专利号:US-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
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-6953850-B1 优先权日:1999-01-18 标题:Protecting groups for carbohydrate synthesis 发明人:DEKANY GYULA; PAPAGEROGIOU JOHN; BORNAGHI LAURENT FRANCOIS 权利人:ALCHEMIA PTY LTD 摘要:The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N 3 ; X 1 is hydrogen, —CH 2 O—, —CH 2 NH—, —CH 3 , —CH 2 N 3 or —COO—; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N 3 , and E is absent when X 1 is hydrogen, CH 3 or N 3 .
专利号:US-2023295162-A1 优先权日:2020-08-06 标 题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity 发明人:CSÃ?MPAI ANTAL; BÃ?RÃ?NY PÉTER; CZUCZI TAMÃ?S; Kovács Imre; ADAMIS BÃ?LINT; NÉMETH ZSÓFIA; MURÃ?NYI JÓZSEF; OLÃ?HNÉ SZABÓ RITA; BOSZE SZILVIA; MEZO GÃ?BOR; KOHIDAI LÃ?SZLÓ; LAJKÓ ESZTER; TAKÃ?CS ANGÉLA; Láng Orsolya; MEZO DIÃ?NA 权利人:EOETVOES LORAND TUDOMANYEGYETEM; SEMMELWEIS EGYETEM 摘要:The present invention relates to compounds of formula (I) (I) or pharmaceutically acceptable salts, and stereoisomers thereof, including enantiomers, racemic mixtures, mixtures of enantiomers, or combinations thereof, which are applicable for use in treating cancer diseases. The present invention further relates to a pharmaceutical composition comprising the above compounds.
专利号:WO-2011090968-A1 优先权日:2010-01-22 标题:Post-synthetic chemical modification of rna at the 2'-position of the ribose ring via 'click' chemistry 发明人:ZEWGE DANIEL; GOSSELIN FRANCIS 权利人:MERCK SHARP & DOHME; ZEWGE DANIEL; GOSSELIN FRANCIS 摘要:This invention relates to the post-synthetic chemical modification of RNA at the 2'-position on the ribose ring via a copper catalyzed Huisgen cycloaddition ('click' chemistry: Kolb, Sharpless Drug Discovery Today 2003, 8, 1128). The invention 1) avoids complex, tedious multi-step syntheses of each desired modified ribonucleoside; 2) allows diverse chemical modifications using high-fidelity chemistry that is completely orthogonal to commonly used alkylamino, carboxylate and disulfide linker reactivities; 3) allows introduction of functional groups that are incompatible with modern automated solid-phase synthesis of RNA and subsequent cleavage-deprotection steps; 4) allows introduction of functional groups useful as targeting ligands; and 5) enables high-throughput structure-activity relationship studies on chemically modified RNA in 96-well format.
专利号:US-8268936-B2 优先权日:2005-01-04 标题:Synthesis of hybrid block copolymers and uses thereof 发明人:BREITENKAMP KURT; SILL KEVIN N 权利人:BREITENKAMP KURT; SILL KEVIN N; INTEZYNE TECHNOLOGIES INC 摘要:The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and methods of preparing the same.
参考标题:Synthesis Of 5-Hydroxy- And 5-Sulfanyl-Substituted [1,2,3]Triazolo[4,5-е][1,4]Diazepines 作者:Sergiy V. Kemskiy,Natalia A. Syrota,Andriy V. Bol'But,Viktor I. Dorokhov,Mykhaylo V. Vovk |发布日期:2018.8 摘要:5-Amino-N-(2,2-Dimethoxyethyl)-1н-1,2,3-Triazole-4-Carboxamides In Formic Acid Were Subjected To Intramolecular Cyclization To 5-Hydroxy[1,2,3]Triazolo[4,5-е][1,4]Diazepines, Which Were Converted By Treatment With S-Nucleophiles To 5-Thio-Functionalized Derivatives.
合成参考文献
参考文献:10.1107/s1600536811009123 摘要:Ouzidan Y, Kandri Rodi Y, Fronczek FR, Venkatraman R, Essassi EM, El Ammari L. 3-[(1-Benzyl-1H-1,2,3-triazol-5-yl)methyl]-6-bromo-2-phenyl-3H-imidazo[4,5-b]pyridine. Acta Crystallogr E Struct Rep Online. 2011 Mar 15;67(4):o890–1. doi: 10.1107/s1600536811009123.