Zanapezil fumarate | 142852-51-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: Zanapezil fumarate
• 英文别名: 3-(1-benzylpiperidin-4-yl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)propan-1-one;(E)-but-2-enedioic acid
• CAS: 142852-51-5；263248-42-6
• 化学式: C29H36N2O5
• 分子量: 492.6
• InChiKey: CWEHWZPCDBRUNO-WLHGVMLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.02
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  107
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-(4-piperidinyl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-1-propanone 以76的产率得到Zanapezil fumarate
  参考文献：
  名称：

  Condensed heterocyclic compounds, their production and use

  摘要：

  一种公式（I）的缩合杂环衍生物：##STR1## 其中X是氧原子、硫原子或R.sup.1 -N<，其中R.sup.1是氢原子、可取代的碳氢基团或可取代的酰基基团；R.sup.2是氢原子或可取代的碳氢基团；环A是苯环，可取代；k是0至3的整数；m是1至8的整数；n是1至6的整数；或其药学上可接受的盐，具有高胆碱酯酶抑制活性，以及其制备方法。

  公开号：

  US05273974A1

文献信息

• COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND CHOLINESTERASE INHIBITORS
  申请人：WATTERSON D. Martin

  公开号：US20120157410A1

  公开（公告）日：2012-06-21

  The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.

  本发明涉及含有吡啶二氮化合物和胆碱酯酶抑制剂的组合物、共轭物和方法，用于调节细胞途径（例如，信号转导途径），用于治疗或预防炎症性疾病（例如，阿尔茨海默病），用于研究、药物筛选和治疗应用。
• Tablets with improved abrasion resistance and method to produce them
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：EP0610854A1

  公开（公告）日：1994-08-17

  A compression-moldable composition comprising an active ingredient, an excipient and an oily or fatty substance having a lower melting point of about 20 to 90°C is compression-molded into uncoated tablets without coating to improve the abrasion resistance. The oily or fatty substance includes a higher fatty acid or a salt thereof, a wax, a fatty acid ester, a hardened oil, a polyalkylene oxide, etc., and the amount thereof is about 0.01 to 10% by weight. The composition may comprise (1) a granulated powder containing the active ingredient and the excipient, and the powdery or granular oily or fatty substance having a lower melting point, or (2) a granulated powder containing the active ingredient, the excipient and said oily or fatty substance. Compression-molding of the composition improves the abrasion resistance of the tablet and significantly inhibits the development of powder by wearing or abrasion even when the oily or fatty substance is used in a small amount of about 0.1 to 0.5% by weight.

  一种由活性成分、赋形剂和熔点较低的油性或脂肪性物质（熔点约为 20 至 90°C）组成的可压模塑组合物，可压模塑成无包衣片剂，无需包衣以提高耐磨性。油性或脂肪性物质包括高级脂肪酸或其盐、蜡、脂肪酸酯、硬化油、聚环氧烷等，其用量约为 0.01 至 10%（按重量计）。组合物可包括：(1) 含有活性成分和赋形剂的粒状粉末，以及具有较低熔点的粉状或粒状油性或脂肪物质；或 (2) 含有活性成分、赋形剂和所述油性或脂肪物质的粒状粉末。即使油性或脂肪性物质的用量较少，约为 0.1%至 0.5%（按重量计），该组合物的压缩成型也能提高片剂的耐磨性，并显著抑制因磨损或磨蚀而产生的粉末。
• Punch and die
  申请人：——

  公开号：US20020024166A1

  公开（公告）日：2002-02-28

  An object of the present invention is to provide a punch or die having excellent corrosion resistance and releasing property which is suitable for a tablet machine particularly for the production of tablets containing corrosive substance(s) and adhesive substance(s). Thus, the present invention relates to a punch or die for compressing granules to prepare tablets, where a high-silicon steel is used as a basis material.

