4-[3-chloro-4-(trifluoromethoxy)phenyl]-1,3-thiazol-2-amine | 1246288-74-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-[3-chloro-4-(trifluoromethoxy)phenyl]-1,3-thiazol-2-amine
• CAS: 1246288-74-3
• 化学式: C₁₀H₆ClF₃N₂OS
• 分子量: 294.685
• InChiKey: MJWHFCUYRHHBNV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  76.4
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-[3-chloro-4-(trifluoromethoxy)phenyl]-1,3-thiazol-2-amine 、 (6-chloro-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro[2,3-d]pyrimidin-5-yl)acetic acid 在 1-羟基苯并三唑 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 48.25h， 生成 N-{4-[3-chloro-4-(trifluoromethoxy)phenyl]-1,3-thiazol-2-yl}-2-(6-chloro-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro[2,3-d]pyrimidin-5-yl)acetamide
  参考文献：
  名称：

  [EN] AMIDES OF HETEROCYCLIC COMPOUNDS AS TRPA1 INHIBITORS
  [FR] AMIDES DE COMPOSÉS HÉTÉROCYCLIQUES À TITRE D'INHIBITEURS DE TRPA1

  摘要：

  提供了杂环化合物的酰胺作为瞬时受体电位亚家族A（TRPA）调节剂。具体来说，本文描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、症状和/或疾病。本文还提供了制备本文描述的化合物的方法、其合成中使用的中间体、药物组合物以及治疗或预防由TRPA1调节的疾病、症状和/或疾病的方法。

  公开号：

  WO2011114184A1

文献信息

• [EN] GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE<br/>[FR] INHIBITEURS DE GLYCOLATE OXYDASE POUR LE TRAITEMENT D'UNE MALADIE
  申请人：BIOMARIN PHARM INC

  公开号：WO2020257487A1

  公开（公告）日：2020-12-24

  Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

  本文描述了化合物、制备这种化合物的方法、含有这种化合物的药物组合物和药物，以及使用这种化合物治疗或预防与甘氧酸代谢缺陷相关的疾病或紊乱的方法，例如与甘氧酸氧化酶（GO）或草酸代谢变化相关的疾病或紊乱。这些疾病或紊乱包括与产生过多草酸相关的甘氧酸代谢紊乱，例如原发性高草酸尿症。
• [EN] PYRIMIDINEDIONE-FUSED HETEROCYCLIC COMPOUNDS AS TRPA1 MODULATORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES FUSIONNÉS À UNE PYRIMIDINE DIONE EN TANT QUE MODULATEURS DE TRPA1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2010125469A1

  公开（公告）日：2010-11-04

  The present invention is related to novel pyrimidinedione-fused heterocyclic compounds as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

  本发明涉及作为TRPA（瞬时受体电位亚家族A）调节剂的新型嘧啶二酮并环杂环化合物。具体地，本文描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、症状和/或疾病。本文还提供了用于制备本文描述的化合物的方法、用于合成的中间体、其药物组成物以及治疗或预防由TRPA1调节的疾病、症状和/或疾病的方法。
• FUROPYRIMIDINEDIONE DERIVATIVES AS TRPAI MODULATORS
  申请人：Chaudhari Sachin Sundarlal

  公开号：US20120178766A1

  公开（公告）日：2012-07-12

  The present invention is related to novel furopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

  本发明涉及新型噻吩嘧啶二酮衍生物作为TRPA（瞬时受体电位亚家族A）调节剂。特别地，本文所描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、情况和/或疾患。本文还提供了用于制备所述化合物的过程，用于其合成的中间体，其制药组合物以及用于治疗或预防由TRPA1调节的疾病、情况和/或疾患的方法。
• ISOTHIAZOLO-PYRIMIDINEDIONE DERIVATIVES AS TRPAI MODULATORS
  申请人：Kumar Sukeerthi

  公开号：US20120010223A1

  公开（公告）日：2012-01-12

  The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

  本发明涉及新型异噻唑并[3,4-d]嘧啶二酮和异噻唑并[5,4-d]嘧啶二酮衍生物作为TRPA（瞬时受体电位A亚家族）调节剂。特别地，本文所描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位A亚家族，成员1）调节的疾病、状况和/或障碍。本文还提供了用于制备所述化合物的过程、用于合成的中间体、其制药组合物以及治疗或预防由TRPA1调节的疾病、状况和/或障碍的方法。
• Glycolate oxidase inhibitors for the treatment of disease
  申请人：BIOMARIN PHARMACEUTICAL INC.

  公开号：US11384055B2

  公开（公告）日：2022-07-12

  Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme glycolate oxidase (GO). Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

  本文描述的是化合物、制造此类化合物的方法、含有此类化合物的药物组合物和药剂，以及使用此类化合物治疗或预防与乙醛酸氧化酶（GO）相关的疾病或紊乱的方法。此类疾病或紊乱包括，例如，与产生过量草酸盐有关的乙醛酸代谢紊乱，包括原发性高草酸尿症。