N-((1R)-1-{N-[(1R)-1-Benzyl-2-((2S)-2-((dimethylamino)methyl)pyrrolidin-1-yl)-2-oxoethyl]-N-methylcarbamoyl)-2-(2-naphthyl)ethyl)-N-methyl-3-((methylamino)methyl)benzamide | 254905-31-2

• 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
• 英文名称: N-((1R)-1-{N-[(1R)-1-Benzyl-2-((2S)-2-((dimethylamino)methyl)pyrrolidin-1-yl)-2-oxoethyl]-N-methylcarbamoyl)-2-(2-naphthyl)ethyl)-N-methyl-3-((methylamino)methyl)benzamide
• 英文别名: N-[(2R)-1-[[(2R)-1-[(2S)-2-[(dimethylamino)methyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-N-methyl-3-(methylaminomethyl)benzamide
• CAS: 254905-31-2
• 化学式: C₄₀H₄₉N₅O₃
• 分子量: 647.861
• InChiKey: GMVVFIATRLQYGY-HKIDPNTFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  48
• 可旋转键数：
  13
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  76.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  三氟乙酸 、 N-(3-[N-((1R)-1-{N-[(1R)-1-benzyl-2-((2S)-2-((dimethylamino)methyl)pyrrolidin-1-yl)-2-oxoethyl]-N-methylcarbamoyl}-2-(2-naphthyl)ethyl)-N-methylcarbamoyl]benzyl}-N-methylcarbamic acid tert-butyl ester 在 二氯甲烷 、 crude product 、 silica 作用下， 以 二氯甲烷 为溶剂， 反应 0.42h， 以to give 436 mg of the title compound的产率得到N-((1R)-1-{N-[(1R)-1-Benzyl-2-((2S)-2-((dimethylamino)methyl)pyrrolidin-1-yl)-2-oxoethyl]-N-methylcarbamoyl)-2-(2-naphthyl)ethyl)-N-methyl-3-((methylamino)methyl)benzamide
  参考文献：
  名称：

  Compounds with growth hormone releasing properties

  摘要：

  本发明涉及公式I的化合物，其中R1、R2、R5、R6、R7、R8、G、J、L、M、a、b、c、d、e和f如规范中所定义，并且含有这些化合物的组合物。这些化合物可用于治疗由生长激素缺乏引起的医学障碍。

  公开号：

  US06919315B1

文献信息

• [EN] COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES<br/>[FR] COMPOSES A PROPRIETES DE LIBERATION DE L'HORMONE DE CROISSANCE
  申请人：NOVO NORDISK AS

  公开号：WO2000001726A1

  公开（公告）日：2000-01-13

  The invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.

  该发明涉及新型化合物、含有它们的组合物以及它们用于治疗由生长激素缺乏引起的医疗障碍的用途。
• COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES
  申请人：NOVO NORDISK A/S

  公开号：EP1100824A1

  公开（公告）日：2001-05-23
• METHODS OF TREATING OR PREVENTING EMESIS USING GROWTH HORMONE SECRETAGOGUES
  申请人：Helsinn Therapeutics (U.S.), Inc.

  公开号：EP2146732A1

  公开（公告）日：2010-01-27
• Method of reducing C-reactive protein using growth hormone secretagogues
  申请人：Polvino J. William

  公开号：US20050261201A1

  公开（公告）日：2005-11-24

  The present invention relates to a method of reducing C-reactive protein in a subject in need of treatment thereof, wherein the subject is at risk of having or the subject has already had a vascular event or suffering from an inflammatory disease or disorder. In one embodiment, the vascular event is a cardiovascular event (e.g., myocardial infarction). In another embodiment, the vascular event is a cerebrovascular event (e.g., stroke (such as transient ischemic attacks (TIAs)). In yet another embodiment the vascular event is a peripheral vascular event (e.g., intermittent claudication). The method comprises administering a therapeutically effective amount of at least one growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. The growth hormone secretagogue can be coadministered with a second growth hormone secretagogue, HMG CoA reductase inhibitor, an ACAT inhibitor, a CETP inhibitor, an anti-inflammatory agent, an ACE inhibitor, a Beta blocker, a cholesterol absorption inhibitor, a nicotonic acid, a fibric acid derivative, a bile acid sequestering agent or a combination thereof.
• Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues
  申请人：Polvino J. William

  公开号：US20070191283A1

  公开（公告）日：2007-08-16

  The present invention relates to a method of stimulating the motility of the gastrointestinal system in a subject in need thereof, wherein the subject suffers from maladies (i.e., disorders or diseases) of the gastrointestinal system. The method comprises administering to a subject in need thereof a therapeutically effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. The growth hormone secretagogue can be co-administered with a laxative, a H 2 receptor antagonist, a serotonin 5-HT 4 agonist, an antacid, an opioid antagonist, a proton pump inhibitor, a motilin receptor agonist, dopamine antagonist, a cholinergic agonist, a cholinesterase inhibitor, somatostatin, octreotide, or any combination thereof.