专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-4033940-A 优先权日:1975-11-12 标 题:Cyclization of peptides 发明人:HUGHES JOHN L; SEYLER JAY K; LIU ROBERT C 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing an amino terminal cystine residue and a cysteine residue located in a position within the amino acid sequence, to give a desired peptide, and placing such intermediate peptide in a solution substantially free of oxygen at a pH of from about 5 to 10 until rearrangement takes place to yield a cyclic disulfide peptide and to displace a molecule of cysteine from the amino terminal cysteine residue. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:US-4388235-A 优先权日:1982-02-12 标 题:Synthesis of peptides 发明人:ORLOWSKI RONALD C; SEYLER JAY K 权利人:ARMOUR PHARMA 摘要:New peptides are disclosed which have biological activity of the same type as known calcitonins and which have a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.
专利号:US-4217268-A 优先权日:1978-07-20 标 题:Synthesis of peptides 发明人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K 权利人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K 摘要:A new peptide is disclosed which has biological activity of the same type as known calcitonins and which has a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.
专利号:US-4062815-A 优先权日:1974-08-12 标 题:Resin peptides 发明人:HUGHES JOHN LAWRENCE; SEYLER JAY KENNETH; LIU ROBERT CHUNG-HUANG 权利人:ARMOUR PHARMA 摘要:Resin peptides useful in the preparation of salmon calcitonin are disclosed along with processes for preparing the same. The invention also embraces peptides from which the resin moiety has been cleaved and which are useful in the synthesis of salmon calcitonin together with processes for preparing the cleaved peptides. In general, the processes involve the solid phase synthesis procedures.
专利号:US-4061626-A 优先权日:1976-04-29 标题 :Somatostatin analogs and intermediates thereto 发明人:SHIELDS JAMES E 权利人:LILLY CO ELI 摘要:The tetradecapeptides in which Y is Gly or D-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. The tetradecapeptide in which Y is Gly as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo inhibition of the release of gastric acid. The tetradecapeptide in which Y is D-Ala as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo stimulation of the release of growth hormone.
参考文献:10.1007/bf01025170 摘要:Ogawa H, Burke GT, Katsoyannis PG. Synthesis and biological evaluation of a modified insulin incorporating the COOH-terminal hexapeptide (“D-region”) of insulin-like growth factor II. The Protein Journal. 1984 Aug;3(4):327–48. doi: 10.1007/bf01025170. 参考文献:10.1007/s13534-016-0239-x 摘要:Lowe B, Nam SY. Synthesis and biocompatibility assessment of a cysteine-based nanocomposite for applications in bone tissue engineering. Biomedical Engineering Letters. 2016 Nov;6(4):271–5. doi: 10.1007/s13534-016-0239-x.