4,5-Dihydro-1-methyl-8-phenylsulfanyl-1H-thieno[3,4-g]indazole-6-carboxylic Acid Ethyl Ester | 364759-99-9

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 4,5-Dihydro-1-methyl-8-phenylsulfanyl-1H-thieno[3,4-g]indazole-6-carboxylic Acid Ethyl Ester
• 英文别名: ethyl 4,5-dihydro-1-methyl-8-phenylsulfanyl-1H-thieno[3,4-g]indazole-6-carboxylate；ethyl 1-methyl-8-phenylsulfanyl-4,5-dihydrothieno[3,4-g]indazole-6-carboxylate
• CAS: 364759-99-9
• 化学式: C₁₉H₁₈N₂O₂S₂
• 分子量: 370.496
• InChiKey: VFRPZNMYCLYHEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  97.7
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4,5-dihydro-1-methyl-8-methylsulfonyl-1H-thieno[3,4-g]indazole-6-carboxylic acid ethyl ester 在 柠檬酸 作用下， 以 四氢呋喃 为溶剂， 以41%的产率得到4,5-Dihydro-1-methyl-8-phenylsulfanyl-1H-thieno[3,4-g]indazole-6-carboxylic Acid Ethyl Ester
  参考文献：
  名称：

  Fused heterocyclic derivatives, their production and use

  摘要：

  披露了一种新型的融合噻吩衍生物，作为用于骨骼或关节疾病的预防和治疗药物，以及用于其生产的工业优势工艺和新型生产中间体。所述融合噻吩衍生物由通式(I)表示：其中R1是可选择地取代的碳氢化合物、杂环、砜基、磺酰基、羟基、硫醇或氨基；R2是氰基、甲酰基、硫代甲酰基等；环A是其中R3是氢或可选择地取代的碳氢化合物、杂环、羟基、氨基、磺酰基或酰基；R14是氢、卤素、可选择地取代的碳氢基团、可选择地取代的杂环基团等；环B代表可选择地取代的5至7成员碳氢环。

  公开号：

  US20030158245A1

文献信息

• Process for producing phospholipid-containing drug
  申请人：——

  公开号：US20030185878A1

  公开（公告）日：2003-10-02

  The present invention provides a pharmaceutical preparation which is safe, little irritate subjects and comprises a water-insoluble or hardly water-soluble drug at a high level, and a simple and convenient process for producing the preparation. A process for producing a pharmaceutical composition comprising a water-insoluble or hardly water-soluble drug coated with phospholipid, said process comprising mixing a solution containing the water-insoluble or hardly water-soluble drug and phospholipid in an organic solvent with an aqueous solvent, emulsifying the resultant mixture and removing the organic solvent from the emulsion thus obtained to form a phospholipid coating film on the surface of the water-insoluble or hardly water-soluble drug.

  本发明提供了一种制药制剂，该制剂安全、对受试者刺激小，并且包含高水平的难溶于水或几乎不溶于水的药物，以及一种简单方便的制备过程。一种制备含有磷脂质包被的难溶于水或几乎不溶于水的药物的制药组合物的方法，该方法包括将含有难溶于水或几乎不溶于水的药物和磷脂质的溶液与有机溶剂混合后与水溶液乳化，然后从所得乳液中去除有机溶剂，以在难溶于水或几乎不溶于水的药物表面形成磷脂质包被膜。
• PROCESS FOR PRODUCING PHOSPHOLIPID-CONTAINING DRUGS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1293197A1

  公开（公告）日：2003-03-19

  The present invention provides a pharmaceutical preparation which is safe, little irritate subjects and comprises a water-insoluble or hardly water-soluble drug at a high level, and a simple and convenient process for producing the preparation. A process for producing a pharmaceutical composition comprising a water-insoluble or hardly water-soluble drug coated with phospholipid, said process comprising mixing a solution containing the water-insoluble or hardly water-soluble drug and phospholipid in an organic solvent with an aqueous solvent, emulsifying the resultant mixture and removing the organic solvent from the emulsion thus obtained to form a phospholipid coating film on the surface of the water-insoluble or hardly water-soluble drug.

  本发明提供了一种安全、对受试者刺激小、含有高浓度水不溶性或难溶性药物的药物制剂，以及一种简单方便的制剂生产工艺。一种药物组合物的生产工艺，该药物组合物包括涂有磷脂的水不溶性或难溶性药物，所述工艺包括将有机溶剂中含有水不溶性或难溶性药物和磷脂的溶液与水溶剂混合，乳化所得混合物，并从所得乳液中除去有机溶剂，从而在水不溶性或难溶性药物表面形成磷脂涂膜。