专利号:WO-2023086801-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 ('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-2022267323-A1 优先权日:2019-07-23 标题 :Synthesis of bicyclic inhibitors of histone deacetylase 发明人:FULLER NATHAN OLIVER; HEWITT MICHAEL CHARLES; ASSELIN SYLVIE M; LUKE WAYNE DOUGLAS 权利人:ALKERMES INC 摘要:Provided herein are synthetic methods for the preparation of compounds having the Formula: (I) and (I′) and salts thereof.
专利号:WO-0061545-A1 优先权日:1999-04-14 标题 :Methods for solid phase combinatorial synthesis of integrin inhibitors 发明人:GOPALSAMY ARIAMALA; YANG HUI YU 权利人:AMERICAN HOME PROD 摘要:Compounds of the formula (I) are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula (I) are also provided.
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:WO-9815532-A1 优先权日:1996-10-09 标 题:Solid phase synthesis of heterocyclic compounds 发明人:MARZINZIK ANDREAS; FELDER EDUARD 权利人:CIBA GEIGY AG; MARZINZIK ANDREAS; FELDER EDUARD 摘要:Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
专利号:US-6235910-B1 优先权日:1998-09-22 标题:Process for the preparation of imidazolidine-2, 4-diones 发明人:BELLER MATTHIAS; ECKERT MARKUS; MORADI WAHED 权利人:DEGUSSA 摘要:A process for the preparation of compounds of the general formula (I)by reacting an aldehyde compound of the general formula (II)with a urea compound of the general formula (III)in the presence of carbon monoxide and a catalytically active metal compound. Compounds of the general formula (I) are important intermediates for the synthesis of alpha-amino acids.
1: Kopecný D, Briozzo P, Popelková H, Sebela M, Koncitíková R, Spíchal L, Nisler J, Madzak C, Frébort I, Laloue M, Houba-Hérin N. Phenyl- and benzylurea cytokinins as competitive inhibitors of cytokinin oxidase/dehydrogenase: a structural study. Biochimie. 2010 Aug;92(8):1052-62. doi: 10.1016/j.biochi.2010.05.006. Epub 2010 May 15.
合成参考文献
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