N-甲基-1H-吡咯并[2,3-b]吡啶-6-胺 | 1018441-16-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 中文名称: N-甲基-1H-吡咯并[2,3-b]吡啶-6-胺
• 英文名称: N-methyl-1H-pyrrolo[2,3-b]pyridin-6-amine
• CAS: 1018441-16-1
• 化学式: C₈H₉N₃
• mdl: MFCD09910035
• 分子量: 147.18
• InChiKey: UTZFGAKTNKRZEJ-UHFFFAOYSA-N

物化性质

• 熔点：
  99.6℃
• 密度：
  1.284±0.06 g/cm3 (20 ºC 760 Torr)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  40.7
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 危险性防范说明：
  P305+P351+P338
• 危险性描述：
  H319

反应信息

• 作为反应物：
  描述：

  N-甲基-1H-吡咯并[2,3-b]吡啶-6-胺 在 tris-(dibenzylideneacetone)dipalladium(0) 、 1-氯-N,N,2-三甲基丙烯胺 、 四丁基氟化铵 、 四丁基溴化铵 、 sodium carbonate 、 potassium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 、 三氟乙酸 、 sodium hydroxide 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 二氯甲烷 、 乙腈 为溶剂， 反应 127.5h， 生成 (S)-N-(3-chloro-1H-pyrrolo[2,3-b]pyridin-6-yl)-N-methyl-3-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-2-oxoimidazolidine-4-carboxamide
  参考文献：
  名称：

  [EN] HETEROCYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF CANCER
  [FR] COMPOSÉS HÉTÉROCYCLIQUES DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DU CANCER

  摘要：

  该申请涉及杂环酰胺衍生物及其在癌症治疗和预防中的应用，以及含有这些衍生物的组合物和其制备方法。(化学式(I))

  公开号：

  WO2021028643A1

文献信息

• [EN] THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSÉS AMINOHÉTÉROARYLE À SUBSTITUTION THIAZOLE UTILISÉS COMME INHIBITEURS DE LA TYROSINE KINASE SPLÉNIQUE
  申请人：MERCK SHARP & DOHME

  公开号：WO2015095444A1

  公开（公告）日：2015-06-25

  The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

  该发明提供了某些噻唑取代氨基杂环芳烃化合物的化学式(I) (I)，或其药用可接受的盐，其中环R1、R2、R3、R4、环A以及下标n1、n2和r如本文所定义。该发明还提供了包含这些化合物的药物组合物，以及利用这些化合物治疗由脾酪氨酸激酶（Syk）介导的疾病或症状的方法。
• Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
  申请人：AC Immune S.A.

  公开号：EP2377860A1

  公开（公告）日：2011-10-19

  The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及一组新化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病，以及与淀粉样蛋白类似蛋白相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织中的病理异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物制备用于治疗或预防与淀粉样和/或淀粉样类似蛋白相关的疾病或病况的药物的用途。还揭示了一种治疗或预防与淀粉样和/或淀粉样类似蛋白相关的疾病或病况的方法。
• Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-like Proteins
  申请人：Kroth Heiko

  公开号：US20110256064A1

  公开（公告）日：2011-10-20

  The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及一组新化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病，以及与淀粉样蛋白相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织中的病理异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物制备用于治疗或预防与淀粉和/或淀粉样蛋白相关的疾病或病况的药物的用途。还公开了一种治疗或预防与淀粉和/或淀粉样蛋白相关的疾病或病况的方法。
• [EN] INHIBITORS OF INTERLEUKIN-1 RECEPTOR ASSOCIATED KINASE (IRAK) /FMS-LIKE RECEPTOR TYROSINE KINASE (FLT3), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF<br/>[FR] INHIBITEURS DE LA KINASE ASSOCIÉE AU RÉCEPTEUR DE L'INTERLEUKINE 1 (IRAK)/TYROSINE KINASE DU RÉCEPTEUR DE TYPE FMS (FLT3), LEURS PRODUITS PHARMACEUTIQUES ET LEURS PROCÉDÉS
  申请人：PHARMABLOCK SCIENCES NANJING INC

  公开号：WO2021159993A1

  公开（公告）日：2021-08-19

  Inhibitors of interleukin-1 receptor associated kinase (IRAK) enzyme/FMS-like receptor tyrosine kinase (FLT3) with Formula (I), a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. In Formula (I), X, X 1, X 2 is selected from N and C; and U, V and W groups are independently of each other a non-hydrogen monovalent group. Pharmaceutical products comprising the IRAK inhibitors and prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, and proliferative diseases, among others, are also provided. The interleukin-1 receptor associated kinase (IRAK) mentioned above can be IRAK4.

  具有公式（I）的白细胞介素-1受体相关激酶（IRAK）酶/类FMS受体酪氨酸激酶（FLT3）的抑制剂，其为药用可接受的盐、酯、前药、复合物、溶剂化物、水合物或其异构体，在任何晶体形式或非晶形式中。在公式（I）中，X、X1、X2从N和C中选择；U、V和W基团是非氢单价基团，彼此独立。还提供了包括IRAK抑制剂的药物产品以及预防和/或治疗炎症性疾病、自身免疫性疾病和增殖性疾病等。上述提到的白细胞介素-1受体相关激酶（IRAK）可以是IRAK4。
• THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3083560B1

  公开（公告）日：2021-10-27