3-碘-2-甲氧基-5-甲基吡啶 | 1203499-63-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 3-碘-2-甲氧基-5-甲基吡啶
• 英文名称: 3-iodo-2-methoxy-5-methylpyridine
• CAS: 1203499-63-1
• 化学式: C₇H₈INO
• 分子量: 249.051
• InChiKey: KPEWLACJKQHYTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险等级：
  IRRITANT

反应信息

• 作为反应物：
  描述：

  3-碘-2-甲氧基-5-甲基吡啶 在 三乙基硅烷 、 bis-triphenylphosphine-palladium(II) chloride 、 copper(l) iodide 、 palladium on activated charcoal 、 三乙胺 、 sodium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 为溶剂， 反应 67.0h， 生成 2-hydroxy-2-(2-(2-methoxy-5-methylpyridin-3-yl)ethyl)-succinic acid
  参考文献：
  名称：

  Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family

  摘要：

  Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate la (PF-06649298) which inhibits the transport of citrate in in vitro and in vivo settings via a specific interaction with NaCT. Herein, we report the optimization of this series leading to 4a (PF-06761281), a more potent inhibitor with suitable in vivo pharmacokinetic profile for assessment of in vivo pharmacodynamics. Compound 4a was used to demonstrate dose dependent inhibition of radioactive [C-14]citrate uptake in liver and kidney in vivo, resulting in modest reductions in plasma glucose concentrations.

  DOI：

  10.1021/acs.jmedchem.5b01752

文献信息

• [EN] MUTANT IDH2 INHIBITOR AND APPLICATION THEREOF<br/>[FR] INHIBITEUR D'IDH2 MUTANTE ET APPLICATION ASSOCIÉE<br/>[ZH] 突变型IDH2抑制剂及其应用
  申请人：BETTA PHARMACEUTICALS CO LTD

  公开号：WO2021057975A1

  公开（公告）日：2021-04-01

  一种作为突变型异柠檬酸脱氢酶2(IDH2)抑制剂的化合物(如式Ⅰ所示)及其制备方法、药物组合物。还涉及上述化合物或其药物组合物在治疗突变型IDH2介导的疾病中的用途。IDH2抑制剂能够抑制携带最常见IDH2突变体的细胞中2-HG的生成，是一种低毒性作用且高效靶向抗肿瘤药物的理想靶标。
• PYRIMIDINE, PYRIDINE AND TRIAZINE DERIVATIVES AS MAXI-K CHANNEL OPENERS
  申请人：Tsuzuki Yasuyuki

  公开号：US20110034435A1

  公开（公告）日：2011-02-10

  A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R 1 is independently halogen, cyano, etc., each of X 1 , X 2 and X 3 is CR 2 or nitrogen, R 2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH 2 COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.
• Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family
  作者：Kim Huard、James R. Gosset、Justin I. Montgomery、Adam Gilbert、Matthew M. Hayward、Thomas V. Magee、Shawn Cabral、Daniel P. Uccello、Kevin Bahnck、Janice Brown、Julie Purkal、Matthew Gorgoglione、Adhiraj Lanba、Kentaro Futatsugi、Michael Herr、Nathan E. Genung、Gary Aspnes、Jana Polivkova、Carmen N. Garcia-Irizarry、Qifang Li、Daniel Canterbury、Mark Niosi、Nicholas B. Vera、Zhenhong Li、Bhagyashree Khunte、Jaclyn Siderewicz、Timothy Rolph、Derek M. Erion

  DOI：10.1021/acs.jmedchem.5b01752

  日期：2016.2.11

  Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate la (PF-06649298) which inhibits the transport of citrate in in vitro and in vivo settings via a specific interaction with NaCT. Herein, we report the optimization of this series leading to 4a (PF-06761281), a more potent inhibitor with suitable in vivo pharmacokinetic profile for assessment of in vivo pharmacodynamics. Compound 4a was used to demonstrate dose dependent inhibition of radioactive [C-14]citrate uptake in liver and kidney in vivo, resulting in modest reductions in plasma glucose concentrations.