Alalevonadifloxacin | 706809-20-3

• 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: Alalevonadifloxacin
• 英文别名: (12S)-8-[4-[(2S)-2-aminopropanoyl]oxypiperidin-1-yl]-7-fluoro-12-methyl-4-oxo-1-azatricyclo[7.3.1.05,13]trideca-2,5,7,9(13)-tetraene-3-carboxylic acid
• CAS: 706809-20-3
• 化学式: C₂₂H₂₆FN₃O₅
• 分子量: 431.5
• InChiKey: OUXXDXXQNWKOIF-RYUDHWBXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• Prodrugs of benzoquinolizine-2-carboxylic acid
  申请人：Patel Vithalbhai Mahesh

  公开号：US20070219227A1

  公开（公告）日：2007-09-20

  The instant invention relates to novel prodrugs of optically pure benzoquinolizine-2-carboxylic acid and pharmaceutical compositions that include the prodrugs. In particular, the present invention relates to the sulfonic acid salts of L-alanine and L-valine prodrugs of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid. The compounds and compositions of the invention can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections, especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.

  本发明涉及光学纯苯并喹啉-2-羧酸的新型前药及包括这些前药的制药组合物。具体而言，本发明涉及S-（-）-9-氟-6,7-二氢-8-（4-羟基哌啶-1-基）-5-甲基-1-氧代-1H，5H-苯并[i，j]喹啉-2-羧酸的L-丙氨酸和L-缬氨酸前药的磺酸盐。本发明的化合物和组合物可用于治疗细菌革兰氏阳性、革兰氏阴性和厌氧感染，特别是由耐药革兰氏阳性菌和革兰氏阴性菌引起的感染，结核分枝杆菌感染和新兴医院感染病原体感染。
• Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
  申请人：Patel Vithalbhai Mahesh

  公开号：US20080044466A1

  公开（公告）日：2008-02-21

  The present invention relates to optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.

  本发明涉及光学纯的S-(−)-苯并喹啉羧酸、其衍生物、盐、伪多晶形、多晶形和水合物，基本上不含它们的R-(+)-异构体，以及制备光学纯的S-(−)-苯并喹啉羧酸、其衍生物、盐、伪多晶形、多晶形和水合物的过程，基本上不含它们的R-(+)-异构体，并且涉及包含S-(−)-苯并喹啉羧酸、其衍生物、盐、伪多晶形、多晶形和水合物的制药组合物。
• (s)-benzoquinolizine carboxylic acids and their use as antibacterial agents
  申请人：Wockhardt Limited

  公开号：EP2030620A1

  公开（公告）日：2009-03-04

  The present invention relates to S-(-)-optically pure benzoquinolizine carboxylic acid of formula I, and their pharmaceutically acceptable salts, substantially free of their R-(+)-isomers, to processes for their preparation and to pharmaceutical compositions comprising an active compound of the invention. The compounds have excellent antibacterial activity. The compounds and compositions can be used for the treatment of local and systemic bacterial infections, diseases and disorders caused by antibiotic-sensitive and antibiotic-resistant microbial strains, without the concomitant liability of adverse effects associated with the racemic mixture of the active compound of the invention.

  本发明涉及式 I 的 S-(-)-光学纯苯喹嗪羧酸及其药学上可接受的盐（基本上不含其 R-(+)-异构体）、其制备工艺以及含有本发明活性化合物的药物组合物。这些化合物具有优异的抗菌活性。这些化合物和组合物可用于治疗由抗生素敏感和抗生素耐药微生物菌株引起的局部和全身性细菌感染、疾病和紊乱，而不会产生与本发明活性化合物外消旋混合物相关的不良反应。
• Polymer conjugate comprising a bioactive agent
  申请人：POLYACTIVA PTY LTD

  公开号：US10758626B2

  公开（公告）日：2020-09-01

  The present invention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety selected from quinolones, NSAIDs and mixtures thereof. The present invention also relates to methods for preparing the polymer conjugates using click cycloaddition chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the post-surgical care to treat or prevent infections, provide analgesia and treat inflammation.

  本发明总体上涉及用于向受试者输送生物活性剂的聚合物-生物活性剂共轭物。聚合物-生物活性剂共轭物的聚合物骨架中含有三唑分子和选自喹诺酮类、非甾体抗炎药及其混合物的生物活性分子。本发明还涉及使用单击环化化学反应制备聚合物共轭物的方法、适用于制备聚合物共轭物的单体-生物活性剂共轭物，以及包含聚合物共轭物的用于手术后治疗或预防感染、提供镇痛和治疗炎症的药物产品。
• (S)-BENZOQUINOLIZINE CARBOXYLIC ACIDS AND THEIR USE AS ANTIBACTERIAL AGENTS
  申请人：Wockhardt Limited

  公开号：EP1175217B8

  公开（公告）日：2009-03-18