tert-butyl 6-amino-3',6'-dihydro-[3,4'-bipyridine]-1'(2'H)-carboxylate | 1279030-84-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: tert-butyl 6-amino-3',6'-dihydro-[3,4'-bipyridine]-1'(2'H)-carboxylate
• 英文别名: tert-butyl 6-amino-3’,6’-dihydro-[3,4‘-bipyridine]-1‘(2‘H)-carboxylate；tert-butyl 6-amino-5',6'-dihydro-[3,4'-bipyridine] -1'(2'H)-carboxylate；6-amino-3',6'-dihydro-2'H-[3,4']bipyridinyl-1'-carboxylic acid tert-butyl ester；tert-butyl 4-(6-aminopyridin-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate；tert-butyl 4-(6-aminopyridin-3-yl)-3,6-dihydro-2H-pyridine-1-carboxylate
• CAS: 1279030-84-0
• 化学式: C₁₅H₂₁N₃O₂
• 分子量: 275.351
• InChiKey: GJKPPQXNOJOCQU-UHFFFAOYSA-N

物化性质

• 沸点：
  426.4±45.0 °C(Predicted)
• 密度：
  1.168±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  68.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 6-amino-3',6'-dihydro-[3,4'-bipyridine]-1'(2'H)-carboxylate 在 盐酸 、 四(三苯基膦)钯 、 palladium 10% on activated carbon 、 氢气 、 potassium carbonate 、 caesium carbonate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 三氟乙酸 作用下， 以 1,4-二氧六环 、 甲醇 、 二氯甲烷 、 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 反应 76.0h， 生成
  参考文献：
  名称：

  [EN] CDK INHIBITORS AND PHARMACEUTICAL USES THEREOF
  [FR] INHIBITEURS DE CDK ET LEURS UTILISATIONS PHARMACEUTIQUES

  摘要：

  The disclosure relates to bifunctional CDK-modulating compounds having the structure W-L-T, where W is a targeting group (1a), 1b) and (1c), that binds specifically to a CDK protein, T is an E3-ligase binding group, and L is absent or is a bivalent linking group that connects W and T together via a covalent linkage. Compounds and pharmaceutical compositions thereof can promote degradation of one or more CDK protein in a cell and are thus useful for treating, inhibiting, and preventing CDK-associated diseases, disorders and conditions, including cancers. Formulas (1a), (1b) & (1c):

  公开号：

  WO2023205892A1
• 作为产物：
  描述：

  6-nitro-3',6'-dihydro-2'H-[3,4']bipyridinyl-1'-carboxylic acid tert-butyl ester 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 10.0h， 以94%的产率得到tert-butyl 6-amino-3',6'-dihydro-[3,4'-bipyridine]-1'(2'H)-carboxylate
  参考文献：
  名称：

  一种三取代嘧啶衍生物对蛋白激酶的抑制作用

  摘要：

  本发明公开了一种三取代嘧啶衍生物，具有通式（Ⅰ）结构，其药学上可接受的盐、酯或溶剂化合物，所述衍生物为蛋白激酶抑制剂，可单独或与其它药物联用，用于癌症的治疗，具有巨大的临床应用价值。通式（Ⅰ）。

  公开号：

  CN110156754A

文献信息

• Aminoheteroaryl benzamides as kinase inhibitors
  申请人：Bagdanoff Jeffrey T.

  公开号：US09242996B2

  公开（公告）日：2016-01-26

  The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.

  本发明提供了化合物的化合物（I）或其盐； 以及这些化合物的治疗用途。本发明还提供了包含这些化合物的药物组合物，以及包含这些化合物与治疗辅助剂的组合物。
• HETEROCYCLIC COMPOUND
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US20160159773A1

  公开（公告）日：2016-06-09

  The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

  本发明提供了一种用于预防或治疗自身免疫性疾病（例如牛皮癣、类风湿关节炎、炎症性肠病、干燥综合征、贝赫切特病、多发性硬化症、系统性红斑狼疮等）等的药剂，其具有优越的Tyk2抑制作用。 本发明涉及一种由下式表示的化合物 其中每个符号如规范中定义的，或其盐。
• Inhibitors of Bruton's Tyrosine Kinase
  申请人：Berthel Steven Joseph

  公开号：US20120040949A1

  公开（公告）日：2012-02-16

  This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y 4 , are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.

  该应用程序根据通用公式I揭示了6-(2-羟甲基苯基)-2-甲基-2H-吡啶并-3-酮衍生物： 其中，变量X、R和Y4如本文所述定义，这些衍生物抑制Btk。本文披露的化合物可用于调节Btk的活性并治疗与过度Btk活性相关的疾病。这些化合物进一步可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，如类风湿性关节炎。还披露了含有公式I化合物和至少一种载体、稀释剂或赋形剂的组合物。
• [EN] PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITOR OF CYCLIN DEPENDENT KINASE<br/>[FR] DÉRIVÉS DE PYRAZOLO-TRIAZINE ET/OU DE PYRAZOLO-PYRIMIDINE EN TANT QU'INHIBITEURS SÉLECTIFS DE KINASE DÉPENDANTE DE LA CYCLINE
  申请人：QURIENT CO LTD

  公开号：WO2019197549A1

  公开（公告）日：2019-10-17

  The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[l,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.

  本发明涉及吡唑并[1,5-a][1,3,5]三嗪和吡唑[1,5-a]嘧啶衍生物和/或其药用可接受盐，以及这些衍生物作为药用活性剂的用途，特别是用于预防和/或治疗细胞增殖性疾病、炎症性疾病、免疫性疾病、心血管疾病和传染病。此外，本发明还涉及含有至少一种吡唑并[1,5-a][1,3,5]三嗪和吡唑[1,5-a]嘧啶衍生物和/或其药用可接受盐的药物组合物。
• GLYCINE COMPOUND
  申请人：Yoshihara Kousei

  公开号：US20120184520A1

  公开（公告）日：2012-07-19

  [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.

  本发明提供了一种化合物，该化合物可用作药物组合物的活性成分，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物。 本发明的解决方案是，本发明者对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性，并且对于预防和/或治疗与VAP-1相关的疾病，特别是糖尿病肾病或糖尿病黄斑水肿，具有用处，从而完成了本发明。本发明还涉及一种药物组合物，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物，其包括本发明的化合物或其盐以及赋形剂。