4-(2-胺乙基)吡啶盐酸盐 | 6429-12-5

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 4-(2-胺乙基)吡啶盐酸盐
• 中文别名: 4-(2-氨基乙基)吡啶盐酸盐
• 英文名称: 4-Pyridineethanamine dihydrochloride
• 英文别名: 2-[4]pyridyl-ethylamine; dihydrochloride；2-[4]Pyridyl-aethylamin; Dihydrochlorid；2-Pyridin-4-ylethylazanium;chloride
• CAS: 6429-12-5；17039-03-1；92334-02-6
• 化学式: C₇H₁₀N₂*2ClH
• 分子量: 195.092
• InChiKey: GQGKWQYHIZXREV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.0
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  38.9
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2933399090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  苯乙酸 、 4-(2-胺乙基)吡啶盐酸盐 在 吡啶 、 三氯化磷 作用下， 生成 phenyl-acetic acid-(2-[4]pyridyl-ethylamide)
  参考文献：
  名称：

  试图模拟士的宁的生物发生。第二部分 3-（2-4'-吡啶基乙酰胺基乙基）吲哚的制备和转化

  摘要：

  DOI：

  10.1039/jr9550002586

文献信息

• [EN] SUBSTITUTED PYRIDONES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP)<br/>[FR] PYRIDONES SUBSTITUES INHIBITEURS DE LA POLY(ADP-RIBOSE) POLYMERASE (PARP)
  申请人：AVENTIS PHARMA INC

  公开号：WO2005097750A1

  公开（公告）日：2005-10-20

  The present invention discloses and claims a series of 2,3,5-substituted pyridone derivatives as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5'-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

  本发明公开并声明了一系列如下定义的2,3,5-取代吡啶酮衍生物。本发明还涉及制备这些化合物的方法。本发明的化合物是多聚腺苷酸二磷酸核糖酶（PARP）的抑制剂，因此在制药剂中特别用于治疗和/或预防各种疾病，包括与中枢神经系统和心血管疾病相关的疾病。
• SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS
  申请人：CZECHTIZKY Werngard

  公开号：US20130065859A1

  公开（公告）日：2013-03-14

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的取代2-(色甘醇-6-氧基)-噻唑衍生物，其中Ar、R2、R3和R4如权利要求中所定义。式I的化合物是钠-钙交换蛋白（NCX）的抑制剂，特别是亚型1的钠-钙交换蛋白（NCX1），适用于处理细胞内钙离子稳态受扰的各种疾病，如心律失常、心力衰竭和中风。本发明还涉及制备式I的化合物的方法，它们作为药物的用途，以及包含它们的药物组合物。
• Chemical Derivatization of Peptide Carboxyl Groups for Highly Efficient Electron Transfer Dissociation
  作者：Brian L. Frey、Daniel T. Ladror、Samuel B. Sondalle、Casey J. Krusemark、April L. Jue、Joshua J. Coon、Lloyd M. Smith

  DOI：10.1007/s13361-013-0701-2

  日期：2013.11.1

  The carboxyl groups of tryptic peptides were derivatized with a tertiary or quaternary amine labeling reagent to generate more highly charged peptide ions that fragment efficiently by electron transfer dissociation (ETD). All peptide carboxyl groups—aspartic and glutamic acid side-chains as well as C-termini—were derivatized with an average reaction efficiency of 99 %. This nearly complete labeling avoids making complex peptide mixtures even more complex because of partially-labeled products, and it allows the use of static modifications during database searching. Alkyl tertiary amines were found to be the optimal labeling reagent among the four types tested. Charge states are substantially higher for derivatized peptides: a modified tryptic digest of bovine serum albumin (BSA) generates ~90% of its precursor ions with z  >  2, compared with less than 40 % for the unmodified sample. The increased charge density of modified peptide ions yields highly efficient ETD fragmentation, leading to many additional peptide identifications and higher sequence coverage (e.g., 70 % for modified versus only 43 % for unmodified BSA). The utility of this labeling strategy was demonstrated on a tryptic digest of ribosomal proteins isolated from yeast cells. Peptide derivatization of this sample produced an increase in the number of identified proteins, a >50 % increase in the sequence coverage of these proteins, and a doubling of the number of peptide spectral matches. This carboxyl derivatization strategy greatly improves proteome coverage obtained from ETD-MS/MS of tryptic digests, and we anticipate that it will also enhance identification and localization of post-translational modifications.

  使用叔胺或季胺标记试剂对胰蛋白酶肽的羧基进行衍生，以产生电荷更高的肽离子，从而通过电子转移解离（ETD）有效地进行碎裂。所有肽的羧基--天冬氨酸和谷氨酸侧链以及 C 端--都进行了衍生，平均反应效率为 99%。这种近乎完全的标记避免了因部分标记产物而使复杂的多肽混合物变得更加复杂，而且还可以在数据库搜索时使用静态修饰。在测试的四种试剂中，烷基叔胺是最佳的标记试剂。衍生肽的电荷状态要高得多：经修饰的牛血清白蛋白（BSA）胰蛋白酶消化物产生的前体离子中约有 90% 的 z > 2，而未经修饰的样品则不到 40%。修饰肽离子电荷密度的增加产生了高效的 ETD 片段，从而增加了许多肽的鉴定率和更高的序列覆盖率（例如，修饰肽离子的鉴定率为 70%，而未修饰 BSA 的鉴定率仅为 43%）。从酵母细胞中分离出来的核糖体蛋白质的胰蛋白酶消化物证明了这种标记策略的实用性。对该样本进行肽衍生处理后，鉴定出的蛋白质数量增加了，这些蛋白质的序列覆盖率提高了 50%以上，肽谱匹配的数量也增加了一倍。这种羧基衍生化策略大大提高了从胰蛋白酶消化物的 ETD-MS/MS 中获得的蛋白质组覆盖率，我们预计它还将提高翻译后修饰的鉴定和定位。
• Antipruritics
  申请人：Yasui Kiyoshi

  公开号：US20050101590A1

  公开（公告）日：2005-05-12

  It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.

  这意味着它旨在提供止痒药（用于控制瘙痒的药物，抗瘙痒剂和止痒药）。研究发现，具有激动性作用的大麻素受体的化合物具有止痒效果。
• 2-oxoquinoline compounds and pharmaceutical uses thereof
  申请人：——

  公开号：US20030191069A1

  公开（公告）日：2003-10-09

  A 2-oxoquinoline compound or its pharmaceutically acceptable salt of general formula [I]: 1 (wherein each symbol in the formula is as determined in the description), and its pharmaceutical use. The compound [I] of the present invention and its pharmaceutically acceptable salts selectively act on cannabinoid receptors, particularly on peripheral type cannabinoid receptors, and have fewer side effects on the central nervous system, having great immunosuppressive action, anti-inflammatory action or antiallergic action. Therefore, these compounds are useful as cannabinoid receptors (particularly peripheral type cannabinoid receptors) modulator, immunosuppressants, anti-inflammatory agents, and antiallergic agents.

  一种2-氧基喹啉化合物或其药学上可接受的盐，其通式为[I]:1（其中公式中的每个符号如说明中所确定的那样），以及其医药用途。本发明的化合物[I]及其药学上可接受的盐，能够选择性地作用于大麻素受体，特别是外周型大麻素受体，并且对中枢神经系统的副作用较少，具有很强的免疫抑制作用、抗炎作用或抗过敏作用。因此，这些化合物可用作大麻素受体（特别是外周型大麻素受体）调节剂、免疫抑制剂、抗炎剂和抗过敏剂。