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-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-9125880-B2 优先权日:2002-12-26 标 题:Polymer conjugates of interferon-beta with enhanced biological potency 发明人:SAIFER MARK G P; MARTINEZ ALEXA L; WILLIAMS L DAVID; SHERMAN MERRY R 权利人:SAIFER MARK G P; MARTINEZ ALEXA L; WILLIAMS L DAVID; SHERMAN MERRY R; MOUNTAIN VIEW PHARMACEUTICALS 摘要:Methods are provided for the synthesis of polymer conjugates of cytokines and receptor-binding antagonists thereof, especially a non-glycosylated interferon-beta, which conjugates retain unusually high biological potency. Preparation of polymer conjugates according to the methods of the present invention diminishes or avoids steric inhibition of receptor-ligand interactions that commonly results from the attachment of polymers to receptor-binding regions of cytokines, as well as to agonistic and antagonistic analogs thereof. The invention also provides conjugates and compositions produced by such methods. The conjugates of the present invention retain a high level of biological potency compared to those produced by traditional polymer coupling methods that are not targeted to avoid receptor-binding domains of cytokines. In assays in vitro, the biological potency of the conjugates of non-glycosylated interferon-beta of the present invention is substantially higher than that of unconjugated interferon-beta and is similar to that of interferon-beta-1a that is glycosylated. The conjugates of the present invention also exhibit an extended half-life in vivo compared to the corresponding unconjugated cytokine. The present invention also provides kits comprising such conjugates and/or compositions, and methods of use of such conjugates and compositions in a variety of diagnostic, prophylactic and therapeutic applications, including treatment of multiple sclerosis.
专利号:US-2024350645-A1 优先权日:2021-07-22 标 题 :Automated synthesis of polymeric drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein L 1 , L 2 , L 3 , R 1 R 2 , M, p, q, m, and n are as defined herein. Additional compounds, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
专利号:US-2023313156-A1 优先权日:2020-08-06 标题 :Chemical synthesis of large and mirror-image proteins and uses thereof 发明人:ZHU TING; Fan Chuyao; DENG QIANG; XU YUAN 权利人:UNIV TSINGHUA 摘要:Provided herein is a general method for producing large (more than 400 aa long) D-amino acids proteins, also referred to as mirror image protein (with respect to their naturally occurring L-amino acids counterparts), including RNA/DNA manipulating enzymes, and uses thereof in a wide range of research, practical data storage and medicinal applications.
专利号:US-2010311946-A1 优先权日:2009-06-03 标 题:Solid Phase Peptide for the Production of Goserelin 发明人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R 权利人:MALLINCKRODT INC 摘要:The present invention provides a process for the production of goserelin. In particular, the process of the invention allows the use of side chain protecting groups during synthesis of the peptide, and the addition of the azaglycine moiety of the peptide.
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合成参考文献
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