2-amino-N-(1(R)-benzyloxymethyl-2-(1,3-dioxo-8a(S)-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-hexahydro-imidazo[1,5-a]pyrazin-7-yl)-2-oxo-ethyl)-2-methyl-propionamide | 218950-65-3

• 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-(1(R)-benzyloxymethyl-2-(1,3-dioxo-8a(S)-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-hexahydro-imidazo[1,5-a]pyrazin-7-yl)-2-oxo-ethyl)-2-methyl-propionamide
• 英文别名: N-[(2R)-1-[(8aS)-1,3-dioxo-8a-(pyridin-2-ylmethyl)-2-(2,2,2-trifluoroethyl)-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl]-1-oxo-3-phenylmethoxypropan-2-yl]-2-amino-2-methylpropanamide
• CAS: 218950-65-3
• 化学式: C₂₈H₃₃F₃N₆O₅
• 分子量: 590.602
• InChiKey: QJEAKIUFGOHGQJ-ZBLYBZFDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  42
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  138
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• Methods of treatment and kits comprising a growth hormone secretagogue
  申请人：——

  公开号：US20030105114A1

  公开（公告）日：2003-06-05

  The present invention relates to methods of treating bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or ameliorating ischemic nerve or muscle damage. The present invention also relates to kits that can be used in the treatment of bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or ameliorating ischemic nerve or muscle damage. The present invention further relates to increasing gastrointestinal motility after surgery and increasing gastrointestinal motility in patients who have been administered an agent that decreases gastrointestinal motility.

  本发明涉及治疗厌食症、男性勃起功能障碍、女性性功能障碍、甲状腺癌、乳腺癌或改善缺血性神经或肌肉损伤的方法。本发明还涉及可用于治疗厌食症、男性勃起功能障碍、女性性功能障碍、甲状腺癌、乳腺癌或改善缺血性神经或肌肉损伤的试剂盒。本发明还涉及术后增加胃肠道蠕动和在接受降低胃肠道蠕动试剂的患者中增加胃肠道蠕动。
• Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and a growth hormone secretagogue
  申请人：Lee G. Andrew

  公开号：US20050065180A1

  公开（公告）日：2005-03-24

  The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2-alkylidene-19-nor-vitamin D derivative and a growth hormone secretagogue or a pharmaceutically acceptable salt or prodrug thereof. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D 3 and a growth hormone secretagogue or a pharmaceutically acceptable salt or prodrug thereof.

  本发明涉及制药组合物和治疗方法，包括向需要的患者施用一种2-烷基亚甲基-19-去氢维生素D衍生物和生长激素分泌素或其药用盐或前药的组合物。特别地，本发明涉及制药组合物和治疗方法，包括向需要的患者施用2-亚甲基-19-去氢-20(S)-1α,25-二羟基维生素D3和生长激素分泌素或其药用盐或前药。
• 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。
• Process and intermediates for growth hormone secretagogues
  申请人：——

  公开号：US20020010335A1

  公开（公告）日：2002-01-24

  This invention relates to a process for preparing compounds of the Formula I, 1 wherein R 1 , R 2 and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R 1 is H, R 2 is 2,2,2-trifluoromethyl and Pt is Boc.

  本发明涉及一种制备式I，其中R1、R2和Pt如规范中所定义的化合物的过程，该化合物是某些生长激素分泌素化合物的合成中间体。本发明还涉及制备生长激素分泌素的过程。本发明还涉及式I的化合物，其中R1为H，R2为2,2,2-三氟甲基，Pt为Boc。
• Process and hydantoin intermediates for the synthesis of growth hormone secretagogues
  申请人：Pfizer Products Inc.

  公开号：EP1004583A2

  公开（公告）日：2000-05-31

  This invention relates to a process for preparing compounds of the Formula wherein R1, R2 and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R1 is H, R2 is 2,2,2-trifluoromethyl and Pt is Boc.

  本发明涉及一种制备式化合物的工艺。 其中 R1、R2 和 Pt 如说明书中所定义，它们是合成某些生长激素促泌剂化合物的中间体。本发明还涉及制备生长激素促泌剂的工艺。本发明还涉及式 I 的化合物，其中 R1 是 H，R2 是 2,2,2-三氟甲基，Pt 是 Boc。