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-2017107577-A1 优先权日:2014-03-11 标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment 发明人:AL-EJEH FARES 权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES 摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.
专利号:US-2022143183-A1 优先权日:2019-02-23 标题:Photoswitchable protacs and synthesis and uses thereof 发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE 权利人:UNIV NEW YORK 摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.
专利号:US-11299491-B2 优先权日:2018-11-16 标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound
1: Yamamoto TM, Iwanaga R, Woodruff ER, Elder AM, Petkov A, Nurmemmedov E, Eisenmesser E, Reigan P, Bitler BG, Brubaker LW. Chromobox2 inhibition: a novel activity of alisertib, an aurora A kinase inhibitor. Mol Cancer Ther. 2026 Jan 24:10.1158/1535-7163.MCT-25-0279. doi: 10.1158/1535-7163.MCT-25-0279. Epub ahead of print. 2: Thakur D, Sengupta D, Kar S, Chakrabarti J, Sen S, Hajra S, Laha A, Mahapatra E, Das S, Karmakar P, Mukherjee S. Aurora Kinase A inhibitor alisertib failed to exert its efficacy on TNBC cells due to consequential enrichment of polyploid giant cancer cells (PGCCs). Discov Oncol. 2025 Nov 5;16(1):2043. doi: 10.1007/s12672-025-03825-0.
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