On December 9, 2021, Blagg, Julian; Roffey, Jon; Drysdale, Martin; Winship, Paul; Clark, David published a patent.Reference of 2,4,6-Trihydroxy-3-methylbenzaldehyde The title of the patent was Heterocyclic benzamide compounds as MLH1 and/or PMS2 proteins inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:
The invention relates to heterocyclic benzamide compounds of formula I that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process. The invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 and/or PMS2 activity is implicated. Compounds of formula I wherein R1 and R3 are independently H,OH, halo, C1-4 alkoxy; provided that as least one of the R1 and R3 is OH; R2 is H, F; R4 is H, halo, C1-6 alkyl, (un)substituted C3-6 cycloalkyl, (un)substituted C3-6 cycloalkyl-C1-2 alkyl, etc.; R6 is C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-2 alkyl, 4- to 7-membered cyclic ring, etc.; R10 is NR11R12; R11 and R12 are taken together with the nitrogen atom attached to form (un)substituted 5- to 7-membered heterocyclic ring fused with 5- to 6-membered monocyclic heteroaryl or with Ph to form 8- to 11-membered bicyclic heteroaryl; and their pharmaceutically acceptable salts, hydrates or solvates as MLH1 and/or PMS2 proteins inhibitors in the treatment of cancer thereof, are claimed. Example compound II was prepared by using amidation and desulfonylation as the key steps. All the invention compounds were evaluated for their MLH1 and/or PMS2 proteins inhibitory activity. The experimental process involved the reaction of 2,4,6-Trihydroxy-3-methylbenzaldehyde(cas: 55743-13-0).Reference of 2,4,6-Trihydroxy-3-methylbenzaldehyde
The Article related to heterocyclic benzamide preparation mlh1 pms2 protein inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 2,4,6-Trihydroxy-3-methylbenzaldehyde
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