On April 15, 2010, Sugita, Kazuyuki; Haginoya,noriyasu published a patent.COA of Formula: C12H14F3NO2 The title of the patent was Preparation of substituted tricyclic heteroaryl compound as squalene and cholesterol synthetase inhibitors. And the patent contained the following:
Title compounds represented by the formula I [wherein R1 = (halo)alkoxy; R2 = halo, (halo)alkyl or alkoxy; R3 = halo, (halo)alkyl or (halo)alkoxy; R4 = hydroxyhaloalkyl; m = 0-4; -X-Y- = a single bond, alkylenecarbonyl-heterocyclyl or alkylene-heterocyclyl; and pharmaceutically acceptable salts thereof] were prepared as squalene and cholesterol synthetase inhibitors. For example, II was provided in a multi-step synthesis starting from 2-bromo-3-hydroxybenzaldehyde. I were tested for inhibition of rat squalene synthetase and rat liver cholesterol synthetase, e.g. II had an IC50 value of 1.7 nM on squalene synthetase and 84% inhibition rate on cholesterol synthetase. Thus, I are useful as squalene and cholesterol synthetase inhibitors for the treatment of hyperlipemia including hypercholesterolemia, hypertriglyceridemia and hypo-HDL cholesterolemia and/or arteriosclerosis in mammals including human. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).COA of Formula: C12H14F3NO2
The Article related to triazolobenzoxazepine preparation squalene cholesterol synthetase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.COA of Formula: C12H14F3NO2
Referemce:
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