3-[2-[4-(6-Fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one;dihydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 3-[2-[4-(6-Fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one;dihydrochloride
• 化学式: C23H29Cl2FN4O2
• 分子量: 483.4
• InChiKey: LMYCMULLDCTGNJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.43
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  61.9
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] WATER SOLUBLE SALTS OF RISPERIDONE<br/>[FR] SELS HYDROSOLUBLES DE RISPERIDONE
  申请人：SYNTHON BV

  公开号：WO2004094414A1

  公开（公告）日：2004-11-04

  The invention relates to a salt of risperidone in solid state having a water solubility of at least 10 mg/ml, to risperidone dihydrochloride, risperidone hydrogenmaleate, risperidone hernitartrate and risperidone (L)-hemimalate, to a process for making a solid state water soluble salt of risperidone, which comprises: contacting a risperidone donor with a suitable acid in an organic solvent to form a water soluble risperidone salt; and precipitating said risperidone salt from said solvent, and to the use for treating psychotic disorders in a mammal.

  该发明涉及一种固态状态下的利培酮盐，其水溶解度至少为10毫克/毫升，以及利培酮二盐酸盐、利培酮氢男酸盐、利培酮苹果酸盐和利培酮(L)-半苹果酸盐，以及制备利培酮固态水溶性盐的方法，包括：将利培酮供体与适当的酸在有机溶剂中接触，形成水溶性利培酮盐；并从溶剂中沉淀所述利培酮盐，并用于治疗哺乳动物的精神疾病。
• Risperidone monohydrochloride
  申请人：——

  公开号：US20040266790A1

  公开（公告）日：2004-12-30

  Monohydrochloride salts of risperidone have been found to have useful properties. A preferred form is crystalline risperidone monohydrochloride hemipentahydrate. The monohydrochloride salts can be used in pharmaceutical compositions and methods such as for use in treating psychotic disorders.

  利培酮的单盐酸盐具有有用的特性。首选形式为晶体利培酮单盐酸盐半五水合物。这些单盐酸盐可以用于制备药物组合物和方法，例如用于治疗精神疾病。
• Antipsychotic injectable depot composition
  申请人：LABORATORIOS FARMACEUTICOS ROVI, S.A.

  公开号：US10085936B2

  公开（公告）日：2018-10-02

  The present invention is directed to a composition that can be used to deliver an antipsychotic drug such as risperidone as an injectable in-situ forming biodegradable implant for extended release providing therapeutic plasma levels from the first day. The composition is in the form of drug suspension on a biodegradable and biocompatible copolymer or copolymers solution using water miscible solvents that is administered in liquid form. Once the composition contacts the body fluids, the polymer matrix hardens retaining the drug, forming a solid or semisolid implant that releases the drug in a continuous manner. Therapeutic plasma levels of the drug can be achieved since the first day up to at least 14 days or more even up to at least four weeks.

  本发明涉及一种组合物，该组合物可用于递送抗精神病药物，如利培酮，作为可注射的原位成型生物可降解植入物，用于延长释放时间，从第一天起提供治疗血浆水平。该组合物以药物悬浮液的形式存在于可生物降解和生物相容的共聚物或共聚物溶液中，使用水溶性溶剂，以液态形式给药。一旦组合物与体液接触，聚合物基质就会硬化，将药物保留下来，形成固体或半固体植入物，以连续的方式释放药物。药物的治疗血浆浓度可从第一天开始达到至少 14 天，甚至至少四周。
• Antipsychotic Injectable Depot Composition
  申请人：LABORATORIOS FARMACEUTICOS ROVI S.A.

  公开号：US10463607B2

  公开（公告）日：2019-11-05

  The present invention is directed to a composition that can be used to deliver an antipsychotic drug such as risperidone, paliperidone or a combination thereof, as an injectable in-situ forming biodegradable implant for extended release providing therapeutic plasma levels from the first day. The composition is in the form of drug suspension on a biodegradable and biocompatible copolymer or copolymers solution using water miscible solvents that is administered in liquid form. Once the composition contacts the body fluids, the polymer matrix hardens retaining the drug, forming a solid or semisolid implant that releases the drug in a continuous manner. Therapeutic plasma levels of the drug can be achieved from the first day up to at least 14 days or more even up to at least four weeks.

  本发明涉及一种组合物，该组合物可用于递送抗精神病药物，如利培酮、帕利培酮或其组合物，作为可注射的原位形成生物可降解植入物，用于延长释放，从第一天起提供治疗血浆水平。该组合物以药物悬浮液的形式存在于可生物降解的生物相容性共聚物或共聚物溶液中，使用水溶性溶剂，以液态形式给药。一旦组合物与体液接触，聚合物基质就会硬化，将药物保留下来，形成固体或半固体植入物，以连续的方式释放药物。药物的治疗血浆水平可从第一天开始达到至少 14 天，甚至至少四周。
• Water soluble salts of risperidone
  申请人：——

  公开号：US20040266791A1

  公开（公告）日：2004-12-30

  Salts of risperidone are provided including solid state salts and water soluble salts. The salts are useful in making pharmaceutical compositions.

  提供的利培酮盐包括固态盐和水溶性盐。这些盐可用于制作药物组合物。