On February 16, 2017, Pourashraf, Mehrnaz; Jacquemot, Guillaume; Claridge, Stephen; Bayrakdarian, Malken; Johnstone, Shawn; Albert, Jeffrey S.; Griffin, Andrew published a patent.Safety of (S)-1-Methoxypropan-2-amine hydrochloride The title of the patent was Substituted benzimidazoles as bromodomain inhibitors, their preparation and their use as pharmaceuticals. And the patent contained the following:
This application relates to substituted benzimidazoles of formula I, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. The application also relates to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasm. Compounds of formula I wherein R1 is (un)substituted C1-6 alkyl, COR11, CONHR11, SO2R11, etc.; R2 is H, (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl etc.; R3 and R6 are independently H, (un)substituted C1-6 alkyl, COR11, NH2 and derivatives, CONH2 and derivatives, etc.; one of R4 and R5 is H, (un)substituted C1-6 alkyl, COR11, NH2 and derivatives, CONH2 and derivatives, etc., and the other one of R4 and R5 is 6-membered nitrogen containing heterocycle; R11 is (un)substituted C1-6 alkyl;and pharmaceutically acceptable salts, solvates, esters and prodrugs thereof, are claimed. Example compound II was prepared by amidation of tetrahydropyran-4-carbonyl chloride with 4-bromo-N2-[2-(trifluoromethoxy)ethyl]benzene-1,2-diamine followed by cyclization; the resulting 6-bromo-2-tetrahydropyran-4-yl-1-[2-(trifluoromethoxy)ethyl]benzimidazole underwent cross-coupling reaction with 1,3-dimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-one to give compound II. The invention compounds were evaluated for their bromodomain inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 0.076 μM to 0.14 μM. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Safety of (S)-1-Methoxypropan-2-amine hydrochloride
The Article related to benzimidazole preparation bromodomain inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Safety of (S)-1-Methoxypropan-2-amine hydrochloride
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