2(R)-(2-Tert-Butoxycarbonylamino-2-Methyl-Propionylamino)-5-Phenyl-Pentanoic Acid | 871100-95-7

• 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(R)-(2-Tert-Butoxycarbonylamino-2-Methyl-Propionylamino)-5-Phenyl-Pentanoic Acid
• 英文别名: 2-(2-tert-Butoxycarbonylamino-2-methyl-propionylamino)-5-phenyl-pentanoic acid；2-[[2-Methyl-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-5-phenylpentanoic acid
• CAS: 871100-95-7
• 化学式: C₂₀H₃₀N₂O₅
• 分子量: 378.469
• InChiKey: RTKMPLVTYSYCTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  27
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  105
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2(R)-(2-Tert-Butoxycarbonylamino-2-Methyl-Propionylamino)-5-Phenyl-Pentanoic Acid 、 (R)-2-(4-Amino-imidazol-1-yl)-2-(4-methoxy-phenyl)-1-pyrrolidin-1-yl-propan-1-one 在 1-羟基苯并三唑 、 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 为溶剂， 反应 18.0h， 生成 [1-(1-{1-[1-(4-methoxy-phenyl)-1-methyl-2-oxo-2-pyrrolidin-1-yl-ethyl]-1H-imidazol-4-ylcarbamoyl}-4-phenyl-butylcarbamoyl)-1-methyl-ethyl]-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Method for treating emesis with ghrelin agonists

  摘要：

  本发明涉及一种方法，包括向被诊断为需要治疗恶心、呕吐或相关症状的患者施用化合物(I)的方法，其中：R1是C6H5CH2OCH2—、C6H5(CH2)3—或indol-3-ylmethyl;Y是吡咯烷基、4-甲基哌啶基或NR2R2;R2各自独立地是C1-C6烷基;R3是2-萘基或苯基对位取代W;W是H、F、CF3、C1-C6烷氧基或苯基; R4是H或CH3;或其药学上可接受的盐或溶剂，用于治疗该患者的恶心、呕吐或相关症状。

  公开号：

  US20050277677A1

文献信息

• Substituted dipeptides as growth hormone secretagogues
  申请人：——

  公开号：US20040058971A1

  公开（公告）日：2004-03-25

  This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for usein the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

  这项发明涉及一种新颖的化合物，可用于调节哺乳动物体内生长激素水平。该发明还涉及用于合成这些化合物的新颖中间体，以及用于这些合成过程的新颖方法。还包括治疗哺乳动物的方法，其中包括给予这些化合物的管理。
• 3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS
  申请人：Ambarkhane Ameet Vijay

  公开号：US20120302540A1

  公开（公告）日：2012-11-29

  The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.

  该发明涉及公式（I）的衍生物，其中取代基如规范中定义；制备这种衍生物的过程；包含这种衍生物的药物组合物；将这种衍生物作为药物；将这种衍生物用于治疗由胃泌素受体介导的疾病或障碍。
• 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。
• 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。
• 3-Spirocyclic Piperidine Derivatives as Ghrelin Receptor Agonists
  申请人：Ambarkhane Ameet Vijay

  公开号：US20130331369A1

  公开（公告）日：2013-12-12

  The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.

  本发明涉及公式（I）的衍生物，其中取代基如规范中所定义；制备此类衍生物的过程；包括此类衍生物的制药组合物；此类衍生物作为药物；此类衍生物用于治疗由胃饥饿素受体介导的紊乱或疾病。