2-bromo-4-(1H-pyrazol-1-yl)pyridine | 1159815-42-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-bromo-4-(1H-pyrazol-1-yl)pyridine
• 英文别名: 2-bromo-4-pyrazol-1-ylpyridine
• CAS: 1159815-42-5
• 化学式: C₈H₆BrN₃
• 分子量: 224.06
• InChiKey: XEEWOMHURIGWAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 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-4-(1H-pyrazol-1-yl)pyridine 、 三丁基氯化锡 在 lithium chloro-isopropyl-magnesium chloride 作用下， 以 四氢呋喃 为溶剂， 反应 2.42h， 生成 4-pyrazol-1-yl-2-tributylstannanyl-pyridine
  参考文献：
  名称：

  Pyrrolopyrazine Kinase Inhibitors

  摘要：

  本发明涉及使用新型吡咯吡嗪衍生物的公式I，其中变量n、p、q、Q、X、X'和Y如本文所述定义，这些衍生物抑制JAK和SYK，并且适用于治疗自身免疫和炎症性疾病。

  公开号：

  US20110230462A1

文献信息

• [EN] C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE<br/>[FR] COMPOSÉS IMINOPYRIMIDINONES CONDENSÉS OXACYCLIQUES EN C5-C6 UTILISÉS COMME INHIBITEURS DE BACE, COMPOSITIONS ET UTILISATION ASSOCIÉES
  申请人：MERCK SHARP & DOHME

  公开号：WO2016085780A1

  公开（公告）日：2016-06-02

  In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

  在其多种实施方式中，本发明提供了某些C5-C6-氧杂环融合咪唑嘧啶酮化合物，包括化合物式（I）所示的化合物或其互变异构体，以及该化合物和该互变异构体的药学上可接受的盐，其中RN、R1、RA、环A、m、n、-L1-、环B、RB和p如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与之相关的各种病理。还披露了包括一种或多种此类化合物（单独使用和与一种或多种其他活性剂组合使用）的药物组合物，以及其制备和使用方法，包括可能用于治疗阿尔茨海默病的方法。
• Pyrrolopyrazine kinase inhibitors
  申请人：Hendricks Robert Than

  公开号：US08518945B2

  公开（公告）日：2013-08-27

  The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

  本发明涉及使用新型吡咯吡嗪衍生物（公式I），其中变量n、p、q、Q、X、X'和Y的定义如本文所述，这些衍生物抑制JAK和SYK，并且对于治疗自身免疫和炎症性疾病有用。
• PYRROLOPYRAZINE KINASE INHIBITORS
  申请人：F.Hoffmann-La Roche AG

  公开号：EP2550273A2

  公开（公告）日：2013-01-30
• 3-METHYL-2-IMINO-HEXAHYDRO-1H-PYRANO[3,4-D]PYRIMIDIN-4-ONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3223820B1

  公开（公告）日：2020-07-22
• C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20170362248A1

  公开（公告）日：2017-12-21

  In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R N , R 1 , R A , ring A, m, n, -L 1 -, ring B, R B , and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.