Boc-Nalpha-methyl-4-chloro-D-phenylalanine

• 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: Boc-Nalpha-methyl-4-chloro-D-phenylalanine
• 英文别名: 3-(4-chlorophenyl)-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]propanoic acid
• 化学式: C₁₅H₂₀ClNO₄
• mdl: MFCD24391027
• 分子量: 313.77
• InChiKey: GVKQCRRZMAVASQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.466
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Boc-Nalpha-methyl-4-chloro-D-phenylalanine 、 N-benzyl-1,5-dipyridin-4-ylpentan-3-amine 在 Boc-Nalpha-methyl-4-chloro-D-phenylalanine 作用下， 生成
  参考文献：
  名称：

  Amino acid derivatives with improved multi-drug resistance activity

  摘要：

  本发明涉及能够维持、增加或恢复细胞对治疗或预防药物的敏感性的化合物。本发明还涉及包含这些化合物的制药组合物。本发明的化合物和制药组合物特别适用于治疗多药耐药细胞、预防多药耐药的发展以及用于多药耐药癌症治疗。

  公开号：

  US05543423A1
• 作为试剂：
  描述：

  Boc-Nalpha-methyl-4-chloro-D-phenylalanine 、 N-benzyl-1,5-dipyridin-4-ylpentan-3-amine 在 Boc-Nalpha-methyl-4-chloro-D-phenylalanine 作用下， 生成
  参考文献：
  名称：

  Amino acid derivatives with improved multi-drug resistance activity

  摘要：

  本发明涉及能够维持、增加或恢复细胞对治疗或预防药物的敏感性的化合物。本发明还涉及包含这些化合物的制药组合物。本发明的化合物和制药组合物特别适用于治疗多药耐药细胞、预防多药耐药的发展以及用于多药耐药癌症治疗。

  公开号：

  US05543423A1

文献信息

• [EN] SUBSTITUTED AMINO TRIAZOLES USEFUL AS CHITINASE INHIBITORS<br/>[FR] AMINOTRIAZOLES SUBSTITUÉS UTILES EN TANT QU'INHIBITEURS DE CHITINASE
  申请人：ONCOARENDI THERAPEUTICS SA

  公开号：WO2021009209A1

  公开（公告）日：2021-01-21

  Disclosed are amino triazole compounds of formula (I). These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.

  公开了化学式（I）的氨基三唑化合物。这些化合物是酸性哺乳动物几丁质酶和几丁三糖酶的抑制剂。还公开了使用这些化合物治疗由过敏原引起的哮喘反应，以及急性和慢性炎症性疾病、自身免疫疾病、牙科疾病、神经系统疾病、代谢性疾病、肝脏疾病、多囊卵巢综合征、子宫内膜异位症和癌症的方法。
• CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS
  申请人：NOVARTIS AG

  公开号：US20200164024A1

  公开（公告）日：2020-05-28

  The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , X 1 , X 2 , and X 3 are described herein.

  该披露涉及对PCSK9的抑制剂，用于治疗胆固醇脂质代谢以及其他PCSK9发挥作用的疾病，其化学式为(I)： 或其药用可接受的盐、水合物、溶剂合物、前药、立体异构体、N-氧化物或互变异构体，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、X1、X2和X3如本文所述。
• Process for production of optically active N-protected-N-methyl-phenylalanine derivative
  申请人：Ajinomoto Co., Inc.

  公开号：EP1069109A1

  公开（公告）日：2001-01-17

  There is provided a process for efficiently producing an optically active N-protected-N-methyl-4-halogenophenylalanine, which is useful as an intermediate for the production of pharmaceutical agents. In the present invention, an optically active N-protected-N-methyl-4-halogenophenylalanine (including the free form and/or the salt form thereof) purified to a high purity is produced by way of the deposition and isolation in the form of salt (DCHA salt or the like) from an optically active N-protected-N-methyl-4-halogenophenylalanine containing at least the optical isomer thereof as an impurity. Because the intended compound at a high purity can be recovered and obtained industrially at a high yield, the process of the present invention is very useful as a process for producing the intermediate for the production of pharmaceutical agents.

  本发明提供了一种高效生产光学活性 N-保护-N-甲基-4-卤代苯丙氨酸的工艺，该工艺可用作生产药物制剂的中间体。 在本发明中，通过从至少含有光学异构体作为杂质的光学活性 N-保护-N-甲基-4-卤代苯丙氨酸中沉积和分离出盐（DCHA 盐或类似盐）的形式，生产出纯度很高的光学活性 N-保护-N-甲基-4-卤代苯丙氨酸（包括游离形式和/或其盐形式）。由于高纯度的预期化合物可以高产率回收和工业化生产，本发明的工艺作为生产药剂中间体的工艺非常有用。
• PRODUCTION METHOD FOR NONCYCLIC PEPTIDE-NUCLEIC ACID COMPLEX HAVING, AT N-TERMINAL, AMINO ACID WITH THIOL GROUP NEAR AMINO GROUP, LIBRARY THEREOF, AND CYCLIC PEPTIDE-NUCLEIC ACID COMPLEX LIBRARY DERIVED FROM SAME
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP3424941A1

  公开（公告）日：2019-01-09

  When the initiation suppression method was used for translation of a peptide having at its N terminus an amino acid residue carrying a thiol group near its amino group with specific protecting groups being introduced to the thiol group and the amino group, it was found that not only the probability of initiation of amino acid translation reaction was improved, but also production of cleaved peptides was suppressed and translation efficiency and purity were improved. Furthermore, it was found that it is possible to efficiently promote the cyclization reaction of the peptide through amide bond formation. Based on these findings, the inventors discovered novel methods for preparing complexes between nucleic acids and peptides containing various unnatural amino acids and having an amide bond-mediated cyclized portion.

  当使用起始抑制法翻译 N 端在氨基附近带有硫醇基的氨基酸残基并在硫醇基和氨基上引入特定保护基团的多肽时，发现不仅提高了氨基酸翻译反应的起始概率，而且抑制了裂解肽的产生，提高了翻译效率和纯度。此外，还发现可以通过酰胺键的形成有效促进肽的环化反应。基于这些发现，发明人发现了制备核酸与含有各种非天然氨基酸并具有酰胺键介导的环化部分的肽之间的复合物的新方法。
• CYCLIC PEPTIDE COMPOUND HAVING HIGH MEMBRANE PERMEABILITY, AND LIBRARY CONTAINING SAME
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP3636807A1

  公开（公告）日：2020-04-15

  The present inventors have found that when screening for cyclic peptide compounds that can specifically bind to a target molecule, the use of a library including cyclic peptide compounds having a long side chain in the cyclic portion can improve the hit rate for cyclic peptide compounds that can specifically bind to the target molecule. Meanwhile, the present inventors have found that tryptophan and tyrosine residues, which have conventionally been used in oral low molecular-weight pharmaceuticals and are amino acid residues having an indole skeleton or a hydroxyphenyl group, are not suitable for peptides intended to attain high membrane permeability.

  本发明人发现，在筛选能与目标分子特异性结合的环肽化合物时，使用包括环状部分具有长侧链的环肽化合物库，可以提高能与目标分子特异性结合的环肽化合物的命中率。同时，本发明者发现色氨酸和酪氨酸残基不适合用于旨在获得高膜渗透性的肽，这两种残基通常用于口服低分子量药物，是具有吲哚骨架或羟基苯基的氨基酸残基。