2-amino-N-{(1R)-2-[3-benzyl-3-(N,N',N'-trimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)-2-oxoethyl)}-2-methylpropionamide | 1048978-11-5

• 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: 2-amino-N-{(1R)-2-[3-benzyl-3-(N,N',N'-trimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)-2-oxoethyl)}-2-methylpropionamide
• 英文别名: 2-amino-N-{(1R)-2-[3-benzyl-3-(N,N',N'-trimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)methyl)-2-oxoethyl}-2-methylpropionamide；2-amino-N-[(2R)-1-[3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide
• CAS: 1048978-11-5
• 化学式: C₃₁H₄₂N₆O₃
• 分子量: 546.713
• InChiKey: VQPFSIRUEPQQPP-SYQKMTEESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  40
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] CRYSTAL FORMS OF (3R)-1-(2-METHYLALANYL-D-TRYPTOPHYL)-3-(PHENYLMETHYL)-3-PIPERIDINECARBOXYLIC ACID 1,2,2-TRIMETHYLHYDRAZIDE<br/>[FR] FORMES CRISTALLINES D'ACIDE (3R)-1-(2-METHYLALANYL-D-TRYPTOPHYL)-3-(PHENYLMETHYL)-3-PIPERIDINECARBOXYLIQUE 1,2,2-TRIMETHYLHYDRAZIDE
  申请人：SAPPHIRE THERAPEUTICS INC

  公开号：WO2006016995A1

  公开（公告）日：2006-02-16

  Crystalline polymorphs of (3 R)-1-(2-methylalanyl-D-tryptophyl)-3­ (phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.

  本发明揭示了作为药物剂的(3R)-1-(2-甲基丙氨酰-D-色氨酸基)-3-(苯甲基)-3-哌嗪羧酸1,2,2-三甲基肼的结晶多晶形态。本发明还揭示了制备和分离这些多晶形态的方法，以及包括这些多晶形态的药物组合物和药物治疗方法。本发明的晶体多晶形态是有用的，因为它们直接作用于垂体细胞以释放生长激素。
• Crystal forms of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide
  申请人：Helsinn Therapeutics (U.S.), Inc.

  公开号：EP2298760A1

  公开（公告）日：2011-03-23

  Crystalline polymorphs of (3 R)-1-(2-methylalanyl-D-tryptophyl)-3 (phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.

  本发明公开了可用作药剂的(3 R)-1-(2-甲基丙氨酰-D-色氨酰)-3(苯基甲基)-3-哌啶羧酸 1,2,2-三甲基肼的结晶多晶体。还公开了这些多晶型物的生产和分离方法以及包括这些多晶型物的药物组合物和药物治疗方法。本发明的结晶多晶物直接作用于垂体细胞，释放生长激素，因此非常有用。
• 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
• CRYSTAL FORMS OF (3R)-1-(2-METHYLALANYL-D-TRYPTOPHYL)-3-(PHENYLMETHYL)-3-PIPERIDINECARBOXYLIC ACID 1,2,2-TRIMETHYLHYDRAZIDE
  申请人：Sapphire Therapeutics, Inc.

  公开号：EP1768976A1

  公开（公告）日：2007-04-04
• Growth Hormone Secretagogue Receptor Type 1A Agonists
  申请人：Andersen Bansholm Maibritt

  公开号：US20070066540A1

  公开（公告）日：2007-03-22

  Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.