N-[(1-丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]噁嗪并[3,2-a]吲哚-10-羧胺盐酸盐

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: N-[(1-丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]噁嗪并[3,2-a]吲哚-10-羧胺盐酸盐
• 中文别名: 哌波色罗盐酸盐
• 英文名称: SB 207266A
• 英文别名: N-[(1-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]-oxazino [3,2-a]indole-10-carboxamide hydrochloride；piboserod；N-[(1-butylpiperidin-4-yl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide;hydron;chloride
• 化学式: C₂₂H₃₁N₃O₂*ClH
• 分子量: 405.968
• InChiKey: UABVCZHWRUGYSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.09
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  46.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-(3-bromopropoxy)-N-[(1-butylpiperidin-4-yl)methyl]-1H-indole-3-carboxamide 以52的产率得到N-[(1-丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]噁嗪并[3,2-a]吲哚-10-羧胺盐酸盐
  参考文献：
  名称：

  J Med Chem 1995, 38, 4760-4763

  摘要：

  DOI：

文献信息

• Novel composition
  申请人：Buxton Christopher Philip

  公开号：US20050148582A1

  公开（公告）日：2005-07-07

  A pharmaceutical composition comprising N-[(1- n butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, wherein at least some of the SB 207266 or salt thereof is in granulated form. Preferably, a filler and/or binder are also present.

  一种药物组合物，包括N-[(1-正丁基-4-哌嗪基)甲基]-3,4-二氢-2H-[1,3]噁嗪[3,2-a]吲哚-10-羧酰胺（SB 207266）或其药学上可接受的盐与一种或多种药学上可接受的载体结合，其中至少一部分SB 207266或其盐为颗粒状。优选地，还存在填充剂和/或粘合剂。
• Pharmaceutical composition comprising n((1-n-butyl-4-piperidinyl)methyl)-3,4-dihydro-2h-(1,3)oxazino(3,2-a)indole-10-carboxamide or salt and process therefor comprising dry granulation
  申请人：Buxton Christopher Philip

  公开号：US20050075335A1

  公开（公告）日：2005-04-07

  The invention provides a process for preparing a pharmaceutical composition comprising N-[(1- n butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carbixamide (pharmaceutical composition) (piboserod) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable excipients, the process comprising forming part or all of the (pharmaceutical composition) or the salt thereof into granules by a dry granulation process. The process is preferably a roller compaction process, preferably followed by milling to a suitable particle size. The granules are usually of increased particle size and/or compacted compared to the SB 207266 or the salt thereof. Preferably, the (pharmaceutical composition) or the salt thereof is present in the composition and/or in the granules in at least 4 weight % and/or up to 60 weight % by weight of the composition and/or by weight of the granules respectively. An intragranular lubricant, filler (e.g. CaHPO 4 ), and/or compression aid (e.g. microcrystalline cellulose) are usually used. The invention also provides a pharmaceutical composition obtainable by the dry granulation process and/or which has been prepared by the dry granulation process.

  本发明提供了一种制备含有N-[(1-正丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]噁唑并[3,2-a]吲哚-10-羧酰胺（药物组合物）（皮博塞罗德）或其药学上可接受的盐与一种或多种药学上可接受的赋形剂的制药组合物的方法，该方法包括通过干法造粒工艺将部分或全部（药物组合物）或其盐制成颗粒。该方法最好是辊压成型工艺，最好后跟适当的粒度磨制。与SB 207266或其盐相比，颗粒通常具有增加的粒径和/或致密度。最好的情况是，（药物组合物）或其盐以至少4重量％和/或高达60重量％的重量存在于组合物和/或颗粒中。通常使用内部润滑剂、填料（例如CaHPO4）和/或压缩助剂（例如微晶纤维素）。本发明还提供了一种通过干法造粒工艺获得的制药组合物和/或通过干法造粒工艺制备的制药组合物。
• Process for the preparation of N-[(1-.sup.n
  申请人：Smithkline Beecham plc

  公开号：US06100397A1

  公开（公告）日：2000-08-08

  A process for the preparation of SB 207266 or a pharmaceutically acceptable salt thereof, which process comprises the reaction of N-(1-.sup.n butyl-4-piperidyl)methylamine with a compound of formula (A), ##STR1## wherein R is alkyl.

  一种制备SB 207266或其药学上可接受的盐的过程，该过程包括将N-(1-正丁基-4-哌啶基)甲基胺与式（A）的化合物反应，其中R是烷基。 ##STR1##
• Pharmaceutical composition comprising condensed indole compound
  申请人：SMITHKLINE BEECHAM PLC

  公开号：EP1867333A1

  公开（公告）日：2007-12-19

  The invention provides a pharmaceutical composition comprising N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, wherein at least some of the SB 207266 or the salt thereof is in granulated form, and wherein the SB 207266 or the salt thereof is present in the composition in at least 4 weight % by weight of the composition, wherein the pharmaceutical composition has been made by a method comprising forming at least some of the SB 207266 or the salt thereof into granules in the presence of a granulating solvent (i.e. using a "wet granulation" process), and wherein the composition includes an excipient which acts as a granulation aid, and wherein the granulation aid is present inside the granules and is present in at least 15 weight % of the composition. The granulation aid is preferably microcrystalline cellulose. The granulating solvent can comprise or be water and/or ethanol. A method of making the pharmaceutical composition is also provided.

  本发明提供了一种药物组合物，该组合物包含 N-[(1-丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺（SB 207266）或其药学上可接受的盐与一种或多种药学上可接受的载体的组合、 其中至少部分 SB 207266 或其盐呈颗粒状，且 SB 207266 或其盐在组合物中的含量至少占组合物重量的 4%、 其中药物组合物的制造方法包括在制粒溶剂存在下将至少部分 SB 207266 或其盐制成颗粒（即使用 "湿制粒 "工艺）、 其中，组合物包括作为造粒助剂的赋形剂，造粒助剂存在于颗粒内部，且至少占组合物的 15 重量百分比。 制粒助剂最好是微晶纤维素。制粒溶剂可以是水和/或乙醇。 还提供了一种制造药物组合物的方法。
• pharmaceutical composition comprising condensed indole compound
  申请人：SMITHKLINE BEECHAM PLC

  公开号：EP1872785A1

  公开（公告）日：2008-01-02

  A pharmaceutical composition comprising N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, wherein at least some of the SB 207266 or the salt thereof is in granulated form. Preferably, a filler and/or binder are also present. The invention also provides a method of making a pharmaceutical composition comprising N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, the method comprising forming at least some of the SB 207266 or the salt thereof into granules. Preferably, the granules are formed in the presence of a granulating solvent, i.e. using a "wet granulation" process.

  一种药物组合物，包含 N-[（1-丁基-4-哌啶基）甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺（SB 207266）或其药学上可接受的盐与一种或多种药学上可接受的载体的组合物，其中至少部分 SB 207266 或其盐呈颗粒状。 最好还含有填充剂和/或粘合剂。 本发明还提供了一种药物组合物的制造方法，该组合物包含 N-[(1-丁基-4-哌啶基)甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺（SB 207266）或其药学上可接受的盐与一种或多种药学上可接受的载体的组合，该方法包括将至少部分 SB 207266 或其盐制成颗粒。 最好是在有造粒溶剂存在的情况下形成颗粒，即使用 "湿造粒 "工艺。