4-溴-3-氟甲苯置于正丁基锂,硼酸三异丙酯体系中,用 四氢呋喃,正己烷,甲苯 用作溶剂,化学反应 2.0H,反应生成2-氟-4-甲基苯硼酸 参考文献: Aza-Bicycloalkyl Ethers And Their Use As Alpha7-Nachr Agonist[fr] Ethers D'Aza-Bicycloalkyle Et Leur Utilisation En Tant Qu'Agoniste De Alpha7-Nachr 标题: Aza-Bicycloalkyl Ethers And Their Use As Alpha7-Nachr Agonist[fr] Ethers D'Aza-Bicycloalkyle Et Leur Utilisation En Tant Qu'Agoniste De Alpha7-Nachr 摘要:本发明涉及式(I)的1-Aza-双环烷基衍生物,其中x是ch2或单键;Y是式(Ii,Iii,Iv)的一个基团,其中r的含义如规范中定义的那样,这些化合物是α7烟碱型乙酰胆碱受体(Nachr)激动剂;以及它们的生产过程,作为药物的使用以及包含它们的药物组合物.
专利号:US-2025304580-A1 优先权日:2021-11-09 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 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 (“TREM2â€?).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-2024233848-A1 优先权日:2023-05-10 标 题:Heterocyclic 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 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:US-12319691-B2 优先权日:2020-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI 权利人:AMGEN INC; 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 (“TREM2â€?).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:US-12428425-B2 优先权日:2020-05-04 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; PANTELEEV JANE; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:AMGEN INC; 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 (“TREM2â€?).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:US-9040704-B2 优先权日:2011-08-12 标题:Fluorescent dyes with large stokes shifts 发明人:PIERS WARREN EDWARD; ARANEDA JUAN FELIPE 权利人:PIERS WARREN EDWARD; ARANEDA JUAN FELIPE; UTI LIMITED PARTNERSHIP 摘要:Herein are disclosed fluorescent dyes based around a framework for a ligand comprising a pyridyl group linked to a diaryl anilido unit. A variety of ligands based on this framework are disclosed. The ligands chelate to a BF 2 center to produce the fluorescent dye. The disclosed dyes combine longer Stokes shifts (approximately 100 nm) with increased quantum yields. They are also photostable in aqueous and organic solutions for several hours. These dyes may be used in the labeling of biomolecules for bioimaging and assays. Also disclosed are methods for the synthesis of these dyes.
专利号:US-8933018-B2 优先权日:2011-02-07 标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof 发明人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA 权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.