Durlobactam | 1467829-71-5

• 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: Durlobactam
• 英文别名: [(2S,5R)-2-carbamoyl-3-methyl-7-oxo-1,6-diazabicyclo[3.2.1]oct-3-en-6-yl] hydrogen sulfate
• CAS: 1467829-71-5
• 化学式: C₈H₁₁N₃O₆S
• 分子量: 277.26
• InChiKey: BISPBXFUKNXOQY-RITPCOANSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  139
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Durlobactam 、 (6S)-tert-butyl 6-((tert-butyldimethylsilyloxy)methyl)-5-methyl-3-(trimethylsilyloxy)-5,6-dihydropyridine-1(2H)-carboxylate 、 (S)-tert-butyl 2-((tert-butyldimethylsilyloxy)methyl)-5-oxo-5,6-dihydropyridine-1(2H)-carboxylate 生成 (6S)-tert-butyl 6-((tert-butyldimethylsilyloxy)methyl)-5-isopropyl-3-(trimethylsilyloxy)-5,6-dihydropyridine-1(2H)-carboxylate
  参考文献：
  名称：

  Beta-Lactamase Inhibitor Compounds

  摘要：

  本发明涉及一种β-内酰胺酶抑制剂化合物。这些化合物及其药学上可接受的盐，与β-内酰胺类抗生素联合使用或单独使用，可用于治疗细菌感染，包括由耐药菌株引起的感染，包括多重耐药菌株。本发明包括公式（Ia）所述的化合物：或其药学上可接受的盐，其中R1、R2、R3和R4的值如本文所述。

  公开号：

  US20150073011A1

文献信息

• [EN] HETEROBICYCLIC COMPOUNDS AS BETA-LACTAMASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROBICYCLIQUES COMME INHIBITEURS DE LA BÊTA-LACTAMASE
  申请人：ASTRAZENECA AB

  公开号：WO2013150296A1

  公开（公告）日：2013-10-10

  The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R 2, R 3 and R 4 are described herein.

  本发明涉及一种β-内酰胺酶抑制剂化合物。这些化合物及其药学上可接受的盐，可与β-内酰胺类抗生素结合使用，或单独使用，用于治疗细菌感染，包括由耐药菌株引起的感染，包括多药耐药菌株引起的感染。本发明包括根据式(Ia)的化合物：或其药学上可接受的盐，其中R1、R2、R3和R4的值如本文所述。
• BETA-LACTAMASE INHIBITOR COMPOUNDS
  申请人：Entasis Therapeutics Limited

  公开号：US20160175290A1

  公开（公告）日：2016-06-23

  The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R 1 , R 2 , R 3 and R 4 are described herein.

  本发明涉及一种β-内酰胺酶抑制剂化合物。该化合物及其药学上可接受的盐可与β-内酰胺类抗生素联合使用或单独使用，用于治疗细菌感染，包括由耐药菌引起的感染，包括多重耐药菌。本发明包括根据式（Ia）描述的化合物：或其药学上可接受的盐，其中R1，R2，R3和R4的值如本文所述。
• Beta-lactamase inhibitor compounds
  申请人：Entasis Therapeutics Limited

  公开号：US09309245B2

  公开（公告）日：2016-04-12

  The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3 and R4 are described herein.

  本发明涉及β-内酰胺酶抑制剂化合物。这些化合物及其药学上可接受的盐，可与β-内酰胺类抗生素联合使用或单独使用，用于治疗细菌感染，包括由耐药菌株引起的感染，包括多重耐药菌株。本发明包括式(Ia)所示的化合物：或其药学上可接受的盐，其中R1、R2、R3和R4的值在此处描述。
• Deuterated O-sulfated beta lactam hydroxamic acids and deuterated N-sulfated beta lactams
  申请人：ARIXA PHARMACEUTICALS, INC.

  公开号：US10093666B2

  公开（公告）日：2018-10-09

  Provided herein are deuterated O-sulfated beta-lactam hydroxamic acids and deuterated N-sulfated beta-lactams, pharmaceutical compositions thereof and methods of treating infectious disease with deuterated compounds or pharmaceutical compositions thereof.

  本文提供了氚代 O-硫酸化β-内酰胺羟肟酸和氚代 N-硫酸化β-内酰胺、其药物组合物以及用氚代化合物或其药物组合物治疗传染病的方法。
• Combination therapy for treatment of resistant bacterial infections
  申请人：Entasis Therapeutics Limited

  公开号：US10376499B2

  公开（公告）日：2019-08-13

  The present invention is directed to combinations of a β-lactamase inhibitor with sulbactam and, optionally, imipenem/cilastatin. The combinations are useful for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant pathogens. More particularly, the invention relates to a combination of β-lactamase inhibitor compound 1: or a pharmaceutically acceptable salt thereof, with sulbactam, or a pharmaceutically acceptable salt thereof, and, optionally, imipenem/cilastatin, or a pharmaceutically acceptable salt thereof.

  本发明涉及β-内酰胺酶抑制剂与舒巴坦和亚胺培南/西司他丁的复方制剂。这些组合物可用于治疗细菌感染，包括由耐药生物（包括耐多药病原体）引起的感染。更具体地说，本发明涉及β-内酰胺酶抑制剂化合物1：或其药学上可接受的盐，与舒巴坦或其药学上可接受的盐，以及亚胺培南/西司他丁或其药学上可接受的盐的复方制剂。