1-Azabicyclo[3.2.0]hept-2-en-7-one | 83961-73-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 1-Azabicyclo[3.2.0]hept-2-en-7-one
• CAS: 83961-73-3
• 化学式: C₆H₇NO
• 分子量: 109.13
• InChiKey: YZBQHRLRFGPBSL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• Novel carbapenem compounds
  申请人：Sunagawa Makoto

  公开号：US20050020566A1

  公开（公告）日：2005-01-27

  A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.

  以下是化合物或其药学上可接受的盐的化学式： 该发明是一种羧甲基青霉烯化合物，具有广谱的抗革兰氏阴性和革兰氏阳性细菌的强效抗菌活性，特别是耐青霉素的肺炎链球菌（PRSP），这些菌株在近年来被高频率地分离出来，因此引起了严重的临床问题，以及流感嗜血杆菌，由于青霉素结合蛋白（PBP）突变，如β-内酰胺酶非产生性氨苄西林耐药（BLNAR）流感嗜血杆菌而对现有的β-内酰胺类抗生素产生了抗药性，并且具有优异的口服吸收性。
• Novel carbapenem compound
  申请人：Sunagawa Makoto

  公开号：US20090029964A1

  公开（公告）日：2009-01-29

  An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R 0 represents hydrogen atom or the like; R 1 represents C 1 -C 3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH 2 (CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH 2 —, —NR a CH 2 — (wherein R a represents hydrogen atom, optionally substituted C 1 -C 4 alkyl group or the like) or the like.

  一种口服抗菌剂，其活性成分为由下式[1]表示的碳青霉烯化合物，其中R0表示氢原子或类似物；R1表示C1-C3烷基，该烷基被羟基或类似物取代；R表示氢原子或通过水解在活体内再生羧基的基团；L表示单键，亚甲基，—OCH2（CO）—或类似物；Het表示由下式[2]表示的基团，其中m和n独立地表示0或1；A和B独立地表示亚甲基，羰基或类似物；Y表示亚甲基，乙烯基，氧原子，—OCH2—，—NRaCH2—（其中Ra表示氢原子，可选取代的C1-C4烷基或类似物）或类似物。
• Novel Carbapenem Compound
  申请人：Sunagawa Makoto

  公开号：US20070265242A1

  公开（公告）日：2007-11-15

  A carbapenem compound represented by a following formula [1], wherein R 1 is C 1 to C 3 alkyl or C 1 to C 3 alkyl substituted by hydroxy. R is hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body, A is a following formula [1a], wherein E is a 5 to 7 membered cyclic ring optionally containing 1 to 3 hetero atoms (excluding benzene ring) which forms a bicyclic ring in corporation with the benzene ring, Y is hydrogen atom, C 1 to C 4 alkyl, C 1 to C 4 alkoxy, trifluoromethoxy, halogen atom or cyano group, or its pharmaceutically acceptable salt.

  一种碳青霉烯化合物，其化学式为[1]，其中R1为C1到C3烷基或C1到C3烷基被羟基取代，R为氢原子或在活体内通过水解再生羧基团的基团，A为以下化学式[1a]，其中E是一个5到7个成员的环状环，可选地含有1到3个杂原子（不包括苯环），与苯环结合形成双环，Y为氢原子，C1到C4烷基，C1到C4烷氧基，三氟甲氧基，卤原子或氰基，或其药学上可接受的盐。
• Pyrrole Derivatives as Dna Gyrase and Topoisomerase Inhibitors
  申请人：Basarab Gregory Steven

  公开号：US20080269214A1

  公开（公告）日：2008-10-30

  Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

  本文介绍了化学式(I)及其药用可接受盐的化合物：化学式(I)。还介绍了它们的制备过程、含有它们的药物组合物、作为药物的用途以及在治疗细菌感染中的应用。
• BRIDGED LIPOGLYCOPEPTIDES THAT POTENTIATE THE ACTIVITY OF BETA-LACTAM ANTIBACTERIALS
  申请人：Gallant Michel

  公开号：US20130244929A1

  公开（公告）日：2013-09-19

  The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a β-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a β-lactam antibiotic.

  本发明提供了一种新型的脂肽多糖肽类化合物，它们是一类信号肽酶抑制剂（SpsB）。本发明的化合物可用于治疗各种细菌相关感染疾病，特别是在与β-内酰胺类抗生素（如亚胺培南和依达拉奉）一起使用时作为增效剂。因此，本发明提供了一种使用本文所述化合物单独或与β-内酰胺类抗生素联合治疗细菌相关感染的方法。