专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:US-2025129021-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), Formula (V)), 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-12006337-B2 优先权日:2018-05-30 标题:Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof 发明人:HOLTZMAN MICHAEL J; ROMERO ARTHUR G; GEROVAC BENJAMIN J; HAN ZHENFU; KEELER SHAMUS P; WU KANGYUN; ZHANG YONG 权利人:WASHINGTON UNIVERSITY ST LOUIS 摘要:Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutically for a variety of diseases, including cancer and respiratory diseases. Methods of synthesis of the compounds are also disclosed.
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 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:US-10844081-B2 优先权日:2015-08-07 标题 :Protected organoboronic acids with tunable reactivity, and methods of use thereof 发明人:BURKE MARTIN D; SCHMIDT MICHAEL; MOREHOUSE GREG; PIPAL ROBERT W 权利人:UNIV ILLINOIS 摘要:Disclosed are a range of protected organoboronic acid reagents useful in the modular assembly of complex organic compounds. The reactivities of the protected organoboronic acid reagents may be varied predictably by changes to the number and identities of their substituents. Also disclosed are methods of using the protected organoboronic acid reagents in the synthesis of organic compounds.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
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