Benzo[d]oxazole-7-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶唑类
• 英文名称: Benzo[d]oxazole-7-carboxamide
• 英文别名: 1,3-benzoxazole-7-carboxamide
• 化学式: C₈H₆N₂O₂
• 分子量: 162.15
• InChiKey: IQHHPMNFYJGULP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  69.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-(piperidin-3-yl)benzo[d]oxazole-7-carboxamide 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 1-羟基苯并三唑 、 三乙胺 、 N,N-二甲基甘氨酸 在 2-(1-(2-dimethylamino)acetyl)piperidin-3-yl 作用下， 以 Dichloride methane 为溶剂， 以13 mg 2-(1-(2-dimethylamino)acetyl)piperidin-3-yl)benzo[d]oxazole-7-carboxamide was obtained的产率得到Benzo[d]oxazole-7-carboxamide
  参考文献：
  名称：

  Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP)

  摘要：

  本文提供了具有以下结构的化合物：公式（I）或公式（II）所示，其中变量Y、R1、R2、R3和R4的定义如本文所述。本文提供了聚（ADP核糖）聚合酶活性抑制剂。本文还描述了包括至少一种本文所述化合物的制药组合物以及使用本文所述的化合物或制药组合物治疗通过抑制PARP活性改善的疾病、疾病和病症。

  公开号：

  US08088760B2

文献信息

• [EN] ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ÉTHYLÈNE DIAMINE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'HYPOCRÉTINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2016100161A1

  公开（公告）日：2016-06-23

  The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及对促进素受体的拮抗剂乙二胺化合物。本发明还涉及所述化合物在潜在的治疗或预防涉及促进素受体的神经和精神障碍和疾病中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在的预防或治疗涉及促进素受体的疾病中的用途。
• [EN] HETEROCYCLIC COMPOUNDS AS AHR MODULATORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QUE MODULATEURS DE L'AHR
  申请人：JAGUAHR THERAPEUTICS PTE LTD

  公开号：WO2020043880A1

  公开（公告）日：2020-03-05

  The present invention relates compounds of the general formula (I) or (III) which are ARH inhibitors, methods for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds and pharmaceutical compositions for the treatment or prevention of diseases, in particular cancer or conditions with dysregulated immune functions, or other conditions associated with aberrant AHR signalling, as a sole agent of in combination with other active ingredients. Such compounds may also be of utility in the expansion of hematopoietic stem cells (HSCs) and the use of HSCs in autologous or allogenic transplantation for the treatment of patients with inherited immunological and autoimmune diseases and diverse hematopoietic disorders.

  本发明涉及一般式(I)或(III)的化合物，这些化合物是ARH抑制剂，制备这些化合物的方法，含有这些化合物的药物组合物和配方以及利用这些化合物和药物组合物治疗或预防疾病，特别是癌症或免疫功能失调的情况，或与异常AHR信号相关的其他病症，作为单一药剂或与其他活性成分组合使用。这些化合物还可能在扩展造血干细胞（HSCs）方面具有用途，并且利用HSCs进行自体或同种异体移植，用于治疗患有遗传免疫和自身免疫疾病以及多种造血障碍的患者。
• BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
  申请人：Chu Daniel

  公开号：US20090197863A1

  公开（公告）日：2009-08-06

  A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R 1 , R 2 , R 3 , and R 4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

  一种具有以下式子（I）或式子（II）结构的化合物：其中变量Y，R1，R2，R3和R4如本文所定义。本文提供了聚(ADP-核糖)聚合酶活性抑制剂。本文还描述了包括至少一种本文所述化合物的制药组合物，以及使用本文所述的化合物或制药组合物来治疗通过抑制PARP活性改善的疾病，障碍和病况。
• HETEROCYCLIC COMPOUNDS AS AHR MODULATORS
  申请人：JAGUAHR THERAPEUTICS PTE LTD

  公开号：EP3843853A1

  公开（公告）日：2021-07-07
• Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP)
  申请人：BioMarin Pharmaceutical Inc.

  公开号：US08088760B2

  公开（公告）日：2012-01-03

  A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

  本文提供了具有以下结构的化合物：公式（I）或公式（II）所示，其中变量Y、R1、R2、R3和R4的定义如本文所述。本文提供了聚（ADP核糖）聚合酶活性抑制剂。本文还描述了包括至少一种本文所述化合物的制药组合物以及使用本文所述的化合物或制药组合物治疗通过抑制PARP活性改善的疾病、疾病和病症。