专利号:US-8058414-B2 优先权日:2008-04-29 标题 :Unnatural polymerase substrates that can sustain enzymatic synthesis of double stranded nucleic acids from a nucleic acid template and methods of use 发明人:MENCHEN STEVEN; ROSENBLUM BARNETT; KENNEY PAUL; KHAN SHOEB; MA ZHAOCHUN; CHEN JER-KANG; LAM JOE Y; HUANG BOLI 权利人:MENCHEN STEVEN; ROSENBLUM BARNETT; KENNEY PAUL; KHAN SHOEB; MA ZHAOCHUN; CHEN JER-KANG; LAM JOE Y; HUANG BOLI; LIFE TECHNOLOGIES CORP 摘要:Nucleotide analogs that can sustain the enzymatic synthesis of double-stranded nucleic acid from a nucleic template are described. The nucleotide analogs include: (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine, uracil and their analogs; (ii) a label attached to the base or analog of the base via a cleavable linker; (iii) a deoxyribose; and (iv) one or more phosphate groups. The linker and/or the label inhibits template directed polymerase incorporation of a further nucleotide substrate onto an extended primer strand. In addition, cleavage of the linker leaves a residue attached to the base which is not present in the natural nucleotide and which does not inhibit extension of the primer strand. The nucleotide analogs can therefore be used as reversible terminators in sequencing by synthesis methods without blocking the 3′ hydroxyl group. Methods of sequencing DNA using the substrates are also described.
专利号:WO-2022260545-A1 优先权日:2021-06-11 标题:Synthesis of a novel glucose-conjugated methotrexate and its application for the treatment and prevention of neoplasms 发明人:AGRAWAL SIDDARTH; WOŹNIAK MARTA; MAKUCH SEBASTIAN; Szeja WiesÅ‚aw; PASTUCH-GAWOÅ?EK GABRIELA; KRAWCZYK MONIKA; WiÅ›niewski Jerzy; GAMIAN ANDRZEJ; ZIÓÅ?KOWSKI PIOTR 权利人:UNIV MEDYCZNY IM PIASTOW SLASKICH WE WROCLAWIU 摘要:The subject of the invention is a new methotrexate-glucose conjugate derivative, its synthesis, and its use in the treatment and prevention of neoplasms, preferably in the treatment and prevention of neoplasms selected from: skin cancer, colorectal cancer, breast cancer, gastric cancer, sarcoma and lung cancer.
专利号:US-2024261416-A1 优先权日:2023-01-31 标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.
专利号:US-9896473-B2 优先权日:2012-04-04 标 题:Thiol compounds and the use thereof for the synthesis of modified oligonucleotides 发明人:MORVAN FRANÇOIS; MEYER ALBERT; VASSEUR JEAN JACQUES; MAYEN JULIE; CHAIX CAROLE; FARRE CAROLE; FOURNIER WIRTH CHANTAL; CANTALOUBE Jean François; LEREAU MYRIAM 权利人:CENTRE NAT RECH SCIENT; UNIV DE MONTPELLIER 1; FRANCAIS DU SANG ETS; UNIV CLAUSE BERNARD LYON 1; FRANCAIS DU SANG ETS 摘要:The present invention relates to a thiol compound suitable for forming a chain of oligomers that can be grafted to an oligonucleotide. The invention also relates to an oligonucleotide grafted by such a compound, thus having one or more thiol functions, suitable for being immobilized on a gold surface or on a grafted surface.
专利号:US-4465845-A 优先权日:1982-04-26 标题:High pressure synthesis of sulfur-selenium fulvalenes 发明人:OKAMOTO YOSHIYUKI; WOJCIECHOWSKI PIOTR S 权利人:KOPPERS CO INC 摘要:A process is disclosed for one-step preparation of sulfur-selenium fulvalenes by reaction of an acetylenic compound with carbon selenide sulfide or with a mixture of carbon diselenide and carbon disulfide under pressures of at least about 1,000 atmospheres. Fulvalene compounds made by the process are characterized in having at least one sulfur atom and at least one selenium atom in the ring structure of the fulvalene compound. Substituted diselenadithiafulvalenes made by this process are precursors to very pure diselenadithiafulvalene which is useful in preparing charge-transfer salts.
专利号:US-12263177-B2 优先权日:2019-02-07 标题:Biologically active ganoderma lucidum compounds and synthesis of anticancer derivatives; ergosterol peroxide probes for cellular localization 发明人:MARTINEZ-MONTEMAYOR MICHELLE M; RIVAS FATIMA 权利人:UNIV CENTRAL DEL CARIBE; ST JUDE CHILDRENS RES HOSPITAL INC 摘要:The bioactive compounds of Ganoderma lucidum extract (GLE) responsible for anticancer activity were elucidated using NMR, X-ray crystallography and analogue derivatization, as well as anti-cancer activity studies. Structures of the seven most abundant GLE compounds are disclosed. Their selective efficacy against triple negative (TNBC) and inflammatory breast cancers (IBC) and other human cancer cell types (solid and blood malignancies) was shown, confirming potential their as anticancer agents.
摘要:Shimizu, M., Science of Synthesis Knowledge Updates, (2010) 3, 26. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 84. 摘要:Kacprzak, K. M.; Skiera, I.; Rutkowski, J., Science of Synthesis, (2021) , 184. 参考文献:10.1021/jm901558p 摘要:Carmi C, Cavazzoni A, Vezzosi S, Bordi F, Vacondio F, Silva C, Rivara S, Lodola A, Alfieri RR, La Monica S, Galetti M, Ardizzoni A, Petronini PG, Mor M. Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. J Med Chem. 2010 Mar 11;53(5):2038–50. doi: 10.1021/jm901558p.