1-((2R)-2-{N-[(2E)4-(1-aminocyclobutyl)but-2-enoyl]-N-methylamino}-3-(biphenyl-4-yl)propionyl)4-benzylpiperidine-4-carboxylic acid methylamide

• 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: 1-((2R)-2-{N-[(2E)4-(1-aminocyclobutyl)but-2-enoyl]-N-methylamino}-3-(biphenyl-4-yl)propionyl)4-benzylpiperidine-4-carboxylic acid methylamide
• 英文别名: 1-{(2R)-2-[N-((2E)-5-Amino-3,5-dimethylhex-2-enoyl)-N-methylamino]-3(biphenyl-4-yl)propionyl}-4-benzylpiperidine-4-carboxylic acid methylamide；1-[(2R)-2-[[(E)-5-amino-3,5-dimethylhex-2-enoyl]-methylamino]-3-(4-phenylphenyl)propanoyl]-4-benzyl-N-methylpiperidine-4-carboxamide
• 化学式: C₃₈H₄₈N₄O₃
• 分子量: 608.824
• InChiKey: PESFKWCDTBEUTE-GWGREKCHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  45
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  95.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (2R)-3-(1,1'-biphenyl-4-yl)-2-(N-tert-butoxycarbonyl-N-methylamino)propionic acid 以 (2E)-5-(tert-butyloxycarbonylamino)-5,3-dimethyl-2-hexenoic acid 为溶剂， 生成 1-((2R)-2-{N-[(2E)4-(1-aminocyclobutyl)but-2-enoyl]-N-methylamino}-3-(biphenyl-4-yl)propionyl)4-benzylpiperidine-4-carboxylic acid methylamide
  参考文献：
  名称：

  Compounds with growth hormone releasing properties

  摘要：

  本发明涉及式I的4,4-二取代和3,3-二取代的哌啶化合物，其中D、E、G、J、R1、a、b、c和d在规范中有定义，包含它们的组合物以及它们用于治疗由于生长激素缺乏引起的医学障碍的用途。

  公开号：

  US06303620B1

文献信息

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

  公开号：WO1999058501A1

  公开（公告）日：1999-11-18

  (EN) The present invention relates to novel compounds, in particular 4,4-disubstituted and 3,3-disubstituted piperidine compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.(FR) La présente invention concerne de nouveaux composés, en particulier des composés de pipéridine 4,4-disubstitué et de 3,3-disubstitué, des compositions contenant ces composés, et l'utilisation desdits composés pour traiter des troubles médicaux résultant d'une déficience d'hormone de croissance.

  （中文）本发明涉及新型化合物，特别是4,4-二取代和3,3-二取代哌啶化合物，以及包含它们的组合物，以及它们用于治疗由于生长激素缺乏引起的医学障碍的用途。
• COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES
  申请人：NOVO NORDISK A/S

  公开号：EP1077941B1

  公开（公告）日：2009-08-12
• METHOD OF REDUCING C-REACTIVE PROTEIN USING GROWTH HORMONE SECRETAGOGUES
  申请人：Sapphire Therapeutics, Inc.

  公开号：EP1735055A1

  公开（公告）日：2006-12-27
• METHOD OF TREATING CELL PROLIFERATIVE DISORDERS USING GROWTH HORMONE SECRETAGOGUES
  申请人：Helsinn Therapeutics (U.S.), Inc.

  公开号：EP2134341A2

  公开（公告）日：2009-12-23
• 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.