5-(2-(4-(1,2-benzisothiazol-3-yl)piperazinyl)ethyl)-6-fluoro-3,3-dimethyloxindole hydrochloride | 122883-94-7

• 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: 5-(2-(4-(1,2-benzisothiazol-3-yl)piperazinyl)ethyl)-6-fluoro-3,3-dimethyloxindole hydrochloride
• 英文别名: 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-fluoro-3,3-dimethyl-1H-indol-2-one;hydrochloride
• CAS: 122883-94-7
• 化学式: C₂₃H₂₅FN₄OS*ClH
• 分子量: 461.003
• InChiKey: OOJUMAZSEGUFDK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.45
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  76.7
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Anxiety treatments with ziprasidone
  申请人：Romano Joseph Steven

  公开号：US20050004138A1

  公开（公告）日：2005-01-06

  The present invention, in one aspect, relates to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for treating, in a mammal, including a human, situational anxiety, for example, anxiety experienced prior to medical procedures (e.g., surgery), public speaking, anxiety associated with swimming or water, anxiety associated with travel (e.g., air travel), or anxiety associated with specific phobias (snakes, spider, rats, sight of blood), comprising administering a pharmaceutically effective amount of a compound of formula I to the mammal. In another aspect, the present invention is directed to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for treating, in a mammal, including a human, treatment-resistant anxiety, which method comprises administering a pharmaceutically effective amount of a compound of formula I to the mammal. The compounds of formula I are defined as follows: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined.

  本发明在某些方面涉及使用以下式子定义的哌嗪基-杂环化合物的方法，用于治疗哺乳动物，包括人类的情境焦虑，例如在医疗程序（例如手术）、公共演讲、与游泳或水有关的焦虑、与旅行（例如空中旅行）有关的焦虑或与特定恐惧症（蛇、蜘蛛、老鼠、血液视觉）有关的焦虑，包括向哺乳动物投与化学有效量的式子I的化合物。在另一个方面，本发明涉及使用以下式子定义的哌嗪基-杂环化合物的方法，用于治疗哺乳动物，包括人类的难治性焦虑，其中该方法包括向哺乳动物投与化学有效量的式子I的化合物。式子I的化合物定义如下：或其药学上可接受的酸盐，其中Ar、n、X和Y如上定义。
• Treatment of psychotic and depressive disorders
  申请人：Romano Joseph Steven

  公开号：US20050004137A1

  公开（公告）日：2005-01-06

  The present invention relates to a method for treating a psychiatric conditions and disorders selected from delusional disorder, psychosis associated with dementia, such as psychosis associated with Alzheimer's disease, psychosis associated with an organic brain syndrome (e.g. stroke, or a viral infection such as an HIV infection), and drug-induced psychosis in mammals, including humans, comprising administering an effective amount of a compound of the formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined The present invention also relates to a method for treating a depressive disorder selected from melancholic depression, severe depression, psychotic depression, and treatment-resistant depression in mammals, including humans, comprising administering a compound of formula I, or a pharmaceutically acceptable acid addition salt of such compound.

  本发明涉及一种治疗精神病症和障碍的方法，所述症状包括妄想症、与痴呆症相关的精神病，例如与阿尔茨海默病相关的精神病、与器质性脑病综合症相关的精神病（例如中风或病毒感染，如HIV感染）以及哺乳动物，包括人类中的药物诱导性精神病，其包括向患者投予化合物I式的有效量，或其药学上可接受的酸盐加合物，其中Ar、n、X和Y如定义所述。本发明还涉及一种治疗哺乳动物，包括人类中的忧郁症的方法，所述忧郁症包括忧郁症、重度抑郁症、精神病性抑郁症和难治性抑郁症，其包括向患者投予化合物I式或其药学上可接受的酸盐加合物。
• Treatment of bipolar disorders and associated symptoms
  申请人：Romano Joseph Steven

  公开号：US20050038036A1

  公开（公告）日：2005-02-17

  The present invention relates to a method for treatments relating to bipolar disorder in a mammal, including a human, the treatments including treatment of rapid-cycling bipolar disorder, treatment of symptoms of bipolar disorder selected from the group consisting of acute mania and depression, treatment for effecting mood stabilization; treatment for preventing relapse into bipolar episodes, and for the treatment of suicidal thoughts and tendencies associated with bipolar disorder, comprising administering to said mammal an effective amount of a compound of the formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined.

