(2S)-2-[[4-[(2-amino-5-formyl-4-oxo-3,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid;5-fluoro-1H-pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: (2S)-2-[[4-[(2-amino-5-formyl-4-oxo-3,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid;5-fluoro-1H-pyrimidine-2,4-dione
• 化学式: C24H26FN9O9
• 分子量: 603.5
• InChiKey: YKHQLXZSQLTWDY-ZEDZUCNESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.53
• 重原子数：
  43
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  274
• 氢给体数：
  9
• 氢受体数：
  12

文献信息

• [EN] SOLID FORMS OF 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, AND THEIR PHARMACEUTICAL COMPOSITIONS AND USES<br/>[FR] FORMES SOLIDES DE 3-(5-AMINO-2-MÉTHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPÉRIDINE-2,6-DIONE, LEURS COMPOSITIONS PHARMACEUTIQUES ET LEURS UTILISATIONS
  申请人：CELGENE CORP

  公开号：WO2018165142A1

  公开（公告）日：2018-09-13

  Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)- piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.

  本发明揭示了包含3-(5-氨基-2-甲基-4-氧代-4H-喹唑啉-3-基)-哌啶-2,6-二酮的固态形式，包含这些固态形式的组合物，制备这些固态形式的方法以及它们的使用方法。
• COMBINATION OF AN IMMUNOSUPPRESSIVE AGENT AND NONSTEROIDAL ANTI -INFLAMMATORY DRUGS TO TREAT DISEASE
  申请人：Wolfe M. Michael

  公开号：US20090291883A1

  公开（公告）日：2009-11-26

  The present invention provides methods and compositions for the treatment and prevention of neoplasia by administering an effective amount of a NSAID in combination with an effective amount of an immunosuppressant agent. In particular, the present invention provides methods and compositions for the treatment and prevention of neoplasia by administering an effective amount of COX-2 inhibitor in combination with an effective amount of an immunosuppressant agent.

  本发明提供了一种方法和组合物，通过给予有效量的NSAID与有效量的免疫抑制剂来治疗和预防肿瘤。特别地，本发明提供了一种方法和组合物，通过给予有效量的COX-2抑制剂与有效量的免疫抑制剂来治疗和预防肿瘤。
• Combination therapy with anti-gastrin G17 antibodies for the treatment of tumors
  申请人：APHTON CORPORATION

  公开号：EP1579863A2

  公开（公告）日：2005-09-28

  Gastrin-dependent tumors, e.g. in colorectal adenocarcinoma, are treated by combination therapy. The combination of: (i) an antibodies to gastrin G17; and (ii) one or more chemotherapeutic agents, e.g. 5-fluorouracil and leucovorin, is suitable for this purpose.

  胃泌素依赖性肿瘤，如结直肠腺癌，可通过联合疗法进行治疗。联合疗法包括： (i) 一种胃泌素 G17 抗体；和 (ii) 一种或多种化疗药物，如 5-氟尿嘧啶和亮菌甲素。
• Compositions and uses of galectin antagonists
  申请人：Prospect Therapeutics, Inc.

  公开号：EP1980257A1

  公开（公告）日：2008-10-15

  The present invention is directed to methods and compositions for augmenting treatment of cancers and other proliferative disorders. In particular embodiments, the invention combines the administration of an agent that inhibits the anti-apoptotic activity of galectin-3 (e.g., a "galectin-3 inhibitor") so as to potentiate the toxicity of a chemotherapeutic agent. In certain preferred embodiments, the conjoint therapies of the present invention can be used to improve the efficacy of those chemotherapeutic agents whose cytotoxicity is influenced by the status of an anti-apoptotic Bcl-2 protein for the treated cell. For instance, galectin-3 inhibitors can be administered in combination with a chemotherapeutic agent that interferes with DNA replication fidelity or cell-cycle progression of cells undergoing unwanted proliferation.

  本发明涉及增强癌症和其他增殖性疾病治疗的方法和组合物。在特定的实施方案中，本发明结合施用抑制galectin-3抗凋亡活性的制剂（如 "galectin-3抑制剂"），从而增强化疗药物的毒性。在某些优选的实施方案中，本发明的联合疗法可用于提高那些细胞毒性受治疗细胞抗凋亡 Bcl-2 蛋白状态影响的化疗药物的疗效。例如，galectin-3抑制剂可与干扰细胞DNA复制保真度或细胞周期进展的化疗药物联合使用。
• Methods and compositions for using suramin, pentosan, polysulfate, telomerase antisense and telomerase inhibitors
  申请人：Au L.-S. Jessie

  公开号：US20050282893A1

  公开（公告）日：2005-12-22

  The invention provides methods and compositions for inhibiting telomerase activity and treatment of telomerase mediated conditions or diseases. The methods, compounds, and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents, surgery, or radiation in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer.

  本发明提供了抑制端粒酶活性和治疗端粒酶介导的病症或疾病的方法和组合物。本发明的方法、化合物和组合物可单独使用，也可与其他药理活性制剂、手术或辐射结合使用，用于治疗端粒酶活性介导的病症或疾病，如治疗癌症。