4a-Benzyl-octahydro-3-oxa-1,6-diaza-naphthalen-2-one | 218953-02-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 4a-Benzyl-octahydro-3-oxa-1,6-diaza-naphthalen-2-one
• 英文别名: 4a-benzyl-4,5,6,7,8,8a-hexahydro-1H-pyrido[4,3-d][1,3]oxazin-2-one
• CAS: 218953-02-7
• 化学式: C₁₄H₁₈N₂O₂
• 分子量: 246.309
• InChiKey: JZYKIHGJGGTQGQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Dipeptide derivatives
  申请人：——

  公开号：US20010041703A1

  公开（公告）日：2001-11-15

  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-H-T920. 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，这些化合物是生长激素分泌促进剂，可以增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松和/或衰弱、充血性心力衰竭、与衰老有关的衰弱、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恢复；改善肌肉力量、运动能力、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（如阿伦膦酸）、雌激素、预马林和可选孕激素、雌激素激动剂或拮抗剂或降钙素联合使用时，也可用于治疗骨质疏松和/或衰弱，以及用于该用途的药物组合物。此外，本发明还涉及用于增加人类或其他动物内源性生长激素的产生或释放的药物组合物，该组合物包括本发明化合物的有效量和从GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-H-T920中选择的生长激素分泌促进剂。本发明还涉及用于制备公式I化合物的中间体。
• DIPEPTIDE DERIVATIVES AS GROWTH HORMONE SECRETAGOGUES
  申请人：PFIZER INC.

  公开号：EP1001970A1

  公开（公告）日：2000-05-24
• 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