5-氯-4-甲基-2-噻吩甲醛 | 65782-04-9

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 中文名称: 5-氯-4-甲基-2-噻吩甲醛
• 英文名称: 5-Chloro-4-methylthiophene-2-carbaldehyde
• CAS: 65782-04-9
• 化学式: C₆H₅ClOS
• 分子量: 160.62
• InChiKey: XYJKBLZSWUYADH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  45.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-氯-4-甲基-2-噻吩甲醛 、 、 叠氮乙酸乙酯 、 1-羟乙基自由基 、 氯化铵 在 乙醚 、 丙-2-烯酸酯 、 水 、 xylenes 作用下， 以 乙醇 为溶剂， 反应 4.08h， 生成 2-氯-3-甲基-4H-噻吩并[3,2-B]吡咯-5-羧酸乙酯
  参考文献：
  名称：

  Bicyclic pyrrolyl amides as glycogen phosphorylase inhibitors

  摘要：

  本发明涉及公式I1化合物或其立体异构体、其药学上可接受的盐或其前药的药学上可接受的盐。本发明还涉及包含公式I化合物的制药组合物，以及治疗糖尿病、胰岛素抵抗、糖尿病神经病变、糖尿病肾病、糖尿病视网膜病变、白内障、高血糖、高胆固醇血症、高血压、高胰岛素血症、高脂血症、动脉硬化或组织缺血的治疗方法。

  公开号：

  US20030195361A1

文献信息

• Use of glycogen phosphorylase inhibitors
  申请人：——

  公开号：US20030004162A1

  公开（公告）日：2003-01-02

  The invention provides methods of treating prophylactically an individual in whom Type 2 diabetes mellitus has not yet presented, but in whom there is an increased risk of developing such condition, which methods comprise administering to an individual in need thereof an effective amount of a glycogen phosphorylase inhibitor; effective amounts of a glycogen phosphorylase inhibitor and a non-glycogen phosphorylase inhibiting anti-diabetic agent; or effective amounts of a glycogen phosphorylase inhibitor and an anti-obesity agent. The invention further provides methods of treating prophylactically an individual in whom Type 2 diabetes mellitus has not yet presented, but in whom there is an increased risk of developing such condition, which methods comprise administering to an individual in need thereof a pharmaceutical composition comprising effective amounts of a glycogen phosphorylase inhibitor and a non-glycogen phosphorylase inhibiting anti-diabetic agent; or effective amounts of a glycogen phosphorylase inhibitor and an anti-obesity agent.

  本发明提供了一种预防性地治疗尚未出现2型糖尿病但存在发展为该病风险的个体的方法，该方法包括向需要该方法的个体施用有效量的糖原磷酸化酶抑制剂；有效量的糖原磷酸化酶抑制剂和非糖原磷酸化酶抑制的抗糖尿病剂；或者有效量的糖原磷酸化酶抑制剂和抗肥胖剂。本发明还提供了一种预防性地治疗尚未出现2型糖尿病但存在发展为该病风险的个体的方法，该方法包括向需要该方法的个体施用包含有效量的糖原磷酸化酶抑制剂和非糖原磷酸化酶抑制的抗糖尿病剂的药物组合物；或者有效量的糖原磷酸化酶抑制剂和抗肥胖剂。
• [EN] 3-HYDROXY-IMIDAZOLIDIN-4-ONE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE<br/>[FR] COMPOSÉS DE 3-HYDROXY-IMIDAZOLIDIN-4-ONE UTILISÉS EN TANT QU'INHIBITEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE
  申请人：NETHERLANDS TRANSLATIONAL RES CENTER B V

  公开号：WO2019043103A1

  公开（公告）日：2019-03-07

  The invention relates to a compound of Formula (I) : Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.

  该发明涉及一种公式(I)的化合物：公式(I)，或其药学上可接受的对映体或盐。本发明还涉及将公式(I)的化合物用作色氨酸2,3-双加氧酶的选择性抑制剂。该发明还涉及使用公式(I)的化合物治疗或预防癌症、感染、中枢神经系统疾病或障碍以及免疫相关疾病，无论是作为单一药物还是与其他治疗方法联合使用。
• Tricyclic pyrrolyl amides as glycogen phosphorylase inhibitors
  申请人：Pfizer Products Inc.

  公开号：EP1391460A1

  公开（公告）日：2004-02-25

  This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.

  本发明涉及式 I 的化合物 或立体异构体、其药学上可接受的盐或原药或原药的药学上可接受的盐。本发明还涉及包含式 I 化合物的药物组合物，以及治疗糖尿病、胰岛素抵抗、糖尿病神经病变、糖尿病肾病、糖尿病视网膜病变、白内障、高血糖、高胆固醇血症、高血压、高胰岛素血症、高脂血症、动脉粥样硬化或组织缺血的方法。
• 3-hydroxy-imidazolidin-4-one compounds as inhibitors of indoleamine 2,3-dioxygenase
  申请人：Netherlands Translational Research Center B.V.

  公开号：US11053230B2

  公开（公告）日：2021-07-06

  The invention relates to a compound of Formula (I): Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.

  本发明涉及一种式（I）化合物：式（I）或药学上可接受的对映体或其盐。本发明还涉及式（I）化合物作为吲哚胺 2，3-二氧化酶选择性抑制剂的用途。本发明还涉及式（I）化合物用于治疗或预防癌症、感染、中枢神经系统疾病或紊乱以及免疫相关紊乱等疾病的用途，可作为单一药物或与其他疗法联合使用。
• 3-HYDROXY-IMIDAZOLIDIN-4-ONE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
  申请人：Netherlands Translational Research Center B.V.

  公开号：EP3676263A1

  公开（公告）日：2020-07-08