专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
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:WO-2025088147-A1 优先权日:2023-10-27 标题 :Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis 发明人:Schäfer Martin; BAUDER-WUEST ULRIKE; ROSCHER MAREIKE; REMDE YVONNE; BENEÅ OVà -SCHÄFER MARTINA; BARINKA CYRIL; KUTILOVà ZSÓFIA; MOTLOVà LUCIA 权利人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OEFFENTLICHEN RECHTS 摘要:The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and radiopharmaceuticals for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. Further the present invention provides synthetic procedures for the synthesis of such PSMA-targeting ligands.
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:WO-2025052429-A1 优先权日:2023-09-04 标 题 :An improved process for the preparation of tirzepatide 发明人:SIRIPRAGADA MAHENDER RAO; GANDAVADI SUNIL KUMAR; PARUMANCHALA SHAIK SHAVALI; TELAKALA HEMA SUNDARA RAO; SHAIK KALESHA 权利人:NEULAND LABORATORIES LTD 摘要:An improved process for the preparation of Tirzepatide having the chemical structural Formula I. The present invention also relates to the compounds of SEQ ID NO. 1 to 14 or a pharmaceutically acceptable salt thereof for use in the synthesis of Tirzepatide or a pharmaceutically acceptable salt thereof. The present invention further relates to the intermediate compounds of Formulae II to Formulae XVIII and its process of preparation, which are used in the preparation of Tirzepatide or a pharmaceutically acceptable salt thereof.