专利号:US-2023407293-A1 优先权日:2021-10-27 标 题:Dna-encoded and affinity-tagged masked-warhead compounds and use thereof in assembling libraries of small molecules enabled for late-stage purification and multiplexed screening of covalent ligands 发明人:MAIANTI JUAN PABLO 权利人:MAIANTI JUAN PABLO 摘要:The present disclosure relates to DNA-encoded and affinity-tagged masked warhead installation compounds and use thereof in the synthesis of electrophilic warhead DNA-Encoded Libraries (eDEL), including substituted and unsubstituted acrylamide warheads, which can be purified from unreacted library intermediates and byproducts.
专利号:US-8076496-B2 优先权日:2000-03-16 标题:Chemoselective ligation 发明人:SAXON ELIANA; BERTOZZI CAROLYN RUTH 权利人:SAXON ELIANA; BERTOZZI CAROLYN RUTH; UNIV CALIFORNIA 摘要:The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-2024109924-A1 优先权日:2021-01-29 标 题 :Ip4-4,6 substituted derivative compounds 发明人:PÉREZ FERRER MARÃ?A DEL MAR; FERRER REYNÉS MIQUEL DAVID; BASSISSI MOHAMAD FIRAS; SALCEDO ROCA CAROLINA; SERRA COMAS CARME; CATENA RUIZ JUAN LORENZO; LLEBARIA SOLDEVILA AMADEU; ORTEGA CASTRO JOAQUÃ?N; PERELLÓ BESTARD JOAN 权利人:SANIFIT THERAPEUTICS S A 摘要:The present invention provides IP4-4,6 substituted derivatives, their methods of synthesis and their uses. In some aspects, the IP4-4,6 derivative is a compound of formula I wherein R1, R3, R7, and R11 are OPO32−, and R5 and R9 are selected from the group consisting of —O(Alkyl)nX, —O(Alkyl)yCy(Alkyl2)y-Z, —O(Alkyl)yA(Alkyl)y-Z′, and their thiophosphate analogs. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.
专利号:US-12188086-B2 优先权日:2018-03-15 标 题:Nucleotide analogues and use thereof for nucleic acid sequencing and analysis preliminary class 发明人:JU JINGYUE; LI XIAOXU; KUMAR SHIV; CHEN XIN; RUSSO JAMES J; CHIEN MINCHEN; JOCKUSCH STEFFEN; TAO CHUANJUAN; WANG XUANTING; KALACHIKOV SERGEY; Morozova Irina; SHI SHUNDI 权利人:UNIV COLUMBIA 摘要:The invention provides various orthogonal nucleotide analogues and methods for using combinations of said various orthogonal nucleotide analogues for sequencing by synthesis.
专利号:CN-116640123-A 优先权日:2022-02-15 标 题:Bifunctional molecule compound for inducing degradation of HK2 protein and synthesis and application thereof
专利号:CN-115433356-A 优先权日:2022-03-11 标 题:A kind of PEG-modified fluorinated Cy7 micelles and its synthesis method and application
参考标题:Design, Synthesis, And Anti-Bacterial Evaluation Of Triazolyl-Pterostilbene Derivatives 作者:Kai-Wei Tang,Shih-Chun Yang,Chih-Hua Tseng 摘要:Scaffold For The Hybrid 1,2,3-Triazole Moiety To Develop A Novel Anti-Mrsa Infection Agent. In This Study, We Demonstrated The Design And Synthesis Of A Series Of Triazolylpterostilbene Derivatives. Among These Compounds, Compound 4D Exhibited The Most Potent Anti-Mrsa Activity With A Minimum Inhibitory Concentration (Mic) Value Of 1.2-2.4 μg/ml And A Minimum Bactericidal Concentration (Mbc) Value Of 19.5-39
合成参考文献
参考文献:10.1055/s-0033-1339312 摘要:Zhu L, Barsoum D, Brassard C, Deeb J, Okashah N, Sreenath K, Simmons J. Synthesis of 5-Iodo-1,2,3-triazoles from Organic Azides and Terminal Alkynes: Ligand Acceleration Effect, Substrate Scope, and Mechanistic Insights. Synthesis. 2013 Jul 19;45(17):2372–86. doi: 10.1055/s-0033-1339312.