专利号:WO-2023039068-A1 优先权日:2021-09-08 标题:Compositions and methods for synthesis of peptide nucleic acid intermediates 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:NEUBASE THERAPEUTICS INC 摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
专利号:US-12122759-B2 优先权日:2017-11-07 标 题:Method for the synthesis of cyclic depsipeptides 发明人:HEIMBACH DIRK; OMURA SATOSHI; SUNAZUKA TOSHIAKI; HIROSE TOMOYASU; NOGUCHI YOSHIHIKO; Köbberling Johannes; WU ZHIJIE; FU SHUIBIAO; WU WEI; QIU JINFENG; HE LIU; WEI XUDONG 权利人:ELANCO ANIMAL HEALTH GMBH; THE KITASATO INST 摘要:The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
专利号:WO-2024261319-A1 优先权日:2023-06-23 标题 :Methods of chemical synthesis of peptides 发明人:AL MUSAIMI OTHMAN; WILLIAMS DARYL ROBERT 权利人:IMPERIAL COLLEGE INNOVATIONS LTD 摘要:The present invention relates to methods for the synthesis of peptides and related compounds supported on a solid polymeric resin. The inventive method provides synthetic schemes that permit the coupling of two or more peptide fragments attached to the same polymeric support, in a fashion that allows access to previously unobtainable structures, and provides a more convenient and higher-yielding approach to known peptides, including those of commercial significance.
专利号:US-12435086-B2 优先权日:2020-04-29 标题:Synthesis of heterocyclic compounds 发明人:LIN JACK; WALTERS JASON 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of Formula 2:wherein R1 is C(O)R2; R2 is alkyl optionally substituted with 1-5 halogens; G is phenyl or a 5-6 membered heteroaryl optionally substituted with 1-2 R3; and each R3 is independently C1-C6 alkyl, CN, C1-C6 alkyl-CN, 3-6 membered cycloalkyl, or 4-6 membered heterocycloalkyl.
专利号:US-11325888-B2 优先权日:2017-08-11 标 题:Method for the synthesis of monoprotected bifunctional prodrugs and antibody drug conjugates based thereon as well as a method for preparing antibody drug conjugates 发明人:TIETZE LUTZ F 权利人:GEORG AUGUST UNIV GOETTINGEN STIFTUNG OEFFENTLICHEN RECHTS 摘要:The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.
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.
参考标题: Process For Preparation Of Lanreotide Acetate Procédé De Préparation D'Acétate De Lanréotide 摘要:The Invention Relates To An Improved Method For The Solution Phase Synthesis Of Lanreotide Acetate (1) Comprising Coupling Of Two Suitably Protected Tetrapeptide Fragments Wherein The Threonine Hydroxyl Is Protected, To Give An Octapeptide, Which On Deprotection, Oxidation, Followed By Treatment With Acetic Acid Provides Lanreotide Acetate (1) Having Desired Purity.
合成参考文献
摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 249. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 296. 摘要:Sato, N., Science of Synthesis Knowledge Updates, (2011) 4, 323. 摘要:Tymoshenko, D. O., Science of Synthesis Knowledge Updates, (2012) 3, 411. 摘要:Ramesh, S.; Cherkupally, P.; Govender, T.; Kruger, H. G.; de la Torre, B. G.; Albericio, F., Science of Synthesis Knowledge Updates, (2017) 1, 362.