专利号:US-2012130699-A1 优先权日:2010-11-22 标 题 :Method of molecular design and synthesis of therapeutic and preventive drugs 发明人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 权利人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 摘要:Industrial Application: This invention may be used in human and veterinary medicine for the design (creation and synthesis) of therapeutic and preventive drugs that are effective for the treatment of oncological and viral human and animal illnesses and for the design of new medicines. n Summary of the Invention: A new method of design and synthesis of therapeutic and preventive drugs in which a biopolymer target (protein, DNA, RNA, or a mixture of these) is used, and in the capacity of a ligand, the same biopolymer target is used, which is cut into oligomer fragments (nucleases, synthetic nucleases, and proteases); the fragments are modified through changing their charges to the opposite charge (acylation of anhydrides of dicarbonate acids or alkylation with halogen-carbonic acids). Also in the capacity of a ligand, the same biopolymer target is used, which is modified by partially changing the molecules' charges to the opposite with the creation of supramolecular biopolymer assemblies. We used supramolecule assemblies made from oligomers that were products of the hydrolysis of biopolymers, but with a change of the charge of the molecules to the opposite charge, as well as the partial change of the charges of the target biopolymers. n Technical Result: A method of molecular design and synthesis of new, unique therapeutic and preventive drugs based on self-organizing systems. The application of the method will allow a significant cut to expenditures on the design and synthesis of new drugs, expand the activity spectra of existing protein gene-engineered drugs, and create new classes of dynamic therapeutic and preventive drugs that self-adapt to the organism and target.
专利号:US-8193384-B2 优先权日:2005-07-29 标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds 发明人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF 权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION 摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.
专利号:US-2024287520-A1 优先权日:2021-06-30 标题:Method for synthesis of linkage modified oligomeric compounds 发明人:RODRIGUEZ ANDREW A 权利人:IONIS PHARMACEUTICALS INC 摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.
专利号:US-10751419-B2 优先权日:2014-05-01 标题:Method for synthesis of reactive conjugate clusters 发明人:MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E 权利人:IONIS PHARMACEUTICALS INC 摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.
专利号:EP-1641812-B1 优先权日:2003-06-30 标题 :PURE d-(17alpha)-13-ETHYL-17-HYDROXY-18,19-DINORPREGN-4-ENE-20-YNE-3-ONE-3E- AND -3Z-OXIME ISOMERS, AS WELL AS PROCESS FOR THE SYNTHESIS OF THE MIXTURE OF ISOMERS AND THE PURE ISOMERS 发明人:TUBA ZOLTAN; MAHO SANDOR; KESERU GYOERGY; KOZMA JOZSEF; HORVATH JANOS; BALOGH GABOR 权利人:RICHTER GEDEON NYRT 摘要:The invention relates to the pure d-(17alpha)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-Â20-yne-3-one-3E-oxime isomer of formula (IA), the pure d-(17alpha)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yne-3-one-3Z-oxime isomer of formula (IB), which are of gestagen activity, as well as the process for the synthesis of the mixture of the above isomers and the pure isomers. The invention also relates to the pharmaceutical compositions - and the process for their synthesis - which contain either the pure isomer of formula (IA) or the pure isomer of formula (IB) as active ingredient as such or in combination with other active ingredients (for example an oestrogen agent) together with pharmaceutical auxiliary materials commonly used in practice.
专利号:WO-0134589-A1 优先权日:1999-11-05 标 题 :Semi-synthesis of baccatin iii from 9-dihydro-13-acetylbaccatin iii 发明人:ZAMIR LOLITA 权利人:ZAMIR LOLITA 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III.
参考文献:10.1016/s1076-6332(03)00815-8 摘要:Chai CM, Almén T, Bååth L, Besjakov J. Adding sodium and calcium ions to the contrast medium iodixanol reduced the risk of ventricular fibrillation during perfusion of the left coronary artery in pigs: effects of electrolytes, viscosity, and chemotoxicity of an isotonic perfusate. Acad Radiol. 2004 May;11(5):583–93. doi: 10.1016/s1076-6332(03)00815-8. 参考文献:10.1007/s00216-008-2016-x 摘要:Sreenath K, Venkatesh YP. Analysis of erythritol in foods by polyclonal antibody-based indirect competitive ELISA. Analytical and Bioanalytical Chemistry. 2008 Mar 28;391(2):609–15. doi: 10.1007/s00216-008-2016-x. 参考文献:10.1016/j.transproceed.2008.01.015 摘要:Park J, Ju MK, Song JS, Huh KH, Kim MS, Kim YS. Effects of mycophenolic Acid on high glucose-induced fibronectin secretion and cellular reactive oxygen species in rat vascular smooth muscle cells. Transplant Proc. 2008 Mar;40(2):467–9. doi: 10.1016/j.transproceed.2008.01.015. 参考文献:10.1016/j.bios.2008.01.033 摘要:Abramov M, Schepers G, Van Aerschot A, Van Hummelen P, Herdewijn P. HNA and ANA high-affinity arrays for detections of DNA and RNA single-base mismatches. Biosens Bioelectron. 2008 Jun 15;23(11):1728–32. doi: 10.1016/j.bios.2008.01.033. 参考文献:10.1016/j.biortech.2011.04.078 摘要:Hu ZC, Zheng YG, Shen YC. Use of glycerol for producing 1,3-dihydroxyacetone by Gluconobacter oxydans in an airlift bioreactor. Bioresour Technol. 2011 Jul;102(14):7177–82. doi: 10.1016/j.biortech.2011.04.078.