40851-95-4Relevant academic research and scientific papers
Pyrido[2,3-b]pyrazine-3(4H)-ketone derivative and application thereof
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, (2021/03/13)
The invention provides a pyrido[2,3-b]pyrazine-3(4H)-ketone derivative and application thereof. The structural general formula of the pyrido[2,3-b]pyrazine-3(4H)-ketone derivative is a formula V, andthe pyrido[2,3-b]pyrazine-3(4H)-ketone derivative comprises pharmaceutically acceptable salt, solvate, hydrate or crystal form thereof. The compound provided by the invention is an active ligand of afibroblast growth factor receptor (FGFR), and research shows that the compound shown in the structure V has good anti-proliferative activity on KATO III gastric cancer cells (FGFR2 amplification) andHuh-7 liver cancer cells (FGFR4 overexpression), and is applied to preparation of drugs for treating tumor-related diseases caused by FGFR abnormal activation as an FGFR inhibitor. The structural general formula V is shown in the description.
Substituted pyridino imidazole compound and application thereof in preparation of drugs for treating malignant tumor diseases
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Paragraph 0058-0060, (2020/08/18)
The invention belongs to the field of medicines, and discloses a substituted pyridino imidazole compound as shown in the specification and an application thereof in preparation of a medicine for treating lung cancer. Cell level experiments prove that the compound can inhibit proliferation, migration, invasion and clone formation of lung cancer cells, induce apoptosis of the lung cancer cells and inhibit the phosphorylation level of STAT3; mouse in-vivo experiments show that the compound can inhibit growth and metastasis of lung cancer cells, specifically inhibit an STAT3 signal path, inhibit growth of lung cancer cell transplantation tumors and patient PDX tumors in an animal model, lay a foundation for subsequent new drug research and development, and have important theoretical significance and wide application prospects.
OXAZOLIDINONE ANTIBIOTIC COMPOUNDS AND PROCESS OF PREPARATION
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Paragraph 000145, (2019/10/23)
The present disclosure relates to compounds of Formula (I), its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivative thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention, or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.
5. 7 - Dichloro - 1 H - imidazo [4, 5 - B] pyridine synthesis method
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Paragraph 0038-0042, (2017/12/06)
The invention discloses a method for synthesizing 5,7-dichloro-1H-imidazo-[4,5-B] pyridine. The method comprises steps as follows: in the presence of ammonium chloride, ethyl acetate and water, a compound 1 is reduced by iron powder to obtain a compound 2; the compound 2 has a reflux reaction with p-toluenesulfonic acid monohydrate and triethyl orthoformate to obtain a compound 3; acetic acid is taken as a solvent, the compound 3 reacts with m-chloroperoxybenzoic acid to a compound 4; the compound 4 has a reflux reaction with phosphorus oxychloride at the temperature of 0-5 DEG C in the presence of DMF (Dimethyl formamide) so as to obtain 5,7-dichloro-1H-imidazo-[4,5-B] pyridine. A brand-new synthesis path of 5,7-dichloro-1H-imidazo-[4,5-B] pyridine is provided, raw materials are easy to obtain, the preparation process is simple, the yield is high, the cost is low, and large-scale production can be realized.
A 2,7-diamino-1,4,8-triazanaphthalene derivative selectively binds to cytosine bulge DNA only at a weakly acidic pH
Aikawa,Yano,Nakatani
, p. 1313 - 1316 (2017/02/15)
The synthesis and properties of 2,7-diamino-1,4,8-triazanaphthalene (azaDANP) are described. AzaDANP is protonated only at a weakly acidic pH to bind to the cytosine bulge DNA duplex selectively. Upon binding of azaDANP to the cytosine bulge DNA, a new absorption band at 407 nm appears, and the absorption change of azaDANP on binding to the target is very sensitive to environmental pH with a bell-shaped pH-absorption profile.
Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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Page/Page column 341; 342, (2016/04/26)
The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
Microwave-Assisted C-2 Direct Alkenylation of Imidazo[4,5-b]pyridines: Access to Fluorescent Purine Isosteres with Remarkably Large Stokes Shifts
Baladi, Tom,Granzhan, Anton,Piguel, Sandrine
, p. 2421 - 2434 (2016/06/01)
We describe herein the first C-2 direct alkenylation of the valuable 3H-imidazo[4,5-b]pyridine promoted by microwave-assisted Pd/Cu co-catalysis. The reaction is rapid and compatible with a wide range of functional groups either on the imidazo[4,5-b]pyridine ring or on the styryl bromides thereby leading to the isolation of 23 compounds with moderate to good yields. The relevance of this method is demonstrated by its application to the synthesis of new cross-conjuguated push-pull 2-vinyl- and 2-alkynylimidazo[4,5-b]pyridines characterized by satisfactory fluorescence quantum yields and remarkable solvatofluorochromic properties.
Lithium Hexamethyldisilazane Transformation of Transiently Protected 4-Aza/Benzimidazole Nitriles to Amidines and their Dimethyl Sulfoxide Mediated Imidazole Ring Formation
Abou-Elkhair, Reham A. I.,Hassan, Abdalla E. A.,Boykin, David W.,Wilson, W. David
supporting information, p. 4714 - 4717 (2016/09/28)
Trimethylsilyl-transient protection successfully allowed the use of lithium hexamethyldisilazane to prepare benzimidazole (BI) and 4-azabenzimidazole (azaBI) amidines from nitriles in 58-88% yields. This strategy offers a much better choice to prepare BI/azaBI amidines than the lengthy, low-yielding Pinner reaction. Synthesis of aza/benzimidazole rings from aromatic diamines and aldehydes was affected in dimethyl sulfoxide in 10-15 min, while known procedures require long time and purification. These methods are important for the BI/azaBI-based drug industry and for developing specific DNA binders for expanded therapeutic applications.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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Page/Page column 66, (2015/02/19)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
Efficient reductions of various nitroarenes with scrap automobile catalyst and NaBH4
Genc, Hayriye
, p. 64 - 67 (2015/04/22)
The effect of scrap automobile catalyst (SAC), a waste material, was investigated as a catalyst for the reduction of nitroarenes to the corresponding amines with sodium borohydride in aqueous ethanol at 5-25 °C. Along with the observed high conversions, the SAC and NaBH4 combination also exhibits a selectively catalyzed reduction in compounds containing other reducible functionalities, such as CN, Br, Cl and I. Recycling automobile wastes into a catalyst for organic reactions will offer both environmental protection and economic advantages. As a result, an effective, easy to use, low-priced and reliable method has been developed.
