D-Leu-NMe | 312968-66-4

• 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: D-Leu-NMe
• 英文别名: (R)-2-Amino-N-methyl-4-methylpentanamide；(2R)-2-amino-N,4-dimethylpentanamide
• CAS: 312968-66-4
• 化学式: C₇H₁₆N₂O
• 分子量: 144.217
• InChiKey: LIBDTAYIDBPBRN-ZCFIWIBFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  D-Leu-NMe 在 palladium on activated charcoal N-甲基吗啉 、 氢气 、 氯甲酸异丁酯 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 52.25h， 生成 (S)-1-Acetyl-pyrrolidine-2-carboxylic acid ((R)-3-methyl-1-methylcarbamoyl-butyl)-amide
  参考文献：
  名称：

  Pietrzynski, Grzegorz; Rzeszotarska, Barbara, Bulletin of the Polish Academy of Sciences: Chemistry, 1991, vol. 39, # 1, p. 1 - 6

  摘要：

  DOI：
• 作为产物：
  描述：

  Z-D-Leu-NMe 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 反应 2.0h， 生成 D-Leu-NMe
  参考文献：
  名称：

  Pietrzynski, Grzegorz; Rzeszotarska, Barbara, Bulletin of the Polish Academy of Sciences: Chemistry, 1991, vol. 39, # 1, p. 1 - 6

  摘要：

  DOI：

文献信息

• [EN] OXYPYRIMIDINES AS SYK MODULATORS<br/>[FR] OXYPYRIMIDINES EN TANT QUE MODULATEURS DE SYK
  申请人：PORTOLA PHARM INC

  公开号：WO2012061415A1

  公开（公告）日：2012-05-10

  The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及式(I)的化合物及其互变异构体或药用可接受的盐、酯和前药，其为Syk激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由Syk激酶活性介导的多种疾病的方法，如不良血栓形成和非霍奇金淋巴瘤。
• ALPHA-(N-SULFONAMIDO)ACETAMIDE DERIVATIVES AS BETA-AMYLOID INHIBITORS
  申请人：Parker F. Michael

  公开号：US20080085894A1

  公开（公告）日：2008-04-10

  There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R 1 , R 2 and R 3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.

  提供了一系列新型α-(N-磺酰胺基)乙酰胺化合物的公式(I)，其中R、R1、R2和R3在此定义，它们是β-淀粉样肽（β-AP）产生的抑制剂，并且在治疗阿尔茨海默病和其他受到抗淀粉样蛋白活性影响的疾病中有用。
• Alpha-(N-Sulfonamido)Acetamide Derivatives as Beta-Amyloid Inhibitors
  申请人：Parker Michael F.

  公开号：US20110105485A1

  公开（公告）日：2011-05-05

  There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R 1 , R 2 and R 3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.

  提供了一系列新型的α-(N-磺酰胺基)乙酰胺化合物(I式)，其中R、R1、R2和R3如本文所定义，它们是β-淀粉样肽（β-AP）产生的抑制剂，并且在治疗阿尔茨海默病和其他受抗淀粉样蛋白活性影响的疾病中有用。
• OXYPYRIMIDINES AS SYK MODULATORS
  申请人：Pandey Anjali

  公开号：US20130317029A1

  公开（公告）日：2013-11-28

  The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及以下式（I）的化合物及其互变异构体或药学上可接受的盐、酯和前药，其为Syk激酶的抑制剂。本发明还涉及制备这种化合物所使用的中间体，制备这种化合物的方法，含有这种化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由Syk激酶活性介导的多种疾病，例如不良血栓形成和非何杰金淋巴瘤的方法。
• COMPOUND AS CYCLIN-DEPENDENT KINASE 9 INHIBITOR AND USE THEREOF
  申请人：CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.

  公开号：EP4074699A1

  公开（公告）日：2022-10-19

  Disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt, a stereoisomer, an isotope derivative or a prodrug thereof. The compound has an excellent activity as a cyclin-dependent kinase 9 (CDK9) inhibitor for treating hyperproliferative diseases. The experimental research on in vitro inhibition of cell proliferation and in vivo suppression of tumors shows that such compounds have a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and have a good selectivity and a low toxicity and few side effects, thereby possessing a good clinical value as novel anti-tumor drugs.

  公开了一种如式（I）所示的化合物或其药学上可接受的盐、立体异构体、同位素衍生物或原药。该化合物作为细胞周期蛋白依赖性激酶 9（CDK9）抑制剂，在治疗过度增殖性疾病方面具有极佳的活性。体外抑制细胞增殖和体内抑制肿瘤的实验研究表明，该化合物对MV4;11细胞和体内肿瘤模型具有较强的抑制作用，且选择性好、毒性低、副作用小，因而作为新型抗肿瘤药物具有较好的临床价值。