5-ethyl-1H-indazol-3-amine | 943247-42-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 5-ethyl-1H-indazol-3-amine
• CAS: 943247-42-5
• 化学式: C₉H₁₁N₃
• 分子量: 161.206
• InChiKey: RYPQOSKIEDCABK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  54.7
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
  申请人：Pinto Donald J.P.

  公开号：US20100016316A1

  公开（公告）日：2010-01-21

  The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L 1 , R 3 , R 4 , R 8a , R 11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

  本发明提供了化合物的结构式（I）或（II）： 或其立体异构体、互变异构体、药学上可接受的盐或溶剂形式，其中变量A、L1、R3、R4、R8a、R11和M如本文所定义。结构式（I）或（II）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶酶的选择性抑制剂；例如凝血酶、Xa因子、XIa因子、IXa因子、VIIa因子和/或血浆激肽。具体而言，涉及选择性XIa因子抑制剂或fXIa和血浆激肽的双重抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物以及使用它们治疗血栓栓塞和/或炎症性疾病的方法。
• METHODS AND COMPOSITIONS FOR TREATMENT OF OPHTHALMIC CONDITIONS
  申请人：Wilson Troy Edward

  公开号：US20110269779A1

  公开（公告）日：2011-11-03

  The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in an ocular tissue. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.

  本发明提供了能够调节特定蛋白激酶（如mTor、酪氨酸激酶和/或脂质激酶如PB激酶）在眼组织中的信号传导的化学实体或化合物以及其制药组合物。本发明还提供了利用这些组合物调节这些激酶中的一个或多个的活性的方法，特别是用于治疗应用。
• THIOPHENE DERIVATIVES AS FACTOR XIA INHIBITORS
  申请人：Han Wei

  公开号：US20090253766A1

  公开（公告）日：2009-10-08

  The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L 1 , R 3 , and R 11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

  本发明提供了式（I）的化合物：或其立体异构体、互变异构体、药学上可接受的盐、溶剂化物或前药，其中变量A、L1、R3和R11如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶酶的选择性抑制剂，例如凝血酶、Xa因子、XIa因子、IXa因子、VIIa因子和/或血浆卡利肌酶。特别地，涉及到选择性XIa因子抑制剂的化合物。本发明还涉及包含这些化合物的制药组合物以及使用它们治疗血栓栓塞和/或炎症性疾病的方法。
• GLUCOKINASE ACTIVATORS
  申请人：Feng Jun

  公开号：US20070244169A1

  公开（公告）日：2007-10-18

  Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

  本发明提供了用于与葡萄糖激酶一起使用的化合物、制药组合物、试剂盒和方法，其中包括所述化合物中选自以下组的化合物：其中所述变量如本文所定义。
• FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS
  申请人：Hangeland Jon J.

  公开号：US20090036438A1

  公开（公告）日：2009-02-05

  The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , R 4 , R 6 , R 11 , X 1 , X 2 , and X 3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

  本发明提供了一种治疗血栓性或炎症性疾病的方法，该方法向需要治疗的患者施用至少一种公式（I）或公式（V）中的化合物的治疗有效量：或其立体异构体或药学上可接受的盐或溶剂形式，其中变量A、L、Z、R3、R4、R6、R11、X1、X2和X3如本文所定义。公式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶酶的选择性抑制剂；例如凝血酶、因子Xa、因子XIa、因子IXa、因子VIIa和/或血浆激肽。特别是，涉及到选择性因子XIa抑制剂的化合物。本发明还提供了公式I范围内的化合物，并涉及包含这些化合物的制药组合物。