2-氨基-4-吡啶乙酸 | 887580-47-4

• 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
• 中文名称: 2-氨基-4-吡啶乙酸
• 英文名称: (2-aminopyridin-4-yl)acetic acid
• 英文别名: 2-Amino-4-pyridineacetic acid；2-(2-aminopyridin-4-yl)acetic acid
• CAS: 887580-47-4
• 化学式: C₇H₈N₂O₂
• mdl: MFCD07367934
• 分子量: 152.153
• InChiKey: MAPLKZRJKHIYAZ-UHFFFAOYSA-N

物化性质

• 沸点：
  387.5±27.0 °C(Predicted)
• 密度：
  1.353

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  76.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-氨基-4-吡啶乙酸 在 氯化亚砜 、 lithium hydroxide monohydrate 、 水 作用下， 以 四氢呋喃 、 甲醇 、 叔丁醇 为溶剂， 反应 34.0h， 生成 [2-({[(2-甲基-2-丙基)氧基]羰基}氨基)-4-吡啶基]乙酸
  参考文献：
  名称：

  [EN] SPIROCYCLIC INDOLINES AS IL-17 MODULATORS
  [FR] INDOLINES SPIROCYCLIQUES UTILISÉES COMME MODULATEURS D'IL-17

  摘要：

  一系列替代的螺环式2-氧吲哚衍生物及其类似物，作为强效的人IL-17活性调节剂，因此在治疗和/或预防各种人类疾病，包括炎症性和自身免疫性疾病方面具有益处。

  公开号：

  WO2018229079A1

文献信息

• [EN] INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL<br/>[FR] INHIBITEURS DU CANAL À POTASSIUM DE LA MEDULLA EXTERNE DU REIN
  申请人：MERCK SHARP & DOHME

  公开号：WO2013090271A1

  公开（公告）日：2013-06-20

  The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

  本发明提供了式（I）的化合物及其药用可接受的盐，这些化合物是ROMK（Kir1.1）通道的抑制剂。这些化合物作为利尿剂和钠利尿剂，并且是治疗和预防包括高血压在内的心血管疾病以及由过多盐分和水潴留导致的疾病的有价值的药用活性化合物。
• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20140336177A1

  公开（公告）日：2014-11-13

  The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

  本发明提供了I式化合物及其药学上可接受的盐，其是ROMK（Kir1.1）通道的抑制剂。这些化合物作为利尿剂和钠利尿剂，是治疗和预防包括高血压和由过度盐和水潴留引起的疾病等医学状况的有价值的药学活性化合物。
• Spirocyclic indolines as IL-17 modulators
  申请人：UCB BIOPHARMA SRL

  公开号：US11052076B2

  公开（公告）日：2021-07-06

  A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

  一系列取代的螺环 2-氧代吲哚啉衍生物及其类似物是人类 IL-17 活性的强效调节剂，因此可用于治疗和/或预防各种人类疾病，包括炎症和自身免疫性疾病。
• [EN] BORONIC ACID DERIVATIVES<br/>[FR] DÉRIVÉS D'ACIDE BORONIQUE<br/>[ZH] 硼酸衍生物
  申请人：SHOUYAO HOLDINGS BEIJING CO LTD

  公开号：WO2021143923A1

  公开（公告）日：2021-07-22

  公开了式(I)化合物或其药学上可接受的盐、溶剂化物、多晶型物或异构体、包含这些化合物的药物组合物，以及此类化合物在治疗跟LMP7相关的疾病中的用途。
• Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases
  作者：Scott J. Hecker、K. Raja Reddy、Maxim Totrov、Gavin C. Hirst、Olga Lomovskaya、David C. Griffith、Paula King、Ruslan Tsivkovski、Dongxu Sun、Mojgan Sabet、Ziad Tarazi、Matthew C. Clifton、Kateri Atkins、Amy Raymond、Kristy T. Potts、Jan Abendroth、Serge H. Boyer、Jeffrey S. Loutit、Elizabeth E. Morgan、Stephanie Durso、Michael N. Dudley

  DOI：10.1021/acs.jmedchem.5b00127

  日期：2015.5.14

  The increasing dissemination of carbapenemases in Gram-negative bacteria has threatened the clinical usefulness of the beta-lactam class of antimicrobials. A program was initiated to discover a new series of serine beta-lactamase inhibitors containing a boronic acid pharmacophore, with the goal of finding a potent inhibitor of serine carbapenemase enzymes that are currently compromising the utility of the carbapenem class of antibacterials. Potential lead structures were screened in silico by modeling into the active sites of key serine beta-lactamases. Promising candidate molecules were synthesized and evaluated in biochemical and whole-cell assays. Inhibitors were identified with potent inhibition of serine carbapenemases, particularly the Klebsiella pneumoniae carbapenemase (KPC), with no inhibition of mammalian serine proteases. Studies in vitro and in vivo show that RPX7009 (9f) is a broad-spectrum inhibitor, notably restoring the activity of carbapenems against KPC-producing strains. Combined with a carbapenem, 9f is a promising product for the treatment of multidrug resistant Gram-negative bacteria.