4-(6-nitrothiazolo[4,5-b]pyridin-2-yl)morpholine | 1418299-26-9

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 4-(6-nitrothiazolo[4,5-b]pyridin-2-yl)morpholine
• 英文别名: 2-morpholino-6-nitrothiazolo[4,5-b]pyridine；4-(6-Nitro-[1,3]thiazolo[4,5-b]pyridin-2-yl)morpholine
• CAS: 1418299-26-9
• 化学式: C₁₀H₁₀N₄O₃S
• 分子量: 266.28
• InChiKey: FDLQKKOBUZFKMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  112
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-(thiazolo[4,5-b]pyridin-2-yl)morpholine 在 硝酸 、 溶剂黄146 作用下， 以50%的产率得到4-(6-nitrothiazolo[4,5-b]pyridin-2-yl)morpholine
  参考文献：
  名称：

  BICYCLIC HETEROCYCLYL DERIVATES AS IRAK4 INHIBITORS

  摘要：

  本发明提供了公式（I）的双环杂环基激酶酶抑制剂化合物，作为激酶抑制剂在治疗上具有疗效，特别是IRAK4抑制剂，在其中A、Y、Z、X1、X2、R1、R3、‘m’、‘n’和‘p’的含义如规范中所给定，并且在治疗和预防疾病或紊乱方面有用，特别是在通过激酶酶介导的疾病或紊乱中的使用，特别是IRAK4酶。本发明还提供了包含至少一种公式（I）的化合物的制剂，与其一起使用的药用载体、稀释剂或赋形剂。

  公开号：

  US20160340366A1

文献信息

• [EN] BICYCLIC HETEROCYCLYL DERIVATIVES AS IRAK4 INHIBITORS<br/>[FR] DÉRIVÉS HÉTÉROCYCLYLES BICYCLIQUES COMME INHIBITEURS DE IRAK4
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2015104688A1

  公开（公告）日：2015-07-16

  The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, 'm', 'n' and 'p' have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式（I）的双环杂环基激酶酶抑制剂化合物，其作为激酶抑制剂在治疗上具有疗效，特别是IRAK4抑制剂。其中A、Y、Z、X1、X2、X3、R1、R3、'm'、'n'和'p'在规范中给出了含义，并且具有治疗和预防疾病或疾病的药用盐或其立体异构体，在特定情况下用于由激酶酶介导的疾病或疾病的治疗。本发明还提供了包括至少一种式（I）化合物的药物组合物，与药用载体、稀释剂或赋形剂一起。
• Regioselective Direct Arylation of Fused 3-Nitropyridines and Other Nitro-Substituted Heteroarenes: The Multipurpose Nature of the Nitro Group as a Directing Group
  作者：Viktor O. Iaroshenko、Ashot Gevorgyan、Satenik Mkrtchyan、Tatevik Grigoryan、Ester Movsisyan、Alexander Villinger、Peter Langer

  DOI：10.1002/cctc.201402715

  日期：2015.1

  We report Pd‐ and Ni‐catalysed, guided and regioselective CH arylations of a series of fused 3‐nitropyridines. The method described here is a facile tool for the chemical functionalisation of drug‐like fused pyridines. The scope and limitations of the reaction, the chemical potential of the nitro group and a putative reaction mechanism are discussed.

  我们报道了一系列融合的3-硝基吡啶的Pd和Ni催化，导向和区域选择性的CH芳基化反应。此处描述的方法是用于药物样融合吡啶的化学功能化的简便工具。讨论了反应的范围和局限性，硝基的化学势以及可能的反应机理。
• METHOD OF PREPARING OXAZOLO[4,5-B]PYRIDINE AND THIAZOLO[4,5-B]PYRIDINE DERIVATIVES AS IRAK4 INHIBITORS FOR TREATING CANCER
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3466955A1

  公开（公告）日：2019-04-10

  The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, 'm', 'n' and 'p' have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式(I)的双环杂环激酶酶抑制剂化合物，它们作为激酶抑制剂，特别是IRAK4抑制剂，具有治疗作用。 其中A、Y、Z、X1、X2、X3、R1、R3、'm'、'n'和'p'具有说明书中给出的含义及其药学上可接受的盐或立体异构体，这些化合物对治疗和预防疾病或紊乱有用，特别是它们在激酶酶，尤其是IRAK4酶介导的疾病或紊乱中的用途。本发明还提供由至少一种式（I）化合物及其药学上可接受的载体、稀释剂或赋形剂组成的药物组合物。
• (R) AND (S) ENANTIOMER OF N-(5-(3-HYDROXYPYRROLIDIN-1-YL)-2-MORPHOLINOOXAZOLO[4,5-B]PYRIDIN-6-YL)-2-(2-METHYLPYRIDIN-4-YL)OXAZOLE-CARBOXAMIDE AS IRAK4 INHIBITORS FOR TREATING CANCER AND INFLAMMATORY DISEASES
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3805233A1

  公开（公告）日：2021-04-14

  Provided are bicyclic heterocyclyl kinase enzyme inhibitor compounds and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme, such as e.g. cancer and inflammatory diseases.

  提供双环杂环激酶抑制剂化合物 及其药学上可接受的盐类，可用于治疗和预防疾病或紊乱，特别是用于由激酶，尤其是IRAK4酶介导的疾病或紊乱，例如癌症和炎症性疾病。
• Bicyclic heterocyclyl derivatives as IRAK4 inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US10640517B2

  公开（公告）日：2020-05-05

  The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式(I)的双环杂环激酶酶抑制剂化合物，它们作为激酶抑制剂，特别是IRAK4抑制剂，具有治疗作用。 其中A、Y、Z、X1、X2、X3、R1、R3、'm'、'n'和'p'具有说明书中给出的含义及其药学上可接受的盐或立体异构体，这些化合物对治疗和预防疾病或紊乱有用，特别是它们在激酶酶，尤其是IRAK4酶介导的疾病或紊乱中的用途。本发明还提供了药物组合物，其中包含至少一种式（I）化合物及其药学上可接受的载体、稀释剂或赋形剂。