1H-噻吩并[2,3-g]吲唑 | 27212-61-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 中文名称: 1H-噻吩并[2,3-g]吲唑
• 英文名称: 1H-thieno[2,3-g]indazole
• 英文别名: 2-H-Thieno<2,3-g>indazol；1(2)H-thieno[2,3-g]indazole
• CAS: 27212-61-9
• 化学式: C₉H₆N₂S
• 分子量: 174.226
• InChiKey: VSOXSBKNAHNHNR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  56.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (R)-(+)-环氧丙烷 、 1H-噻吩并[2,3-g]吲唑 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以15%的产率得到(2R)-1-(1H-thieno[2,3-g]indazol-1-yl)propan-2-ol
  参考文献：
  名称：

  一系列取代的2-（1H-呋喃[2,3-g]吲唑-1-基）乙胺衍生物作为5-HT2C受体激动剂的合成及构效关系。

  摘要：

  合成了一系列新颖的吲唑衍生物，并检查了它们的结构-活性关系，以鉴定有效的和选择性的5-HT 2C受体激动剂。在这些化合物中，（S）-2-（7-乙基-1H-呋喃[2,3-g]吲唑-1-基）-1-甲基乙胺（YM348）具有良好的体外特性，即高激动性对人5-HT2C受体亚型的活性（EC50 = 1.0 nM）和对5-HT2A受体的高选择性。口服给予该化合物在大鼠阴茎勃起模型中也有效

  DOI：

  10.1016/j.bmc.2007.10.100
• 作为产物：
  描述：

  4,5-dihydro-1H-thieno[2,3-g]indazole 在 2,3-二氯-5,6-二氰基-1,4-苯醌 作用下， 以 1,4-二氧六环 为溶剂， 以78%的产率得到1H-噻吩并[2,3-g]吲唑
  参考文献：
  名称：

  一系列取代的2-（1H-呋喃[2,3-g]吲唑-1-基）乙胺衍生物作为5-HT2C受体激动剂的合成及构效关系。

  摘要：

  合成了一系列新颖的吲唑衍生物，并检查了它们的结构-活性关系，以鉴定有效的和选择性的5-HT 2C受体激动剂。在这些化合物中，（S）-2-（7-乙基-1H-呋喃[2,3-g]吲唑-1-基）-1-甲基乙胺（YM348）具有良好的体外特性，即高激动性对人5-HT2C受体亚型的活性（EC50 = 1.0 nM）和对5-HT2A受体的高选择性。口服给予该化合物在大鼠阴茎勃起模型中也有效

  DOI：

  10.1016/j.bmc.2007.10.100

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。
• PROCESS FOR PRODUCING DRUG ULTRAMICROPARTICLE AND APPARATUS THEREFOR
  申请人：Eisai Co., Ltd.

  公开号：EP1652515A1

  公开（公告）日：2006-05-03

  The present invention provides fine drug particles with submicron sizes excellent in long-term dispersibility. Specifically, it provides a method for producing ultrafine drug particles having an average particle size of 10 nm to 1000 nm, by 1) dissolving a drug in a good solvent or a mixture of good solvents to prepare a drug-containing solution; 2) mixing the drug-containing solution with a solvent being a poor solvent or a mixture of poor solvents for the drug and being miscible with the drug-containing solution in the good solvent or a mixture of good solvents; and 3) subjecting the prepared mixture directly to emulsification under a set processing pressure using a high-pressure homogenizer without carrying out a pretreatment step for adjusting the drug to have an average particle size of 100 µm or less, and an apparatus for producing the particles.

  本发明提供长期分散性极佳的亚微米级精细药物颗粒。具体地说，本发明提供了一种生产平均粒径为 10 纳米至 1000 纳米的超细药物颗粒的方法，具体方法是：1）将药物溶解在良好溶剂或良好溶剂的混合物中，制备含药溶液；2）将含药溶液与药物的劣溶剂或劣溶剂的混合物混合，并在良好溶剂或良好溶剂的混合物中与含药溶液混溶；3) 使用高压匀浆器在设定的加工压力下直接对制备好的混合物进行乳化，而不进行预处理步骤，以调整药物的平均粒径为 100 微米或更小，以及生产颗粒的设备。
• MEDICINAL COMPOSITION AND PROCESS FOR PRODUCING THE SAME
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP1834624A1

  公开（公告）日：2007-09-19

  A production process which comprises (1) a step in which a raw liquid containing a drug is prepared so that the drug is contained in an amount which exceeds the saturation amount thereof as determined at the temperature to be used in a treatment with a high-pressure homogenizer and is less than the amount which is larger than that drug saturation amount by 1 g per 100 mL of a solvent and that the raw liquid contains substantially no surface modifiers; and (2) a step in which the raw liquid is treated with a high-pressure homogenizer at a pressure of 15-300 MPa while regulating the temperature of the raw liquid so as to exceed the solidifying point of the liquid and be lower than the boiling point thereof. By the process, fine solid particles of a drug and a medicinal composition containing the fine solid drug particles can be obtained.

  一种生产工艺，它包括：(1) 第一步，制备含有药物的原液，使药物含量超过在高压匀浆器处理温度下测定的饱和量，且小于每 100 mL 溶剂中大于药物饱和量 1 g 的量，且原液基本上不含表面改性剂；(2) 在此步骤中，使用压力为 15-300 兆帕的高压匀浆器处理原液，同时调节原液的温度，使其超过液体的凝固点并低于其沸点。通过该工艺，可获得细小的固体药物颗粒和含有细小固体药物颗粒的药物组合物。
• QUICK DISINTEGRATION TABLET AND METHOD OF PRODUCING THE SAME
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP1839650A1

  公开（公告）日：2007-10-03

  To provide a production method of a rapidly disintegrating tablet, the method that has versatility and, without a specialized device, can efficiently produce rapidly disintegrating tablets having a desired rapid disintegration property and sufficient strength. And also to provide such rapidly disintegrating tablets produced by the method, the tablets that can be easily swallowed by people such as the elderly, children and patients having a poor swallowing capability and that have sufficient strength, so that they can endure breakage and abrasion in processes such as distribution and storage and dispensing processes by tablet packing machines. The method of such rapidly disintegrating tablet includes: (1) mixing an active ingredient, an acrylic copolymer and at least a pharmaceutically acceptable additive to obtain a mixture thereof (2) tableting the mixture to obtain a compact, and (3) isothermally heating the compact at a temperature of 50°C to 100°C for a given period of time. And also to provide such rapidly disintegrating tablets produced by the production method of a rapidly disintegrating tablet.

  提供一种快速崩解片剂的生产方法，该方法具有多功能性，无需专用设备即可高效生产出具有所需快速崩解特性和足够强度的快速崩解片剂。同时，提供用该方法生产的快速崩解片剂，这些片剂易于被老人、儿童和吞咽能力差的病人等人群吞咽，并具有足够的强度，使其能够在片剂包装机的分发、储存和分装等过程中经受破损和磨损。这种快速崩解片剂的方法包括(1) 将一种活性成分、一种丙烯酸共聚物和至少一种药学上可接受的添加剂混合，以获得其混合物；(2) 将该混合物制成片剂，以获得压制物；以及 (3) 在 50°C 至 100°C 的温度下等温加热该压制物一段时间。并提供通过快速崩解片剂的生产方法生产的这种快速崩解片剂。