(2S)-2-氨基-5-[(2-碘乙酰基)氨基]戊酸 | 35748-65-3

• 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
• 中文名称: (2S)-2-氨基-5-[(2-碘乙酰基)氨基]戊酸
• 中文别名: (S)-(+)-2-氨基-5-(碘乙酰氨基)戊酸；NΔ-碘乙酰基-L-鸟氨酸
• 英文名称: (+)-S-2-amino-5-iodoacetamidopentanoic acid
• 英文别名: (S)-(+)-2-amino-5-iodoacetamidopentanoic acid；N(sup 5)-(Iodoacetyl)-L-ornithine；(2S)-2-amino-5-[(2-iodoacetyl)amino]pentanoic acid
• CAS: 35748-65-3
• 化学式: C₇H₁₃IN₂O₃
• 分子量: 300.096
• InChiKey: ZDWGLSKCVZNFLT-YFKPBYRVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2924199090

反应信息

• 作为产物：
  描述：

  L-鸟氨酸 、 4-硝基苯酯碘乙酸 在 copper(II) carbonate 、 sodium hydroxide 作用下， 生成 (2S)-2-氨基-5-[(2-碘乙酰基)氨基]戊酸
  参考文献：
  名称：

  Olomucki,M. et al., Bulletin de la Societe Chimique de France, 1971, p. 4524 - 4525

  摘要：

  DOI：

文献信息

• Use of L-arginine optionally combined with magnesium for the treatment of sickle cell disease and/or pulmonary hypertension
  申请人：Children's Hospital & Research Center at Oakland

  公开号：EP2397128A1

  公开（公告）日：2011-12-21

  The invention features methods and compositions for treatment of conditions associated with decreased nitric oxide bioavailability, such as a condition associated with elevated arginase activity, using an arginine-based therapy, including combination therapy with an arginase inhibitor and/or magnesium

  本发明的特点是使用基于精氨酸的疗法，包括与精氨酸酶抑制剂和/或镁的联合疗法，来治疗与一氧化氮生物利用率降低有关的病症，如与精氨酸酶活性升高有关的病症的方法和组合物。
• ARGINASE AS BIOMARKER AND DRUG TARGET FOR PCOS
  申请人：Johann Wolfgang Goethe-Universität Frankfurt am Main

  公开号：EP3696281A1

  公开（公告）日：2020-08-19

  The invention is based on the surprising finding that in women with polycystic ovary syndrome (PCOS) an increased activity and/or expression of arginase is detected. The invention uses therefore various arginase associated biomarkers as indicators for the occurrence with the disease. More importantly the invention describes genetic variations associated with increased arginase expression/activity, and further being associated with PCOS. Hence, the invention provides enzymatic, immunological, and genetic diagnostic approaches for the detection and monitoring of PCOS in a subject. Furthermore the invention shows that the causal link of PCOS and arginase activity and hence provides the use of arginase inhibitors as a treatment approach.

  本发明基于一个惊人的发现，即在患有多囊卵巢综合症（PCOS）的妇女体内，发现精氨酸酶的活性和/或表达量增加。因此，本发明使用各种与精氨酸酶相关的生物标志物作为疾病发生的指标。更重要的是，本发明描述了与精氨酸酶表达/活性增加相关的遗传变异，并进一步与多囊卵巢综合症相关。因此，本发明提供了用于检测和监测受试者多囊卵巢综合症的酶学、免疫学和遗传学诊断方法。此外，本发明还表明了多囊卵巢综合症与精氨酸酶活性之间的因果关系，因此提供了使用精氨酸酶抑制剂的治疗方法。
• Electrospraying formation of particles including agents
  申请人：Elektrofi, Inc.

  公开号：US11077059B2

  公开（公告）日：2021-08-03

  The invention provides methods for the preparation of particles including one or more agents, e.g., therapeutic or diagnostic agents. The particles can be formed by creating droplets of a first liquid, e.g., including an agent, and removing the first liquid, e.g., through its dispersal in a second liquid and/or evaporation, to solidify the droplets. Advantageously, the process of forming the particles does not significantly alter the structure or activity of the agents and may enhance the stability of the agents. For example, the particles may be stored for long periods of time without significant loss of activity, and in some embodiments, without the need for refrigeration. These particles may be used to generate stabilized pharmaceutical compositions for storage or other logistical purposes, pharmaceutical suspensions, pharmaceutical powder formulations (e.g., inhalable powders, injectable powders), creams or other topical pastes, nutraceuticals, or cosmetics.

  本发明提供了制备包括一种或多种药剂（如治疗或诊断药剂）的颗粒的方法。颗粒的形成可以通过制造第一种液体的液滴，例如包括一种药剂，然后除去第一种液体，例如通过将其分散在第二种液体中和/或蒸发，使液滴凝固。有利的是，形成颗粒的过程不会明显改变药剂的结构或活性，并可提高药剂的稳定性。例如，颗粒可长期储存而不会明显丧失活性，在某些实施方案中，还无需冷藏。这些微粒可用于生产用于储存或其他物流目的的稳定药物组合物、药用悬浮液、药用粉末制剂（如可吸入粉末、可注射粉末）、膏霜或其他外用膏剂、营养保健品或化妆品。
• Metal salts and uses thereof
  申请人：Inspirna, Inc.

  公开号：US11174220B2

  公开（公告）日：2021-11-16

  The present invention relates to metal salts of 2-[3-[(3R)-3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]butoxy]phenyl]acetic acid which exhibit improved physical properties and stability. The invention also relates to pharmaceutical compositions including an effective amount of the metal salts, as well as methods of treating cancer including administration of a pharmaceutical composition including a salt of the invention to a subject in need thereof.

  本发明涉及 2-[3-[(3R)-3-[[2-氯-3-(三氟甲基)苯基]甲基-(2,2-二苯基乙基)氨基]丁氧基]苯基]乙酸的金属盐，其物理性质和稳定性均有所改善。本发明还涉及包括有效量金属盐的药物组合物，以及治疗癌症的方法，包括向有需要的受试者施用包括本发明盐的药物组合物。
• Polymorphs and uses thereof
  申请人：Inspirna, Inc.

  公开号：US11214536B2

  公开（公告）日：2022-01-04

  The present invention relates to new polymorphs of LXRβ agonists which exhibit improved physical properties. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of an LXRβ agonist, as well as methods of treating cancer including administration of a formulation including an LXRβ agonist to a subject in need thereof.

  本发明涉及 LXRβ 激动剂的新多晶型，其物理性质有所改善。本发明还涉及包括药学有效量的 LXRβ 激动剂的药物组合物，以及治疗癌症的方法，包括向有需要的受试者施用包括 LXRβ 激动剂的制剂。