达格吡酮 | 14166-26-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 中文名称: 达格吡酮
• 中文别名: 他各酰胺；氧哌冰胺；他谷酿胺
• 英文名称: 2-(2,6-dioxo-piperidin-3-yl)-hexahydro-4,7-methano-isoindole-1,3-dione
• 英文别名: taglutimide；4-(2,6-dioxopiperidin-3-yl)-4-azatricyclo[5.2.1.02,6]decane-3,5-dione
• CAS: 14166-26-8
• 化学式: C₁₄H₁₆N₂O₄
• 分子量: 276.292
• InChiKey: URPJPYAYMWPUPR-UHFFFAOYSA-N

物化性质

• 熔点：
  234-236℃
• 沸点：
  553.3±43.0 °C(Predicted)
• 密度：
  1.434

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  83.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Compositions and methods to effect the release profile in the transdermal administration of active agents
  申请人：——

  公开号：US20020004065A1

  公开（公告）日：2002-01-10

  Compositions and methods for the transdermal delivery of active agents up to a period of seven days or more at substantially a zero-order release rate comprising a pharmaceutically acceptable adhesive matrix and a polymeric plastic material that provides a release rate regulating effect on the active agents.

  本发明涉及一种用于经皮递送活性药剂的组合物和方法，该组合物和方法能够在持续时间为七天或更长时间内以几乎零阶释放速率递送活性药剂，包括一种药学上可接受的粘合基质和一种聚合物塑料材料，该聚合物塑料材料对活性药剂具有释放速率调节作用。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Compositions for the treatment of cancer comprising a topoisomerase inhibitor and thalidomide
  申请人：CELGENE CORPORATION

  公开号：EP1676577A1

  公开（公告）日：2006-07-05

  This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment orprevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.

  本发明涉及由沙利度胺和另一种可用于治疗或预防癌症的抗癌药物组成的组合物。首选的抗癌药物是拓扑异构酶抑制剂。一种特殊的组合物包含沙利度胺或其药学上可接受的盐、溶液或凝胶，以及伊立替康。本发明还涉及治疗或预防癌症的方法，其中包括向需要这种治疗或预防的病人施用沙利度胺和另一种抗癌药物。本发明还涉及减少或避免与化疗或放疗相关的不良副作用的方法，其中包括向需要减少或避免不良副作用的患者施用沙利度胺。