专利号:US-12435042-B2 优先权日:2019-07-04 标题:Process for the preparation of key intermediates for the synthesis of Eltrombopag or salt thereof 发明人:STABILE PAOLO; SEMERARO FLORIANA 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.
专利号:WO-2013049605-A1 优先权日:2011-09-28 标题 :Processes for the preparation of an intermediate in the synthesis of eltrombopag 发明人:AVDAGIC AMIR; BARAN PHIL S 权利人:ASSIA CHEM IND LTD; TEVA PHARMACEUTICAL USA INC 摘要:3'-Amino-2'-hydroxybiphenyl-3-carboxylic acid (BPCA) and related compounds have been prepared using compounds such as: wherein R 1 is -H, -Cl or -F; R 2 is -Br or -I; and R 3 is -H or -N0 2 . BPCA is useful, for example, in the preparation of Eltrombopag.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
专利号:US-2022298116-A1 优先权日:2019-07-04 标题:Process for the preparation of key intermediates for the synthesis of eltrombopag or salt thereof
专利号:WO-2021001044-A1 优先权日:2019-07-04 标题 :Process for the preparation of key intermediates for the synthesis of eltrombopag or salt thereof
专利号:CN-114072386-A 优先权日:2019-07-04 标题 :Improved process for the preparation of key intermediates for the synthesis of eltrombopag or salts thereof
1: Iriondo J, Zubicaray J, Río P, Català A, Solsona M, Sanz A, Gómez A, Sebastián E, de la Cruz A, Galán A, Navarro S, Larcher L, de Andoin NG, Uriz JJ, Vagace JM, Gonzalez de Pablo J, Pujol MR, Nicoletti E, Surrallés J, Martín-Prado S, Schwartz JD, Soulier J, Bueren JA, Sevilla J. Eltrombopag for Bone Marrow Failure in Fanconi Anemia: Results From the Phase II Clinical Trial FANCREV. Eur J Haematol. 2025 Jul 16. doi: 10.1111/ejh.70007. Epub ahead of print. 57(3):193-195. doi: 10.4103/ijp.ijp_777_22. Epub 2025 Jul 9. 16:1595774. doi: 10.3389/fimmu.2025.1595774. 4: Wang S, Ju M, Kong F, Jiang Y, Tu Y, Zou J, Zou Z, Tan G, Li F. CDKN1A as a potential target for Eltrombopag treatment in ITP and its regulation of the communication between macrophages and transitional B cells in ITP. Ann Hematol. 2025 Jun 14. doi: 10.1007/s00277-025-06436-5. Epub ahead of print.
合成参考文献
参考文献:10.2165/11207390-000000000-00000 摘要:Garnock-Jones KP. Eltrombopag: a review of its use in treatment-refractory chronic primary immune thrombocytopenia. Drugs. 2011 Jul 09;71(10):1333–53. doi: 10.2165/11207390-000000000-00000.