4-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butan-1-amine

• 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: 4-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butan-1-amine
• 化学式: C₁₆H₂₅N₃O₂
• 分子量: 291.393
• InChiKey: WKUPOALMGMWHEM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  51
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  对氟苯甲酰氯 、 4-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butan-1-amine 以 二氯甲烷 为溶剂， 生成 N-{4-[4-(2,3-Dihydro-benzo[1,4]dioxin-5-yl)-piperazin-1-yl]-butyl}-4-fluoro-benzamide
  参考文献：
  名称：

  Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands structure-activity relationships

  摘要：

  The agonistic/antagonistic profile of a series of 10 N4-substituted1-(2,3-dihydro-1,4-benzodioxin- 5-yl)piperazines is evaluated in the in vitro adenylyl cyclase assay. The profile is severely affected by the characteristics of the N4-substituents ranging from full agonism (benzamidoethyl derivative 1), mixed agonism/antagonism (phthalimidobutyl derivative 7) to predominantly antagonism (saccharinbutyl derivate 9). A novel full antagonist 10, as potent as WAY 100635, is obtained by substitution of Cl at C-7 of the benzodioxinyl moiety in 9. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00406-5
• 作为产物：
  描述：

  1-(2,3-二氢-1,4-苯并二烷-5-基)哌嗪盐酸盐 在 lithium aluminium tetrahydride 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 生成 4-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butan-1-amine
  参考文献：
  名称：

  Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands structure-activity relationships

  摘要：

  The agonistic/antagonistic profile of a series of 10 N4-substituted1-(2,3-dihydro-1,4-benzodioxin- 5-yl)piperazines is evaluated in the in vitro adenylyl cyclase assay. The profile is severely affected by the characteristics of the N4-substituents ranging from full agonism (benzamidoethyl derivative 1), mixed agonism/antagonism (phthalimidobutyl derivative 7) to predominantly antagonism (saccharinbutyl derivate 9). A novel full antagonist 10, as potent as WAY 100635, is obtained by substitution of Cl at C-7 of the benzodioxinyl moiety in 9. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00406-5

文献信息

• [EN] ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES<br/>[FR] ARYLSULFAMIDES POUR LE TRAITEMENT DE MALADIES DU SNC
  申请人：ADAMED SP ZOO

  公开号：WO2012035123A1

  公开（公告）日：2012-03-22

  Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.

  化学式（I）的芳基磺酰胺衍生物及其药用盐。这些化合物可能对中枢神经系统的治疗和/或预防具有用处。
• ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES
  申请人：Kolaczkowski Marcin

  公开号：US20130172365A1

  公开（公告）日：2013-07-04

  Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.

  化学式（I）的芳基磺胺衍生物及其药用盐。这些化合物可能对中枢神经系统疾病的治疗和/或预防有用。
• [EN] SUBSTITUTED ALKYL-PYRIDAZINONES FOR THE TREATMENT OF MEMORY AND LEARNING MALFUNCTIONS<br/>[FR] ALKYLE-PYRIDAZINONES SUBSTITUES POUR LE TRAITEMENT DE DYSFONCTIONNEMENTS DE LA MEMOIRE ET DE L'APPRENTISSAGE
  申请人：EGYT GYOGYSZERVEGYESZETI GYAR

  公开号：WO2004043465A1

  公开（公告）日：2004-05-27

  The compounds of the general Formula I, wherein R1 stands for hydrogen or lower alkyl; one of symbols X and Y stands for hydrogen or halogen and the other represents a group of the general Formula II, R2 is hydrogen or lower alkyl; n is 1, 2 or 3; R3 is hydrogen, lower alkyl or aryl-lower alkyl; Z is -0-; or R3 and Z together with the intermediate atoms form a piperazino ring; Q and W independently from each other stands for -CH= or -N=; and R4, R5 and R6 can be the same or different and stand for hydrogen, halogen, trifluoromethyl or lower alkoxy; or R4 and R5 together form an ethylenedioxy group) and pharmaceutically acceptable salts thereof can be used for the treatment or prophylaxis of malfunctions of memory and/or cognitive decline or prevention of decline of learning abilities.

  通式I的化合物，其中R1代表氢或低碳基；符号X和Y中的一个代表氢或卤素，另一个代表通式II的基团，其中R2代表氢或低碳基；n为1、2或3；R3代表氢、低碳基或芳基-低碳基；Z为-0-；或者R3和Z与中间原子一起形成哌嗪环；Q和W独立地代表-CH=或-N=；R4、R5和R6可以相同也可以不同，代表氢、卤素、三氟甲基或低烷氧基；或者R4和R5一起形成乙二氧基基团。这些化合物及其药学上可接受的盐可以用于治疗或预防记忆失灵和/或认知衰退或预防学习能力下降。
• [EN] SUBSTITUTED ALKYLAMINOPYRIDAZINONE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME<br/>[FR] DERIVES SUBSTITUES D'ALKYLAMINOPYRIDAZINONE, PROCEDES DE PREPARATION ET COMPOSITION PHARMACEUTIQUE LES CONTENANT
  申请人：EGYT GYOGYSZERVEGYESZETI GYAR

  公开号：WO2003027097A1

  公开（公告）日：2003-04-03

  The invention relates to new substituted alkylaminopyridazinone derivatives of the general Formula (I), (wherein R1 is hydrogen or alkyl having 1-4 carbon atoms; one of X and Y stands for hydrogen or halogen and the other represents a group of the general Formula (II), R2 is hydrogen or alkyl having 1-4 carbon atoms; n is 1, 2 or 3; R3 stands for hydrogen, alkyl having 1-4 carbon atoms or aryl-(C1-4 alkyl); Z stands for oxygen; or R3 and Z together with the groups placed between them form a piperazine ring; and R4 stands for hydrogen, halogen, trifluoromethyl or alkoxy having 1-4 carbon atoms) and pharmaceutically acceptable acid addition salts thereof. The invention compounds are useful in the treatment of anxiolytic conditions and cognitive disorders.

  本发明涉及一种新的取代烷基氨基吡嗪酮衍生物，其通式为（I），其中R1为氢或具有1-4个碳原子的烷基；X和Y中的一个代表氢或卤素，另一个代表通式（II）的基团，R2为氢或具有1-4个碳原子的烷基；n为1、2或3；R3代表氢、具有1-4个碳原子的烷基或芳基-(C1-4烷基)；Z代表氧；或R3和Z与它们之间放置的基团一起形成哌嗪环；R4代表氢、卤素、三氟甲基或具有1-4个碳原子的烷氧基；以及其药学上可接受的酸加盐。本发明化合物在治疗抗焦虑症和认知障碍方面有用。
• NOVEL CHROMENE AND THIOCHROMENE CARBOXAMIDE DERIVATIVES, METHODS FOR PREPARING SAME AND THERAPEUTIC APPLICATIONS OF SAME
  申请人：Sokoloff Pierre

  公开号：US20100029682A1

  公开（公告）日：2010-02-04

  The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.

  本发明涉及新型香豆素或硫代香豆素羧酰胺衍生物、其制备方法、相应的药物组成物以及将其用作中枢神经系统疾病的多巴胺D3受体配体的药物。