7-氯-1,2,3,4-四氢-萘-1-胺盐酸盐 | 215315-62-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 7-氯-1,2,3,4-四氢-萘-1-胺盐酸盐
• 中文别名: 7-氟-四氢萘基-1-胺
• 英文名称: 7-fluoro-1,2,3,4-tetrahydronaphthalen-1-amine
• 英文别名: 7-fluoro-1,2,3,4-tetrahydro-naphthalen-1-ylamine；7-fluoro-1,2,3,4-tetrahydro-1-naphthylamine
• CAS: 215315-62-1
• 化学式: C₁₀H₁₂FN
• mdl: MFCD07373978
• 分子量: 165.21
• InChiKey: ZUUYTHBAQDOFSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-氯苯并咪唑 、 7-氯-1,2,3,4-四氢-萘-1-胺盐酸盐 在 (1H-benzoimidazol-2-yl)-(7-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)amine 作用下， 生成 (1H-benzoimidazol-2-yl)-(7-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)amine
  参考文献：
  名称：

  2-amino benzimidazole derivatives and their use as modulators of small-conductance calcium-activated potassium channels

  摘要：

  本发明涉及一种新型的2-氨基苯并咪唑衍生物，可用作小电导钙激活钾通道（SK通道）的调节剂。在其他方面，本发明涉及这些化合物在治疗方法中的使用，以及包含本发明化合物的制药组合物。

  公开号：

  US07737167B2
• 作为产物：
  描述：

  在 硼烷四氢呋喃络合物 作用下， 以 四氢呋喃 为溶剂， 生成 7-氯-1,2,3,4-四氢-萘-1-胺盐酸盐
  参考文献：
  名称：

  Synthesis and Structure−Activity Relationship Studies of 2-(N-Substituted)-aminobenzimidazoles as Potent Negative Gating Modulators of Small Conductance Ca²⁺-Activated K⁺ Channels

  摘要：

  Small conductance Ca2+-activated K+ channels (SK channels) participate in the control of neuronal excitability, in the shaping of action potential firing patterns, and in the regulation of synaptic transmission. SK channel inhibitors have the potential of becoming new drugs for treatment of various psychiatric and neurological diseases such as depression, cognition impairment, and Parkinson's disease. In the present study we describe the structure-activity relationship (SAR) of a class of 2-(N-substituted)-2-aminobenzimidazoles that constitute a novel class of selective SK channel inhibitors that, in contrast to classical SK inhibitors, do not block the pore of the channel. The pore blocker apamin is not displaced by these compounds in binding studies, and they still inhibit SK channels in which the apamin binding site has been abolished by point mutations. These novel SK inhibitors shift the concentration-response curve for Ca2+ toward higher values and represent the first example of negative gating modulation as a mode-of-action for inhibition of SK channels. The first described compound in this class is NS8593 (14), and the most potent analogue identified in this study is the racemic compound 39 (NS11757), which reversibly inhibits SK3-rnediated currents with a K-d value of 9 nM.

  DOI：

  10.1021/jm800809f

文献信息

• ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
  申请人：Centre National de la Recherche Scientifique

  公开号：US20210009581A1

  公开（公告）日：2021-01-14

  The present invention concerns a compound of following general formula (I): where: either R is an R 1 group and R′ is an -A 1 -Cy 1 group, or R is an -A 1 -Cy 1 group and R′ is an R 1 group, R 1 particularly being H or (C 1 -C 6 )alkyl group; A 1 being an —NH— radical or —NH—CH 2 — radical; Cy 1 particularly being a phenyl group, A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.

  本发明涉及以下一般式（I）的化合物： 其中： R是R1基团且R′是-A1-Cy1基团，或者R是-A1-Cy1基团且R′是R1基团， 其中R1特别是H或（C1-C6）烷基基团； A1是—NH—基团或—NH—CH2—基团； Cy1特别是苯基， A是具有5到7个原子的融合（杂）芳香环， 用于治疗癌症。
• [EN] 2,7,9-SUBSTITUTED PURINONE DERIVATIVES FOR IMMUNOSUPPRESSION<br/>[FR] DÉRIVÉS DE PURINONE SUBSTITUÉS EN POSITION 2, 7 ET 9 POUR L'IMMUNOSUPPRESSION
  申请人：PHARMACOPEIA INC

  公开号：WO2009048474A1

  公开（公告）日：2009-04-16

  The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula (I).

  本发明提供了一种新型的嘌呤酮和相关衍生物，用于预防和治疗自身免疫疾病、炎症性疾病、肥大细胞介导的疾病和移植排斥反应。这些化合物的一般结构式为（I）。
• Mapping the substrate scope of monoamine oxidase (MAO-N) as a synthetic tool for the enantioselective synthesis of chiral amines
  作者：Susanne Herter、Florian Medina、Simon Wagschal、Cyril Benhaïm、Friedemann Leipold、Nicholas J. Turner

  DOI：10.1016/j.bmc.2017.07.023

  日期：2018.4

  library of 132 racemic chiral amines (α-substituted methylbenzylamines, benzhydrylamines, 1,2,3,4-tetrahydronaphthylamines (THNs), indanylamines, allylic and homoallylic amines, propargyl amines) was screened against the most versatile monoamine oxidase (MAO-N) variants D5, D9 and D11. MAO-N D9 exhibited the highest activity for most substrates and was applied to the deracemisation of a comprehensive set

  针对最通用的单胺氧化酶（MAO-N）筛选了132种外消旋手性胺（α-取代的甲基苄基胺，二苯甲基胺，1,2,3,4-四氢萘胺（THNs），茚满胺，烯丙基和均烯丙基胺，炔丙基胺）的文库）变体D5，D9和D11。MAO-N D9对大多数底物都表现出最高的活性，并被用于脱脂一系列选定的伯胺。在所有情况下，均实现了优异的对映选择性（ee > 99％），产率中等至良好（55-80％）。使用THN作为模板处理底物负载，酶制剂的性质，缓冲液系统，硼烷源和有机助溶剂，可以进一步优化使用MAO-N /硼烷系统对伯胺进行脱氨的条件。
• [EN] BENZIMIDAZOLYL-ACETAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS<br/>[FR] DÉRIVÉS DE BENZIMIDAZOLYL-ACÉTAMIDE UTILES EN TANT QUE MODULATEURS DES CANAUX POTASSIQUES
  申请人：ACESION PHARMA APS

  公开号：WO2013104577A1

  公开（公告）日：2013-07-18

  This invention relates to novel benzimidazolyl-acetamide derivatives to formula (l) and their use as modulators of small-conductance calcium-activated potassium channels (SK channels). Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.

  本发明涉及一种新的苯并咪唑乙酰胺衍生物，其化学式为（l），并且它们的用途是作为小电导钙激活钾离子通道（SK通道）的调节剂。此外，本发明还涉及用于治疗或缓解与钾离子通道活性相关的疾病或疾病的药物组合物。
• Novel 2-amino benzimidazole derivatives and their use as modulators of small-conductance calcium-activated potassium channels
  申请人：Sorensen Svane Ulrik

  公开号：US20070197618A1

  公开（公告）日：2007-08-23

  This invention relates to novel 2-amino benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

  本发明涉及一种新颖的2-氨基苯并咪唑衍生物，可用作小电导钙激活钾通道（SK通道）的调节剂。在其他方面，本发明涉及这些化合物在治疗方法中的使用，以及包含本发明化合物的制药组合物。