2-amino-N-[3-(5-fluoro-1H-indol-3-yl)-1-(5-fluoro-1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxopropan-2-yl]-2-methylpropanamide

• 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-[3-(5-fluoro-1H-indol-3-yl)-1-(5-fluoro-1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxopropan-2-yl]-2-methylpropanamide
• 化学式: C₂₈H₃₃F₂N₅O₄S
• 分子量: 573.7
• InChiKey: GBUGJAAPZWCQRO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  40
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  137
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• [EN] ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE<br/>[FR] ANTAGONISTES DE LA GONADOLIBERINE
  申请人：MERCK & CO INC

  公开号：WO2000004013A1

  公开（公告）日：2000-01-27

  The present invention relates to compounds of formula (I) which are non-peptide antagonists of GnRH which can be used to treat a variety of sex-hormone related conditions in men and women, to methods for their preparation, and to methods and pharmaceutical compositions containing said compounds for use in mammals.

  本发明涉及式(I)的化合物，它们是GnRH的非肽拮抗剂，可用于治疗男性和女性的各种与性激素相关的疾病，以及它们的制备方法和包含所述化合物的方法和制药组合物，用于哺乳动物。
• [EN] COMBINATION OF BISPHOSPHONATES AND GROWTH HORMONE SECRETAGOGUES<br/>[FR] COMBINAISON DE BIPHOSPHONATES ET DE SECRETAGOGUES DE L'HORMONE DE CROISSANCE
  申请人：MERCK & CO., INC.

  公开号：WO1995011029A1

  公开（公告）日：1995-04-27

  (EN) Bisphosphonates in combination with growth hormone secretagogues reduce the deleterious effects of osteoporosis in elderly patients.(FR) Des biphosphonates administrés en combinaison avec des sécrétagogues d'hormone de croissance réduisent les effets néfastes de l'ostéoporose chez les patients âgés.

  （ZH）联合使用双磷酸盐和生长激素分泌剂可以减少老年患者骨质疏松症的不良影响。
• Spiro piperidines and homologs which promote release of growth hormone
  申请人：MERCK & CO. INC.

  公开号：EP0615977A1

  公开（公告）日：1994-09-21

  There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

  已公开的某些新型化合物被鉴定为螺哌啶和同源物，它们能促进人和动物体内生长激素的释放。这种特性可用于促进食用动物的生长，使可食用肉类产品的生产更有效率；在人类中，可用于治疗以生长激素分泌不足为特征的生理或医学病症，如生长激素缺乏症儿童的身材矮小，以及治疗因生长激素的同化作用而得到改善的医学病症。此外，还公开了含有此类螺化合物作为活性成分的生长激素释放组合物。
• ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE
  申请人：Merck & Co., Inc. (a New Jersey corp.)

  公开号：EP0873336B1

  公开（公告）日：2002-03-27
• EP0986557A4
  申请人：——

  公开号：EP0986557A4

  公开（公告）日：2001-03-14