专利号:WO-2023086799-A1 优先权日:2021-11-09 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:CN-101781245-A 优先权日:2009-06-26 标题 :A new method for the synthesis of substituted pyridine-3-carboxylic acids and analogues
专利号:US-7879885-B2 优先权日:2004-03-24 标 题:Thioalkeneamides as transketolase inhibitors 发明人:BOYD STEVEN A; CONDROSKI KEVIN R; THOMAS ALLEN; GONZALES STEPHEN S; GUNAWARDANA INDRANI W; HUEROU YVAN LE; ROMOFF TODD T; SULLIVAN FRANCIS X 权利人:ARRAY BIOPHARMA INC 摘要:The present invention provides thioalkeneamides of formula (I) which are useful as transketolase inhibitors: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R a -R d , n and ring A are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.
参考文献:10.3389/fmolb.2022.880432 摘要:Thomas SE, McCarthy WJ, El Bakali J, Brown KP, Kim SY, Blaszczyk M, Mendes V, Abell C, Floto RA, Coyne AG, Blundell TL. Structural Characterization of Mycobacterium abscessus Phosphopantetheine Adenylyl Transferase Ligand Interactions: Implications for Fragment-Based Drug Design. Front Mol Biosci. 2022;9():880432.