专利号:US-2022259202-A1 优先权日:2019-06-17 标题:1-(4-(aminomethyl)benzyl)-2-butyl-2h-pyrazolo[3,4-c]quinolin-4-amine derivatives and related compounds as toll-like receptor (tlr) 7/8 agonists, as well as antibody drug conjugates thereof for use in cancer therapy and diagnosis 发明人:MEIMETIS LABROS 权利人:SUTRO BIOPHARMA INC 摘要:1-(4-(aminomethyl)benzyl)-2-butyl-2H-pyrazolo[3,4-c]quinolin-4-amine derivatives thereof and related compounds of formula (I) as toll-like receptor (TLR) 7/8 agonists for cancer therapy. Linker payload compounds thereof, and antibody conjugates thereof for cancer diagnosis. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 145 to 156; examples 1 to 3; biological examples 1 to 6; tables 1 and 2).
1: Bowman CE, da Silva RG, Pham A, Young SW. An Exceptionally Potent Inhibitor of Human CD73. Biochemistry. 2019 Aug 6;58(31):3331-3334. doi: 10.1021/acs.biochem.9b00448. Epub 2019 Jul 23.
合成参考文献
参考文献:10.1021/acs.jmedchem.0c01044 摘要:Jeffrey JL, Lawson KV, Powers JP. Targeting Metabolism of Extracellular Nucleotides via Inhibition of Ectonucleotidases CD73 and CD39. J Med Chem. 2020 Nov 25;63(22):13444–65. doi: 10.1021/acs.jmedchem.0c01044.