1-Amino-1,3,3-trimethylcyclohexane

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-Amino-1,3,3-trimethylcyclohexane
• 英文别名: 1,3,3-trimethylcyclohexylamine；1,3,3-Trimethylcyclohexan-1-amine
• 化学式: C₉H₁₉N
• 分子量: 141.257
• InChiKey: QTXWDXKTMLBHIW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  3,3-二甲基环己酮 在 lithium aluminium tetrahydride 、 三(2-氯乙基)胺 、 四氯化钛 作用下， 以 乙醚 、 氯仿 为溶剂， 反应 30.0h， 生成 1-Amino-1,3,3-trimethylcyclohexane
  参考文献：
  名称：

  Synthesis and structure–affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site

  摘要：

  A series of 1,3,5-alkylsubstituted cyclohexylamines 2 were synthesized as ligands for the N-methyl-D-aspartate (NMDA) receptor phencyclidine (PCP) binding site. Pure diastereomers with defined configuration of amino group 2-ax and 2-eq were obtained. The optimal size of 1,3,5-substituents was determined for cyclohexylamines 2 with an equatorial amino group in the lowest energy conformation using Hansch analysis. According to the data, the lipophilic part of cyclohexylamines 2 does not discriminate between hydrophobic regions of the PCP binding site but rather recognizes this site as a whole lipophilic pocket. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

  DOI：

  10.1016/s0223-5234(00)00153-7

文献信息

• Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
  申请人：——

  公开号：US20040087658A1

  公开（公告）日：2004-05-06

  The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.

  该发明涉及一种新型药物组合疗法，可用于治疗痴呆，包括给予一种1-氨基环己烷衍生物，如美万特或奈拉美喜，以及一种乙酰胆碱酯酶抑制剂（AChEI），如加兰他明、他克林、多奈哌齐或利伐替明。
• Novel treatment for alzheimer's disease
  申请人：EPFL Ecole Polytechnique Fédérale de Lausanne

  公开号：EP2111858A1

  公开（公告）日：2009-10-28

  The present invention concerns a new pharmaceutical composition comprising an antagonist and a co-agonist of the N-methyl-D-aspartate-type glutamate receptor (NMDAR). The inventors found that the co-administration of these two compounds effectively inhibits production of amyloide-β peptide. In patient's suffering from Alzheimer's disease, these peptides are deposited in the extracellular matrix forming neuritic "plaques". Therefore, the present inventors identified a new possibility for prophylaxis and/or treatment of Alzheimer's disease by stopping the continued formation of neuropathological extracellular deposits.

  本发明涉及一种新的药物组合物，包括N-甲基-D-天门冬氨酸型谷氨酸受体（NMDAR）的拮抗剂和共激动剂。发明人发现这两种化合物的联合使用有效地抑制了淀粉样β肽的产生。在患有阿尔茨海默病的患者中，这些肽沉积在细胞外基质中形成神经突起“斑块”。因此，本发明人发现了一种新的预防和/或治疗阿尔茨海默病的可能性，即通过阻止神经病理性细胞外沉积物的持续形成。
• METHODS OF TREATING CNS DISORDERS
  申请人：PAPADAKIS Kelly

  公开号：US20090275597A1

  公开（公告）日：2009-11-05

  The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.

  本发明涉及治疗各种中枢神经系统疾病的方法，例如躁狂症、双相情感障碍和精神分裂症，通过单独或与多巴胺受体拮抗剂联合给予NMDA受体拮抗剂。
• [EN] 1-AMINOVYCLOHEXANE DERIVATIVES FOR THE TREATMENT OF AGITATION AND OTHER BEHAVIORAL DISORDERS, ESPECIALLY THOSE ASSOCIATED WITH ALZHEIMER'S DISEASE<br/>[FR] DERIVES DE 1-AMINOCYCLOHEXANE POUR LE TRAITEMENT DE L'AGITATION ET D'AUTRES TROUBLES DU COMPORTEMENT, EN PARTICULIER CEUX QUI SONT ASSOCIES A LA MALADIE D'ALZHEIMER
  申请人：MERZ PHARMA GMBH & CO KGAA

  公开号：WO2005084655A1

  公开（公告）日：2005-09-15

  The present invention relates to the treatment of behavioral disorders, especially agitation, associated with a central nervous system (CNS) disorder, especially Alzheimer's disease (AD), cerebrovascular disease (VaD), or Down's Syndrome, in a mammal, comprising administering to said mammal an 1-aminocyclohexane, alone or in combination with a acetylcholinesterase inhibitor. In one embodiment, the 1-aminocyclohexane is memantine.

  本发明涉及治疗行为障碍，特别是与中枢神经系统（CNS）疾病相关的激动不安，特别是阿尔茨海默病（AD），脑血管疾病（VaD）或唐氏综合症，在哺乳动物中治疗，包括给予该哺乳动物1-氨基环己烷，单独或与乙酰胆碱酯酶抑制剂联合使用。在一种实施方式中，1-氨基环己烷是美金刚烷。
• [EN] THE USE OF 1-AMINOCYCLOHEXANE DERIVATIVES TO MODIFY DEPOSITION OF FIBRILLOGENIC Aß PEPTIDES IN AMYLOIDOPATHIES<br/>[FR] UTILISATION DE DERIVES DE 1-AMINOCYCLOHEXANE POUR MODIFIER LE DEPOT DE PEPTIDES A DOLLAR G(B) FIBRILLOGENES DANS DES AMYLOIDOPATHIES
  申请人：MERZ PHARMA GMBH & CO KGAA

  公开号：WO2005079779A1

  公开（公告）日：2005-09-01

  The invention relates to the use of NMDA receptor antagonists such as 1-aminocyclohexane derivatives to modify deposition of potentially toxic and fibrillogenic Aß peptides in amyloidopathies. Specifically, the invention relates to the ability of memantine to intervene in the processing of APP and decrease the levels of fibrillogenic Aß peptides.

  本发明涉及使用NMDA受体拮抗剂，如1-氨基环己烷衍生物，以改变淀粉样病变中潜在有毒和纤维化Aß肽的沉积。具体而言，本发明涉及美金刚烷干预APP处理并降低纤维化Aß肽水平的能力。