On February 14, 2019, Zablocki, Mary-Margaret; Guerin, David J.; Ng, Pui Yee; Wang, Zhongguo; Shelekhin, Tatiana; Caravella, Justin; Li, Hongbin; Ioannidis, Stephanos published a patent.Electric Literature of 227940-70-7 The title of the patent was Heteroaryl carboxamide derivatives as ubiquitin-specific protease inhibitors and their preparation. And the patent contained the following:
The invention relates to compounds of formula I, their use as modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors and methods of using the inhibitors in the treatment of cancers, among other ailments. Compounds of formula I, wherein X is CRARB and O; RA and RB are independently H, halo, hydroxy, etc.; R1 is 6 – 12 membered (un)substituted fused and (un)substituted nonfused heteroaryls, R2 is N-linked (un)substituted 4 – 12 membered heterocyclyls, (un)substituted C-linked 4 – 12 membered heterocyclyls and (un)substituted O-linked 4 – 12 member heterocyclyl; R3 is independently H, C1-6 alkyl, C1-6 alkoxy, etc.; n is 0, 1, 2 and 3; R4 is H, C1-6 alkyl, C1-6 alkoxy, etc.; R5 is H, deuterium and Me; Y1, Y2 and Y3 are independently CR3 and N; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared using a multistep procedure (procedure given). Compound II was evaluated for its USP28 and USP25 inhibitory activities giving an IC50 of 0.05-2 μM and 0.2-2 μM, resp. Compounds of the invention were evaluated for their inhibitory activity (data given). The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Electric Literature of 227940-70-7
The Article related to heteroaryl carboxamide preparation usp28 usp25 modulator inhibitor cancer, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Electric Literature of 227940-70-7
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics