2-Benzyl-2,3a,4,5,6,7-hexahydro-pyrazolo[4,3-c]pyridin-3-one hydrochloride | 193274-48-5

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 2-Benzyl-2,3a,4,5,6,7-hexahydro-pyrazolo[4,3-c]pyridin-3-one hydrochloride
• 英文别名: 2-benzyl-4,5,6,7-tetrahydro-3aH-pyrazolo[4,3-c]pyridin-3-one;hydrochloride
• CAS: 193274-48-5
• 化学式: C₁₃H₁₅N₃O*ClH
• 分子量: 265.743
• InChiKey: KVRPJMXBVVDDIQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.42
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  44.7
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Growth-hormone secretagogues
  申请人：——

  公开号：US20020049196A1

  公开（公告）日：2002-04-25

  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, 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 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，是生长激素分泌素，能够增加内源性生长激素的水平。本发明的化合物用于治疗和预防骨质疏松症、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、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、孕马血浆、以及可选的孕激素搭配使用时，也有用于治疗骨质疏松症的作用，或与降钙素一起使用，以及药学组合物的使用方法。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产生或释放的药学组合物，该组合物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。本发明还涉及用于制备公式I化合物的中间体。
• Treatment of insulin resistance with growth hormone secretagogues
  申请人：——

  公开号：US20030100561A1

  公开（公告）日：2003-05-29

  This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, 1 where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and the compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

  本发明涉及治疗哺乳动物胰岛素抵抗的方法，包括向该哺乳动物施用公式I，其中变量在说明书中定义的化合物的有效量，或其立体异构混合物、对映异构体富集物、对映异构体纯物、对映异构体纯物或其药学上可接受的盐和前药。公式I的化合物是生长激素分泌素，因此对于增加内源性生长激素水平非常有用。在另一个方面，本发明提供了某些中间体，这些中间体在合成上述化合物中非常有用，并且提供了某些合成上述中间体和公式I化合物的方法。本发明还涉及向人类或其他动物施用功能性生长抑素拮抗剂（如α-2肾上腺素受体激动剂）和公式I化合物的组合的方法。
• GROWTH-HORMONE SECRETAGOGUES
  申请人：PFIZER INC.

  公开号：EP0869968B1

  公开（公告）日：2007-05-02
• TREATMENT OF INSULIN RESISTANCE WITH GROWTH HORMONE SECRETAGOGUES
  申请人：Pfizer Products Inc.

  公开号：EP1000085B1

  公开（公告）日：2005-09-28
• US6107306A
  申请人：——

  公开号：US6107306A

  公开（公告）日：2000-08-22