{1-[2-(8a(S)-Benzyl-2-methyl-3-oxo-hexahydro-imidazo[1,5-a]pyrazin-7-yl)-1-(R)-benzyloxymethyl-2-oxo-ethylcarbamoyl]-1-methyl-ethyl}-carbamic acid tert-butyl ester | 218952-59-1

• 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: {1-[2-(8a(S)-Benzyl-2-methyl-3-oxo-hexahydro-imidazo[1,5-a]pyrazin-7-yl)-1-(R)-benzyloxymethyl-2-oxo-ethylcarbamoyl]-1-methyl-ethyl}-carbamic acid tert-butyl ester
• 英文别名: tert-butyl N-[1-[[(2R)-1-[(8aS)-8a-benzyl-2-methyl-3-oxo-1,5,6,8-tetrahydroimidazo[1,5-a]pyrazin-7-yl]-1-oxo-3-phenylmethoxypropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]carbamate
• CAS: 218952-59-1
• 化学式: C₃₃H₄₅N₅O₆
• 分子量: 607.75
• InChiKey: PVMMJUXMYCWIDL-UTONBFNKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  44
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  121
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Dipeptide derivatives
  申请人：——

  公开号：US20020002165A1

  公开（公告）日：2002-01-03

  This invention is directed to compounds of the formula 1 and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

  本发明涉及公式1的化合物及其药学上可接受的盐，其中取代基如规范中所定义，它们是生长激素分泌素，可以增加内源性生长激素水平。本发明的化合物可用于治疗和预防骨质疏松和/或虚弱，充血性心力衰竭，与衰老有关的虚弱，肥胖症；加速骨折修复，减轻重大手术后的蛋白质分解反应，减少因慢性病而引起的消瘦和蛋白质流失，加速伤口愈合，或加速烧伤患者或接受重大手术的患者的康复；改善肌肉力量，机动性，皮肤厚度维持，代谢稳态或肾脏稳态。本发明的化合物在与双磷酸盐化合物（如阿仑膦酸盐）、雌激素、孕马素和可选的孕激素受体激动剂或拮抗剂、降钙素联合使用时，也可用于治疗骨质疏松和/或虚弱，以及其药学组合物的制备方法。此外，本发明还涉及一种在人类或其他动物中增加内源性生长激素产生或释放的药物组合物，其包括本发明化合物的有效量和选择自GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-HT920的生长激素分泌素。本发明还涉及制备公式I化合物的中间体。
• DIPEPTIDE DERIVATIVES AS GROWTH HORMONE SECRETAGOGUES
  申请人：PFIZER INC.

  公开号：EP1001970B1

  公开（公告）日：2007-03-07
• US6251902B1
  申请人：——

  公开号：US6251902B1

  公开（公告）日：2001-06-26
• US6429313B2
  申请人：——

  公开号：US6429313B2

  公开（公告）日：2002-08-06
• US6432945B1
  申请人：——

  公开号：US6432945B1

  公开（公告）日：2002-08-13