N-甲氧基-1-(1-甲基-5,6-二氢-2H-吡啶-3-基)甲烷亚胺盐酸盐 | 139886-04-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: N-甲氧基-1-(1-甲基-5,6-二氢-2H-吡啶-3-基)甲烷亚胺盐酸盐
• 中文别名: N-[1-(3’-苄氧基苯基)乙基]-N-甲基胺
• 英文名称: Milameline hydrochloride
• 英文别名: CI-979；milameline；(E)-N-methoxy-1-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)methanimine;hydrochloride
• CAS: 139886-04-7
• 化学式: C₈H₁₄N₂O*ClH
• 分子量: 190.673
• InChiKey: WEBMRZODPLSRKR-MLBSPLJJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  24.8
• 氢给体数：
  1
• 氢受体数：
  3

制备方法与用途

盐酸米拉梅林（CI 979）是一种毒蕈碱受体激动剂，能够改善认知功能。

反应信息

• 作为产物：
  描述：

  甲氧基胺盐酸盐 、 1-methyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde hydrochloride 以 水 为溶剂， 反应 1.0h， 以54%的产率得到N-甲氧基-1-(1-甲基-5,6-二氢-2H-吡啶-3-基)甲烷亚胺盐酸盐
  参考文献：
  名称：

  1-Alkyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-alkyl-oximes: a new class of potent orally active muscarinic agonists related to arecoline

  摘要：

  On the basis of the knowledge acquired from basic studies of several known arecoline derivatives about the structural requirements for potent agonistic activity and oral efficacy, a series of 1-alkyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-alkyl-oximes was synthesized and biologically evaluated in a battery of in vitro and in vivo assays. The most interesting molecules to emerge from the primary screening, 1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-methyloxime hydrochloride (11, RU 35963), 1-methyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-methyloxime hydrochloride (12, RU 35926), and 1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-propargyloxime hydrochloride (30, RU 47029) and 1-methyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde-O-propargyloxime hydrochloride (33, RU 35986), were evaluated more extensively, and their cholinomimetic profile was compared with that of the parent molecule, arecoline. The pharmacological results after oral administration to mice and rats revealed that their efficacy is 2-3 orders of magnitude higher than that of arecoline, and, in addition, they show a longer duration of action. The 4 aldoximes showed anti-amnesic properties in many respects superior to those of arecoline. Their anti-amnesic doses were 2 orders of magnitude lower than those inducing obvious cholinergic symptoms, and 3-5 orders of magnitude lower than the lethal doses. These new compounds can be regarded as potential candidates for clinical studies in AD (Alzheimer's disease) patients.

  DOI：

  10.1016/0223-5234(91)90128-a

文献信息

• [EN] BENZAMIDE COMPOUNDS AND THEIR USE AS HERBICIDES<br/>[FR] COMPOSÉS DE BENZAMIDE ET LEUR UTILISATION EN TANT QU'HERBICIDES
  申请人：BASF SE

  公开号：WO2019016385A1

  公开（公告）日：2019-01-24

  The present invention relates to benzamide compounds of the formula (I) and the N-oxides and salts thereof and to compositions comprising the same. The variables are as defined in the claims and the description. The invention also relates to the use of the benzamide compounds or of the compositions comprising such compounds for controlling unwanted vegetation. Furthermore, the invention relates to methods of applying such compounds.

  本发明涉及公式（I）的苯甲酰胺化合物及其N-氧化物和盐，以及包含它们的组合物。变量如权利要求和说明书中所定义。本发明还涉及使用苯甲酰胺化合物或包含这种化合物的组合物来控制不良植被。此外，本发明还涉及应用这种化合物的方法。
• Compositions and methods for the detection of mycobacterium kansasii
  申请人：GEN-PROBE INCORPORATED

  公开号：EP0808907A2

  公开（公告）日：1997-11-26

  The featured invention discloses and claims oligonucleotide hybridization assay probes and helper oligonucleotides which are designed to be complementary to specific regions of M. kansasii rRNA or the DNA encoding it, or to an oligonucleotide or nucleic acid comprising, consisting essentially of, or consisting of, a M. kansasii rRNA or rDNA nucleotide sequence. The hybridization probes of the present invention are designed to hybridize to a target nucleic acid in a region of the molecule having a specific target nucleotide sequence under conditions which allow the selective detection of the target nucleic acid. The probes are further designed to detect M. kansasii typical as well as atypical strains. The present invention also discloses and claims double-stranded nucleic acid hybrid molecules formed between the hybridization probes and their specific target nucleic acids.

  本发明公开并要求寡核苷酸杂交检测探针和辅助寡核苷酸，这些探针和辅助寡核苷酸被设计成与堪萨斯氏菌rRNA或编码它的DNA的特定区域互补，或与由堪萨斯氏菌rRNA或rDNA核苷酸序列组成、基本上由其组成或由其组成的寡核苷酸或核酸互补。 本发明的杂交探针被设计成在分子中具有特定靶核苷酸序列的区域与靶核酸杂交，杂交条件允许选择性地检测靶核酸。探针还可用于检测典型和非典型堪萨斯霉菌株。 本发明还公开并声称了杂交探针与其特定靶核酸之间形成的双链核酸杂交分子。
• Muscarinic combinations and their use for combating hypocholinergic disorders of the central nervous system
  申请人：Chase Pharmaceuticals Corporation

  公开号：US10307409B2

  公开（公告）日：2019-06-04

  A combination of a muscarinic cholinergic receptor agonist, a non-anticholinergic antiemetic agent and a non-selective, peripheral anticholinergic agent for the treatment of hypocholinergic disorders of the central nervous system.

  一种毒蕈碱胆碱能受体激动剂、一种非抗胆碱能止吐药和一种非选择性外周抗胆碱能药的复方制剂，用于治疗中枢神经系统的低胆碱能紊乱。
• PHARMACEUTICAL COMPOSITIONS COMPRISING CYCLODEXTRIN INCLUSION COMPLEXES OF THE COMPOUND CI-979
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0681471A1

  公开（公告）日：1995-11-15
• PERIPHERAL-ANTICHOLINERGIC MUSCARINIC AGONIST COMBINATION
  申请人：Chase Pharmaceuticals Corporation

  公开号：EP3265466A1

  公开（公告）日：2018-01-10