(-)-cis-3-acetoxy-5-(2-(dimethylamino)ethyl)-2,3-dihydro-8-methyl-2-(4-methylphenyl)-1,5-benzothiazepin-4(5H)-one maleate | 150591-06-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并硫氮卓类
• 英文名称: (-)-cis-3-acetoxy-5-(2-(dimethylamino)ethyl)-2,3-dihydro-8-methyl-2-(4-methylphenyl)-1,5-benzothiazepin-4(5H)-one maleate
• 英文别名: TA-993；TA-993 maleate；(Z)-but-2-enedioic acid;[(2R,3R)-5-[2-(dimethylamino)ethyl]-8-methyl-2-(4-methylphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate
• CAS: 150591-06-3
• 化学式: C₄H₄O₄*C₂₃H₂₈N₂O₃S
• 分子量: 528.626
• InChiKey: KILCEIIRMKHOSB-IVANRGOOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.69
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  150
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• Pharmaceutical composition for inhibiting platelet aggregation
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0476854A1

  公开（公告）日：1992-03-25

  There is disclosed a pharmaceutical composition for inhibiting the platelet aggregation comprising acetylsalicyclic acid or a pharmaceutically acceptable salt thereof and a 1,5-benzothiazepine derivative of the formula: wherein R¹ is a lower alkyl group or a lower alkoxy group, R² is hydrogen atom or a lower alkanoyl group, R³ is a lower alkyl group, R⁴ is hydrogen atom or a lower alkyl group and R⁵ is a lower alkyl group or a halogen atom, or a pharmaceutically acceptable salt thereof.

  本发明公开了一种抑制血小板聚集的药物组合物，该组合物由乙酰基水杨酸或其药学上可接受的盐和式 1,5-苯并硫氮杂卓衍生物组成： 其中，R¹为低级烷基或低级烷氧基，R²为氢原子或低级烷酰基，R³为低级烷基，R⁴为氢原子或低级烷基，R⁵为低级烷基或卤素原子，或其药学上可接受的盐。
• PROCESS FOR PRODUCING SPHERICAL FINE PARTICLES CONTAINING DRUG
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1125576A1

  公开（公告）日：2001-08-22

  The present invention discloses an efficient preparation method of spherical fine particles containing a drug for an easily-swallowed, controlled-release preparation comprising the production of drug-containing spherical fine particles (mean particle size: 60-200 µ m) by adding a binder solution to a mixture containing an excipient powder having the property of retaining solvent (and preferably having a mean length of the long axis of 40 µ m or less) and a drug powder (preferably having a mean length of the long axis of 50 µ m or less), followed by high-speed mixing granulation.

  本发明公开了一种用于易吞服控释制剂的含药球形细颗粒的高效制备方法，包括通过向含有具有保留溶剂特性的赋形剂粉末（长轴平均长度最好在 40 µ m 或以下）和药物粉末（长轴平均长度最好在 50 µ m 或以下）的混合物中添加粘合剂溶液，然后进行高速混合造粒，制备含药球形细颗粒（平均粒径：60-200 µ m）。
• SUSTAINED-RELEASE PARTICLES
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1125586A1

  公开（公告）日：2001-08-22

  The present invention discloses sustained release particles having a mean particle size of 300 µm, or less, comprising a drug-containing core substance coated with a mixed coating of a hydrophobic organic compound-water-insoluble polymer, which prevents sticking during compression molding when producing oral sustained release tablets, a preparation method of those sustained release particles, and a preparation method of tablets using those sustained release particles.

  本发明公开了平均粒径为 300 微米或更小的缓释颗粒，该颗粒由含药核心物质和疏水性有机化合物-水不溶性聚合物混合包衣组成，在生产口服缓释片时可防止压缩成型过程中的粘连；本发明还公开了这些缓释颗粒的制备方法，以及使用这些缓释颗粒制备片剂的方法。
• SUSTAINED-RELEASE PREPARATION AND PROCESS FOR PRODUCING THE SAME
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1252887A1

  公开（公告）日：2002-10-30

  The present invention is to provide a sustained release preparation comprising a drug-containing core substance and a multilayered coating layer covering the core substance, wherein all adjacent layers in the multilayered coating layer contain mutually different hydrophobic organic compound-water-soluble polymer mixtures; and, a method of producing a sustained release preparation, having a multilayered coating layer in which adjacent layers contain different hydrophobic organic compound-water-soluble polymer mixtures, which comprises spray-coating a solution containing a hydrophobic organic compound-water-soluble polymer mixture onto a drug-containing core substance, continuing to spray-coat a solution containing a different hydrophobic organic compound-water-soluble polymer mixture onto the resulting coating layer, and repeating this step.

  本发明旨在提供一种缓释制剂，包括含药核心物质和覆盖核心物质的多层包衣层，其中多层包衣层中的所有相邻层含有相互不同的疏水性有机化合物-水溶性聚合物混合物；以及一种生产缓释制剂的方法，该制剂具有多层包衣层，其中相邻层含有不同的疏水性有机化合物-水溶性聚合物混合物，该方法包括将含有疏水性有机化合物-水溶性聚合物混合物的溶液喷涂到含药核心物质上，继续将含有不同疏水性有机化合物-水溶性聚合物混合物的溶液喷涂到所得包衣层上，并重复此步骤。
• FUNCTIONAL GRAIN-CONTAINING PREPARATIONS QUICKLY DISINTEGRATED IN THE ORAL CAVITY
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1405635A1

  公开（公告）日：2004-04-07

  The present invention provides a process for producing an orally fast disintegrating preparation containing functional particles, which comprises filling in a mold an aqueous dispersion containing (a) a dispersant showing a dispersion maintaining ratio of about 75% or more and a viscosity of about 100 mPa.s or less at 25°C in case of being contained homogeneously in water at 1% by weight, (b) a water-soluble saccharide, and (c) functional particles; and then removing water; and an orally fast disintegrating preparation containing functional particles, which comprises (a) a dispersant showing a dispersion maintaining ratio of 75% or more and a viscosity of 100 mPa.s or less at 25°C in case of being contained homogeneously in water at 1% by weight, (b) a water-soluble saccharide, and (c) functional particles.

  本发明提供了一种含有功能性颗粒的口服快速崩解制剂的生产工艺，该工艺包括在模具中填充含有(a)分散剂的水分散液，该分散剂在25°C时的分散保持率约为75%或以上，粘度约为100 mPa.s或更低，(b)水溶性糖和(c)功能性微粒；然后除去水；以及一种含有功能性微粒的口服快速崩解制剂，它包含(a)分散剂，其分散保持率为75%或更高，在25°C时的粘度为100 mPa.s或更低，其均匀地包含在水中，重量百分比为1%，(b)水溶性糖和(c)功能性微粒。