On January 9, 2020, Glick, Gary; Roush, William; Venkatraman, Shankar; Shen, Dong-Ming; Ghosh, Shomir; Seidel, Hans Martin; Franchi, Luigi; Winkler, David Guenther; Opipari, Anthony William, Jr.; Katz, Jason published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Aryl and heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:
The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl, SONR11R12 and CR11R12NR11R12; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; R11 and R12 are independently H and (un)substituted C1-6 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by chlorination of 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetic acid; the resulting 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetyl chloride underwent amidation with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide to give compound II. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.04μM to < 0.2μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate
The Article related to heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica