申请人：Jia Zhaozhong J.

  公开号：US20120142671A1

  公开（公告）日：2012-06-07

  The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk 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 Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

  本发明涉及公式I的化合物及其药学上可接受的盐、酯和前药，这些化合物是Syk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，含有这种化合物的药物组合物，抑制Syk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Syk激酶活性介导的多种疾病，如非霍奇金淋巴瘤的方法。
• NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
  申请人：FUJIFILM Corporation

  公开号：EP2589592A1

  公开（公告）日：2013-05-08

  An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl g roup, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R4 and R5 e ach independently represent a hydrogen atom; and R2 and R4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

  本发明的目的是提供一种化合物和药物组合物，其具有优异的抑制 Syk 的活性。本发明提供了一种烟酰胺衍生物，由以下式（I）表示 其中 R1 代表卤素原子；R2 代表 C1-12 烷基、C2-12 烯基、C2-12 炔基、C3-8 环烷基、芳基、ar-C1-6 烷基或杂环基，每个基团可选择具有至少一个取代基；R3 代表芳基或杂环基，每个基团可选择具有至少一个取代基；以及 R4 和 R5 分别独立地代表一个氢原子；R2 和 R4 可与它们结合的氮原子一起形成一个环状氨基，该氨基可选择具有至少一个取代基）或其盐，以及一种用于治疗 Syk 相关疾病的药物组合物，该药物组合物包含烟酰胺衍生物或其盐。
• US8772320B2
  申请人：——

  公开号：US8772320B2

  公开（公告）日：2014-07-08
• US8846928B2
  申请人：——

  公开号：US8846928B2

  公开（公告）日：2014-09-30