专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-5331096-A 优先权日:1992-04-01 标题 :2- and 3-sulfur derivatives of 1,5-iminosugars 发明人:KOSZYK FRANCIS J; MUELLER RICHARD A 权利人:SEARLE & CO 摘要:Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
专利号:US-5342951-A 优先权日:1992-04-01 标题:2- and 3-sulfur derivatives of 1,5-iminosugars 发明人:KOSZYK FRANCIS J; MUELLER RICHARD A 权利人:SEARLE & CO 摘要:Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
专利号:US-5268482-A 优先权日:1992-04-01 标 题:2- and 3-sulfur derivatives of 1,5-iminosugars 发明人:KOSZYK FRANCIS J; MUELLER RICHARD A 权利人:SEARLE & CO 摘要:Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
专利号:US-9185909-B2 优先权日:2007-09-17 标 题:Synthesis of resveratrol-based natural products 发明人:SNYDER SCOTT ALAN; BREAZZANO STEVEN P; ROSS AUDREY G; LIN YUNQING; ZOGRAFOS ALEXANDROS L 权利人:SNYDER SCOTT ALAN; BREAZZANO STEVEN P; ROSS AUDREY G; LIN YUNQING; ZOGRAFOS ALEXANDROS L; UNIV COLUMBIA 摘要:Processes for synthesizing resveratrol-based oligomers are provided. In addition, resveratrol-based oligomer compounds free of plant extract are provided.
专利号:WO-0018790-A1 优先权日:1998-09-25 标 题 :Synthesis of cyclic peptides