- Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation
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CDK8 regulates transcription either by phosphorylation of transcription factors or, as part of a four-subunit kinase module, through a reversible association of the kinase module with the Mediator complex, a highly conserved transcriptional coactivator. D
- Yu, Mingfeng,Teo, Theodosia,Yang, Yuchao,Li, Manjun,Long, Yi,Philip, Stephen,Noll, Benjamin,Heinemann, Gary K.,Diab, Sarah,Eldi, Preethi,Mekonnen, Laychiluh,Anshabo, Abel T.,Rahaman, Muhammed H.,Milne, Robert,Hayball, John D.,Wang, Shudong
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- Technology for synthesizing N-substituted pyrazol-4-borate
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The invention discloses a technology for synthesizing N-substituted pyrazol-4-borate. The technology comprises the following steps: taking 2-bromomalonaldehyde as a raw material; firstly, causing the 2-bromomalonaldehyde and triethyl orthoformate to react to obtain acetal; transforming bromine into bi(diisopropylamine)boron; then, carrying out a condensation reaction on the bi(diisopropylamine)boron and substituted hydrazine; and finally, causing an obtained product to react with different glycols to obtain the N-substituted pyrazol-4-borate. The method has the advantage of easy obtaining of raw materials, simple synthesis steps and high reaction yield and is suitable for industrialization amplification production.
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Paragraph 0018
(2016/12/01)
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- HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
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The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
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Paragraph 00690
(2016/01/25)
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- PHOSPHATIDYLINOSITOL 3 KINASE INHIBITORS
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Provided are compounds according to Formula (I), or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6 , R7, and R8 are as defined, which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PB -kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.
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Page/Page column 134
(2010/01/12)
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- Investigation of the scope and regiochemistry of alkynylboronate cycloadditions with sydnones
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The cycloaddition of alkynylboronates and sydnones provides a convenientand highly regioselective method for the synthesis of a broad range of di-, tri-, and tetrasubstituted pyrazole boronic esters. The origins of an observed regiochemical divergence in the reactions of terminal alkyny lboronates with their more substituted analogues have been studied by DFT methods.
- Browne, Duncan L.,Vivat, Jerome F.,Plant, Andrew,Gomez-Bengoa, Enrique,Harrity, Joseph P. A.
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supporting information; experimental part
p. 7762 - 7769
(2009/10/16)
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- A sydnone cycloaddition route to pyrazole boronic esters
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(Chemical Equation Presented) From dipole to diazole! A direct and regioselective route to functionalized pyrazole boronic esters is developed that employs the cycloaddition of alkynylboronates with sydnones. Functionalization of these products by Suzuki coupling and N-deprotection processes highlight the potential synthetic utility of these species.
- Browne, Duncan L.,Helm, Matthew D.,Plant, Andrew,Harrity, Joseph P. A.
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p. 8656 - 8658
(2008/09/18)
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