78495-63-3Relevant academic research and scientific papers
IMPROVED SYNTHESIS OF KRAS G12C INHIBITOR COMPOUND
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Paragraph 0158, (2021/05/21)
The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2,2',2"-(1,3,5,2,4,6-trioxatriborinane-2,4,6-triyl)tris(3-fluorophenol), useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
IMPROVED SYNTHESIS OF KEY INTERMEDIATE OF KRAS G12C INHIBITOR COMPOUND
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Page/Page column 70-71, (2020/06/05)
The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure (I), useful for the synthesis of compounds that target KRAS G12C mutations, such as (II).
COMBINATION THERAPY INCLUDING A KRASG12C INHIBITOR AND ONE OR MORE ADDITIONAL PHARMACEUTICALLY ACTIVE AGENTS FOR THE TREATMENT OF CANCERS
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Page/Page column 82; 96, (2020/06/10)
The present invention provides combination therapy that includes an KRASG12C inhibitor, such as (see Formula), 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 KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Kopka, Ihor E,Lin, Linus S,Mumford, Richard A,Lanza Jr., Thomas,Magriotis, Plato A,Young, David,DeLaszlo, Stephen E,MacCoss, Malcolm,Mills, Sander G,Van Riper, Gail,McCauley, Ermengilda,Lyons, Kathryn,Vincent, Stella,Egger, Linda A,Kidambi, Usha,Stearns, Ralph,Colletti, Adria,Teffera, Yohannes,Tong, Sharon,Owens, Karen,Levorse, Dorothy,Schmidt, John A,Hagmann, William K
, p. 2415 - 2418 (2007/10/03)
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-(L)-prolyl- and (L)-azetidyl-beta-biaryl beta-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins.
