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-9751911-B2 优先权日:2012-11-27 标 题:Solomonamide analogue compounds, pharmaceuticals containing solomonamide analogue compounds, and processes for the preparation thereof 发明人:REDDY DUMBALA SRINIVASA; KOMIRISHETTY KASHINATH; NATARAJAN VASUDEVAN 权利人:COUNCIL SCIENT IND RES 摘要:Solomanamide analogs of Formula-I having anti-inflammatory activity, and viable synthetic routes for the preparation of such analogs, including the synthesis of macrocyclic core of Salomanamide analogs. The Solomanamide analogs of Formula-I or their pharmaceutical salt may be provided in a pharmaceutical composition and administered in an effective amount for the treatment of inflammation and/or pain.
专利号:US-2786049-A 优先权日:1956-02-20 标 题:Synthesis of peptide structures 发明人:LUNDGREN HAROLD P; WALDEN MAYO K; GORDON ROSE WILLIAM 权利人:LUNDGREN HAROLD P; WALDEN MAYO K; GORDON ROSE WILLIAM
专利号:IL-142499-A 优先权日:1994-06-08 标题 :Building units for synthesis of backbone cyclized peptide analogs
专利号:US-6265375-B1 优先权日:1994-06-08 标题 :Conformationally constrained backbone cyclized peptide analogs 发明人:GILON CHAIM; EREN DORON; ZELTSER IRINA; SERI-LEVY ALON; BITAN GAL; MULLER DAN 权利人:YISSUM RES DEV CO; PEPTOR LTD 摘要:Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are Nalpha(omega-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nalpha(omega-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
参考标题:Solomonamide Analogue Compounds, Pharmaceuticals Containing Solomonamide Analogue Compounds, And Processes For The Preparation Thereof 摘要:Solomanamide Analogues Of Formula-I Having Anti-Inflammatory Activity, And Viable Synthetic Routes For The Preparation Of Such Analogues, Including The Synthesis Of Macrocyclic Core Of Salomanamide Analogues. The Solomanamide Analogues Of Formula-I Or Their Pharmaceutical Salt May Be Provided In A Pharmaceutical Composition And Administered In An Effective Amount For The Treatment Of Inflammation And/or Pain.
合成参考文献
参考文献:10.1074/jbc.m501453200 摘要:Schumacher M, Mizuno K, Bächinger HP. The Crystal Structure of the Collagen-like Polypeptide (Glycyl-4(R)-hydroxyprolyl-4(R)-hydroxyprolyl)9 at 1.55 Å Resolution Shows Up-puckering of the Proline Ring in the Xaa Position. Journal of Biological Chemistry. 2005 May;280(21):20397–403. doi: 10.1074/jbc.m501453200.