Pd−P(t-Bu)3-Catalyzed Consecutive Cross-Coupling of p-Phenylenedizinc Compound with Two Different Electrophiles Leading to Unsymmetrically 1,4-Disubstituted Benzenes
摘要:
[GRAPHICS]Pd-P(t-BU)(3) was found to be a chemoselective catalyst for the reaction of p-phenylenedizinc compound with equimolar amounts of carbon electrophiles to afford the single cross-coupling products in good yields, effectively suppressing the formation of double cross-coupling products. The subsequent additions of other electrophiles to the resulting solutions caused the second cross-coupling of the incipient products to take place, achieving a novel and efficient one-pot synthesis of unsymmetrically 1,4-disubstituted benzenes. The origin of the observed high chemoselectivity was speculated.
[EN] 1,2,6-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS<br/>[FR] BENZIMIDAZOLES 1,2,6-SUBSTITUÉS COMME MODULATEURS DE FLAP
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2014151380A1
公开(公告)日:2014-09-25
The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1', X1'', R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
[EN] COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS<br/>[FR] THÉRAPIE D'ASSOCIATION UTILISANT DES INHIBITEURS DE TRANSCRIPTION ET DES INHIBITEURS DE KINASES
申请人:DANA FARBER CANCER INST INC
公开号:WO2016201370A1
公开(公告)日:2016-12-15
The present disclosure provides combination therapy of a transcription inhibitor and a kinase inhibitor. The combination of the transcription inhibitor and the kinase inhibitor may be useful in treating and/or preventing in a subject a proliferative disease, such as proliferative a disease that is resistant to the transcription inhibitor alone or the kinase inhibitor alone. In certain embodiments, the proliferative disease is a cancer. The combination of the transcription inhibitor and the kinase inhibitor is expected to be synergistic.