7'-bromo-4',5'-dihydrospiro[cyclopropane-1,3'-pyrido[2,3-e][1,4]diazepin]-2'(1'H)-one

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 7'-bromo-4',5'-dihydrospiro[cyclopropane-1,3'-pyrido[2,3-e][1,4]diazepin]-2'(1'H)-one
• 英文别名: 7-bromospiro[4,5-dihydro-1H-pyrido[2,3-e][1,4]diazepine-3,1'-cyclopropane]-2-one
• 化学式: C₁₀H₁₀BrN₃O
• 分子量: 268.113
• InChiKey: ATCZCCSUUDZZBC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  54
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-氨基-5-溴烟醛氢溴酸盐 在 sodium hydride 、 三乙胺 作用下， 以 甲醇 、 二甲基亚砜 为溶剂， 反应 35.0h， 生成 7'-bromo-4',5'-dihydrospiro[cyclopropane-1,3'-pyrido[2,3-e][1,4]diazepin]-2'(1'H)-one
  参考文献：
  名称：

  [EN] TETRAHYDROPYRIDINE DERIVATIVES AS FabI INHIBITORS
  [FR] DÉRIVÉS DE TÉTRAHYDROPYRIDINE SERVANT D'INHIBITEURS DE FABI

  摘要：

  本发明涉及式（1）的四氢吡啶衍生物，可作为抗菌剂，更具体地作为FabI抑制剂的治疗用途。其中X、Y、Z和“n”的含义与说明书中给出的含义相同，并且其药学上可接受的盐和立体异构体在治疗和预防疾病或紊乱方面具有用处，特别是在抑制烯酰-ACP还原酶酶（FabI）活性具有优势的疾病或紊乱的治疗中的应用。本发明还提供了合成和给药FabI抑制化合物的方法。本发明还提供了包含至少一种FabI抑制化合物以及药学上可接受的载体、稀释剂或赋形剂的药物制剂。

  公开号：

  WO2014195844A1

文献信息

• [EN] TETRAHYDROPYRIDINE DERIVATIVES AS FabI INHIBITORS<br/>[FR] DÉRIVÉS DE TÉTRAHYDROPYRIDINE SERVANT D'INHIBITEURS DE FABI
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014195844A1

  公开（公告）日：2014-12-11

  The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明涉及式（1）的四氢吡啶衍生物，可作为抗菌剂，更具体地作为FabI抑制剂的治疗用途。其中X、Y、Z和“n”的含义与说明书中给出的含义相同，并且其药学上可接受的盐和立体异构体在治疗和预防疾病或紊乱方面具有用处，特别是在抑制烯酰-ACP还原酶酶（FabI）活性具有优势的疾病或紊乱的治疗中的应用。本发明还提供了合成和给药FabI抑制化合物的方法。本发明还提供了包含至少一种FabI抑制化合物以及药学上可接受的载体、稀释剂或赋形剂的药物制剂。
• TETRAHYDROPYRIDINE DERIVATIVES AS FabI INHIBITORS
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3004099A1

  公开（公告）日：2016-04-13
• US20140275019A1
  申请人：——

  公开号：US20140275019A1

  公开（公告）日：2014-09-18
• US9062075B2
  申请人：——

  公开号：US9062075B2

  公开（公告）日：2015-06-23
• [EN] FUSED PYRIDINE DERIVATIVES AS ANTIBACTERIAL AGENTS<br/>[FR] DÉRIVÉS PYRIDINE FONDUS, EN TANT QU'AGENTS ANTIBACTÉRIENS
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014072930A2

  公开（公告）日：2014-05-15

  The present invention relates to fused pyridine derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors, in which P, Q, R1, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.