3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole | 524699-72-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole
• 英文别名: ASP6537；FK881；3-methoxy-1,5-bis(4-methoxyphenyl)-1,2,4-triazole
• CAS: 524699-72-7
• 化学式: C₁₇H₁₇N₃O₃
• 分子量: 311.34
• InChiKey: OBAICMYWONZOSZ-UHFFFAOYSA-N

物化性质

• 沸点：
  490.2±55.0 °C(Predicted)
• 密度：
  1.20±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  58.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  N,N,O-trimethylisourea sulfate 以65.5的产率得到3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole
  参考文献：
  名称：

  Triazole derivatives

  摘要：

  化合物的式子（I）：其中R1是低碳基，可选地取代卤素，氰基，N,N-二（低）烷基氨基甲酰基，苯基，可选地取代卤素，或杂环基，环（低）烷基，低炔基，或N,N-二（低）烷基氨基甲酰基；R2是低碳基，低烷氧基，氰基，或1H-吡咯-1-基；R3是低碳基，低烷氧基，或氰基；X是O，S，SO或SO2；Y和Z分别是CH或N；且m为0或1；或其盐，作为药物有用。

  公开号：

  US20030191155A1

文献信息

• MICROPARTICLE OF HARDLY-SOLUBLE SUBSTANCE HAVING ENTERIC BASE MATERIAL ADSORBED ON THE SURFACE OF THE SUBSTANCE
  申请人：Astellas Pharma Inc.

  公开号：EP1923051A1

  公开（公告）日：2008-05-21

  The present invention relates to fine particles of a poorly soluble drug to provide pharmaceutical preparation having an improved absorption by improving dissolution profile of a poorly soluble drug having a poor absorbability, as well as a method for producing the same. In particular, the present invention relates to fine particles of a poorly soluble drug, having an average particle diameter of 1 nm to 1,000 nm, wherein a particular type of an enteric base material is adsorbed on the surface of the poorly soluble drug, fine particles which further comprises a saccharide, as well as a method for producing the same. It is possible to efficiently and safely produce in a short amount of time fine particles with which absorption of a poorly soluble drug that is poorly absorbed in humans, and the like can be improved, and a pharmaceutical preparation with excellent dispersion stability can be provided, by using the fine particles of the present invention having an improved dissolution profile.

  本发明涉及通过改善吸收性差的难溶性药物的溶解曲线来提供具有改善吸收性的药物制剂的难溶性药物细颗粒，以及生产这种药物制剂的方法。特别是，本发明涉及平均粒径为 1 纳米至 1,000 纳米的微粒，其中一种特定类型的肠基材料吸附在微粒表面，微粒进一步包含糖，以及生产微粒的方法。通过使用本发明的细颗粒，可以在短时间内高效、安全地生产出细颗粒，从而改善人体吸收率低的难溶性药物等的吸收，并提供分散稳定性极佳的药物制剂。
• PREVENTIVE AND/OR REMEDY FOR VASCULAR DISEASES
  申请人：Astellas Pharma Inc.

  公开号：EP2258364A1

  公开（公告）日：2010-12-08

  [Object] To provide an excellent pharmaceutical composition for preventing and/or treating vascular diseases. [Means for Solution] Useful to provide a pharmaceutical composition for preventing and/or treating vascular diseases, which comprises 1) a COX-1 selective inhibitor and 2) clopidogrel or a pharmaceutically acceptable salt thereof. The present invention is useful as an excellent pharmaceutical composition for preventing and/or treating vascular diseases is provided and is particularly useful as a pharmaceutical composition for preventing and/or treating arterial thrombosis, ischemic heart disease, ischemic brain disease, pulmonary embolism, peripheral circulation disorder, restenosis and reocclusion, essential thrombocytosis and so on is provided.

  [目的]提供一种预防和/或治疗血管疾病的优良药物组合物。 [解决手段]本发明提供一种预防和/或治疗血管疾病的药物组合物，该药物组合物包括：1）COX-1 选择性抑制剂；2）氯吡格雷或其药学上可接受的盐。本发明的用处在于提供了一种预防和/或治疗血管疾病的优良药物组合物，特别是提供了一种预防和/或治疗动脉血栓、缺血性心脏病、缺血性脑病、肺栓塞、外周循环障碍、再狭窄和再闭塞、必需性血小板增多症等疾病的药物组合物。
• SOLID DISPERSION COMPRISING TRIAZOLE COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP2581084A1

  公开（公告）日：2013-04-17

  A solid dispersion comprising a poorly soluble pharmaceutical compound, such as 3-methoxy-1,5-bis(4-methoxyphenyl)- 1H-1,2,4-triazole, which has excellent ease of handling and stability is provided. The solid dispersion comprises a polymeric carrier (for example, a polymer selected from a group consisting of polyvinylpyrrolidone and copolyvidone) and further comprising hydroxypropyl methylcellulose as desired.

  本发明提供了一种固体分散体，它包含一种溶解性较差的药物化合物，如 3-甲氧基-1,5-双（4-甲氧基苯基）-1H-1,2,4-三唑，具有极佳的易操作性和稳定性。固体分散体包括聚合物载体（例如，选自聚乙烯吡咯烷酮和共聚维酮组成的聚合物），并根据需要进一步包括羟丙基甲基纤维素。
• [EN] TREATMENT OF NEUROINFLAMMATORY DISEASE WITH SELECTIVE COX1 INHIBITORS<br/>[FR] TRAITEMENT D'UNE MALADIE NEURO-INFLAMMATOIRE PAR DES INHIBITEURS SÉLECTIFS DE COX1
  申请人：CARDEUS PHARMACEUTICALS INC

  公开号：WO2012170839A3

  公开（公告）日：2013-02-21
• TRIAZOLE DERIVATIVES AS CYCLOOXYGENASE (COX) INHIBITORS
  申请人：Astellas Pharma Inc.

  公开号：EP1442026B1

  公开（公告）日：2009-04-08