4-N-[2-[(E)-2-(4-chlorophenyl)ethenyl]benzo[g]quinazolin-4-yl]-1-N,1-N-diethylpentane-1,4-diamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4-N-[2-[(E)-2-(4-chlorophenyl)ethenyl]benzo[g]quinazolin-4-yl]-1-N,1-N-diethylpentane-1,4-diamine
• 化学式: C₂₉H₃₃ClN₄
• 分子量: 473.0
• InChiKey: JWLITWATDRVAKE-SAPNQHFASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.6
• 重原子数：
  34
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  41
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Small molecule toll-like receptor (TLR) antagonists
  申请人：Lipford B. Grayson

  公开号：US20070232622A1

  公开（公告）日：2007-10-04

  The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

  本发明提供了用于调节通过Toll样受体信号传导的方法和组合物。该方法涉及使用一个包含至少两个环的核心结构的小分子接触TLR表达的细胞。其中某些化合物是4-主氨基喹啉。许多化合物和方法特别适用于抑制至少一个TLR9、TLR8、TLR7和TLR3的免疫刺激。该方法可能在治疗自身免疫、炎症、过敏、哮喘、移植排斥、移植物抗宿主病、感染、败血症、癌症和免疫缺陷方面有用。
• US7410975B2
  申请人：——

  公开号：US7410975B2

  公开（公告）日：2008-08-12
• [EN] COMPOSITIONS AND METHODS FOR TREATING, REDUCING, AMELIORATING, ALLEVIATING, OR PREVENTING DRY EYE<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR TRAITER, RÉDUIRE, AMÉLIORER, SOULAGER OU PRÉVENIR LA KÉRATOCONJONCTIVITE SÈCHE
  申请人：BAUSCH & LOMB

  公开号：WO2009002790A2

  公开（公告）日：2008-12-31

  [EN] Compositions and methods for treating, reducing, ameliorating, alleviating, or preventing a dry eye condition or an ophthalmologic disorder that has an etiology in inflammation comprise an antagonist to a toll-like receptor ("TLR"), a coreceptors thereof, or a combination thereof. The compositions can also include another anti¬ inflammatory medicament.
  [FR] L'invention concerne des compositions et des procédés pour traiter, réduire, améliorer, soulager ou prévenir la kératoconjonctivite sèche, ou des troubles ophtalmologiques qui ont une étiologie inflammatoire, avec un antagoniste d'un récepteur de type Toll (=TLR =), des co-récepteurs de celui-ci, ou une combinaison de ceux-ci. Les compositions peuvent également contenir un autre médicament anti-inflammatoire.
• [EN] COMPOSITIONS AND METHODS FOR TREATING OR CONTROLLING INFECTIONS AND SEQUELAE THEREOF<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR TRAITER OU CONTRÔLER DES INFECTIONS ET LES SÉQUELLES DE CELLES-CI
  申请人：BAUSCH & LOMB

  公开号：WO2009006141A2

  公开（公告）日：2009-01-08

  Compositions for treating or controlling an infection and sequelae thereof comprise an antagonist to a toll-like receptor ('TLR'), a coreceptor thereof, or a combination thereof, and an anti-infective agent. The compositions can also include another anti-inflammatory medicament.
• [EN] COMPOSITIONS COMPRISING TOLL-LIKE RECEPTOR OR CORECEPTOR ANTAGONISTS AND METHODS FOR OCULAR NEUROPROTECTION<br/>[FR] COMPOSITIONS COMPRENANT DES ANTAGONISTES DU RÉCEPTEUR OU DU CO-RÉCEPTEUR DE TYPE TOLL ET PROCÉDÉS DE NEUROPROTECTION OCULAIRE
  申请人：BAUSCH & LOMB

  公开号：WO2009089399A2

  公开（公告）日：2009-07-16

  Compositions for treating or controlling degeneration of at least a component of the human optic nerve system comprise an antagonist to a toll-like receptor, a coreceptor thereof, or a combination thereof. The compositions can also include an anti- inflammatory medicament. Such compositions can be administered to provide neuroprotection to a patient suffering from an ocular disease, such as glaucoma, AMD, DR, or retinitis pigmentosa.