2-bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 2-bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine
• 英文别名: 2-bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c']dipyridine；2-Bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c']dipyridine；11-bromo-8-methyl-4,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene
• 化学式: C₁₁H₈BrN₃
• 分子量: 262.109
• InChiKey: XSDBRVKSBZRJNB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  30.7
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine 在 三乙胺 、 sodium hydroxide 、 氢氟酸 作用下， 以 二氯甲烷 、 二甲基亚砜 、 N,N-二甲基甲酰胺 、 正丁醇 为溶剂， 反应 4.77h， 生成 2-((4-¹⁸F)-fluoropiperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine
  参考文献：
  名称：

  Carbazole and Carboline Compounds for Use in the Diagnosis, Treatment, Alleviation or Prevention of Disorders Associated with Amyloid or Amyloid-Like Proteins

  摘要：

  本发明涉及可用于诊断、治疗、缓解或预防与淀粉样蛋白和类淀粉样蛋白相关的一组疾病和异常的新化合物，如阿尔茨海默病。本发明还提供了制备这些化合物的前体。

  公开号：

  US20170002005A1
• 作为产物：
  描述：

  2-bromo-6-(1-methylhydrazinyl)pyridine 在 manganese(IV) oxide 、 硫酸 作用下， 以 1,4-二氧六环 、 5,5-dimethyl-1,3-cyclohexadiene 为溶剂， 反应 31.0h， 生成 2-bromo-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine
  参考文献：
  名称：

  DIHYDROPYRIDOPYRROLE DERIVATIVES AS TAU-PET-LIGANDS

  摘要：

  本发明涉及一种可以用于选择性Tau检测与Tau聚集物相关的疾病和异常，如阿尔茨海默病和其他Tau病理学，利用正电子发射断层扫描（PET）成像的新化合物的公式（I）。公式（I）：

  公开号：

  EP3118202A1

文献信息

• [EN] CARBAZOLE AND CARBOLINE COMPOUNDS FOR USE IN THE DIAGNOSIS, TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH AMYLOID OR AMYOLID-LIKE PROTEINS<br/>[FR] COMPOSÉS DE CARBAZOLE ET DE CARBOLINE DESTINÉS À ÊTRE UTILISÉS DANS LE DIAGNOSTIC, LE TRAITEMENT, L'ATTÉNUATION OU LA PRÉVENTION DE TROUBLES ASSOCIÉS AUX PROTÉINES AMYLOÏDES ET DE TYPE AMYLOÏDE
  申请人：AC IMMUNE SA

  公开号：WO2015110263A1

  公开（公告）日：2015-07-30

  The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.

  本发明涉及一种新型化合物，可用于诊断、治疗、缓解或预防与淀粉样蛋白和类淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病。本发明还提供了制备这些化合物的前体。
• DIHYDROPYRIDOPYRROLE DERIVATIVES AS TAU-PET-LIGANDS
  申请人：AC Immune S.A.

  公开号：EP3118202A1

  公开（公告）日：2017-01-18

  The present invention relates to novel compounds of formula (I) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other Tauopathies using Positron Emission Tomography (PET) Imaging. Formula (I):

  本发明涉及一种可以用于选择性Tau检测与Tau聚集物相关的疾病和异常，如阿尔茨海默病和其他Tau病理学，利用正电子发射断层扫描（PET）成像的新化合物的公式（I）。公式（I）：
• Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins
  申请人：AC IMMUNE SA

  公开号：US10662193B2

  公开（公告）日：2020-05-26

  The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.

  本发明涉及可用于诊断、治疗、缓解或预防与淀粉样蛋白和淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病的新型化合物。本发明还提供了用于制备根据本发明的化合物的前体。
• <b>PI-2620</b> Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer’s Disease and Other Tauopathies
  作者：Heiko Kroth、Felix Oden、Jerome Molette、Hanno Schieferstein、Emanuele Gabellieri、Andre Mueller、Mathias Berndt、Nampally Sreenivasachary、Andreia Monica Serra、Francesca Capotosti、Heribert Schmitt-Willich、David Hickman、Andrea Pfeifer、Ludger Dinkelborg、Andrew Stephens

  DOI：10.1021/acs.jmedchem.1c00861

  日期：2021.9.9
• [EN] TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE<br/>[FR] COMPOSÉS CIBLANT LA PROTÉINE TAU ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2021011913A1

  公开（公告）日：2021-01-21

  The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.