(1-{1(R)-Benzyloxymethyl-2-[8a(S)-(4-fluoro-benzyl)-7.7-dimethyl-6,8-dioxo-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl]-2-oxo-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester | 218953-55-0

• 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-{1(R)-Benzyloxymethyl-2-[8a(S)-(4-fluoro-benzyl)-7.7-dimethyl-6,8-dioxo-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl]-2-oxo-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester
• 英文别名: tert-butyl N-[1-[[(2R)-1-[(8aS)-8a-[(4-fluorophenyl)methyl]-7,7-dimethyl-6,8-dioxo-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-1-oxo-3-phenylmethoxypropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]carbamate
• CAS: 218953-55-0
• 化学式: C₃₅H₄₅FN₄O₇
• 分子量: 652.763
• InChiKey: GRCPWIDRJPOVRA-IJAHGLKVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  47
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.51
• 拓扑面积：
  134
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  3(R)-benzyloxy-2-(2-tert-butoxycarbonylamino-2-methyl-propionyl-amino)-propionic acid 、 8a-(4-Fluoro-benzyl)-7,7-dimethyl-tetrahydro-pyrrolo[1,2-a]pyrazine-6,8-dione 、 碳酸氢钠 生成 (1-{1(R)-Benzyloxymethyl-2-[8a(S)-(4-fluoro-benzyl)-7.7-dimethyl-6,8-dioxo-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl]-2-oxo-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Dipeptide derivatives
  申请人：——

  公开号：US20030216399A1

  公开（公告）日：2003-11-20

  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化合物及其药学上可接受的盐，其中取代基如规范中定义，它们是生长激素促分泌剂，可以增加内源性生长激素水平。本发明的化合物用于治疗和预防骨质疏松和/或虚弱、充血性心力衰竭、与衰老相关的虚弱、肥胖症；加速骨折修复、减轻重大手术后的蛋白质分解反应、减少慢性疾病引起的消瘦和蛋白质丢失、加速伤口愈合，或加速烧伤患者或接受重大手术的患者的恢复；改善肌肉力量、运动能力、皮肤厚度的维持、代谢稳态或肾脏稳态。本发明的化合物在与双膦酸盐类化合物（如阿伦膦酸）、雌激素、孕激素和选择性雌激素受体调节剂或拮抗剂、降钙素组合使用时，也可用于治疗骨质疏松和/或虚弱，并提供了相应的药物组合。此外，本发明还涉及对人类或其他动物内源性生长激素的生产或释放量进行增加的药物组合，其中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的生长激素促分泌剂。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