  本发明涉及一种治疗哺乳动物（包括人类）的双相障碍的方法，包括治疗快速循环型双相障碍，治疗选自急性躁狂和抑郁症状的双相障碍症状，治疗以影响情绪稳定为目的的治疗，预防双相障碍复发的治疗，以及治疗与双相障碍相关的自杀思想和倾向。该方法包括向该哺乳动物施用以下化合物的有效量：式I的化合物或其药学上可接受的酸盐加合物，其中Ar、n、X和Y如定义。
• Method for enhancing cognition using ziprasidone
  申请人：Romano Joseph Steven

  公开号：US20050014764A1

  公开（公告）日：2005-01-20

  The present invention, in one aspect, relates to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for enhancing cognition in a mammal, including a human, for example a mammal afflicted with psychosis, autism, dementia, or mental retardation, comprising administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for reducing or ameliorating in a mammal, including a human, afflicted with a disorder or condition selected from autism, mental retardation, obsessive-compulsive disorder, and dementia, positive symptoms (e.g. excessive aggression, disinhibited sexual behavior, inappropriate sexual behavior, agitation, compulsive behavior such as head banging, lip bighting, self mutilation, or stereotypic behavior) associated with the aforementioned disorders or conditions, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for treating pediatric bipolar disorder in a mammal, including a human, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. The compounds of compound of the formula I are defined as follows: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined.

  本发明在某个方面涉及使用式I的哌嗪基-杂环化合物的方法，如下所定义，用于增强哺乳动物，包括人类，例如患有精神病、自闭症、痴呆或智力障碍的哺乳动物的认知能力，包括向哺乳动物投与式I的化合物的有效量（例如ziprasidone）。在另一个方面，本发明涉及一种用于减轻或改善患有自闭症、智力障碍、强迫症和痴呆等疾病或症状的哺乳动物，包括人类的阳性症状（例如过度攻击、失控的性行为、不当的性行为、激动、强迫性行为，如头撞击、咬唇、自我伤害或刻板行为），该方法包括向哺乳动物投与式I的化合物的有效量（例如ziprasidone）。在另一个方面，本发明涉及一种用于治疗哺乳动物，包括人类的小儿双相情感障碍的方法，该方法包括向哺乳动物投与式I的化合物的有效量（例如ziprasidone）。化合物I的定义如下：或其药学上可接受的酸加成盐，其中Ar、n、X和Y如上所定义。
• METHOD FOR TREATING PEDIATRIC BIPOLAR DISORDER
  申请人：Romano Steven Joseph

  公开号：US20080269246A1

  公开（公告）日：2008-10-30

  The present invention, in one aspect, relates to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for enhancing cognition in a mammal, including a human, for example a mammal afflicted with psychosis, autism, dementia, or mental retardation, comprising administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for reducing or ameliorating in a mammal, including a human, afflicted with a disorder or condition selected from autism, mental retardation, obsessive-compulsive disorder, and dementia, positive symptoms (e.g. excessive aggression, disinhibited sexual behavior, inappropriate sexual behavior, agitation, compulsive behavior such as head banging, lip biting, self mutilation, or stereotypic behavior) associated with the aforementioned disorders or conditions, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for treating pediatric bipolar disorder in a mammal, including a human, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. The compounds of the formula I are defined as follows: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined.

  本发明在某些方面涉及使用公式I所定义的哌嗪基-杂环化合物的方法，以增强哺乳动物（包括人类）的认知能力，例如患有精神病、自闭症、痴呆或智力低下的哺乳动物，包括给哺乳动物（例如齐拉西酮）的公式I化合物的有效剂量。在另一个方面，本发明涉及一种方法，用于减轻或改善患有自闭症、智力低下、强迫症和痴呆症等疾病或症状的哺乳动物（包括人类）的阳性症状（例如过度攻击、解禁性行为、不当性行为、焦虑、强迫行为，如头撞击、咬唇、自残或刻板行为），该方法包括向哺乳动物（例如齐拉西酮）的有效剂量的公式I化合物的管理。在另一个方面，本发明涉及一种用于治疗哺乳动物（包括人类）的儿童双相情感障碍的方法，该方法包括向哺乳动物（例如齐拉西酮）的有效剂量的公式I化合物的管理。公式I化合物定义如下：或其药学上可接受的酸盐，其中Ar，n，X和Y如定义。