专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:WO-2022127920-A1 优先权日:2020-12-18 标 题:Preparation method for and intermediate of 5'-nucleoside prodrug 发明人:SHEN JINGSHAN; HU TIANWEN; XIE YUANCHAO; ZHU FUQIANG 权利人:TOPHARMAN SHANGHAI CO LTD 摘要:Provided in the present invention are a preparation method for and an intermediate of a 5'-nucleoside prodrug. Specifically, provided in the present invention is a method for preparing a compound of formula VI. The method comprises the steps of: (a) reacting a compound of formula I and a compound of formula II to obtain a compound of formula III; (b) reacting the compound of formula III and reagent M to obtain a compound of formula IV; (c) reacting the compound of formula IV in the presence of reagent N to obtain a compound of formula V; and (d) reacting the compound of formula V with reagent O to obtain a compound of formula VI. The preparation method provided by the present invention has the advantages of having low costs, high yield, good product purity and the like, and is capable of achieving the efficient synthesis of 5'-nucleoside prodrugs.
专利号:US-2025129050-A1 优先权日:2022-01-26 标 题 :Synthesis of a kif18a inhibitor 发明人:CAILLE SEBASTIEN; GREENE DANIEL GERARD; CORBETT MICHAEL THOMAS; WEI CAROLYN 权利人:AMGEN INC 摘要:The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).
专利号:WO-2023146973-A1 优先权日:2022-01-26 标题 :Synthesis of a kif18a inhibitor
专利号:EP-4469437-A1 优先权日:2022-01-26 标 题 :Synthesis of a kif18a inhibitor
专利号:CN-118922406-A 优先权日:2022-01-26 标题 :Synthesis of KIF18A inhibitors