NSC-305884 | 79152-85-5

• 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: NSC-305884
• 英文别名: N-methyl-N-[4-(7-methyl-1H-imidazo[4,5-f]quinolin-9-ylamino)-phenyl]-acetamide；acodazole；acodazole hydrochloride；N-methyl-N-[4-[(7-methyl-3H-imidazo[4,5-f]quinolin-9-yl)amino]phenyl]acetamide
• CAS: 79152-85-5
• 化学式: C₂₀H₁₉N₅O
• 分子量: 345.404
• InChiKey: XJXLRNPVSQADMZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  73.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] PHENOXY-PYRIDYL-PYRIMIDINE COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS PHÉNOXY-PYRIDYL-PYRIMIDINE ET MÉTHODES D'UTILISATION ASSOCIÉES
  申请人：GENENTECH INC

  公开号：WO2020056089A1

  公开（公告）日：2020-03-19

  Described herein are phenoxy-pyridyl -pyrimidine compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I structure or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

  本文描述了具有肌醇需要酶1（IRE1）调节活性或功能的苯氧基吡啶基嘧啶化合物，其具有Formula I结构或立体异构体、互变异构体或其药用可接受的盐，并具有所述的取代基和结构特征。还描述了包括Formula I化合物的药物组合物和药物，以及使用这种IRE1调节剂的方法，单独或与其他治疗剂联合使用，用于治疗通过雌激素受体介导或依赖的疾病或症状。
• Immunosuppressive effects of pteridine derivatives
  申请人：——

  公开号：US20040077859A1

  公开（公告）日：2004-04-22

  This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

  这项发明涉及一组三取代和四取代的嘌呤衍生物，它们的药用盐、N-氧化物、溶剂化物、二氢和四氢衍生物及对映异构体，具有意想不到的、令人满意的药理性质，尤其是作为高度活性的免疫抑制剂，因此可用于治疗移植排斥反应和/或治疗某些炎症性疾病。这些化合物还用于预防或治疗心血管疾病、过敏性疾病、中枢神经系统疾病和细胞增殖紊乱。
• [EN] TRIOXOLANE AGENTS<br/>[FR] AGENTS TRIOXOLANE
  申请人：UNIV CALIFORNIA

  公开号：WO2019005977A1

  公开（公告）日：2019-01-03

  Disclosed herein, inter alia, are trioxolane compounds and methods of using the same for treatment and detection of diseases.

  本文披露了三氧杂环戊烷化合物及其在治疗和检测疾病中的应用方法。
• COATING FOR A MEDICAL DEVICE HAVING AN ANTI-THROMBOTIC CONJUGATE
  申请人：Zhao Jonathon Z.

  公开号：US20080200421A1

  公开（公告）日：2008-08-21

  A conjugate between an anti-thrombotic agent and a bioabsorbable polymer is provided. In addition, a method is provided for applying a coating comprising an anti-thrombotic agent and a bioabsorbable polymer conjugate to at least a portion of an implantable device to prevent or reduce the formation of thrombosis on the surface of the device. A first or sub-layer of the coating is prepared by mixing a polymeric material and a biologically active agent with a solvent, thereby forming a homogeneous solution. A second or outer layer comprises an anti-thrombotic heparin-bioabsorbable polymer conjugate. This coating may be applied over the inner drug-containing layers using, for example, a dip coating or spray coating process. After drying, the anti-thrombotic heparin bioabsorbable polymer conjugate remains in the outer layer of the coating, allowing agent from the inner layer to be eluted there through. In addition, the outmost layer prevents the formation of thrombosis, and also serves to modulate the release kinetics of the agent(s) contained within an inner layer(s) of the coating.

  提供了一种抗血栓药物与可生物吸收聚合物的共轭物。此外，提供了一种方法，用于将包含抗血栓药物和可生物吸收聚合物共轭物的涂层应用于可植入设备的至少部分表面，以预防或减少设备表面的血栓形成。涂层的第一或次表层通过将聚合物材料和生物活性剂与溶剂混合制备而成，从而形成均匀溶液。第二或外层包括抗血栓肝素-可生物吸收聚合物共轭物。该涂层可以通过浸涂或喷涂工艺覆盖在内部含药层上。干燥后，抗血栓肝素可生物吸收聚合物共轭物保留在涂层的外层，使内层的药物能够通过其释放。此外，最外层防止了血栓形成，并且还用于调节涂层内部层中所含药物的释放动力学。
• [EN] SUBSTITUTED CYCLOLAKYLS AS MODULATORS OF THE INTEGRATED STRESS PATHWAY<br/>[FR] CYCLOLALKYLES SUBSTITUÉS EN TANT QUE MODULATEURS DE LA VOIE DE STRESS INTÉGRÉE
  申请人：CALICO LIFE SCIENCES LLC

  公开号：WO2020223536A1

  公开（公告）日：2020-11-05

  Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.

  本文提供了用于调节综合应激反应（ISR）并治疗相关疾病、疾病和症状的化合物、组合物和方法。