On November 29, 2018, Bellenie, Benjamin Richard; Cheung, Kwai Ming Jack; Davis, Owen Alexander; Hoelder, Swen; Huckvale, Rosemary; Lloyd, Matthew Garth published a patent.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of 4,6-diamino-quinolin-2(1H)-one derived inhibitors of Bcl6 for treatment of cancer. And the patent contained the following:
The invention relates to compounds of formula I that function as inhibitors of Bcl6 (B-cell lymphoma 6) useful for treatment of disorders involving Bcl6 activity such as proliferative disorders including cancers. Addnl., the invention comprises synthetic processes for the preparation of I and pharmaceutical compositions containing I. Compounds of formula I [wherein X1 = N, CH, C-alkyl, C-halo, etc.; X2 and X3 independently = N, CH, CF, CCl, etc.; R1 = H, CH3, 2-(methoxyethoxy)ethyl, etc.; R2 = 2,3-dichloro-pyridin-4-yl, 2-chloro-4-cyano-pyridin-4-yl, 2-chloro-5-methoxy-pyrimidin-4-yl, etc.; R3 = H, C1-2 alkyl, cyano, etc.; R4 = cyano, C1-4 alkyl, C1-4 haloalkyl, etc.; R5 = H, C1-4 alkyl, cyano, nitro, acetylenyl, Ph, etc.; with provisos] and pharmaceutically acceptable salts or solvates thereof, are claimed and exemplified. Example compound II was prepared from the reaction of 6-amino-1-methyl-4-[(1-methyl-1-pyrimidin-2-ylethyl)amino]quinolin-2-one and 2,4-dichloropyridine-3-carbonitrile under microwave heating for 1 h at 160°C. Pharmacol. activity of I was evaluated using a HTRF assay and Trx-6xHis-Bcl6 derived from the human Bcl6 BRB domain from which II demonstrated a pIC50 value of 7.38 μM. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate
The Article related to quinolinone diamino derivative preparation inhibitor bcl6 inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate
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