专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-12247037-B2 优先权日:2018-12-12 标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders 发明人:BRANDT GARY 权利人:NEUMORA THERAPEUTICS INC 摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:WO-2025128873-A1 优先权日:2023-12-12 标题:Heterocyclic pyridinone compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 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:WO-2023131254-A1 优先权日:2022-01-06 标 题 :Pseudouridine modified at n1 position and use thereof in mrna synthesis 发明人:LI SONG; GUO CHUANXIN; CAI XIAORU; QIAN QIJUN 权利人:MAXIRNA SHANGHAI PHARMACEUTICAL CO LTD; MAXIRNA ZHEJIANG TECH CO LTD 摘要:Provided in the present invention are a pseudouridine modified at an N1 position and the use thereof in mRNA synthesis. Specifically, the compound of the present invention comprises compounds represented by formula I and formula II, and the definition of each group in the formula is as described herein. The compound of the present invention can be used for preparing mRNA to reduce the autoimmunogenicity of the mRNA, improve the stability of the mRNA itself, and/or enhance the expression time and expression efficiency of the mRNA in a target cell.
专利号:US-2024409557-A1 优先权日:2023-05-09 标 题 :5,6-fused and 6,6-fused bicyclic alcohols and ethers and compositions for use as 15-prostaglandin dehydrogenase modulators 发明人:GREENMAN KEVIN LLOYD; PICKRELL ALEXANDER J; LI KEXUE; AMEGADZIE ALBERT K; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; BOURBEAU MATTHEW P 权利人:AMGEN INC 摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A).Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).
专利号:US-11858943-B2 优先权日:2017-06-05 标题:Vasopressin receptor antagonists and products and methods related thereto 发明人:JONES ROBERT M; URBANO MARIANGELA; BRANDT GARY; HARDICK DAVID; KNIGHT CHRIS; TIERNEY JASON 权利人:NEUMORA THERAPEUTICS INC 摘要:Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof:wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.
参考文献:10.1055/s-0037-1610237 摘要:Ryabukhin S, Melnykov K, Granat D, Volochnyuk D, Grygorenko O. Multigram Synthesis of C4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks. Synthesis. 2018 Aug 20;50(24):4949–57. doi: 10.1055/s-0037-1610237. 参考文献:10.1007/s00044-023-03088-w 摘要:Wehn PM, Yang S, Grina JA, Rizzi JP, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Czerwinski RM, Ged EL, Huang H, Halfmann MM, Maddie MA, Morton ER, Olive SR, Tan H, Xie S, Josey JA, Wallace EM. Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→π*Ar interaction. Med Chem Res. 2023 Jul;32(7):1510–31. doi: 10.1007/s00044-023-03088-w.