[EN] MACROCYCLES AS PIM INHIBITORS<br/>[FR] MACROCYCLES EN TANT QU'INHIBITEURS DE PIM
申请人:AMGEN INC
公开号:WO2014022752A1
公开(公告)日:2014-02-06
The invention relates to compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
[EN] PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS<br/>[FR] INHIBITEURS DE PYRROLO[2,3-B]PYRIDINE CDK9 KINASE
申请人:ABBVIE INC
公开号:WO2014139328A1
公开(公告)日:2014-09-18
Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa).
A versatile and practical route to both enantiomers of a wide variety of 4-substituted 2-oxazolidinones from the parent heterocycle is provided by regioselective substitutions via 4-methoxy derivative followed by chromatographic separation of the diastereomers derived from N-2-exo-methoxy-1-apocamphanecarbonylation.
Concise Synthesis of Fungal Metabolite (+)-Fusarochromanone via Rhodium(III)-catalyzed Oxidative sp<sup>2</sup>C–H Bond Olefination
作者:Yuji Takahama、Yu Shibata、Ken Tanaka
DOI:10.1246/cl.160530
日期:2016.10.5
with a chiral functionalized electron-rich alkene, catalyzed by an electron-deficient (η5-cyclopentadienyl)rhodium(III) complex, [CpERhCl2]2, under ambient conditions as the key step. This protocol was applied to various acetanilides and functionalized electron-rich alkenes for the syntheses of fusarochromanone analogs.
作者:Nolwenn Derrien、James S. Sharley、Aleksandr E. Rubtsov、Andrei V. Malkov
DOI:10.1021/acs.orglett.6b03525
日期:2017.1.6
An expedient procedure for catalytic oxidative azo–ene cyclization of allylic and homoallylic 1,2-hydrazinedicarboxylates is reported. The reaction produced a wide range of cyclic carbamate derivatives featuring an appended alkene fragment ready for further functionalization.