1-ethyl-3-hydroxy-2(1H)-pyridinone | 90037-19-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-ethyl-3-hydroxy-2(1H)-pyridinone
• 英文别名: 1-ethyl-3-hydroxypyrid-2-one；1-Ethyl-3-hydroxypyridin-2(1H)-one；1-ethyl-3-hydroxypyridin-2-one
• CAS: 90037-19-7
• 化学式: C₇H₉NO₂
• 分子量: 139.154
• InChiKey: PFMJLYROOSGHMN-UHFFFAOYSA-N

物化性质

• 熔点：
  109-110 °C
• 沸点：
  316.0±42.0 °C(Predicted)
• 密度：
  1.229±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  吡啶-2,3-二醇 、 碘乙烷 生成 1-ethyl-3-hydroxy-2(1H)-pyridinone
  参考文献：
  名称：

  STREATER, MICHAEL;TAYLOR, PAUL D.;HIDER, ROBERT C.;PORTER, JOHN, J. MED. CHEM., 33,(1990) N, C. 1749-1755

  摘要：

  DOI：

文献信息

• ANTICANCER DRUGS INCLUDING THE CHEMICAL STRUCTURES OF AN ANDROGEN RECEPTOR LIGAND AND A HISTONE DEACETYLASE INHIBITOR
  申请人：Wayne State University

  公开号：US20170217903A1

  公开（公告）日：2017-08-03

  A novel class of drugs for treating androgen receptor (AR) positive cancer including prostate cancer and breast cancer are described. The drugs include the chemical scaffolds of a high affinity androgen receptor ligand and a histone deacetylase inhibitor. Also described are compositions including the novel drugs and methods of treating AR positive cancer using the compositions.

  描述了一类新型药物，用于治疗雄激素受体（AR）阳性癌症，包括前列腺癌和乳腺癌。这些药物包括高亲和力的雄激素受体配体和组蛋白去乙酰化酶抑制剂的化学支架。还描述了包含这些新型药物的组合物以及使用这些组合物治疗AR阳性癌症的方法。
• [EN] ENPP1 INHIBITORS AND THEIR USE FOR THE TREATMENT OF CANCER<br/>[FR] INHIBITEURS D'ENPP1 ET LEUR UTILISATION POUR LE TRAITEMENT DU CANCER
  申请人：UNIV LELAND STANFORD JUNIOR

  公开号：WO2019051269A1

  公开（公告）日：2019-03-14

  Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.

  提供了用于抑制ENPP1的化合物、组合物和方法。所述方法的方面包括将样品与ENPP1抑制剂接触以抑制ENPP1的cGAMP水解活性。在某些情况下，ENPP1抑制剂是细胞不透过的。还提供了用于治疗癌症的组合物和方法。方法的方面包括向受试者施用治疗有效量的ENPP1抑制剂以治疗受试者的癌症。在某些情况下，癌症是实体肿瘤癌。还提供了在向受试者施用ENPP1抑制剂之前或之后进行放射治疗的方法。放射治疗可以以有效剂量和/或频率对受试者减少放射损伤。在某些情况下，该方法与化疗药物、或检查点抑制剂、或两者结合使用。
• HETEROCYCLIC DERIVED METALLOPROTEASE INHIBITORS
  申请人：Zhang Yue-Mei

  公开号：US20080103129A1

  公开（公告）日：2008-05-01

  This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

  这项发明提供了一种新颖的杂环衍生物基质金属蛋白酶抑制剂的化学式，以及包含同样化合物的药物组合物，用于治疗通过拮抗基质金属蛋白酶而改善的疾病。该发明还提供了使用即时药物组合物的治疗和预防方法。
• [EN] ENPP1 INHIBITORS AND METHODS OF MODULATING IMMUNE RESPONSE<br/>[FR] INHIBITEURS D'ENPP1 ET MÉTHODES DE MODULATION DE RÉPONSE IMMUNITAIRE
  申请人：ANGARUS THERAPEUTICS INC

  公开号：WO2021226136A1

  公开（公告）日：2021-11-11

  Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a cell impermeable ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP 1. Also provided are vaccine compositions and methods relate thereto. Aspects of the methods include administering to a subject an effective amount of a cell impermeable ENPP1 inhibitor to inhibit the hydrolysis of cGAMP in combination with a vaccine.

  本发明提供了用于抑制ENPP1的化合物、组合物和方法。该方法的一些方面包括使用细胞不透性的ENPP1抑制剂与样品接触，以抑制ENPP1的cGAMP水解活性。还提供了疫苗组合物和相关方法。该方法的一些方面包括向受体施用细胞不透性的ENPP1抑制剂的有效量，以结合疫苗抑制cGAMP的水解。
• Novel 2-Heteroaryl-Substituted Benzimidazole Derivative
  申请人：Nonoshita Katsumasa

  公开号：US20080070928A1

  公开（公告）日：2008-03-20

  A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X 1 , X 2 , X 3 and X 4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R 1 represents an aryl, etc.; R 2 represents a hydroxy, etc.; R 3 represents a —C 1-6 alkyl, etc.; R 4 represents a —C 1-6 alkyl, etc.; X 5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

  提供了一种葡萄糖激酶激活剂；提供了糖尿病的治疗和/或预防，或者提供了糖尿病的治疗和/或预防，例如视网膜病变、肾病、神经病、缺血性心脏病、动脉硬化，以及肥胖症的治疗和/或预防。葡萄糖激酶激活剂的特征在于包含通式（I-0）的2-杂环芳基取代苯并咪唑衍生物或其药学上可接受的盐：[在公式中，X表示碳原子或氮原子；X1、X2、X3和X4分别独立地表示碳原子或氮原子；环A表示公式（II）的5-或6-成员含氮芳香杂环：（在公式中，X表示碳原子或氮原子）；R1表示芳基等；R2表示羟基等；R3表示-C1-6烷基等；R4表示-C1-6烷基等；X5表示-O-等；a表示1、2或3的整数；q表示0到2的整数；m表示0到2的整数]。