Z-苏氨酸甲酯置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 D-苏氨醇 参考文献:Enantioselective Incorporation Of Azobenzenes Into Oligodeoxyribonucleotide For Effective Photoregulation Of Duplex Formation 标题:Enantioselective Incorporation Of Azobenzenes Into Oligodeoxyribonucleotide For Effective Photoregulation Of Duplex Formation 摘要:A Drop In Melting Point Of 21.5oc Is Induced By The Uv-Photolytic Trans->cis Isomerization Of The Duplex Formed Between An Oligonucleotide Bearing Two D-Threoninol-Tethered Azobenzene Moieties In The Side Chain And Its Complementary Counterpart. On Irradiation With Visible Light,The Dissociated Single-Stranded Oligonucleotides Regenerate The Duplex. DOI:10.1002/1521-3773(20010716)40:14<2671::Aid-Anie2671>3.0.Co;2-Z
专利号:US-7659244-B2 优先权日:2003-11-03 标题:Rapamycin peptides conjugates: synthesis and uses thereof 发明人:SHARMA SANJAY K; WOO THOMAS; NAICKER SELVARAJ 权利人:QUEST PHARMATECH INC 摘要:The present invention relates to new rapamycin derivatives for the inhibition of cell proliferation. The compounds can advantageously target two proteins in dividing cells and interfere with cell cycle. There is thus provided derivatives of rapamycin in which the 42 position of rapamycin is linked to an amino acid or a peptide through a carbamate ester linkage. These rapamycin derivatives can be synthesized by reacting 42-O-(4-Nitrophenoxycarbonyl) rapamycin and an amino acid or a free amino peptide under basic conditions. These rapamycin derivatives can be used to inhibit the cell cycle and are therefore useful for treating cell proliferation disorders.
专利号:US-8450342-B2 优先权日:2007-09-12 标题:Perharidines as CDK inhibitors 发明人:MEIJER LAURENT; BETTAYEB KARIMA; GALONS HERVE; DEMANGE LUC; OUMATA NASSIMA 权利人:MEIJER LAURENT; BETTAYEB KARIMA; GALONS HERVE; DEMANGE LUC; OUMATA NASSIMA; CENTRE NAT RECH SCIENT; UNIV RENNES; UNIV PARIS DESCARTES 摘要:The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them. n The compounds of the invention are imidazo[4,5b]pyridines. n The first general synthesis of 3,5,7 imidazo[4,5b]pyridines is disclosed in the description. n The invention founds application, in particular, in the pharmaceutical field.
专利号:US-2003130186-A1 优先权日:2001-07-20 标 题:Conjugates and compositions for cellular delivery 发明人:VARGEESE CHANDRA; MATULIC-ADAMIC JASENKA; KARPEISKY ALEXANDER; BEIGELMAN LEONID; BLATT LAWRENCE; ZINNEN SHAWN 摘要:This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.
专利号:WO-2024256496-A1 优先权日:2023-06-14 标题 :[1,2,4]-triazolo[4,3-b]pyridazine derivatives useful as a medicament 发明人:ELIE JONATHAN; GEORGE PASCAL; MIEGE FRÉDÉRIC; MEIJER LAURENT 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I) or any of its pharmaceutically acceptable salt. The present invention further relates to a synthesis process for manufacturing compound of formula (I) or any of its pharmaceutically acceptable salts, comprising at least a step of reacting a compound of formula (II) with an amine of formula (IV) NHR5R6 for example in a molar ratio ranging from 1 to 20 eq, with respect to the compound of formula (II), in an aprotic solvent or without solvent or else in a protic solvent.
专利号:US-2023313274-A1 优先权日:2022-03-29 标 题 :Photo-responsive oligonucleotides 发明人:PERBOST MICHAEL; PINARD ROBERT; HOSONO SEIYU; NEIL EMILY 权利人:MILTENYI BIOTEC BV & CO KG 摘要:The present invention is to provide a method for hybridization of a photo-responsive oligonucleotide to a nucleic acid by providing the nucleic acid with a complementary oligonucleotide, wherein the oligonucleotide functions as a starting point for a polymerase for nucleic acid synthesis characterized in that the photo-responsive oligonucleotide comprises at least two photo-responsive elements which change from a first to a second conformation upon irradiation with light thereby disabling or enabling the oligonucleotide hybridization. In addition to that, the current invention provides a method for spatially controlled oligonucleotide hybridization to specific sites by spatial illumination of areas of no interest, thus changing the oligonucleotide conformation to a non-binding state. The reversable hybridization of the oligonucleotide can be used for controlling several reactions such as rolling circle amplification and a sequencing reaction.
专利号:US-2025215615-A1 优先权日:2021-11-24 标 题:Method for evaluating dna-encoded library 发明人:NIWA MASATOSHI; TOKUGAWA Munefumi; HAYASHIDA JUN 权利人:NISSAN CHEMICAL CORP 摘要:The invention provides a method of inducing a DNA-encoded library (DEL) comprising cleavable site(s) in the DNA strand to a cross linker-modified double-stranded DEL and evaluating the DEL. Both the merits of the hairpin-stranded DEL and the double-stranded DEL are achieved in the invention by introducing the cleavable site(s) such as deoxyuridine into the DNA strand. The invention further provides a technique for screening a compound in which both “simple DEL synthesis methodâ€? and “expansion and improvement of the DEL evaluation methodâ€? are achieved by easily inducing the compound into a cross linker-modified DEL.
参考文献:10.1002/0471142700.nc0445s46 摘要:Asanuma H, Nishioka H, Ishikawa T, Liang X. Preparation of photoresponsive DNA tethering ortho-methylated azobenzene as a supra-photoswitch. Curr Protoc Nucleic Acid Chem. 2011 Sep;Chapter 4():Unit 4.45.1–18. doi: 10.1002/0471142700.nc0445s46. 参考文献:10.1007/s40242-023-2329-5 摘要:Ding Y, Li Y, Yang B, Pan Y, Cheng J, Meng S, Liu D, Xu L, Dong Y. Preparation of Photo-responsive DNA Supramolecular Hydrogels and Their Application as UV Radiometers. Chem. Res. Chin. Univ. 2023 Jan 09;39(1):115–20. doi: 10.1007/s40242-023-2329-5. 参考文献:10.1007/978-981-19-3987-7_6 摘要:Kuzuya A. Molecular Material for Molecular Robots. 2022. In: Molecular Robotics. 参考文献:10.1007/978-981-19-9776-1_22 摘要:Nagatsugi F. Cross-Linking Duplex of Nucleic Acids with Modified Oligonucleotides. 2023. In: Handbook of Chemical Biology of Nucleic Acids. 参考文献:10.1007/978-981-19-9776-1_86 摘要:Matsuura K, Inaba H. Biomaterials Based on DNA Conjugates and Assemblies. 2023. In: Handbook of Chemical Biology of Nucleic Acids.