- Piperazine ureido derivative, preparation method thereof and application of piperazine ureido derivative in medicine
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The invention relates to piperazine ureido derivatives, a preparation method thereof and an application of the piperazine ureido derivatives in medicine. In particular, the invention relates to piperazine ureido derivatives as shown in a general formula (I), a preparation method thereof, pharmaceutical compositions containing the derivatives, and uses thereof as capsid protein inhibitors, especially in prevention and/or treatment of hepatitis B, influenza, herpes, AIDS and other diseases. Wherein the definition of each group in the general formula (I) is the same as that in the specification.
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- Thienopyrimidine and furan and pyrimidine derivatives, its preparation process and its use in medicine
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Disclosed are thienopyrimidine and furopyrimidine derivatives, the preparation method thereof and the medical use thereof. The derivatives have a structure as shown in formula V. The thienopyrimidine and furopyrimidine derivatives provided in the present invention have dominant EGFR inhibiting activity, and some of these compounds also have dominant inhibiting activity against VEGFR; therefore, same can expect to be developed as tyrosine kinase EGFR and/or VEGFR inhibitors, and to be used for preparing the drugs for preventing or treating the diseases related to epidermal growth factor receptor EGFR and/or vascular endothelial growth factor receptor VEGFR. Provided is a new development direction and approach for developing novel tyrosine kinase inhibitor drugs having low drug resistance or able to relieve drug resistance to the inhibitor in the early stages, thereby having extensive application prospects and medical value.
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Paragraph 0121-0123
(2016/10/09)
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- Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)
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Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalysed coupling of substit
- Flanagan, Jack U.,Atwell, Graham J.,Heinrich, Daniel M.,Brooke, Darby G.,Silva, Shevan,Rigoreau, Laurent J.M.,Trivier, Elisabeth,Turnbull, Andrew P.,Raynham, Tony,Jamieson, Stephen M.F.,Denny, William A.
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p. 967 - 977
(2014/02/14)
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