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    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-2024218014-A1
    优先权日:2022-11-21
    标 题:Synthesis of a cyclic peptide
    发明人:BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL
    权利人:JANSSEN PHARMACEUTICA NV
    摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.

    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:WO-2006038872-A1
    优先权日:2004-10-08
    标 题:New process for the preparation of phosphinic acid
    发明人:IOANNIDIS PANAGIOTIS; NILSSON MATHS
    权利人:ASTRAZENECA AB; IOANNIDIS PANAGIOTIS; NILSSON MATHS
    摘要:A new process for the synthesis of a compound of formula [Chemical formula should be inserted here. Please see paper copy] wherein A represents O or N; R1 represents a C?1#191-C?6#191 alkyl; R2 and R3 each independently represents C?1#191-C?10#191 alkyl, optionally substituted or interrupted by cyclic C?3#191-C?6#191 alkyl, cyclic C?3#191-C?6#191 heteroalkyl, aryl or heteroaryl; and X is selected from F, Cl, Br, or I, by a halogenation procedure comprising the consecutive sequence of following reactions: a) dienalkylation; b) formation of a leaving group on the alcohol function; and c) halogenation, is provided by the present invention as well as the compounds obtainable by the process.

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    摘要:Antibiotics and Chemotherapy, 9(715), 1959
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