T-900607 | 261944-52-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: T-900607
• 英文别名: T607；N-[3-[(aminocarbonyl)amino]-4-methoxyphenyl]-2,3,4,5,6-pentafluorobenzenesulfonamide；Unii-IC9O2HT1X1；[2-methoxy-5-[(2,3,4,5,6-pentafluorophenyl)sulfonylamino]phenyl]urea
• CAS: 261944-52-9
• 化学式: C₁₄H₁₀F₅N₃O₄S
• 分子量: 411.309
• InChiKey: FSXLOWIFSZNIMV-UHFFFAOYSA-N

物化性质

• 密度：
  1.686±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  119
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  以92的产率得到T-900607
  参考文献：
  名称：

  Arylsulfonanilide ureas

  摘要：

  本发明提供了与新型芳基磺酰苯胺衍生物相关的化合物、组合物和方法，并将其用作药理活性剂。这些组合物在治疗疾病状态，特别是癌症、银屑病、血管再狭窄、感染、动脉粥样硬化和高胆固醇血症方面，具有特殊的药理作用，或作为开发这些药物的先导化合物。

  公开号：

  US06214880B1

文献信息

• Stabilized oral pharmaceutical composition
  申请人：——

  公开号：US20030105144A1

  公开（公告）日：2003-06-05

  An orally deliverable pharmaceutical composition is provided comprising an aminosulfonyl-comprising drug, for example a selective cyclooxygenase-2 inhibitory drug such as celecoxib, and a solvent liquid comprising a polyethylene glycol and one or more free radical-scavenging antioxidants. At least a substantial part of the drug is in dissolved form in the solvent liquid. The composition has rapid-onset properties and is useful in treatment of cyclooxygenase-2 mediated conditions and disorders.

  一种可口服给药的药物组合物由含氨磺酰的药物（例如塞来昔布等选择性环氧化酶-2抑制剂）和含聚乙二醇及一种或多种自由基清除抗氧化剂的溶剂液组成。至少有相当一部分药物以溶解形式存在于溶剂液中。该组合物具有快速起效的特性，可用于治疗环氧化酶-2 介导的病症和紊乱。
• Oral dosage form of a sulfonamide prodrug
  申请人：——

  公开号：US20030100595A1

  公开（公告）日：2003-05-29

  A pharmaceutical composition that is substantially free of water comprises at least one orally deliverable dosage unit comprising a therapeutically effective amount of a sulfonamide prodrug and, where the prodrug is readily degradable ex vivo, has means to inhibit such degradation prior to oral administration. Illustratively the prodrug is parecoxib or a water-soluble salt thereof, and the composition has means to inhibit conversion of the parecoxib to valdecoxib. A method of treating or preventing a COX-2 mediated disorder in a subject comprises (a) dissolving at least one dosage unit of such a composition in a pharmaceutically acceptable aqueous vehicle to form a solution, and (b) orally administering the solution to the subject before substantial precipitation of insoluble matter occurs in the solution.

  一种基本上不含水的药物组合物包含至少一个口服给药剂量单位，其中含有治疗有效量的磺胺原药，如果原药在体内外容易降解，则在口服给药前具有抑制这种降解的方法。举例来说，原药是帕瑞昔布或其水溶性盐，组合物具有抑制帕瑞昔布转化为缬癸昔布的方法。一种治疗或预防受试者 COX-2 介导的疾病的方法包括：(a)将至少一个剂量单位的这种组合物溶解在药学上可接受的水性载体中以形成溶液，和(b)在溶液中出现大量不溶物沉淀之前将溶液口服给受试者。
• Medical devices to treat or inhibit restenosis
  申请人：Hezi-Yamit Ayala

  公开号：US20050154455A1

  公开（公告）日：2005-07-14

  Implantable medical devices having anti-restenotic coatings are disclosed. Specifically, implantable medical devices having coatings of certain antiproliferative agents, particularly a certain beta-tubulin inhibitor, are disclosed. The anti-restenotic beta-tubulin inhibitor is T-900607, and pharmaceutically acceptable derivatives thereof. The anti-restenotic medical devices include stents, catheters, micro-particles, probes and vascular grafts. Intravascular stents are preferred medical devices. The medical devices can be coated using any method known in the art including compounding the beta-tubulin inhibitor with a biocompatible polymer prior to applying the coating. Moreover, medical devices composed entirely of biocompatible polymer-beta-tubulin inhibitor blends are disclosed. Additionally, medical devices having a coating comprising at least one beta-tubulin inhibitor in combination with at least one additional therapeutic agent are also disclosed. Furthermore, related methods of using and making the anti-restenotic implantable devices are also disclosed.

  本研究公开了具有抗血管狭窄涂层的植入式医疗器械。具体来说，本发明公开了具有某些抗增殖剂涂层的可植入医疗器械，特别是某种β-微管蛋白抑制剂。抗再狭窄的β-微管蛋白抑制剂是 T-900607 及其药学上可接受的衍生物。抗血管再狭窄的医疗器械包括支架、导管、微颗粒、探针和血管移植物。血管内支架是首选的医疗器械。这些医疗器械可采用本领域已知的任何方法进行涂层，包括在涂覆前将β-微管蛋白抑制剂与生物相容性聚合物复合。此外，还公开了完全由生物相容性聚合物-β-微管蛋白抑制剂混合物组成的医疗器械。此外，还公开了具有包含至少一种β-微管蛋白抑制剂的涂层和至少一种额外治疗剂的医疗器械。此外，还公开了使用和制造抗血管狭窄植入装置的相关方法。
• Combination therapy comprising a Cox-2 inhibitor and an antineoplastic agent
  申请人：Masferrer L. Jaime

  公开号：US20050227929A1

  公开（公告）日：2005-10-13

  A method for treating or preventing neoplasia or a neoplasia-related disorder in a subject is provided, the method comprising administering to the subject an effective amount of a combination comprising a Cox-2 inhibitor and an antineoplastic agent.

  提供了一种治疗或预防受试者肿瘤或肿瘤相关疾病的方法，该方法包括向受试者施用有效量的包含 Cox-2 抑制剂和抗肿瘤药的组合物。
• ORALLY DELIVERABLE PHARMACEUTICAL COMPOSITION COMPRISING AN ACTIVE COMPOUND HAVING AN AMINOSULFONYL GROUP (COX-2 INHIBITOR), A POLYETHYLENE GLYCOL AND A FREE-RADICAL SCAVENGING ANTIOXIDANT
  申请人：Pharmacia Corporation

  公开号：EP1494666A1

  公开（公告）日：2005-01-12