📜2-氟-4-(3-甲氧基苯基)苯胺,1-环戊烯-1,2-二羧酸酐 反应生成 维多氟拉迪莫 参考文献:Sar,Species Specificity,And Cellular Activity Of Cyclopentene Dicarboxylic Acid Amides As Dhodh Inhibitors 标题:Sar,Species Specificity,And Cellular Activity Of Cyclopentene Dicarboxylic Acid Amides As Dhodh Inhibitors 摘要:Novel Dhodh Inhibitors Were Developed Based On A Previously Described Series By Introduction Of Heteroatoms Into The Cyclopentene Ring And Hydroxyl Groups Attached To It. Also,The Hydrophobic Biphenyl Side Chain Was Replaced With Benzyloxy Phenyl Groups. Activities On Human,Rat,And Mouse Enzymes Indicate A Species Specificity Of These Inhibitors. (C) 2005 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2005.07.053
专利号:WO-2025215126-A1 优先权日:2024-04-12 标题:Synthesis of vidofludimus and its calcium salt 发明人:VITT DANIEL; IGLICAR PETRA; GEGE CHRISTIAN; Mühler Andreas; KOHLHOF HELLA; GRÖPPEL MANFRED 权利人:IMMUNIC AG 摘要:The invention relates to the process of preparation of 2-fluoro-4-(3-methoxyphenyl)aniline (3) as an intermediate. Said intermediate 2-fluoro-4-(3-methoxyphenyl)aniline (3) is obtained in a Suzuki coupling reaction from (3-methoxyphenyl)boronic acid (1) and 4-bromo-2-fluoro-aniline (2). The invention further relates to the synthesis of vidofludimus (5) from said intermediate 2-fluoro-4-(3-methoxy-phenyl)aniline (3) and from 1-cyclopentene-1,2-dicarboxylic anhydride (4). The invention further relates to the synthesis of vidofludimus calcium (6) from said vidofludimus (5) and from a calcium salt, preferably Ca(OH)2.
专利号:US-11285169-B2 优先权日:2013-03-13 标题 :Methods for modulating chemotherapeutic cytotoxicity 发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R 权利人:US HEALTH 摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.
1: D'Haens G, Stardelova KG, Sadiku E, Kizlova N, Skybalo S, Shehovtsova Y, Abramescu M, Vitt D, Kohlhof H, Muehler A. Vidofludimus Calcium in Patients with Moderate-to-Severe Ulcerative Colitis: A Randomized, Placebo-Controlled, Phase 2 Trial. Clin Transl Gastroenterol. 2025 Jan 10. doi: 10.14309/ctg.0000000000000813. Epub ahead of print. 55(1):173. doi: 10.1186/s13567-024-01447-y. Erratum for: Vet Res. 2023 Dec 20;54(1):124. doi: 10.1186/s13567-023-01251-0. 3: Gege C, Hahn F, Wangen C, Häge S, Herrmann A, Uhlig N, Eberlein V, Issmail L, Klopfleisch R, Grunwald T, Marschall M, Kohlhof H, Vitt D. Synthesis and Characterization of DHODH Inhibitors Based on the Vidofludimus Scaffold with Pronounced Anti-SARS-CoV-2 Activity. ChemMedChem. 2024 Oct 1;19(19):e202400292. doi: 10.1002/cmdc.202400292. Epub 2024 Aug 6. EMPhASIS investigators. Safety and Dose-Response of Vidofludimus Calcium in Relapsing Multiple Sclerosis: Extended Results of a Placebo-Controlled Phase 2 Trial. Neurol Neuroimmunol Neuroinflamm. 2024 May;11(3):e200208. doi: 10.1212/NXI.0000000000200208. Epub 2024 Apr 25. 5: Sriwastava S, Elkhooly M, Amatya S, Shrestha K, Kagzi Y, Bhatia D, Gupta R, Jaiswal S, Lisak RP. Recent advances in the treatment of primary and secondary progressive Multiple Sclerosis. J Neuroimmunol. 2024 May 15;390:578315. doi: 10.1016/j.jneuroim.2024.578315. Epub 2024 Feb 17. 96(1):e29372. doi: 10.1002/jmv.29372. 15(12):2416. doi: 10.3390/v15122416.
合成参考文献
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