On April 3, 2008, Johansson, Rolf; Karlstroem, Sofia; Kers, Annika; Nordvall, Gunnar; Rein, Tobias; Slivo, Can published a patent.Synthetic Route of 87674-15-5 The title of the patent was Preparation of [(pyridinyl)ethyl]thio[(hydroxymethyl)alkyl]amino[1,3]thiazolo[4,5-d]pyrimidinone derivatives for use as therapeutic agents. And the patent contained the following:
Title compounds I [R1 = Me or CF3; R2 = halo, CN, or alkyl; R3 and R4 independently = H or Me; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as therapeutic agents. Thus, e.g., II was prepared by oxidation of (2R)-2-[[5-[[(1S)-1-(5-chloropyridin-2-yl)ethyl]thio]-2-methoxy[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol (preparation given). Select I were evaluated in recombinant human fractalkine hCX3CR1 binding assay, e.g., II demonstrated a Ki value of 5.8 (nM). Title compounds I are disclosed as therapeutic agents of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Synthetic Route of 87674-15-5
The Article related to pyrimidinone pyridinylethylthio hydroxymethylalkylamino thiazolo derivative preparation nervous system disease, pyridinylethylthio hydroxymethylalkylamino thiazolopyrimidinone derivative preparation atherosclerosis multiple sclerosis asthma and other aspects.Synthetic Route of 87674-15-5
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