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-2009275727-A1 优先权日:1998-03-24 标题:Peptide turn mimetics 发明人:CASSIDY PETER J; ALEWOOD PAUL FRANCIS; VERNALL ANDREA JOY 权利人:MIMETICA PTY LTD 摘要:This invention provides novel compounds useful for the synthesis of peptide mimetics, and describes the use of these compounds for the synthesis of novel reverse turn mimetics. The reverse turn mimetics of the invention have the general structure X wherein the variables are as defined herein.
专利号:US-6534530-B1 优先权日:1999-08-04 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:DRAGOVICH PETER SCOTT; ZHOU RU; WEBBER STEPHEN EVAN; PRINS THOMAS J; REICH SIEGFRIED HEINZ; KEPHART SUSAN E; RUI YUANJIN 权利人:AGOURON PHARMA 摘要:Compounds of the formula:where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:WO-2009045497-A1 优先权日:2007-10-04 标题 :Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
专利号:US-12304912-B2 优先权日:2020-07-28 标 题 :Fused bicyclic RAF inhibitors and methods for use thereof 发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA 权利人:JAZZ PHARMACEUTICALS IRELAND LTD 摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
专利号:US-2010113305-A1 优先权日:1999-03-22 标题:Oxazole and thiazole combinatorial libraries 发明人:MARTIN LENORE M; HU BI-HUANG 权利人:RHODE ISLAND EDUCATION 摘要:This invention provides a novel method for synthesizing an ensemble of peptides that allows for the generation of an unlimited number of antibiotic compounds. More specifically, the method comprises utilizes synthetic heterocyclic amino acids containing thaizole and/or oxazole as building blocks in a solid phase combinatorial synthesis to yield natural and unnatural antibiotic compounds.