324769-11-1Relevant articles and documents
Four-ring-fused compound as well as preparation method and application thereof
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Paragraph 0415; 0439-0442, (2021/02/10)
The invention discloses a compound shown as a formula (I), an optical isomer and pharmacologically acceptable salts thereof, and application of the compound as a KRAS inhibitor.
KRAS G12C INHIBITORS
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Paragraph 0220, (2020/07/25)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with in Vivo Activity
Fell, Jay B.,Fischer, John P.,Baer, Brian R.,Ballard, Joshua,Blake, James F.,Bouhana, Karyn,Brandhuber, Barbara J.,Briere, David M.,Burgess, Laurence E.,Burkard, Michael R.,Chiang, Harrah,Chicarelli, Mark J.,Davidson, Kevin,Gaudino, John J.,Hallin, Jill,Hanson, Lauren,Hee, Kenneth,Hicken, Erik J.,Hinklin, Ronald J.,Marx, Matthew A.,Mejia, Macedonio J.,Olson, Peter,Savechenkov, Pavel,Sudhakar, Niranjan,Tang, Tony P.,Vigers, Guy P.,Zecca, Henry,Christensen, James G.
supporting information, p. 1230 - 1234 (2018/12/11)
KRAS is the most frequently mutated driver oncogene in human cancer, and KRAS mutations are commonly associated with poor prognosis and resistance to standard treatment. The ability to effectively target and block the function of mutated KRAS has remained elusive despite decades of research. Recent findings have demonstrated that directly targeting KRAS-G12C with electrophilic small molecules that covalently modify the mutated codon 12 cysteine is feasible. We have discovered a series of tetrahydropyridopyrimidines as irreversible covalent inhibitors of KRAS-G12C with in vivo activity. The PK/PD and efficacy of compound 13 will be highlighted.
SEROTONERGIC BENZOTHIOPHENES
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Page 19, (2010/02/08)
The present invention provides serotonergic benzothiophenes of Formula (I), where A, R, R, R, R, and R are as described in the specification.