1,4-dibenzyl-2-piperazinecarboxaldehyde | 54969-29-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1,4-dibenzyl-2-piperazinecarboxaldehyde
• 英文别名: 1,4-dibenzylpiperazine-2-carboxaldehyde；1,4-dibenzylpiperazine-2-carbaldehyde；1,4-dibenzyl-2-formylpiperazine
• CAS: 54969-29-8
• 化学式: C₁₉H₂₂N₂O
• 分子量: 294.396
• InChiKey: GPGHMUYOZRAMNQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1,4-dibenzyl-2-piperazinecarboxaldehyde 在 palladium on activated charcoal 氢气 、 sodium hydride 作用下， 以 乙二醇二甲醚 、 乙醇 为溶剂， 20.0 ℃ 、344.75 kPa 条件下， 反应 10.0h， 生成 六氢吡咯并[1,2-a]吡嗪-6-酮
  参考文献：
  名称：

  1、4-二氮杂双环[4.3.0] nonan-9-ones作为一类新型强力促智药物的设计，合成和初步药理评估。

  摘要：

  已经合成了几种4-取代的1,4-二氮杂双环[4.3.0] nonan-9-one，并在小鼠被动回避测试中进行了体内测试，以评估其促智活性。结果表明，它们代表了一类新型促智药物，其药理学特性与吡乙酰胺非常相似，相对于参考文献显示出更高的功效。在研究的化合物中，有7种（DM 232）具有出色的效力，在0. 001 mg kg（-1）sc剂量下具有活性。

  DOI：

  10.1021/jm991170t
• 作为产物：
  描述：

  N,N'-二苄基乙二胺 在 二异丁基氢化铝 、 N,N-二异丙基乙胺 作用下， 以 甲苯 为溶剂， 反应 1.0h， 生成 1,4-dibenzyl-2-piperazinecarboxaldehyde
  参考文献：
  名称：

  QUINOLINE DERIVATIVES AS SMO INHIBITORS

  摘要：

  公开号：

  EP3124482B1

文献信息

• Hexahydroimidazopyrazin-3-one compounds useful as modulators of androgen receptor function
  申请人：Balog Aaron James

  公开号：US20070088039A1

  公开（公告）日：2007-04-19

  The present invention is directed to compounds having the formula (I), and/or pharmaceutically-acceptable salts thereof, useful in the treatment of androgen-receptor associated conditions, wherein Ar is aryl, substituted aryl, heteroaryl, or substituted heteroaryl; L is a linker as defined in the specification; R 1 may be hydrogen, cyano, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclo, substituted heterocyclo, heteroaryl, or substituted heteroaryl, as defined in the specification; R 2 is hydrogen, lower alkyl, or substituted lower alkyl; and R 3 , R 4 and R 5 are optionally non-interfering substituents as defined in the specification.

  本发明涉及具有以下式(I)的化合物和/或其药学上可接受的盐，用于治疗雄激素受体相关疾病，其中Ar是芳基、取代芳基、杂芳基或取代杂芳基；L是规范中定义的连接物；R1可能是氢、氰基、烷基、取代烷基、芳基、取代芳基、环烷基、取代环烷基、杂环烷基、取代杂环烷基、杂芳基或取代杂芳基，如规范中所定义；R2是氢、较低烷基或取代较低烷基；R3、R4和R5是根据规范定义的可选的非干扰取代基。
• Novel aminoglycoside derivatives
  申请人：Shionogi & Co., Ltd.

  公开号：US04200628A1

  公开（公告）日：1980-04-29

  Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is acylated by a group represented by the formula: ##STR1## (wherein R is 4 to 6 membered heterocyclic group containing 1 to 2 nitrogen atoms which may optionally be substituted.) effective in treatment of infectious diseases caused by gram positive and gram negative bacteria.

  含有2-脱氧链霉素结构单元的新型氨基糖苷衍生物及其盐，其中1-氨基团被表示为以下式的基团酰化：##STR1##（其中R是含有1到2个氮原子的4到6元杂环基团，可选择性地被取代）。对治疗由革兰氏阳性和革兰氏阴性细菌引起的传染病有效。
• Composition Comprising An NK-1 Receptor Antagonist And An SSRI For The Treatment Of Tinnitus And Hearing Loss
  申请人：Christensen Soren Rahn

  公开号：US20100317666A1

  公开（公告）日：2010-12-16

  The present invention relates to methods for treating a subject suffering from tinnitus, hearing loss, or tinnitus and hearing loss comprising administering to the subject an effective amount of an NK1 receptor antagonist alone, or in combination with an effective amount of a selective serotonin reuptake inhibitor. Compositions and pharmaceutical formulations are also provided.

  本发明涉及治疗患有耳鸣、听力丧失或耳鸣和听力丧失的方法，包括向受试者单独或与选择性5-羟色胺再摄取抑制剂的有效量结合，给予有效量的NK1受体拮抗剂。同时还提供了组合物和药物配方。
• 2-(R)-(4-fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof
  申请人：Glaxo Group Limited

  公开号：US07652012B2

  公开（公告）日：2010-01-26

  The present invention relates to piperidine derivatives of formula (I) specifically 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof, useful in the treatment of conditions mediated by tachykinins.

  本发明涉及公式（I）的哌啶衍生物，特别是2-（R）-（4-氟-2-甲基苯基）-4-（S）-（（8aS）-6-氧代-六氢-吡咯[1,2-a]-吡嗪-2-基）-哌啶-1-羧酸[1-（R）-（3,5-双三氟甲基苯基）-乙基]-甲基酰胺酒石酸盐及其制药组合物，用于治疗由速激肽介导的疾病。
• [EN] PIPERIDINE DERIVATIVES<br/>[FR] DERIVES DE LA PIPERIDINE
  申请人：GLAXO GROUP LTD

  公开号：WO2003066635A1

  公开（公告）日：2003-08-14

  The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl; R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen , C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of condition mediated by tachykinins.

  本发明涉及式(I)的哌啶衍生物： R代表卤素或C1-4烷基；R1代表C1-4烷基；R2或R3独立地代表氢或C1-4烷基；R4代表三氟甲基、C1-4烷基、C1-4烷氧基、三氟甲氧基或卤素；R5代表氢、C1-4烷基或C3-7环烷基；R6为氢，R7为式(W)的基团：R6为式(W)的基团，R7为氢；X代表CH2、NR5或O；Y代表氮，Z为CH，或者Y代表CH，Z为氮；A代表C(O)或S(O)q，但当Y为氮，Z为CH时，A不是S(O)q；m为零或1到3的整数；n为1到3的整数；p和q独立地为1到2的整数；以及其药学上可接受的盐和溶剂化物。其制备方法及其在由Tachykinins介导的疾病治疗��的应用。