磷雷夫康唑 | 351227-64-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 磷雷夫康唑
• 英文名称: 4-[2-[(1R,2R)-2-(2,4-difluorophenyl)-1-methyl-2-[(phosphonooxy)methoxy]-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazol]benzonitrile
• 英文别名: fosravuconazole；[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1,2,4-triazol-1-yl)butan-2-yl]oxymethyl dihydrogen phosphate；E1224
• CAS: 351227-64-0
• 化学式: C₂₃H₂₀F₂N₅O₅PS
• 分子量: 547.479
• InChiKey: SYTNEMZCCLUTNX-NPMXOYFQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  37
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  172
• 氢给体数：
  2
• 氢受体数：
  12

反应信息

• 作为反应物：
  描述：

  磷雷夫康唑 在 L-赖氨酸 作用下， 以 甲醇 为溶剂， 反应 4.5h， 生成 (2R,3R)-3-(4-(4-cyanophenyl)-thiazol-2-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-((dihydrogenphosphonoxy)methoxy)butane, bis-L-lysine salt
  参考文献：
  名称：

  WO2006/118351

  摘要：

  公开号：
• 作为产物：
  描述：

  (2R,3R)-3-(4-(4-cyanophenyl)-thiazol-2-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-((di-tert-butylphosphonpxy)-methoxy)-butane 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 生成 磷雷夫康唑
  参考文献：
  名称：

  WO2006/118351

  摘要：

  公开号：

文献信息

• COMPOSITION CONTAINING STABILITY-IMPROVED CHLOROMETHYL PHOSPHATE DERIVATIVE AND PROCESS FOR PRODUCING SAME
  申请人：Sato Keizo

  公开号：US20100094001A1

  公开（公告）日：2010-04-15

  The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine, (wherein R1 and R2 are identical or different from each other, and represent a C1-C6 alkyl group, a C2-C6 alkenyl group or a C6-C14 aryl C1-C6 alkyl group which may have a substituent, and R1 and R2 may together form a ring), the process comprising the step of adding the tertiary amine having a boiling point at 1 atmosphere of 150° C. or higher to the compound represented by formula (I).

  本发明提供了一种用于制备氯甲基磷酸酯衍生物的工艺或类似工艺，该工艺用于制备水溶性前药，从操作性、可操作性和节能性等角度来看都非常优秀。根据本发明，提供了一种制备含有化合物(I)和三级胺的组合物的工艺，其中化合物(I)的结构式如下：（其中R1和R2相同或不同，分别代表C1-C6烷基，C2-C6烯基或C6-C14芳基C1-C6烷基，其上可能带有取代基，且R1和R2可以形成环），该工艺包括将具有1大气压下沸点高于150℃的三级胺加入化合物(I)的步骤。
• STABILIZED PHARMACEUTICAL COMPOSITION
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP1987830A1

  公开（公告）日：2008-11-05

  It is an object of the present invention to provide a pharmaceutical composition containing a stable azole-based compound, which is useful as an antifungal agent. According to the present invention, the above-mentioned object can be achieved by adding magnesium hydroxide carbonate, triethylamine, arginine, or another such basic substance to an azole-based compound that is unstable in acids. The above-mentioned pharmaceutical composition is stable enough that the compound will not degrade if the temperature, humidity, or other such conditions should change during production or storage. Also, this composition is useful as a therapeutic agent for deep mycoses because systemic administration is possible by applying it to an oral agent or an injection.

  本发明的目的是提供一种含有稳定的唑基化合物的药物组合物，它可用作抗真菌剂。根据本发明，上述目的可以通过向在酸中不稳定的唑基化合物中添加氢氧化镁碳酸盐、三乙胺、精氨酸或其他此类碱性物质来实现。上述药物组合物足够稳定，即使在生产或储存过程中温度、湿度或其他条件发生变化，化合物也不会降解。此外，这种组合物还可作为深部真菌病的治疗剂，因为通过将其应用于口服药物或注射剂，可以实现全身给药。
• COMBINED PHARMACEUTICAL COMPOSITION AS ANTIFUNGAL AGENT
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP2636409A1

  公开（公告）日：2013-09-11

  An object of the present invention is to provide a pharmaceutical composition having superior antifungal activity. The present invention provides a pharmaceutical composition comprising 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-ylamine or 2-amino-1-((phosphonooxy)methyl)-3-(3((4-((2-pyridinyloxy)methyl)phenyl)methyl)-5-isoxazolyl)-pyridinium or a salt thereof in combination with an antifungal agent.

  本发明的目的是提供一种具有优异抗真菌活性的药物组合物。本发明提供了一种药物组合物，包括 3-(3-(4-(吡啶-2-基氧基甲基)-苄基)-异恶唑-5-基)-吡啶-2-胺或 2-氨基-1-((磷酰氧基)甲基)-3-(3((4-((2-吡啶基氧基)甲基)苯基)甲基)-5-异恶唑基)-吡啶鎓或其盐与抗真菌剂的组合物。
• ENCAPSULATED FORMULATION
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP2839835A1

  公开（公告）日：2015-02-25

  An object of the present invention is to provide a capsule formulation comprising a phosphonooxymethyl derivative of ravuconazole which suppresses delay in dissolution due to storage regardless of an encapsulated amount of the phosphonooxymethyl derivative of ravuconazole. The present invention provides a capsule formulation comprising an encapsulated material comprising [(1R,2R)-2-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-1-(2,4-difluorophenyl)-1-(1H-1,2,4-tria zol-1-ylmethyl)propyl]oxy}methyl dihydrogen phosphate or a pharmacologically acceptable salt thereof, or a solvate of any of the foregoing, and a capsule shell not comprising gelatin.

  本发明的目的是提供一种胶囊制剂，该制剂包含一种雷公唑的膦酰氧甲基衍生物，无论雷公唑的膦酰氧甲基衍生物的封装量如何，该制剂都能抑制因储存而导致的溶解延迟。本发明提供了一种胶囊制剂，其包封材料包括[(1R,2R)-2-[4-(4-氰基苯基)-1,3-噻唑-2-基]-1-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基甲基)丙基]氧基}甲基磷酸二氢盐或其药理学上可接受的盐，或上述任何物质的溶液，以及不包括明胶的胶囊壳。
• Dosing regimens for the treatment of fungal infections
  申请人：Seren Pharmaceuticals Inc.

  公开号：US11324728B2

  公开（公告）日：2022-05-10

  Described herein are dosing regimens for the treatment of fungal infections such as onychomycosis using ravuconazole or a salt, solvate or prodrug thereof.

  本文描述了使用雷康唑或其盐、溶液剂或原药治疗真菌感染（如甲真菌病）的给药方案。