3,4-二甲氧基吡啶-2-甲醛 | 142470-53-9

• 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
• 中文名称: 3,4-二甲氧基吡啶-2-甲醛
• 英文名称: 3,4-dimethoxy-2-formylpyridine
• 英文别名: 3,4-dimethoxypicolinaldehyde；3,4-dimethoxypyridine-2-carbaldehyde
• CAS: 142470-53-9
• 化学式: C₈H₉NO₃
• 分子量: 167.164
• InChiKey: QBEYSYWMWVZVFG-UHFFFAOYSA-N

物化性质

• 沸点：
  273.5±35.0 °C(Predicted)
• 密度：
  1.174±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  48.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-甲氧基吡啶 在 盐酸 、 过氧乙酸 、 tetrafluoroboric acid 、 正丁基锂 、 硼酸三甲酯 、 乙醇 、 苯基锂 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 12.0h， 生成 3,4-二甲氧基吡啶-2-甲醛
  参考文献：
  名称：

  New synthesis of Orelline by metalation of methoxypyridines

  摘要：

  A new total synthesis in five steps of the alkaloid Orelline is reported. The methodology of methoxypyridines to afford 2-halo-3,4-dimethoxypyridine on which an homocoupling reaction is performed to but the 2,2'-bipyridyl structure of the alkaloid.

  DOI：

  10.1016/s0040-4020(01)81920-7

文献信息

• [EN] TRPML MODULATORS<br/>[FR] MODULATEURS DE TRPML
  申请人：CASMA THERAPEUTICS INC

  公开号：WO2021127337A1

  公开（公告）日：2021-06-24

  The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

  本发明提供了化合物、药学上可接受的组合物以及使用这些化合物的方法。
• [EN] BCL-2 INHIBITOR<br/>[FR] INHIBITEUR DE BCL -2
  申请人：BEIGENE LTD

  公开号：WO2021208963A1

  公开（公告）日：2021-10-21

  Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.

  本文披露了一种用于抑制Bcl-2野生型和突变型Bcl-2（特别是Bcl-2 G101V和D103Y）的化合物（I）以及使用本文披露的该化合物治疗失调的凋亡性疾病的方法。
• TRICYCLIC COMPOUND
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP1939205A1

  公开（公告）日：2008-07-02

  The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R1, R2, R2', R3, R4, X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.

  本发明涉及一种三环化合物，每种化合物由以下式（I）表示：（其中，R1、R2、R2'、R3、R4、X、Y和Z的含义与规范中定义的含义相同）；以及含有该化合物的药物。由于根据本发明的化合物表现出优异的角鲨烯合酶抑制作用和胆固醇合成抑制作用，因此它们可用作哺乳动物（包括人类）的疾病预防和/或治疗药物，例如高脂血症，如高胆固醇血症、高甘油三酯血症、低高密度脂蛋白胆固醇血症和/或动脉粥样硬化。
• [EN] CANCER THERAPEUTICS<br/>[FR] TRAITEMENTS ANTICANCÉREUX
  申请人：UNIV VIRGINIA PATENT FOUND

  公开号：WO2016025744A1

  公开（公告）日：2016-02-18

  This invention relates to compounds that bind to wild-type CBFβ and inhibit CBFβ binding to RUNX proteins. The potent compounds of the invention inhibit this protein-protein interaction at low micromolar concentrations, using allosteric mechanism to achieve inhibition, displace wild-type CBFβ from RUNX1 in cells, change occupancy of RUNX1 on target genes, and alter gene expression of RUNX1 target genes. These inhibitors show clear biological effects consistent with on-target RUNX protein activity. Pharmaceutical compositions containing a compound of the invention and a pharmaceutically acceptable carrier represent a separate embodiment of the invention. Another embodiment of the invention are methods of treating a RUNX-signaling-dependent cancer that expresses wild-type CBFβ in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention. In one embodiment, the cancer is selected from the group consisting of a RUNX-signaling-dependent leukemia that expresses wild-type CBFβ, lung cancer, bladder cancer, ovarian cancer, uterine cancer, endometrial cancer, breast cancer, liver cancer, pancreatic cancer, stomach cancer, cervical cancer, lymphoma, leukemia, acute myeloid leukemia, acute lymphocytic leukemia, salivary gland cancer, bone cancer, brain cancer, colon cancer, rectal cancer, colorectal cancer, kidney cancer, skin cancer, melanoma, squamous cell carcinoma of the tongue, pleomorphic adenoma, hepatocellular carcinoma, pancreatic cancer, squamous cell carcinoma, and/or adenocarcinoma. In another embodiment, the compounds of the invention can be used to treat a leukemia, lung cancer, ovarian cancer, and/or breast cancer.

  本发明涉及与野生型CBFβ结合并抑制CBFβ与RUNX蛋白结合的化合物。本发明的有效化合物以低微摩尔浓度抑制这种蛋白质-蛋白质相互作用，利用变构机制实现抑制，从细胞中置换野生型CBFβ从而改变RUNX1在靶基因上的占位率，改变RUNX1靶基因的基因表达。这些抑制剂表现出与靶向RUNX蛋白活性一致的明显生物学效应。含有本发明化合物和药学可接受载体的制药组合物代表该发明的另一实施形式。该发明的另一实施形式是通过向需要治疗的主体施用本发明化合物的治疗有效量来治疗表达野生型CBFβ的RUNX信号依赖性癌症。在一种实施形式中，该癌症被选自RUNX信号依赖性白血病，肺癌，膀胱癌，卵巢癌，子宫癌，子宫内膜癌，乳腺癌，肝癌，胰腺癌，胃癌，宫颈癌，淋巴瘤，白血病，急性髓性白血病，急性淋巴细胞白血病，涎腺癌，骨癌，脑癌，结肠癌，直肠癌，结直肠癌，肾癌，皮肤癌，黑色素瘤，舌鳞状细胞癌，多形性腺瘤，肝细胞癌，胰腺癌，鳞状细胞癌和/或腺癌。在另一实施形式中，本发明的化合物可用于治疗白血病，肺癌，卵巢癌和/或乳腺癌。
• TRICYCLIC COMPOUNDS
  申请人：Sugita Kazuyuki

  公开号：US20090181942A1

  公开（公告）日：2009-07-16

  The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R 1 , R 2 , R 2′ , R 3 , R 4 , X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.

  本发明涉及由以下公式（I）表示的三环化合物（其中，R1，R2，R2'，R3，R4，X，Y和Z的含义如说明书所定义）；以及含有该化合物的药物。由于本发明的化合物表现出优异的角鲨烷合酶抑制作用和胆固醇合成抑制作用，因此它们可用作哺乳动物（包括人类）疾病的预防和/或治疗药物，例如高脂血症、例如高胆固醇血症、高三酰甘油血症和低高密度脂蛋白胆固醇血症和/或动脉硬化。