专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
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-2013296346-A1 优先权日:2010-11-23 标题 :Diphenyl-amine derivatives: uses, process of synthesis and pharmaceutical compositions 发明人:RODES SOLANES ROSA; GARCIA DOMINGUEZ NEFTALI; LOPEZ ORTEGA BEATRIZ; ALVAREZ DE MON SOTO MELCHOR; DE LA HERA MARTINEZ ANTONIO; MUNOZ MUNOZ ANA; LEDO GOMEZ FRANCISCO 权利人:RODES SOLANES ROSA; GARCIA DOMINGUEZ NEFTALI; LOPEZ ORTEGA BEATRIZ; ALVAREZ DE MON SOTO MELCHOR; DE LA HERA MARTINEZ ANTONIO; MUNOZ MUNOZ ANA; LEDO GOMEZ FRANCISCO; FAES FARMA SA 摘要:The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
专利号:US-6228988-B1 优先权日:1995-02-24 标题:Synthesis of hydroxamic acid derivatives 发明人:FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN 权利人:BRITISH BIOTECH PHARM 摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.
专利号:US-2024051897-A1 优先权日:2022-07-26 标题:Synthesis of complex 15n-labeled molecules 发明人:DORSHEIMER JULIA; ROVIS TOMISLAV 权利人:UNIV COLUMBIA 摘要:Methods for conversion of a broad range of amines to their 15N isotopic counterparts and the compounds produced thereby.
专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
参考标题:Synthesis And Biological Activity Of Peptide α-Ketoamide Derivatives As Proteasome Inhibitors 作者:Salvatore Pacifico,Valeria Ferretti,Valentina Albanese,Anna Fantinati,Eleonora Gallerani,Francesco Nicoli,Riccardo Gavioli,Francesco Zamberlan,Delia Preti,Mauro Marastoni |发布日期:2019.7.11 摘要:Proteasome Activity Affects Cell Cycle Progression As Well As The Immune Response, And It Is Largely Recognized As An Attractive Pharmacological Target For Potential Therapies Against Several Diseases. Herein We Present The Synthesis Of A Series Of Pseudodi/tripeptides Bearing At The C-Terminal Position Different α-Ketoamide Moieties As Pharmacophoric Units For The Interaction With The Catalytic Threonine
合成参考文献
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