IRA-378

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: IRA-378
• 英文别名: 2-[(2S)-8-chloro-2-(trifluoromethyl)-1,2,3,4-tetrahydroquinolin-6-yl]acetic Acid
• 化学式: C₁₂H₁₁ClF₃NO₂
• 分子量: 293.673
• InChiKey: QCFOHJJGMFEJSE-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  Methyl 1,2,3,4-tetrahydro-2-trifluoromethylquinoline-6-acetate 在 sodium hydroxide 、 N-氯代丁二酰亚胺 、 氯化亚砜 作用下， 以 乙醇 、 1,2-二氯乙烷 、 N,N-二甲基甲酰胺 为溶剂， 生成 IRA-378
  参考文献：
  名称：

  Synthesis and antirheumatic activity of novel tetrahydro-6-quinolineacetic acid derivatives

  摘要：

  A study of the structural optimization of tetrahydroquinoline-6-acetic acid and the development of a novel DMARD with prompt action are detailed. (S)-(+)-8-Chloro-1,2,3,4-tetrahydro-2-trifluoromethyl-6-quinolineacetic acid (IRA-378) exhibits the: effect against both acute and chronic inflammations. It also has suppressive effects of bone destruction in adjuvant arthritis and Ca release from bones in vitro. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00262-x

文献信息

• NOVEL COMPOSITION FOR TREATING METABOLIC SYNDROME AND OTHER CONDITIONS
  申请人：Chen Chien-Hung

  公开号：US20120183600A1

  公开（公告）日：2012-07-19

  The invention relates to a composition that includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5′-monophosphate-activated protein kinase (AMPK) activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.
• US8486922B2
  申请人：——

  公开号：US8486922B2

  公开（公告）日：2013-07-16
• [EN] METHODS OF TREATING BEHAVIORIAL AND/OR MENTAL DISORDERS<br/>[FR] MÉTHODES DE TRAITEMENT DE TROUBLES COMPORTEMENTAUX ET/OU MENTAUX
  申请人：CHAU DAVID T

  公开号：WO2014176460A1

  公开（公告）日：2014-10-30

  One embodiment of an aspect of the present invention is a method for lessening the symptoms of mental and behavioral disorders including depressive disorders; bipolar disorders; anxiety disorders; obsessive-compulsive disorders; substance use disorder; trauma- and stressor-related disorders; and disruptive, impulsive-control, and conduct disorders comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of such mental and behavioral disorders. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.
• Synthesis and antirheumatic activity of novel tetrahydro-6-quinolineacetic acid derivatives
  作者：Yasushi Kohno、Katsuya Awano、Mitsutomo Miyashita、Takayoshi Ishizaki、Kazuhiko Kuriyama、Yasuhiko Sakoe、Shinji Kudoh、Koji Saito、Eisuke Kojima

  DOI：10.1016/s0960-894x(97)00262-x

  日期：1997.6

  A study of the structural optimization of tetrahydroquinoline-6-acetic acid and the development of a novel DMARD with prompt action are detailed. (S)-(+)-8-Chloro-1,2,3,4-tetrahydro-2-trifluoromethyl-6-quinolineacetic acid (IRA-378) exhibits the: effect against both acute and chronic inflammations. It also has suppressive effects of bone destruction in adjuvant arthritis and Ca release from bones in vitro. (C) 1997 Elsevier Science Ltd.