N²-methyl-DL-ornithine | 7431-86-9

• 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: N²-methyl-DL-ornithine
• 英文别名: N²-Methyl-DL-ornithin；N²-Methyl-ornithin；N-Me-Orn-OH；5-amino-2-(methylamino)pentanoic acid
• CAS: 7431-86-9
• 化学式: C₆H₁₄N₂O₂
• mdl: MFCD19205072
• 分子量: 146.189
• InChiKey: OZRWQPFBXDVLAH-UHFFFAOYSA-N

物化性质

• 熔点：
  82-100 °C
• 沸点：
  277.8±35.0 °C(Predicted)
• 密度：
  1.082±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -3.1
• 重原子数：
  10
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N²-methyl-DL-ornithine 、 2-甲基-2-疏基硫酸脲 在 sodium hydroxide 作用下， 生成 N^α-methyl-DL-arginine
  参考文献：
  名称：

  Izumiya, Nippon Kagaku Zasshi, 1951, vol. 72, p. 550

  摘要：

  DOI：
• 作为产物：
  描述：

  L-精氨酸 在 barium dihydroxide 、 barium carbonate 作用下， 生成 N²-methyl-DL-ornithine
  参考文献：
  名称：

  Zimmermann; Canzanelli, Hoppe-Seyler's Zeitschrift fur Physiologische Chemie, 1933, vol. 219, p. 207,210

  摘要：

  DOI：

文献信息

• [EN] ANTI-MICROBIAL AGENT-POLYMER CONJUGATES AND METHODS OF USE THEREOF<br/>[FR] CONJUGUÉS D'AGENT ANTIMICROBIEN-POLYMÈRE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：UNIV CALIFORNIA

  公开号：WO2018195078A1

  公开（公告）日：2018-10-25

  The present disclosure provides a conjugate comprising an anti-microbial agent and a hydrophilic polymer; and compositions, including pharmaceutical compositions, comprising the conjugates. The present disclosure provides a conjugate comprising a polymyxin covalently linked to a maltodextrin polymer; and compositions, including pharmaceutical compositions, comprising the conjugates. The present disclosure provides methods of inhibiting growth of a bacterium, and methods of treating a bacterial infection.

  本公开提供了一种包含抗微生物剂和亲水性聚合物的共轭物；以及包括药物组合物在内的组合物。本公开提供了一种包含共价连接到麦芽糖聚合物的多粘菌素的共轭物；以及包括药物组合物在内的组合物。本公开提供了抑制细菌生长的方法，以及治疗细菌感染的方法。
• [EN] NOVEL CYP-EICOSANOID DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS CYP-ÉICOSANOÏDE
  申请人：MAX DELBRÜCK CT FÜR MOLEKULARE MEDIZIN

  公开号：WO2015110262A1

  公开（公告）日：2015-07-30

  The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias.

  本发明涉及一般式（I）的化合物，这些化合物是由细胞色素P450（CYP）酶从ω-3（n-3）多不饱和脂肪酸（PUFAs）产生的环氧代谢产物的类似物。本发明还涉及含有这些化合物中的一个或多个的组合物，以及利用这些化合物或组合物治疗或预防与炎症、增殖、高血压、凝血、免疫功能、病理性血管生成、心力衰竭和心律失常相关的疾病和症状。
• POTENT AND SELECTIVE INHIBITORS OF NAV1.7
  申请人：AMGEN INC

  公开号：US20160024159A1

  公开（公告）日：2016-01-28

  Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Na V 1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Na V 1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

  本文揭示了一种物质组合物，包括一种孤立的多肽，该多肽是一种外周限制的NaV1.7抑制剂。在一些公开的实施方式中，这种孤立的多肽是NaV1.7的抑制剂。其他实施方式是该物质组合物的共轭实施方式和含有该物质组合物的药物组合物。还揭示了编码一些创新多肽的孤立核酸和表达载体以及含有它们的重组宿主细胞。还揭示了一种治疗或预防疼痛的方法。
• [EN] METHOD FOR PREPARATION OF DIFLUOROMETHYLORNITHINE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DIFLUOROMÉTHYLORNITHINE
  申请人：LONZA AG

  公开号：WO2019057951A1

  公开（公告）日：2019-03-28

  The invention discloses a method for preparation of protected difluoromethylornithine by a difluoromethylation of dibenzaldimine ornithine ester using CHF3 and LiHMDS (lithium bis(trimethylsilyl)amide), which can be converted to a salt of unprotected difluoromethylornithine by a subsequent deprotection under acidic conditions in the presence of water.

  该发明揭示了一种通过使用CHF3和LiHMDS（双(三甲基硅基)胺锂）对二苯基二亚苄基鸟氨酸酯进行二氟甲基化而制备受保护二氟甲基鸟氨酸的方法，该方法可在水存在的酸性条件下进行后续去保护反应，将其转化为未受保护二氟甲基鸟氨酸的盐。
• POLYMYXIN DERIVATIVES AND USES THEREOF
  申请人：VAARA Martti Sakari

  公开号：US20090215677A1

  公开（公告）日：2009-08-27

  The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a subject, caused by a Gram-negative bacterium by administering a therapeutically effective amount of a derivative according to the present invention to said subject; to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; for reducing the nephrotoxicity, for improving the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. Finally, the invention relates to a process for preparing such polymyxin derivatives.

  本发明涉及一种聚霉素衍生物，其中R1，R2和R3是可选的，而R1、R2、R3、R5、R8和R9是阳离子或中性氨基酸残基，选定这些残基使得在生理pH下正电荷总数至少为两个但不超过三个；以及包含至少两种这种衍生物的组合物。本发明还涉及一种通过向受体内给予本发明所述的衍生物的治疗有效量来治疗、缓解或改善由革兰氏阴性菌引起的感染的方法；一种通过同时或顺序给予治疗有效量的抗菌药物和本发明所述的衍生物来使革兰氏阴性菌对抗菌药物敏感的方法；一种开发新型抗生素的方法；降低天然聚霉素和八肽霉素的肾毒性，改善其药代动力学特性的方法；以及使临床重要细菌对存在于血清中的宿主防御机制补体敏感的方法。最后，本发明涉及一种制备这种聚霉素衍生物的方法。