专利号:US-2021130409-A1 优先权日:2017-09-01 标 题 :Method for the Solid-Phase Synthesis of Cyclic Pentapeptides 发明人:ZHENGGUO JIANG; LUCIANO FORNI; ROBERTSON ALAN 权利人:Alsonex Pty Ltd 摘要:A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; n n n n n n n n n n n n wherein R 1 and R 2 are, independently, —H, or —C(O)R 3 where R 3 is —CH 2 Ph, —CH 2 CH 2 Ph, —CHâ•?CHPh, —C(NHAC)CH 2 Ph;n nthe method comprising the steps of;n nforming a linear proline-D-cyclohexylalanine-tryptophan-arginine-ornithine pentapeptide of Formula B, attached to a polymeric resin;n n n n n n n n n n n n n n n n n wherein R 1 is as for Formula A, RES indicates the polymeric resin, and P 1 and P 2 are protecting groups;n ncyclising the linear pentapeptide of Formula B to form a cyclic pentapeptide of Formula C, attached to the polymeric resin;n n n n n n n n n n n n n n n cleaving the cyclic peptide of Formula C from the resin providing a cleaved cyclic pentapeptide having a free amine group of an ornithine residue;n noptionally substituting the free amine group of the ornithine residue of the cleaved cyclic peptide;n nremoving the protecting groups P 1 and P 2 , to providethe cyclic peptide of Formula A.
专利号:US-10087221-B2 优先权日:2013-03-21 标题 :Synthesis of hydantoin containing peptide products 发明人:HENKEL BERND 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.
专利号:US-2015148524-A1 优先权日:2012-07-06 标题:Amino acid analogues and methods for their synthesis 发明人:WANG ZHEN; ROBINSON ANDREA; SPICCIA NICOLAS DANIEL; JACKSON WILLIAM ROY 权利人:UNIV MONASH 摘要:A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R 1 and R 2 are independently selected from H and substituted or unsubstituted C 1 to C 4 alkyl; each R 3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C 1 to C 20 alkyl, and a substituted or unsubstituted C 1 to C 20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse step (i) also catalyses step (ii).
专利号:WO-2008098280-A1 优先权日:2007-02-16 标题:Methods for the synthesis of dicarba bridges in growth hormone peptides 发明人:ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 权利人:POLYCHIP PHARMACEUTICALS PTY; UNIV MONASH; ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 摘要:The invention relates to peptides comprising the carboxy terminal sequence of a growth hormone or an analogue of such a peptide in which the disulfide bridge is replaced by a dicarba bridge. Compositions containing such dicarba bridged peptides and method of treating obesity in an animal such as a human comprising administration of such dicarba bridged peptides are also disclosed.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
参考文献:10.1371/journal.pone.0019823 摘要:Opitz CA, Litzenburger UM, Opitz U, Sahm F, Ochs K, Lutz C, Wick W, Platten M. The Indoleamine-2,3-Dioxygenase (IDO) Inhibitor 1-Methyl-D-tryptophan Upregulates IDO1 in Human Cancer Cells. PLoS ONE. 2011 May 20;6(5):e19823. doi: 10.1371/journal.pone.0019823. 参考文献:10.1007/s004240100633 摘要:Kudo Y, Boyd C. The physiology of immune evasion during pregnancy; the critical role of placental tryptophan metabolism and transport. Pflügers Archiv - European Journal of Physiology. 2001 Aug;442(5):639–41. doi: 10.1007/s004240100633.