6-碘-2,3-二氢-[1,4]二恶英[2,3-b]吡啶 | 1246088-42-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 6-碘-2,3-二氢-[1,4]二恶英[2,3-b]吡啶
• 英文名称: 6-iodo-2,3-dihydro-[1,4]dioxino[2,3-b]pyridine
• CAS: 1246088-42-5
• 化学式: C₇H₆INO₂
• 分子量: 263.035
• InChiKey: KVTOLQOVTRGNSI-UHFFFAOYSA-N

物化性质

• 沸点：
  311.1±42.0 °C(Predicted)
• 密度：
  1.968±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  31.4
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  6-碘-2,3-二氢-[1,4]二恶英[2,3-b]吡啶 在 sodium tetrahydroborate 、 四(三苯基膦)钯 、 乙醇 作用下， 以 甲苯 为溶剂， 生成 1-(2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-6-yl)ethan-1-ol
  参考文献：
  名称：

  [EN] PYRAZOLOPYRIDINONE COMPOUNDS
  [FR] COMPOSÉS PYRAZOLOPYRIDINONES

  摘要：

  Disclosed herein is a compound of Formula (I) for activating T cells, promoting T cell proliferation, and/or exhibiting antitumor activity, a method of using the compounds disclosed herein for treating cancer, and a pharmaceutical composition comprising the same.

  公开号：

  WO2023011456A1
• 作为产物：
  描述：

  2-((2-chloro-6-iodopyridin-3-yl)oxy)ethan-1-ol 在 四丁基氟化铵 、 potassium hydroxide 作用下， 以 甲苯 为溶剂， 以29 %的产率得到6-碘-2,3-二氢-[1,4]二恶英[2,3-b]吡啶
  参考文献：
  名称：

  [EN] PYRAZOLOPYRIDINONE COMPOUNDS
  [FR] COMPOSÉS PYRAZOLOPYRIDINONES

  摘要：

  Disclosed herein is a compound of Formula (I) for activating T cells, promoting T cell proliferation, and/or exhibiting antitumor activity, a method of using the compounds disclosed herein for treating cancer, and a pharmaceutical composition comprising the same.

  公开号：

  WO2023011456A1

文献信息

• [EN] 1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE<br/>[FR] DÉRIVÉS DE DIOXYDE DE 1,4-THIAZINE ET DE DIOXYDE DE 1,2,4-THIADIAZINE EN TANT QU'INHIBITEURS DE BÊTA-SÉCRÉTASE ET PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2018112094A1

  公开（公告）日：2018-06-21

  The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.

  本公开提供了一类化合物，用于调节β-分泌酶（BACE）活性。这些化合物具有一般的化学式I：其中化学式I中的变量A、X、R2、R2'、R3、R4、R5、R6和R7在此处定义。本公开还提供了包含这些化合物的药物组合物，以及这些化合物和组合物用于治疗与Aβ斑块形成和沉积相关的疾病和/或症状的用途，这些疾病和症状是由BACE的生物活性引起的。这种由BACE介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍和其他中枢神经系统疾病。
• Oxadiazolopyridine Derivates for Use as Ghrelin O-Acyl Transferase (GOAT) Inhibitors
  申请人：Boehringer Ingelheim International GmbH

  公开号：US20180037594A1

  公开（公告）日：2018-02-08

  The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.

  本发明涉及通式I的化合物，其中基团R1、R2和n的定义如权利要求书中所述，该化合物具有有价值的药理学特性，特别是结合到生长激素释放激素酰基转移酶（GOAT）并调节其活性。这些化合物适用于治疗和预防可能受该受体影响的疾病，如代谢性疾病，特别是肥胖症。
• Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
  申请人：Boehringer Ingelheim International GmbH

  公开号：US10308667B2

  公开（公告）日：2019-06-04

  The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.

  本发明涉及通式 I 的化合物、 其中基团 R1、R2 和 n 的定义如权利要求 1 所述，这些化合物具有重要的药理特性，特别是能与胃泌素 O-酰基转移酶（GOAT）结合并调节其活性。这些化合物适用于治疗和预防受该受体影响的疾病，如代谢性疾病，特别是肥胖症。
• 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
  申请人：AMGEN INC.

  公开号：US11021493B2

  公开（公告）日：2021-06-01

  The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2′, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.

  本公开提供了一类可用于调节β-分泌酶（BACE）活性的化合物。这些化合物具有通式 I： 其中式 I 的变量 A、X、R2、R2′、R3、R4、R5、R6 和 R7 在本文中定义。本公开还提供了包含这些化合物的药物组合物，以及这些化合物和组合物用于治疗与 BACE 的生物活性导致的 Aβ 斑块形成和沉积有关的疾病和/或病症的用途。此类 BACE 介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍和其他中枢神经系统疾病等。
• OXADIAZOLOPYRIDINE DERIVATES FOR USE AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP3494120A1

  公开（公告）日：2019-06-12