116922-22-6Relevant articles and documents
Palladium-catalysed amination reactions using cobalt-containing bulky phosphane ligands
Lee, Jian-Cheng,Wang, Ming-Gin,Hong, Fung-E.
, p. 5011 - 5017 (2005)
Aminations of aryl bromides by morpholine have been investigated using palladium complexes as catalyst precursors modified by the cobalt-containing phosphane ligand [(μ-PPh2CH2PPh2)Co 2(CO)4][μ,η-PhC≡
NOTCH INHIBITORS AND USES THEREOF
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Paragraph 0732; 0733-0734, (2021/11/26)
Disclosed herein, inter alia, are compounds for inhibiting Notch and uses thereof.
DDX3X Helicase Inhibitors as a New Strategy to Fight the West Nile Virus Infection
Brai, Annalaura,Martelli, Francesco,Riva, Valentina,Garbelli, Anna,Fazi, Roberta,Zamperini, Claudio,Pollutri, Alessandro,Falsitta, Lucia,Ronzini, Stefania,Maccari, Laura,Maga, Giovanni,Giannecchini, Simone,Botta, Maurizio
, p. 2333 - 2347 (2019/03/07)
Increased frequency of arbovirus outbreaks in the last 10 years represents an important emergence for global health. Climate warming, extensive urbanization of tropical regions, and human migration flows facilitate the expansion of anthropophilic mosquitos and the emerging or re-emerging of new viral infections. Only recently the human adenosinetriphosphatase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against infectious diseases. Herein, starting from our previous studies, a new family of DDX3X inhibitors was designed, synthesized, validated on the target enzyme, and evaluated against the West Nile virus (WNV) infection. Time of addition experiments after virus infection indicated that the compounds exerted their antiviral activities after the entry process, likely at the protein translation step of WNV replication. Finally, the most interesting compounds were then analyzed for their in vitro pharmacokinetic parameters, revealing favorable absorption, distribution, metabolism, and excretion values. The good safety profile together with a good activity against WNV for which no treatments are currently available, make this new class of molecules a good starting point for further in vivo studies.
Aromatic amine compound, EphB4 kinase inhibitor and its derivatives, and preparation methods thereof
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Paragraph 0085-0087, (2019/11/04)
The invention provides an aromatic amine compound, an EphB4 kinase inhibitor and its derivatives, and preparation methods thereof. Aryl boronic acid or aryl boronate and O-benzoyl hydroxylamine compounds which are used as starting raw materials are stirred and reacted in an organic solvent at 30-100 DEG C in an air atmosphere under the action of a palladium catalyst, a norbornene derivative and analkali, and separation and purification are carried out after the reaction in order to obtain the aromatic amine compound. The method has the advantages of inexpensive and readily available raw materials, no halide ion residual after the completion of the reaction, and mild reaction conditions. The invention also provides the method for synthesizing the EphB4 kinase inhibitor and its derivatives.The EphB4 kinase inhibitor and its derivatives can be synthesized from the synthesized 3,5-diminated halogenobenzene or halogenoid benzene only through a simple step.