4-溴-2,7-萘啶-1-胺 | 959558-28-2

• 物质功能分类: 化学试剂 - 有机试剂 - 多环化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 4-溴-2,7-萘啶-1-胺
• 英文名称: 4-bromo-2,7-naphthyridin-1-ylamine
• 英文别名: 4-bromo-2,7-naphthyridin-1-amine；CAS 959558-28-2
• CAS: 959558-28-2
• 化学式: C₈H₆BrN₃
• 分子量: 224.06
• InChiKey: GIFGLLRPNLFCGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  51.8
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H317,H319

反应信息

• 作为反应物：
  描述：

  4-溴-2,7-萘啶-1-胺 在 亚硝酸异戊酯 作用下， 以 四氢呋喃 为溶剂， 生成 4-Brom-2,7-naphthyridin
  参考文献：
  名称：

  [EN] MPRO TARGETING ANTIVIRAL COMPOUNDS
  [FR] COMPOSÉS ANTIVIRAUX CIBLANT LES MPRO

  摘要：

  公开了根据式（I）的新型病毒 Mpro 抑制剂、它们的药学上可接受的盐及其药物组合物。还公开了使用此类化合物和组合物抑制 Mpro 和/或治疗各种病毒感染的方法；特别是与冠状病毒有关的病毒感染。本公开的化合物和组合物在治疗广谱冠状病毒方面可能特别有用。

  公开号：

  WO2023180189A1
• 作为产物：
  描述：

  3-氰基-4-甲基吡啶 在 溴 、 甲酸铵 、 溶剂黄146 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 93.0h， 生成 4-溴-2,7-萘啶-1-胺
  参考文献：
  名称：

  7-AZAINDOLE-2,7-NAPHTHYRIDINE DERIVATIVE FOR THE TREATMENT OF TUMOURS

  摘要：

  化合物4-(2-甲基-1H-吡咯并[2,3-b]吡啶-3-基)-2,7-萘啶-1-基胺及其药用盐和/或互变异构体。该化合物用于治疗肿瘤、肿瘤生长、肿瘤转移和/或艾滋病。

  公开号：

  US20150252041A1

文献信息

• [EN] HETARYL-[1,8]NAPHTHYRIDINE DERIVATIVES<br/>[FR] DÉRIVÉS D'HÉTARYL-[1,8]NAPHTYRIDINE
  申请人：MERCK PATENT GMBH

  公开号：WO2011095196A1

  公开（公告）日：2011-08-11

  Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

  新型杂环-[1,8]萘啶衍生物的化学式（I），其中R1、R2、W1、W3、W5和W6的含义如权利要求书中所述，是ATP消耗蛋白的抑制剂，可用于治疗肿瘤。
• Hetaryl-[1,8]naphthyridine derivatives
  申请人：Jonczyk Alfred

  公开号：US20120295902A1

  公开（公告）日：2012-11-22

  Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W 1 , W 3 , W 5 and W 6 have the meaning according to claim 1 , are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

  新型杂芳基-[1,8]萘啶衍生物的化学式（I），其中R1、R2、W1、W3、W5和W6的含义如权利要求书中所述，是ATP消耗蛋白的抑制剂，可用于治疗肿瘤。
• 7-AZAINDOLE-2,7-NAPHTHYRIDINE DERIVATIVE FOR THE TREATMENT OF TUMOURS
  申请人：MERCK PATENT GMBH

  公开号：US20150252041A1

  公开（公告）日：2015-09-10

  The compound 4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2,7-naphthyridin-1-ylamine and pharmaceutically usable salts and/or tautomers thereof. The use of this compound for the treatment of tumours, tumour growth, tumour metastases and/or AIDS.

  化合物4-(2-甲基-1H-吡咯并[2,3-b]吡啶-3-基)-2,7-萘啶-1-基胺及其药用盐和/或互变异构体。该化合物用于治疗肿瘤、肿瘤生长、肿瘤转移和/或艾滋病。
• [EN] PYRIDO [2, 3 - B] PYRAZINE DERIVATIVES AND THEIR THERAPEUTICAL USES<br/>[FR] DÉRIVÉS DE PYRIDO-[2,3-B]PYRAZINE ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：MERCK PATENT GMBH

  公开号：WO2012119690A1

  公开（公告）日：2012-09-13

  The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

  本发明涉及新型的式（I）的吡啶并[2,3-b]吡嗪衍生物，以及利用这些化合物在ATP消耗蛋白质如激酶的信号转导的抑制、调节和/或调制中发挥作用，特别是TGF-beta受体激酶的抑制剂，以及利用这些化合物治疗激酶诱导的疾病，特别是治疗肿瘤。
• Identification of nicotinamide aminonaphthyridine compounds as potent RET kinase inhibitors and antitumor activities against RET rearranged lung adenocarcinoma
  作者：Modi Wang、N. Naganna、Herman O. Sintim

  DOI：10.1016/j.bioorg.2019.103052

  日期：2019.9

  RET rearrangement is a recently identified oncogenic mutation in lung adenocarcinoma (LADC) that accounts for approximately 2% of all NSCLCs. More than six fusion partners have been identified in NSCLC, such as KIF5B, CCDC6, NCOA4, TRIM33, CLIP1 and ERC1. Many RET inhibitors have been reported and some have progressed to the clinic. Similar to most kinase inhibitors, patients often respond to current RET inhibitors but relapse can occur due to the emergence of mutant RET kinases, such as RET (S904F) and (V804L/M), which are resistant to inhibition. Our group previously reported that the benzamide aminonaphthyridine HSN356, a multikinase inhibitor, also inhibited RET. In this study, we prepared various nicotinamide analogs of HSN356 and investigated RET inhibition to uncover the salient moieties on HSN356 that are important for kinase inhibition and to also evaluate if HSN356 and analogs thereof could inhibit mutant RET kinases, such as RET (S904F) and (V804L/M). Compound 3 (HSN608), the nicotinamide analog of HSN356, inhibits RET and mutant forms better than reported RET inhibitors such as Alectinib, Sorafenib, Vandetanib and Apatinib, and comparable to BLU667. HSN608 inhibited the growth of CCDC6-RET driven LC-2/ad cell line with IC50 of similar to 3 nM. Under similar conditions, BLU667 and vandetanib (two drugs being evaluated against RET-driven cancers in the clinic) inhibited the growth of LC-2/ad with IC50 values of similar to 10 and 328 nM respectively.