6-(4-amino-2,6-dichlorophenoxy)-5-isopropylpyridazin-3(2H)-one

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-(4-amino-2,6-dichlorophenoxy)-5-isopropylpyridazin-3(2H)-one
• 英文别名: 3-(4-amino-2,6-dichlorophenoxy)-4-propan-2-yl-1H-pyridazin-6-one
• 化学式: C₁₃H₁₃Cl₂N₃O₂
• 分子量: 314.16
• InChiKey: YIJLVXXZHZTTGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  76.7
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• METHOD OF SYNTHESIZING THYROID HORMONE ANALOGS AND POLYMORPHS THEREOF
  申请人：Madrigal Pharmaceuticals, Inc.

  公开号：US20160243126A1

  公开（公告）日：2016-08-25

  The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

  该披露描述了合成吡啶并酮化合物作为甲状腺激素类似物及其前药的方法。根据该披露的首选方法可允许大规模制备高纯度的吡啶并酮化合物。在某些实施例中，根据该披露的首选方法还可允许比以前用于制备此类化合物的方法更好地制备吡啶并酮化合物。此外，还披露了一种吡啶并酮化合物的形态形式。进一步披露了一种治疗至少具有一种TRβ突变的主体的甲状腺激素抵抗的方法。
• [EN] PROCESS FOR THE PREPARATION OF 6-(4-NITRO-PHENOXY)-2H-PYRIDAZIN-3-ONE AND 6-(4-AMINO-PHENOXY)-2H-PYRIDAZIN-3-ONE DERIVATIVES AS INTERMEDIATES OF THYROID HORMONE ANALOGUES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE 6-(4-NITRO-PHÉNOXY)-2H-PYRIDAZIN-3-ONE ET DE 6-(4-AMINO-PHÉNOXY)-2H-PYRIDAZIN-3-ONE EN TANT QU'INTERMÉDIAIRES D'ANALOGUES DES HORMONES THYROÏDIENNES
  申请人：MADRIGAL PHARMACEUTICALS INC

  公开号：WO2022087141A1

  公开（公告）日：2022-04-28

  The disclosure describes a method of preparing pyridazinone derivatives comprising contacting a compound of formula (I) or a salt thereof: (I) with a compound of formula (II) or a salt thereof: (II) to form a compound of formula (III) or a salt thereof: (III). A compound of formula (III) can then be converted to a compound of formula (IV):(IV), which can be used for preparing compounds for treating a liver disease or disorder, or a lipid disease or disorder.

  该公开说明了一种制备吡啶二酮衍生物的方法，包括将式（I）的化合物或其盐：（I）与式（II）的化合物或其盐：（II）接触以形成式（III）的化合物或其盐：（III）。然后可以将式（III）的化合物转化为式（IV）的化合物：（IV），可用于制备用于治疗肝脏疾病或紊乱，或脂质疾病或紊乱的化合物。
• Methods of synthesizing thyroid hormone analogs and polymorphs thereof
  申请人：Madrigal Pharmaceuticals, Inc.

  公开号：US10376517B2

  公开（公告）日：2019-08-13

  The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

  本公开描述了作为甲状腺激素类似物及其原药的哒嗪酮化合物的合成方法。根据本公开的优选方法，可以大规模制备高纯度的哒嗪酮化合物。在某些实施例中，根据本公开的优选方法还能以比以前使用的制备此类化合物的方法更好的收率制备哒嗪酮化合物。还公开了哒嗪酮化合物的形态形式。进一步公开了一种治疗具有至少一种TRβ突变的受试者对甲状腺激素抗性的方法。
• METHODS OF SYNTHESIZING THYROID HORMONE ANALOGS AND POLYMORPHS THEREOF
  申请人：Madrigal Pharmaceuticals, Inc.

  公开号：US20210161904A1

  公开（公告）日：2021-06-03

  The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
• US9266861B2
  申请人：——

  公开号：US9266861B2

  公开（公告）日：2016-02-23