5-phenyloxazole-2-carboxamide | 90770-99-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-phenyloxazole-2-carboxamide
• 英文别名: 5-phenyl-oxazole-2-carboxylic acid amide；5-Phenyl-oxazol-carbonsaeure-(2)-amid；5-Phenyl-2-oxazolecarboxamide；5-phenyl-1,3-oxazole-2-carboxamide
• CAS: 90770-99-3
• 化学式: C₁₀H₈N₂O₂
• 分子量: 188.186
• InChiKey: WCTKUVRVFILAKE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 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

• 作为反应物：
  描述：

  5-phenyloxazole-2-carboxamide 在 硝酸 、 phosphorus pentoxide 作用下， 生成 5-(4-nitro-phenyl)-oxazole-2-carbonitrile
  参考文献：
  名称：

  Sycheva,T.P. et al., Journal of general chemistry of the USSR, 1962, vol. 32, p. 3597 - 3599

  摘要：

  DOI：
• 作为产物：
  描述：

  5-苯基噁唑-2-羧酸乙酯 在 ammonium hydroxide 作用下， 生成 5-phenyloxazole-2-carboxamide
  参考文献：
  名称：

  Sycheva,T.P. et al., Journal of general chemistry of the USSR, 1962, vol. 32, p. 3597 - 3599

  摘要：

  DOI：

文献信息

• [EN] 3-ARYLOXY AND 3-HETEROARYLOXY SUBSTITUTED BENZO(B) THIOPHENES AS THERAPEUTIC AGENTS WITH PI3K ACTIVITY<br/>[FR] BENZO[B]THIOPHENES A SUBSTITUTION 3-ARYLOXY ET 3-HETEROARYLOXY EN TANT QU'AGENTS THERAPEUTIQUES A ACTIVITE PI3K
  申请人：WARNER LAMBERT CO

  公开号：WO2004108715A1

  公开（公告）日：2004-12-16

  The present invention provides benzo[b]thiophenes of Formula (I), wherein R1, R2, R3, R4, R5, and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (I).

  本发明提供了式(I)的苯并[b]噻吩，其中R1、R2、R3、R4、R5和L具有规范中为其定义的任何值，以及药用可接受的盐，这些盐作为治疗疾病和状况的药剂是有用的，包括炎性疾病、心血管疾病和癌症。另外还提供了包含一个或多个式(I)化合物的药物组合物。
• [EN] PYRIDINESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF<br/>[FR] DÉRIVATIFS DE PYRIDINESULFONAMIDE POUVANT ÊTRE UTILISÉS COMME MODULATEURS TRAP1 ET LEURS UTILISATIONS
  申请人：AMATHUS THERAPEUTICS INC

  公开号：WO2021188907A1

  公开（公告）日：2021-09-23

  The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor ("TNF") receptor associated protein 1 ("TRAP1") modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 ("PINK1") loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as a-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).

  本公开提供了化合物的化学式（I）和药学上可接受的盐、溶剂化合物、水合物、多晶型、共晶体、互变异构体、立体异构体、同位素标记化合物以及其前药。所提供的化合物可能是肿瘤坏死因子（"TNF"）受体相关蛋白1（"TRAP1"）调节剂（例如，TRAP1激活剂）。所提供的化合物还可能恢复PTEN诱导的激酶1（"PINK1"）功能丧失情况下的活性。所提供的化合物还可能改善线粒体的健康、功能、质量、数量和/或活性，和/或减少活性氧自由基的产生。所提供的化合物还可能对聚集或错误折叠的蛋白质（如α-突触核蛋白）进行重折叠或溶解。本公开还提供了包括所提供化合物的药物组合物；包括所提供化合物或药物组合物的试剂盒；以及使用所提供的化合物和药物组合物的方法（例如，用于治疗需要的受试者的疾病）。
• Oxazole compounds for the treatment of neurodegenerative disorders
  申请人：Chen L. Yuhpyng

  公开号：US20050032859A1

  公开（公告）日：2005-02-10

  The present invention relates to compounds of the Formula wherein R 3 , R 5 , R 6 , R 7 , and Z, and other variables enumerated under one or more of R 3 , R 5 , R 6 , R 7 , and Z, are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

  本发明涉及公式I的化合物，其中R3、R5、R6、R7和Z以及在R3、R5、R6、R7和Z中枚举的其他变量的定义如下。公式I的化合物具有抑制Aβ肽产生的活性。本发明还涉及包含公式I的化合物的制药组合物和治疗疾病（例如神经退行性疾病，例如阿尔茨海默病）的方法，其中该疾病在哺乳动物中进行治疗。
• 3-Aryloxy and 3-heteroaryloxy substituted benzo[b]thiophenes as therapeutic agents
  申请人：——

  公开号：US20040259926A1

  公开（公告）日：2004-12-23

  The present invention provides benzo[b]thiophenes of Formula I: 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 , and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

  本发明提供了式I的苯并[b]噻吩化合物：1其中R1、R2、R3、R4、R5和L在规范中定义的任何值，以及其药学上可接受的盐，可用作治疗疾病和病症的药物，包括炎症性疾病、心血管疾病和癌症。还提供了包含一个或多个式I化合物的药物组合物。
• Pyrazole-amides and -sulfonamides
  申请人：Atkinson N. Robert

  公开号：US20050049237A1

  公开（公告）日：2005-03-03

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazole-amides and -sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.

  本发明提供了一种通过抑制电压依赖性钠通道中的钠离子流来治疗疾病的化合物、组合物和方法。更具体地，本发明提供了吡唑酰胺和磺酰胺，以及其组合物和方法，这些化合物、组合物和方法对于治疗中枢或外周神经系统疾病特别是疼痛和慢性疼痛非常有用，通过阻止与所述疾病的发作或复发有关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制包括PN3亚基的通道中的离子流来治疗神经病理性或炎性疼痛。