5-[3-(dimethylamino)propylamino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4-dione

• 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: 5-[3-(dimethylamino)propylamino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4-dione
• 化学式: C₁₈H₂₃N₅O₂
• 分子量: 341.4
• InChiKey: LNRUPMPQQGPSQT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  68.2
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• PROGNOSTIC BIOMARKER FOR CANCER
  申请人：Universitat Autònoma de Barcelona

  公开号：EP3231875A1

  公开（公告）日：2017-10-18

  The invention relates to an in vitro method for determining the prognosis of a patient suffering from cancer, wherein the cancer is not hepatocarcinoma, based on CDK5RAP3 gene expression levels. The invention also relates to in vitro methods for predicting the clinical response of a patient suffering from cancer to a treatment with a DNA damaging agent, or for selecting a patient suffering from cancer for a therapy with a DNA damaging agent or for selecting a therapy for a patient suffering from cancer.

  本发明涉及一种根据CDK5RAP3基因表达水平确定癌症患者预后的体外方法，其中癌症不是肝癌。本发明还涉及一种体外方法，用于预测癌症患者对 DNA 损伤剂治疗的临床反应，或用于选择癌症患者接受 DNA 损伤剂治疗，或用于选择癌症患者的治疗方法。
• METHOD FOR REMOVING SENESCENT CELL, AND METHOD FOR PREPARING SENESCENT CELL
  申请人：The University of Tokyo

  公开号：EP3878470A1

  公开（公告）日：2021-09-15

  Solutions to the problem of the invention are a method for selectively killing or removing a senescent cell, substance identification, and a method for purifying a senescent cell. Specifically, the invention includes an agent for removing a senescent cell, which is a drug for removing an in vivo senescent cell, the agent containing an inhibitor for glutaminase as an active ingredient, and a pharmaceutical composition containing the agent. The invention further includes a method for preparing a senescent cell, including the following steps (a) to (c): (a) synchronizing a cell with the G2 phase; (b) activating an intracellular p53 protein in the cell synchronized with the G2 phase; and (c) inhibiting polo-like kinase 1 (PLK1) activity in the cell treated in the step (b).

  解决本发明问题的方法是一种选择性杀死或清除衰老细胞的方法、物质鉴定和纯化衰老细胞的方法。具体来说，本发明包括一种去除衰老细胞的药剂，它是一种去除体内衰老细胞的药物，该药剂含有谷氨酰胺酶抑制剂作为活性成分，以及含有该药剂的药物组合物。本发明还包括一种制备衰老细胞的方法，包括以下步骤(a)至(c)：(a)使细胞同步进入 G2 期；(b)在同步进入 G2 期的细胞中激活细胞内 p53 蛋白；(c)抑制在步骤(b)中处理过的细胞中多聚样激酶 1 (PLK1) 的活性。
• DRUG COMBINATIONS TO TREAT HYPERPROLIFERATIVE DISORDERS
  申请人：Maurer Barry James

  公开号：US20100035911A1

  公开（公告）日：2010-02-11

  A method of treating a hyperproliferative disorder, including a cancer, in a subject in need of such treatment, comprising administering to said subject a pharmaceutical combination containing a treatment effective amount of: (a) a vitamin A derivative (i.e., a retinoid), or a pharmaceutically acceptable salt thereof, and an inhibitor of microtubule structure or function; or (b) a combination containing fenretinide (i.e., N-(4-hydrophenyl) retinamide, 4-HPR) and ABT-751 (i.e., N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide). Vitamin A derivatives that may be useful for this invention according to (a) include, but are not limited to, all-trans-retinoic acid, 13-cis-retinoic acid, and fenretinide. Microtubule inhibitors that may be useful for this invention according to (a) include, but are not limited to, inhibitors of the Vinca binding domain (e.g., vincristine, vinblastine, vinorelbine, and cryptophycin 52), inhibitors of the Taxane domain (e.g., paclitaxel, docetaxel, and epothilones), and inhibitors of the colchicine site (e.g., colchicine, ABT-751, CI-980, and combretastatin). A preferred retinoid according to (a) is fenretinide. A preferred microtubule inhibitor according to (b) is ABT-751.
• HIGHLY SOLUBLE PYRIMIDO-DIONE-QUINOLINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
  申请人：Weissman Allan

  公开号：US20100056549A1

  公开（公告）日：2010-03-04

  The present invention features pyrimido-dione-quinoline compounds having improved solubility, pharmaceutical compositions of substituted pyrimido-dione-quinoline compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more pyrimido-dione-quinoline compounds of the invention.
• COMPOSITIONS AND METHODS FOR TREATING SENESCENCE-ASSOCIATED DISEASES AND DISORDERS
  申请人：Unity Biotechnology, Inc.

  公开号：US20180193458A1

  公开（公告）日：2018-07-12

  Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders. Also included herein are methods for extending lifespan.