dansyl-D,L-Gln | 186776-25-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: dansyl-D,L-Gln
• 英文别名: Dansylglutamin；N2-{[5-(dimethylamino)-1-naphthyl]sulfonyl}-L-glutamine；N2-((5-(Dimethylamino)-1-naphthyl)sulphonyl)-L-glutamine；5-amino-2-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]-5-oxopentanoic acid
• CAS: 186776-25-0
• 化学式: C₁₇H₂₁N₃O₅S
• 分子量: 379.437
• InChiKey: AMOCBWNWZULALT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  138
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  dansyl-D,L-Gln 生成 丹磺酰-L-谷氨酰胺 、 (2R)-5-amino-2-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]-5-oxopentanoic acid
  参考文献：
  名称：

  Lehotay, Jozef; Hrobonova; Krupcik, Pharmazie, 1998, vol. 53, # 12, p. 863 - 865

  摘要：

  DOI：

文献信息

• [EN] SOLUBLE COMPLEXES OF DRUG ANALOGS AND ALBUMIN<br/>[FR] COMPLEXES SOLUBLES D'ANALOGUES DE MÉDICAMENT ET D'ALBUMINE
  申请人：FL THERAPEUTICS LLC

  公开号：WO2014121033A1

  公开（公告）日：2014-08-07

  The present invention provides novel, non-covalently bound complexes of serum albumin and analogs of poorly soluble drugs, such as camptothecin. The novel complexes are significantly more water-soluble than the camptothecin analogs and are useful as prodrug forms of the camptothecin analogs for the treatment of mammalian cell proliferative diseases, such as cancer.

  本发明提供了血清白蛋白与溶解度较差药物的类似物（如喜树碱）的新型非共价结合复合物。这些新型复合物比喜树碱类似物更易溶于水，并可用作喜树碱类似物的前药形式，用于治疗哺乳动物细胞增殖性疾病，如癌症。
• [EN] ABIRATERONE DERIVATIVES AND NON-COVALENT COMPLEXES WITH ALBUMIN<br/>[FR] DÉRIVÉS D'ABIRATÉRONE ET COMPLEXES NON COVALENTS AVEC L'ALBUMINE
  申请人：FL THERAPEUTICS LLC

  公开号：WO2015200837A1

  公开（公告）日：2015-12-30

  The present disclosure provides derivatives of abiraterone, non-covalently bound complexes of the abiraterone derivatives with serum albumin, pharmaceutical compositions of the same, and methods of use thereof. The non-covalently bound complexes are significantly more water-soluble than abiraterone and are useful for the treatment of a disease or condition that can benefit from CYP17 inhibition, such as prostate cancer.

  本公开提供了阿比特龙的衍生物，阿比特龙衍生物与血清白蛋白的非共价结合复合物，以及这些药物组合物的制备方法和使用方法。这些非共价结合复合物比阿比特龙具有更高的水溶性，可用于治疗需要CYP17抑制的疾病或病况，如前列腺癌。
• Methods and compositions for optimizing blood and tissue stability of camptothecin and other albumin-binding therapeutic compounds
  申请人：——

  公开号：US20020193318A1

  公开（公告）日：2002-12-19

  The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

  本发明提供了一种优化喜树碱药物（包括喜树碱及其相关似物，如9-氨基喜树碱和9-硝基喜树碱）的抗癌和抗HIV活性的方法和配方。该发明涉及限制人血清白蛋白介导的喜树碱的抗癌和抗HIV效应减少的方法和配方，并提供了联合治疗方法，其中通过给予竞争性药物来调节喜树碱药物与人血清白蛋白的结合。减少喜树碱药物与人血清白蛋白的结合可以导致喜树碱自由药物水平升高，从而提高涉及这些药物的治疗方案的有效性。进一步的药物，如甲氨蝶呤和AZT，也可用于使用喜树碱药物的癌症和HIV阳性患者。
• METHODS AND COMPOSITIONS FOR OPTIMIZING BLOOD AND TISSUE STABILITY OF CAMPTOTHECIN AND OTHER ALBUMIN-BINDING THERAPEUTIC COMPOUNDS
  申请人：Burke Thomas G.

  公开号：US20100240602A1

  公开（公告）日：2010-09-23

  The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent such as ibuprofen, clofibrate or clofibric acid that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

  本发明提供了一种优化喜树碱类药物（包括喜树碱及其相关类似物，如9-氨基喜树碱和9-硝基喜树碱）的抗癌和抗艾滋病活性的方法和配方。本发明涉及限制人血清白蛋白介导的喜树碱类药物抗癌和抗艾滋病效应降低的方法和配方，提供结合疗法，其中通过给予竞争性药物（如布洛芬、氯贝特或氯贝酸等）来调节喜树碱类药物与人血清白蛋白的结合。减少喜树碱类药物与人血清白蛋白的结合可以导致升高喜树碱游离药物水平，从而提高涉及这些药物的治疗方案的有效性。进一步的药物如甲氨蝶呤和AZT也可用于使用喜树碱类药物的癌症和艾滋病阳性患者。
• 3-substituted piperidine-2, 6-diones and non-covalent complexes with albumin
  申请人：Zhuhai Beihai Biotech Co., Ltd.

  公开号：US10201617B2

  公开（公告）日：2019-02-12

  The present disclosure provides derivatives of 3-substituted piperidine-2, 6-diones, non-covalently bound complexes with serum albumin, pharmaceutical compositions of the same, and methods of use thereof. The non-covalently bound complexes are significantly more water-soluble than the parent compounds, and are useful for the treatment of a cancer, such as multiple myeloma.

  本公开提供了 3-取代哌啶-2，6-二酮的衍生物、与血清白蛋白的非共价结合复合物、其药物组合物及其使用方法。非共价结合复合物的水溶性明显高于母体化合物，可用于治疗癌症，如多发性骨髓瘤。