4-[2-羟基-3-[(异丙基)氨基]丙氧基]苯基乙酰胺盐酸盐 | 51706-40-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-[2-羟基-3-[(异丙基)氨基]丙氧基]苯基乙酰胺盐酸盐
• 中文别名: 香豆素,5,6-二羟基-4,7-二甲基-(6CI)
• 英文名称: Atenolol hydrochloride
• 英文别名: Hydron;2-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide;chloride；hydron;2-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide;chloride
• CAS: 51706-40-2
• 化学式: C₁₄H₂₂N₂O₃*ClH
• 分子量: 302.801
• InChiKey: FFDDLJYKJQGSPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.87
• 重原子数：
  20
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  84.6
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-[2-羟基-3-[(异丙基)氨基]丙氧基]苯基乙酰胺盐酸盐 在 盐酸 、 sodium nitrite 作用下， 反应 6.0h， 以86%的产率得到4-[2-羟基-3-[(1-甲基乙基)亚硝基氨基]丙氧基]苯乙酰胺
  参考文献：
  名称：

  Mazzei; Sottofattori; Balbi, Il Farmaco, 1991, vol. 46, # 9, p. 1043 - 1049

  摘要：

  DOI：

文献信息

• THERAPEUTIC PEPTIDES
  申请人：Strom Morten

  公开号：US20130035296A1

  公开（公告）日：2013-02-07

  The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

  本发明提供了一种具有至少+2的净正电荷并且包含二取代β氨基酸的肽、肽类似物或氨基酸衍生物，β氨基酸中的每个取代基（可能相同也可能不同）包括至少（7）个非氢原子，具有亲脂性并且至少有一个环状基团，一个或多个取代基内的环状基团可以连接或融合到另一个取代基内的一个或多个环状基团中，当环状基团以这种方式融合时，两个取代基的非氢原子的总数至少为（12），用作溶细胞治疗剂；以及这些分子的非治疗用途以及从该定义中确定的某些新化合物。
• Crystalline forms of sartans like telmisartan with beta blockers
  申请人：Laboratorios del. Dr. Esteve, S.A.

  公开号：EP2649996A1

  公开（公告）日：2013-10-16

  The present invention relates to crystalline forms comprising telmisartan and at least one beta blocker, especially a selective β1 receptor blocker, especially to salts or co-crystals of telmisartan and a beta blocker, preferably selected from selective β1 receptor blockers, processes for preparation of the same and their use as medicament or in pharmaceutical formulations, more particularly for the treatment of hypertension, heart failure and myocardial infarction.

  本发明涉及包含替米沙坦和至少一种β受体阻滞剂的结晶形式，特别是选择性β1受体阻滞剂，尤其是替米沙坦和β受体阻滞剂的盐或共晶，优选从选择性β1受体阻滞剂中选择，以及其制备方法和作为药物或制药配方的用途，更具体地用于治疗高血压、心力衰竭和心肌梗塞。
• HIGH PENETRATION COMPOSITIONS AND USES THEREOF
  申请人：Yu Chongxi

  公开号：US20090238763A1

  公开（公告）日：2009-09-24

  The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for non-steroidal anti-inflammatory agents (NSAIAs), which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes. For example, the HPPs can be locally delivered to an action site of a condition with a high concentration due to their ability of penetrating biological barriers and thus obviate the need for a systematic administration. For another example, the HPPs herein can be systematically administer to a biological subject and enter the general circulation with a faster rate.

  本发明涉及新型高渗透性组合物或高渗透性前药（HPP）的组成和用途，特别是用于非甾体抗炎药（NSAIAs）的HPP，其能够高效地穿过生物屏障。这里的HPP能够在穿过生物屏障后转化为父活性药物或药物代谢物，从而可以治疗与父药物或代谢物相关的疾病。此外，由于能够穿过生物屏障，这里的HPP能够到达父药物可能无法进入或无法在目标区域产生足够浓度的区域，从而提供新的治疗方法。这里的HPP可以通过各种给药途径给予受试者。例如，由于其穿透生物屏障的能力，HPP可以在局部给药到疾病作用部位并以高浓度存在，从而避免系统性给药的需要。另一个例子是，这里的HPP可以被系统性地给药到生物体内，并以更快的速率进入循环系统。
• MATRIX-TYPE CONTROLLED RELEASE PREPARATION COMPRISING BASIC SUBSTANCE OR SALT THEREOF, AND PROCESS FOR PRODUCTION OF THE SAME
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP1832298A1

  公开（公告）日：2007-09-12

  A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution /dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

  本发明提供了一种基质型缓释制剂及其制造方法，在该制剂中，可在溶出试验中确保碱性药物或其盐在溶出初期以较低的 pH 值溶解，并且随着溶出试验的进行、碱性药物或其盐在酸性试验溶液中的溶出率与碱性药物或其盐在中性试验溶液中的溶出率之比（酸性试验溶液中的溶出率/中性试验溶液中的溶出率）在溶出后期随溶出时间的延长而降低，与溶出初期相比。根据本发明，基质型缓释制剂含有碱性药物或其盐和至少一种肠道聚合物，其中碱性药物或其盐在 0.1 N 盐酸溶液和 pH 值为 6.0 的中性水溶液中的溶解度高于在 pH 值为 8.0 的碱性水溶液中的溶解度。
• Dry-binders for tablets based on polyethylene glycol-polyvinyl alcohol graft polymers, the production and use thereof
  申请人：BASF SE

  公开号：US11154508B2

  公开（公告）日：2021-10-26

  A finely divided binder in powder form consisting of a polyethylene glycol-polyvinyl alcohol graft polymer particles, wherein the particles have an average particle size D[4,3] in the range of from 10 to 70 μm.

  由聚乙二醇-聚乙烯醇接枝聚合物颗粒组成的粉末状精细粘结剂，其中颗粒的平均粒径 D[4,3] 在 10 到 70 μm 之间。