quinolizine | 255-58-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹嗪类
• 英文名称: quinolizine
• 英文别名: 2H-quinolizine
• CAS: 255-58-3
• 化学式: C₉H₉N
• 分子量: 131.177
• InChiKey: MHBPDRSACQBQET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS
  申请人：Hutchinson H. John

  公开号：US20070105866A1

  公开（公告）日：2007-05-10

  Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

  本发明描述了调节5-脂氧合酶激活蛋白(FLAP)活性的化合物和含有该化合物的药物组合物。本发明还描述了单独使用和与其他化合物联合使用FLAP调节剂，用于治疗呼吸系统、心血管系统和其他白三烯依赖性或白三烯介导的状况或疾病。
• [EN] REDUCTION OF PRO-INFLAMMATORY HDL USING A LEUKOTRIENE INHIBITOR<br/>[FR] RÉDUCTION DE HDL PRO-INFLAMMATOIRE À L'AIDE D'UN INHIBITEUR DE LEUCOTRIÈNE
  申请人：AUTOIMMUNE PHARMA LLC

  公开号：WO2018152405A1

  公开（公告）日：2018-08-23

  A method involving the administration of a therapeutically effective amount of a leukotriene inhibitor, a pharmaceutically acceptable salt, a pharmaceutically acceptable N-oxide, a pharmaceutically active metabolite, a pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate thereof to a human for reducing a level of pro-inflammatory HDL in the human. Various examples of leukotriene inhibitors, including 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin- 3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2, 2-dimethyl-propionic acid, are disclosed for administration for the reduction of pro-inflammatory HDL in a human. Reduction of pro-inflammatory HDL by the leukotriene inhibitor may include conversion of at least a portion of pro-inflammatory HDL to anti-inflammatory HDL.

  一种方法，涉及给人类施用治疗有效量的白细胞三烯抑制剂、药物可接受的盐、药物可接受的N-氧化物、药物活性代谢物、药物可接受的的前药或其药物可接受的溶剂化物，以降低人类中的前炎症高密度脂蛋白(HDL)水平。公开了各种白细胞三烯抑制剂，包括3-[3-叔丁基硫基-1-[4-(6-乙氧基-吡啶-3-基)-苄基]-5-(5-甲基-吡啶-2-基甲氧基)-1H-吲哚-2-基]-2,2-二甲基丙酸，用于施用以降低人类中的前炎症HDL。通过白细胞三烯抑制剂降低前炎症HDL可能包括将至少部分前炎症HDL转化为抗炎症HDL。
• SUBSTITUTED INDOLO [2,3-A] QUINOLIZINES
  申请人：Waldmann Herbert

  公开号：US20120316192A1

  公开（公告）日：2012-12-13

  The present invention relates to novel substituted indolo[2,3-a]quinolizines and stereoisomeric forms thereof and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these substituted indolo[2,3-a]quinolizines together with pharmaceutically acceptable carrier, excipient and/or diluents. Said novel substituted indolo[2,3-a]quinolizines have been identified as useful for the prophylaxis and treatment of cancer by the induction of strong mitotic delays, chromosomal misalignments and mitotic tri- and multipolarization leading to cell cycle stop and apoptosis. Furthermore a synthesis for preparation of the substituted indolo[2,3-a]quinolizines is disclosed in the present invention.

  本发明涉及新型的取代吲哚[2,3-a]喹诺里嗪及其立体异构体和/或这些化合物的药用可接受盐，以及包含至少一种这些取代吲哚[2,3-a]喹诺里嗪的药物组合物，以及药用可接受的载体、辅料和/或稀释剂。所述新型取代吲哚[2,3-a]喹诺里嗪已被确认为通过诱导强烈的有丝分裂延迟、染色体错位和有丝分裂三极和/或多极化导致细胞周期停止和凋亡，用于癌症的预防和治疗的有用物质。此外，本发明还公开了取代吲哚[2,3-a]喹诺里嗪的合成方法。
• Substituted indolo [2,3-a] quinolizines in the treatment of cancer
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2532664A1

  公开（公告）日：2012-12-12

  The present invention relates to novel substituted indolo [2,3-a] quinolizines of the general formula (I) and stereoisomeric forms thereof and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these substituted indolo [2,3-a] quinolizines together with pharmaceutically acceptable carrier, excipient and/or diluents. Said novel substituted indolo [2,3-a] quinolizines have been identified as useful for the prophylaxis and treatment of cancer by the induction of strong mitotic delays, chromosomal misalignments and mitotic tri- and multipolarization leading to cell cycle stop and apoptosis. Furthermore a synthesis for preparation of the substituted indolo [2,3-a] quinolizines is disclosed in the present invention.

  本发明涉及新颖的取代吲哚[2,3-a]喹啉化合物，其一般式为(I)，以及其立体异构体和/或这些化合物的药学上可接受的盐，以及含有至少一种这些取代吲哚[2,3-a]喹啉的药物组合物，其中还包括药学上可接受的载体、赋形剂和/或稀释剂。所述的新颖取代吲哚[2,3-a]喹啉已被确定为用于预防和治疗癌症的有用药物，通过诱导强烈的有丝分裂延迟、染色体错位和有丝分裂三价和多价化导致细胞周期停滞和凋亡。此外，本发明还公开了一种用于制备取代吲哚[2,3-a]喹啉的合成方法。
• Antibacterial chiral 8-(substituted piperidino)-benzo [i,j] quinolizines, processes, compositions and methods of treatment
  申请人：WOCKHARDT RESEARCH CENTER

  公开号：US20020165227A1

  公开（公告）日：2002-11-07

  The present invention relates to optically pure 8-(substituted piperidino)-benzo[i,j]quinolizines, their isomers, derivatives, salts, pseudopolymorphs, polymorphs prodrugs and hydrates thereof, to processes for their preparation, and to pharmaceutical compositions comprising 8-(substituted piperidino)-benzo[i,j]quinolizines their isomers, derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions possess potent activity in treating local and systemic infections, particularly infections caused by sensitive and resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and nosocomial pathogens, and particularly those belonging to the staphylococcus, streptococcus and enterococcus groups. Methods for treating the diseases and disorders arising from the foregoing infections in humans and animals are described by administering the compounds of the invention to said humans and animals.

  本发明涉及光学纯的8-(取代哌啶基)-苯[i,j]喹啉，它们的异构体、衍生物、盐、伪多晶体、多晶体、前药和水合物，以及它们的制备方法和包含8-(取代哌啶基)-苯[i,j]喹啉、它们的异构体、衍生物、盐、伪多晶体、多晶体和水合物的药物组合物。这些化合物和组合物在治疗局部和全身感染方面具有强效活性，特别是对敏感和耐药革兰氏阳性菌感染、革兰氏阴性菌感染、分枝杆菌感染和医院感染病原体，特别是属于葡萄球菌、链球菌和肠球菌群的感染具有活性。通过将本发明的化合物用于人类和动物治疗上述感染引起的疾病和疾病的方法也被描述。