GP-6 | 1400802-18-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: GP-6
• 英文别名: 4-[(1R,4R,5R)-5-amino-2-azabicyclo[2.2.1]heptan-2-yl]-6-fluoro-N-methyl-2-(2-methylpyrimidin-5-yl)oxy-9H-pyrimido[4,5-b]indol-8-amine
• CAS: 1400802-18-7
• 化学式: C₂₂H₂₃FN₈O
• 分子量: 434.476
• InChiKey: LQLBTQWLWFCOGN-AXAPSJFSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  118
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• [EN] TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS<br/>[FR] INHIBITEURS TRICYCLIQUES DE GYRASE UTILISABLES COMME AGENTS ANTIBACTÉRIENS
  申请人：TRIUS THERAPEUTICS INC

  公开号：WO2014043272A1

  公开（公告）日：2014-03-20

  Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

  本文披露了具有化学式I结构的化合物及其药用盐、酯和前药，这些化合物可用作抗菌有效的三环酶抑制剂。此外，本文还披露了三环酶抑制剂化合物的种属。还考虑了相关的药用组合物、用途和制备这些化合物的方法。
• TRICYCLIC GYRASE INHIBITORS
  申请人：Bensen Daniel

  公开号：US20120238751A1

  公开（公告）日：2012-09-20

  Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

  本文披露了具有式I结构的化合物，以及作为抗菌有效的三环酶抑制剂的药用盐、酯和前药，相关的药物组合物、用途和制备该化合物的方法也在考虑之中。
• [EN] ARYL COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION<br/>[FR] COMPOSÉS ARYLE POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION BACTÉRIENNE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2020109191A1

  公开（公告）日：2020-06-04

  The present invention relates to novel compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as DNA gyrase and/or topoisomerase IV inhibitors in the treatment and/or prophylaxis of bacterial infection.

  本发明涉及公式（I）的新化合物，其中R1、R2、R3、R4、R5和R6如本文所述，并且它们的药用盐、对映体或二对映体，以及包括这些化合物的组合物和使用这些化合物作为DNA旋转酶和/或拓扑异构酶IV抑制剂在治疗和/或预防细菌感染的方法。
• [EN] TRICYCLIC COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION<br/>[FR] COMPOSÉS TRICYCLIQUES POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION BACTÉRIENNE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2020109190A1

  公开（公告）日：2020-06-04

  The present invention relates to novel compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as DNA gyrase and/or topoisomerase IV inhibitors in the treatment and/or prophylaxis of bacterial infection.

  本发明涉及式（I）的新化合物，其中R1、R2、R3、R4、R5和R6如本文所述，以及它们的前药或药学上可接受的盐、对映体或二对映体，以及包括这些化合物的组合物和使用这些化合物作为DNA旋转酶和/或拓扑异构酶IV抑制剂治疗和/或预防细菌感染的方法。
• Tricyclic Gyrase inhibitors
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US10865216B2

  公开（公告）日：2020-12-15

  Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

  本文公开了具有式 I 结构的化合物及其药学上适用的盐、酯和原药，它们可作为抗菌有效的三环回旋酶抑制剂。此外，本文还公开了三环回旋酶抑制剂化合物的种类。 还考虑了相关的药物组合物、用途和化合物的制造方法。