On March 10, 2016, Bergman, Ylva Elisabet; Lessene, Romina; Ganame, Danny; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stupple, Paul Anthony published a patent.Application of 1014631-89-0 The title of the patent was Preparation of aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5 inhibitors. And the patent contained the following:
The invention relates to compounds of formula I, II and III as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, II and III wherein n = 1 and 2; R is H and Me; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4a is OH, NH2, CONH2 and CH2OH; R4b is H and Me; R5 is H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound IV was prepared by acylation of 1-amino-3-((2,3-dihydro-1H-inden-2-yl)amino)propan-2-ol with 4-chlorobenzoic acid. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example IV exhibited IC50 value of 0.792 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0
The Article related to aminoindane aminotetrahydronaphthalene aminobenzocyclobutane preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics