尔法来星 | 60173-73-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 尔法来星
• 中文别名: 阿法拉新
• 英文名称: abamectin
• 英文别名: Succinamoyl-Arg-Val-Tyr-Val-His-Pro-Phegly；arfalasin；(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-amino-4-oxobutanoyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-2-phenylacetic acid
• CAS: 60173-73-1
• 化学式: C₄₈H₆₇N₁₃O₁₁
• 分子量: 1002.14
• InChiKey: IBGNPQRJAXAGJH-MBNHCIONSA-N

物化性质

• 密度：
  1.43±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  72
• 可旋转键数：
  27
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  389
• 氢给体数：
  12
• 氢受体数：
  13

文献信息

• [EN] COCRYSTALS OF PTEROSTILBENE AND COMPOSITIONS COMPRISING THEM<br/>[FR] CO-CRISTAUX DE PTÉROSTILBÈNE ET COMPOSITIONS COMPRENANT CEUX-CI
  申请人：CENTER FOR INTELLIGENT RES IN CRYSTAL ENGINEERING S L

  公开号：WO2021123162A1

  公开（公告）日：2021-06-24

  The present disclosure relates to a cocrystal of pterostilbene and a coformer capable to form hydrogen bond interactions, to a process for the preparation thereof, and to its use as a medicament or a dietary supplement. The present disclosure also relates to a composition comprising the cocrystal.

  本公开涉及一种可形成氢键相互作用的紫檀酸甲酯和共晶体形成物，其制备过程及其作为药物或膳食补充剂的用途。本公开还涉及包含该共晶体的组合物。
• Process for preparing schiff base adducts of amines with o-hydroxy aldehydes and compositions of matter based thereon
  申请人：——

  公开号：US20030125528A1

  公开（公告）日：2003-07-03

  An improved process is described for preparing Schiff base condensation adduct final products whose components comprise a protein having beneficial activity in animals, and an aromatic o-hydroxy aldehyde, which comprises bringing together the above-mentioned components in an aqueous environment at a pH of 7.0 or higher to form a reaction mixture, under conditions effective to drive said condensation reaction substantially to completion by removing from about 97.0% to about 99.9% by weight, preferably from about 98.0% to about 99.0% by weight of the water already present or produced during said condensation reaction, consistent with maintaining the integrity of the condensation reactants and adduct final product, and to assure a rate of conversion to said condensation adduct final product, i.e., with resulting yield of said condensation adduct final product of equal to or greater than about 98.5% by weight, preferably equal to or greater than about 99.5% by weight based on the weight of the reactants. Preferred aromatic o-hydroxy aldehydes comprise o-vanillin; salicylaldehyde; 2,3-dihydroxybenzaldehyde; 2,6-dihydroxybenz-aldehyde; 2-hydroxy-3-ethoxybenzaldehyde; or pyridoxal. A very wide range of proteins may be employed. The improved process provides yields over 90% and substantially quantitative conversion of the aldehyde and protein to the condensation adduct.

  本文描述了一种改进的方法，用于制备Schiff碱缩合加合物的最终产物，其组分包括在动物中具有有益活性的蛋白质和芳香族o-羟基醛。该方法包括在pH为7.0或更高的水环境中将上述组分结合在一起以形成反应混合物，通过有效的条件将缩合反应驱动到几乎完成，其中从已有的水分中或在缩合反应期间产生的水分中除去大约97.0%到99.9%的重量，最好是从98.0%到99.0%的重量，保持缩合反应物和加合物最终产物的完整性，并确保转化为所述缩合加合物最终产物的速率，即所得缩合加合物最终产物的产率等于或大于约98.5%的重量，最好等于或大于约99.5%的重量，基于反应物的重量。首选的芳香族o-羟基醛包括邻香草醛；水杨醛；2,3-二羟基苯甲醛；2,6-二羟基苯甲醛；2-羟基-3-乙氧基苯甲醛；或吡哆醛。可以使用非常广泛的蛋白质。改进的方法提供了超过90%的产率和几乎定量的醛和蛋白质转化为缩合加合物。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Disubstituted and trisubstituted 1,2,3-triazoles as Wnt inhibitors
  申请人：The Board of Regents of the University of Texas System

  公开号：US10793544B2

  公开（公告）日：2020-10-06

  The present disclosure provides compounds that may be useful for inhibiting Wnt pathway comprising compounds of the formula: (Ia) or (Ib) wherein the variables are as defined herein. In some aspects, the compounds may be used to inhibit the Wnt pathway and used to treat cancer, myocardial infarction, osteopetrosis, or used in the maturation of a precursor cell to a mature cell. Also provided herein in are pharmaceutical compositions of the compounds described herein.

  本公开提供了可用于抑制 Wnt 通路的化合物，其中包括式：(Ia)或(Ib)，其中变量如本文所定义。在某些方面，这些化合物可用于抑制 Wnt 通路，并用于治疗癌症、心肌梗塞、骨质疏松，或用于前体细胞向成熟细胞的成熟。本文还提供了本文所述化合物的药物组合物。
• IMPROVED PROCESS FOR PREPARING SCHIFF BASE ADDUCTS OF AMINES WITH O-HYDROXY ALDEHYDES AND COMPOSITIONS OF MATTER BASED THEREON
  申请人：Pfizer Products Inc.

  公开号：EP1087989A1

  公开（公告）日：2001-04-04