2-[3,5-dichloro-4-[(6-oxo-4-propan-2-yl-1H-pyridazin-3-yl)oxy]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-[3,5-dichloro-4-[(6-oxo-4-propan-2-yl-1H-pyridazin-3-yl)oxy]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile
• 化学式: C₁₇H₁₂Cl₂N₆O₄
• 分子量: 435.2
• InChiKey: OUZKCFDHKSJCGZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  7

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。
• 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
• US9968612B2
  申请人：——

  公开号：US9968612B2

  公开（公告）日：2018-05-15