📜2-氯-6-甲氧基苯并噻唑置于三溴化硼,Potassium Carbonate,三乙胺体系中,用 四氢呋喃,N-甲基吡咯烷酮,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 83.0H,反应生成 化合物blz945 参考文献:Blz945 Derivatives For Pet Imaging Of Colony Stimulating Factor-1 Receptors In The Brain 标题:Blz945 Derivatives For Pet Imaging Of Colony Stimulating Factor-1 Receptors In The Brain 摘要: DOI:10.1016/j.Nucmedbio.2021.06.005
专利号:US-2024066133-A1 优先权日:2020-03-06 标 题 :Therapeutic agents and conjugates thereof 发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.
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: Zheng C, Zhong Q, Yi K, Kong H, Cao F, Zhuo C, Xu Y, Shi R, Ju E, Song W, Tao Y, Chen X, Li M. Anti-phagocytosis-blocking repolarization-resistant membrane- fusogenic liposome (ARMFUL) for adoptive cell immunotherapy. Sci Adv. 2023 Aug 9;9(32):eadh2413. doi: 10.1126/sciadv.adh2413. Epub 2023 Aug 9. 2: Dye CN, Franceschelli D, Leuner B, Lenz KM. Microglia depletion facilitates the display of maternal behavior and alters activation of the maternal brain network in nulliparous female rats. Neuropsychopharmacology. 2023 Jun 17. doi: 10.1038/s41386-023-01624-1. Epub ahead of print. 636:122849. doi: 10.1016/j.ijpharm.2023.122849. Epub 2023 Mar 17.
合成参考文献
参考文献:10.1021/acs.jmedchem.0c00936 摘要:Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E, Kovacs JJ, Feng N, Gera S, Harris AL, Liu Z, Mullinax RA, Pang J, Parker CA, Spencer ND, Yu SS, Wu Q, Tremblay MR, Mikule K, Wilcoxen K, Heffernan TP, Draetta GF, Jones P. Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R. J Med Chem. 2020 Sep 10;63(17):9888–911. doi: 10.1021/acs.jmedchem.0c00936.