On November 13, 2008, Bonnert, Roger Victor; McInally, Thomas; Thom, Stephen published a patent.Product Details of 142327-44-4 The title of the patent was Preparation of imidazoquinolines as TLR7 immunomodulators. And the patent contained the following:
Title compounds I [R1 = (un)substituted alkyl; Z1 = alkylene or cycloalkylene; X1 = NR5, NCOR5, CONR5, NR5CO, SO2NR5, etc.; Y1 = single bond or alkylene; each R2 independently = halo, CN, OH, thiol, alkyl, etc.; R3 = (un)substituted alkyl; each Ra independently = halo, CN, OH, thiol, alkyl, hydroxyalkyl, etc.; R5 = H, 3- to 8-membered saturated heterocyclic ring, (un)substituted alkyl or cycloalkyl; or R5 = alkylene which may be linked to a carbon atom within a alkylene group Z1 so as to form a saturated 4- to 7-membered nitrogen containing ring; with the proviso; m, n, p and q independently = 0-2; A = monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl], and their pharmaceutically acceptable salts, are prepared and disclosed as toll-like receptors (TLR7) modulators. Thus, e.g., II was prepared in 8 steps starting from 4-hydroxyquinoline. II exhibited pEC50 value of 6.5 in human TLR7 assay. Having immuno-modulating properties via TLR7, I are useful in the treatment of viral or allergic diseases and cancers, etc. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Product Details of 142327-44-4
The Article related to imidazoquinoline preparation tlr7 immunomodulator allergy antiviral antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 142327-44-4
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