COMBINATION THERAPY INCLUDING A KRAS G12C INHIBITOR AND ONE OR MORE ADDITIONAL PHARMACEUTICALLY ACTIVE AGENTS FOR THE TREATMENT OF CANCERS
申请人:Amgen Inc.
公开号:US20200222407A1
公开(公告)日:2020-07-16
The present invention provides combination therapy that includes an KRAS
G12C
inhibitor, such as
or a pharmaceutically acceptable salt thereof, and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an KRAS
G12C
inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.
SYNTHESIS OF KEY INTERMEDIATE OF KRAS G12C INHIBITOR COMPOUND
申请人:Amgen Inc.
公开号:US20220220112A1
公开(公告)日:2022-07-14
The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure
useful for the synthesis of compounds that target KRAS G12C mutations, such as
Exploration of catalytic activity of newly developed Pd/KLR and Pd-Cu/KLR nanocomposites (NCs) for synthesis of biologically active novel heterocycles via Suzuki cross-coupling reaction
comparative study of both Pd-KLR and Pd-Cu-KLR nanocatalysts is studied. However, the heterogeneous Pd-KLR nanocomposite showed excellent catalytic activity for the heterocyclic SuzukiCross-Couplingreaction. The yield of the reaction of 3-amino-2-chloropyridine with phenylboronic acid using EtOH solvent in the presence of NaOH base and a very little amount of Pd0.02/KLR (0.1 mmol%) catalyst at 78 °C temperature