On March 10, 2016, Bergman, Ylva Elisabet; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.SDS of cas: 1014631-89-0 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as PRMT5 inhibitors. And the patent contained the following:
The invention relates to tetrahydroisoquinoline derivatives of formula I as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, wherein n = 1 and 2; p is 0 and 1; 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; R4 is H and Me; R5 is H and Me; R6a and R6b are independently H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound II was prepared by amidation of 2-fluoro-4-(morpholine-4-carbonyl)benzoic acid with tert-Bu (S)-3-((R)-2-amino-1-hydroxyethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate followed by BOC-deprotection. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example II exhibited IC50 value of 0.383 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).SDS of cas: 1014631-89-0
The Article related to tetrahydroisoquinoline preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.SDS of cas: 1014631-89-0
Referemce:
Pyrazole – Wikipedia,
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