专利号:US-2023272006-A1 优先权日:2021-08-31 标题:Peptidomimetics and method of synthesis thereof 发明人:NEFZI ADEL 权利人:NEFZI ADEL; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides compounds, peptidomimetics, and methods of synthesis thereof. The subject invention provides the synthesis and use of guanidino acids and/or poly guanidino acids not only as vehicles for drug delivery but as toolbox for drug discovery. The peptidomimetic of the subject invention comprises oligo(guanidino acid)s or poly(guanidino acid)s with guanidines as peptide bond surrogates. The incorporation of the guanidine as amide bond surrogates offers significant differences in polarity, hydrogen bonding capability, and acid-base character.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
专利号:CN-104284891-A 优先权日:2012-03-17 标 题:Conformational Restricted Total Synthesis of Macrocyclic Compounds
专利号:US-6872745-B2 优先权日:2000-04-14 标 题 :Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:JOHNSON JR THEODORE O; HUA YE; LUU HIEP T; DRAGOVICH PETER S 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n n nwhere 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:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-2024124517-A1 优先权日:2020-12-25 标题:Method for producing peptide compound containing n-substituted-amino acid residue 发明人:MORITA YUYA; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:An object of the present invention is to provide a method for efficiently producing a high-purity peptide compound with a high yield. It has been found that the object can be achieved by supporting a peptide on a solid phase synthesis resin prior to a first elongation reaction in a solid phase process.
参考标题:First Total Synthesis Of Versicotide D And Analogs 作者:Laura Posada,Gloria Serra |发布日期:2019.11 摘要:The First Total Synthesis Of Cyclotetrapeptide Versicotide D Has Been Achieved In 21% Overall Yield Using Solid Phase Peptide Synthesis And Solution Cyclization. In Addition, In The Search For Candidates Of Antimalarial New Drugs, One Cyclic Tetrapeptide Analog Which Differs In The Sequence, And Four Cyclic Pentapeptide Containing N-Methyl Amino Acids, Were Prepared. The Obtained Compunds Were Evaluated