SM-9018 (free base)

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: SM-9018 (free base)
• 英文别名: 2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione
• 化学式: C₂₃H₃₀N₄O₂S
• 分子量: 426.6
• InChiKey: FBVFZWUMDDXLLG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  85
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• Combination treatment for anxiety, depression, obsessive compulsive disorder and psychosis
  申请人：Pfizer Inc.

  公开号：US20020123490A1

  公开（公告）日：2002-09-05

  The present invention relates to a method of treating depression, obsessive compulsive disorder and psychosis in a mammal, including a human, by administering to the mammal an atypical antipsychotic in combination with an antidepressant agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, an atypical antipsychotic, and an SRI.

  本发明涉及一种治疗哺乳动物，包括人类，的抑郁症、强迫症和精神病的方法，通过向哺乳动物投予一种非典型抗精神病药物与抗抑郁药物的组合，以提高效率。它还涉及含有一种药学上可接受的载体、一种非典型抗精神病药物和一种SRI的药物组合。
• Prodrugs for the Treatment of Schizophrenia and Bipolar Disease
  申请人：Blumberg Laura Cook

  公开号：US20110166156A1

  公开（公告）日：2011-07-07

  Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.

  本文披露了公式I和公式II的化合物及其用于治疗神经系统和精神障碍，包括与双相I型障碍伴有或不伴有精神症状的精神分裂症和躁狂或混合发作的治疗。
• Quaternary Ammonium Salt Prodrugs
  申请人：Almarsson Orn

  公开号：US20110178068A1

  公开（公告）日：2011-07-21

  The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X − . In one embodiment, the present invention provides a prodrug compound of Formula I: where R 1 -R 5 are defined in the written description of the invention. The prodrug compounds of the invention can be used to treat any condition for which the tertiary amine-containing parent drug or tertiary imine-containing parent drug is useful as a treatment.

  本发明提供了一种持续释放三级胺含有的母药的方法，包括向患者施用本发明的前药化合物的有效量，其中在向患者施用时，母药从前药中的释放是持续释放的。适用于本发明方法的前药化合物是由醛基连接的前药基团衍生的，这些前药基团可以减少前药化合物在参考pH下的溶解度与母药相比。这些衍生物的物理、化学和溶解度特性可以通过选择阴离子X-来进一步调节。在一种实施方式中，本发明提供了式I的前药化合物：其中R1-R5在发明的书面描述中被定义。本发明的前药化合物可用于治疗任何需要使用三级胺含有的母药或三级亚胺含有的母药进行治疗的情况。
• Combination of a serotonin reuptake inhibitor and an atypical antipsychotic for use in depression, obsessive compulsive disorder and psychosis
  申请人：Pfizer Products Inc.

  公开号：EP1238676A1

  公开（公告）日：2002-09-11

  The present invention relates to a method of treating depression, obsessive compulsive disorder and psychosis in a mammal, including a human, by administering to the mammal an atypical antipsychotic in combination with an antidepressant agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, an atypical antipsychotic, and an SRI.

  本发明涉及一种治疗哺乳动物（包括人类）抑郁症、强迫症和精神病的方法，其方法是向哺乳动物施用一种非典型抗精神病药与一种抗抑郁药联用，以提高疗效。它还涉及含有药学上可接受的载体、非典型抗精神病药和 SRI 的药物组合物。
• FMO3 inhibitors for treating pain
  申请人：Akron Molecules GmbH

  公开号：EP2674161A1

  公开（公告）日：2013-12-18

  The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.

  本发明涉及治疗疼痛和相关疾病的新疗法，以及用于上述疗法的药物化合物。