专利号:US-2025313590-A1 优先权日:2024-03-16 标题:Phosphoramidite morpholino monomers towards synthesis/convergent synthesis of PMO, TMO, their chimera oligos in 5 prime to 3 prime direction 发明人:SINHA SURAJIT; GHOSH ATANU; BANERJEE ARPAN 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:The present invention relates to 5′-morpholino amidite monomers as 5′-CE/5′- t Bu phosphoramidite morpholino monomers (2) and process chemistry for the efficient synthesis of N-Trityl or monomethoxytrityl (MMTr)-protected 5′-morpholino amidite monomers and their use in the synthesis of phosphorodiamidate morpholino oligonucleotides (PMO), thiophosphoramidate morpholino oligonucleotides (TMO) and their chimeras which can be used for antisense technology or in general oligonucleotides related research.
专利号:US-12012427-B2 优先权日:2019-10-31 标 题 :Synthesis of Fmoc-protected morpholino monomers and their use in the synthesis of morpholino oligomer 发明人:SINHA SURAJIT; KUNDU JAYANTA; GHOSH UJJWAL 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:Present invention relates to stable Fmoc protected Morpholino monomers and corresponding oligonucleotides (PMO) and efficient synthesis of the same involving chlorophosphoramidate and H-Phosphonate chemistry. Successful syntheses of the oligonucleotide with higher yield and lesser time have been accomplished employing solid phase synthesis and easy deprotection of Fmoc group with Piperidine.
专利号:US-8981076-B2 优先权日:2008-11-29 标 题 :Synthesis of N-FMOC protected deoxy nucleosides, ribo nucleosides, modified deoxy and ribo nucleosides, and phosphoramidites, and their use in oligonucleotide synthesis 发明人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P 权利人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P; CHEMGENES CORP 摘要:This invention relates to synthesis of novel -N-FMOC protected nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-FMOC as nucleoside base protecting group, which is highly base labile protecting group is a novel approach to obtain highest purity oligonucleotides. This approach is designed to lead to very high purity and very clean oligonucleotide, after efficient removal of the protecting groups and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform. The deprotection of FMOC protecting groups of the natural deoxy and ribonucleosides occurs under very mild deprotection conditions such as mild bases, secondary and tertiary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application. This approach is further designed to use FMOC protecting group on various base sensitive nucleoside, and for use in oligo peptide synthesis and for support bound oligo nucleotides. DNA oligonucleotides containing 3′-end dA at the 3′-terminal will be produced using the FMOC-dA-supports would lead to much reduced M−1 deletion sequences, and thereby high purity.
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-2010143980-A1 优先权日:2007-02-22 标题:Synthesis of novel xylosides and potential uses thereof 发明人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM 权利人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM 摘要:The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Clickâ€? chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.
专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
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