专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:WO-2022238500-A1 优先权日:2021-05-12 标题 :Radiosynthesis of [18f] talazoparib 发明人:BOWDEN GREGORY DAVID; MAURER ANDREAS; STOTZ SOPHIE; KINZLER PAUL JOHANNES OSKAR MARIA; LAEMMERHOFER MICHAEL; ZENDER LARS; PICHLER BERND 权利人:UNIV TUEBINGEN MEDIZINISCHE FAKULTAET 摘要:The present invention relates to the synthesis of Poly (ADP ribose) polymerase (PARP) inhibitors and particularly to the radiosynthesis of PARP 1 inhibitors, more particularly to the synthesis of [18F] talazoparib.
专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
1: Moniot A, Schneider C, Chardin L, Yaniz-Galende E, Genestie C, Etiennot M, Henry A, Drelon C, Le Formal A, Langlois B, Venat L, Louvet C, Favier L, Lortholary A, Berton-Rigaud D, Dohollou N, Desauw C, Fabbro M, Malaurie E, Dubot C, Kurtz JE, Bonichon Lamichhane N, Pujade-Lauraine É, Jeanne A, Leary A, Dedieu S. The CD47/TSP-1 axis: a promising avenue for ovarian cancer treatment and biomarker research. Mol Cancer. 2024 Aug 14;23(1):166. doi: 10.1186/s12943-024-02073-0. 14:1414112. doi: 10.3389/fonc.2024.1414112. 3: Liu Y, Zhu J, Zhou S, Hou Y, Yan Z, Ao X, Wang P, Zhou L, Chen H, Liang X, Guan H, Gao S, Xie D, Gu Y, Zhou PK. Low-dose ionizing radiation-induced RET/PTC1 rearrangement via the non-homologous end joining pathway to drive thyroid cancer. MedComm (2020). 2024 Aug 12;5(8):e690. doi: 10.1002/mco2.690.
合成参考文献
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