  本发明的目的是提供一种冲头或模具，它具有优异的耐腐蚀性和脱模性，适用于片剂机，特别是用于生产含有腐蚀性物质和粘性物质的片剂。因此，本发明涉及一种用于压缩颗粒以制备片剂的冲头或模具，其中使用高硅钢作为基础材料。
• High throughput functional genomics
  申请人：——

  公开号：US20030065452A1

  公开（公告）日：2003-04-03

  This invention focuses on the marriage of solid-state electronics and neuronal function to create a new high-throughput electrophysiological assay to determine a compound's acute and chronic effect on cellular function. Electronics, surface chemistry, biotechnology, and fundamental neuroscience are integrated to provide an assay where the reporter element is an array of electrically active cells. This innovative technology can be applied to neurotoxicity, and to screening compounds from combinatorial chemistry, gene function analysis, and basic neuroscience applications. The system of the invention analyzes how the action potential is interrupted by drugs or toxins. Differences in the action potentials are due to individual toxins acting on different biochemical pathways, which in turn affects different ion channels, thereby changing the peak shape of the action potential differently for each toxin. Algorithms to analyze the action potential peak shape differences are used to indicate the pathway(s) affected by the presence of a new drug or compound; from that, aspects of its function in that cell are deduced. This observation can be exploited to determine the functional category of biochemical action of an unknown compound. An important aspect of the invention is surface chemistry that permits establishment of a high impedance seal between cell and a metal microelectrode. This seal recreates the interface that enables functional patch-clamp electrophysiology with glass micropipettes, and allows extracellular electrophysiology on a microelectrode array. Thus, the invention teaches the feasibility of using living cells as diagnostics for high throughput real-time assays of cell function.

  本发明的重点是将固态电子学与神经元功能相结合，创造出一种新的高通量电生理学检测方法，以确定化合物对细胞功能的急性和慢性影响。电子学、表面化学、生物技术和基础神经科学融为一体，提供了一种以电活性细胞阵列为报告元件的检测方法。这项创新技术可应用于神经毒性、组合化学化合物筛选、基因功能分析和基础神经科学应用。本发明的系统可分析药物或毒素如何干扰动作电位。动作电位的差异是由于不同的毒素作用于不同的生化途径，进而影响不同的离子通道，从而使每种毒素的动作电位峰值形状发生不同的变化。分析动作电位峰值形状差异的算法可用于指出受新药或化合物影响的途径，并由此推断其在该细胞中的功能。这种观察结果可用于确定未知化合物的生化作用功能类别。本发明的一个重要方面是表面化学，可在细胞和金属微电极之间建立高阻抗密封。这种密封再现了可使用玻璃微量移液管进行功能性膜片钳电生理学研究的界面，并可在微电极阵列上进行细胞外电生理学研究。因此，本发明证明了将活细胞作为诊断设备用于高通量实时细胞功能测试的可行性。
• Pharmaceutical composition for neurotrophic action
  申请人：——

  公开号：US20030130262A1

  公开（公告）日：2003-07-10

  The present invention provides a composition for neurotrophic action which comprises a compound of the formula: 1 wherein Ar is an optionally condensed phenyl group which may be substituted; n is an integer of 1 to 10; R is a hydrogen atom or a hydrocarbon group which may be substituted; and Y is an amino group which may be substituted or a nitrogen-containing saturated heterocyclic group which may be substituted; or a salt thereof, which compounds are useful for preventing and/or treating (1) neurodegenerative diseases (e.g. senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, Creutzfelt-Jakob disease, amyotrophic lateral sclerosis, diabetic neuropathy, etc.), (2) neuropathy in cerebrovascular diseases (e.g. impairment of cerebral blood flow based on cerebral infarction, cerebral hemorrhage, cerebral sclerosis, etc.), brain trauma, spiral cord injury, cerebritis sequela and cerebral palsy, (4) mental diseases (e.g. depression, panic disorder, schizophrenia, etc.), etc.

  本发明提供了一种具有神经营养作用的组合物，该组合物包含一种式化合物： 1 其中 Ar 是可被取代的任选缩合苯基； n 是 1 至 10 的整数； R 是氢原子或可被取代的烃基；以及 Y 是可被取代的氨基或可被取代的含氮饱和杂环基团；或其盐、 其中的化合物可用于预防和/或治疗 (1) 神经退行性疾病（如老年痴呆症、阿尔茨海默病、唐氏综合征、帕金森病、克雅氏病、肌萎缩性脊髓侧索硬化症、糖尿病神经病变等），(2) 脑血管疾病中的神经病变（如脑血流障碍、脑卒中、颅内出血等），(3) 中枢神经系统疾病中的神经病变（如颅内出血、颅内感染等），(4) 中枢神经系统疾病中的神经病变（如颅内出血、颅内感染等）。(2) 脑血管疾病（如脑梗塞、脑出血、脑硬化症等引起的脑血流障碍）、脑外伤、脊髓损伤、脑膜炎后遗症和脑瘫引起的神经病变；(4) 精神疾病（如抑郁症、惊恐障碍、精神分裂症等）等。