On March 15, 2018, Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Fell, Jay Bradford; Fischer, John P.; Gaudino, John J.; Hicken, Erik James; Hinklin, Ronald Jay; Lee, Matthew Randolf; Marx, Matthew Arnold; Mejia, Macedonio J.; Rodriguez, Martha E.; Savechenkov, Pavel; Tang, Tony P.; Vigers, Guy P.A.; Zecca, Henry J. published a patent.Category: pyrimidines The title of the patent was Preparation of substituted pyrido[3,4-d]pyrimidine compounds as KRas G12C inhibitors. And the patent contained the following:
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds I [X = (un)substituted 4-12 membered saturated or partially saturated monocyclic, bridged or spirocyclic ring; Y = a bond, O, S or NR5; R1 = C(O)C(R)(= or ๎)C(R’)p, or SO2C(R)(= or ๎)C(R’)p; R2 = H, alkyl, hydroxyalkyl, etc.; Z = alkylene; R3 = (independently) alkyl, oxo, or haloalkyl; L = a bond, C(O), or alkylene; R4 = H, cycloalkyl, heterocyclyl, etc.; R5 = (independently) H or alkyl; R = absent, H, or alkyl; R’ = (independently) H, alkyl, alkylaminylalkyl, etc.; p = 0-1; m = 0-2] that irreversibly inhibit the activity of KRas G12C, to pharmaceutical compositions comprising the compounds and methods of use therefor. Over 400 compounds I were prepared E.g., a multi-step synthesis of (2S)-II, starting from (S)-tert-Bu 2-(hydroxymethyl)pyrrolidine-1-carboxylate, was described. Exemplified compounds I were tested in the KRas G12C modification assay, and for inhibition of KRas G12C-dependent cell growth (data given). The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Category: pyrimidines
The Article related to pyridopyrimidine preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia