3-(N'-((2-Fluorobenzoyl)Oxy)Carbamimidoyl)Benzoic Acid 以 叔丁醇 作为反应溶剂,化学反应 24.0H,以88.4%的收率获得产物3-[5-(2-氟苯基)-1,2,4-恶二唑-3-基]苯甲酸 参考文献:Process For Preparing Ataluren And Its Intermediates 标题:Process For Preparing Ataluren And Its Intermediates 摘要:本发明提供了制备阿塔卢伦的工艺.还提供了制备阿塔卢伦的中间体.
专利号:US-8367841-B2 优先权日:2006-09-08 标 题 :Processes for the preparation of 1,2,4-oxadiazole benzoic acids 发明人:ALMSTEAD NEIL G; HWANG PETER SEONGWOO; PINES SEEMON; MOON YOUNG-CHOON; TAKASUGI JAMES J 权利人:PTC THERAPEUTICS INC; ALMSTEAD NEIL G; HWANG PETER SEONGWOO; PINES SEEMON; MOON YOUNG-CHOON; TAKASUGI JAMES J 摘要:Provided herein are processes for the preparation of compounds useful for the treatment, prevention or management of diseases associated with a nonsense mutation. More specifically, provided herein are processes for the synthesis of 1,2,4-oxadiazoles. In particular, provided herein are processes useful for the preparation of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid.
专利号:US-9470680-B2 优先权日:2011-02-28 标 题:Fluorescence-based approach to monitor release factor-catalyzed termination of protein synthesis 发明人:GONZALEZ JR RUBEN L; STERNBERG SAMUEL H; PULUKKUNAT DILEEP K 权利人:GONZALEZ JR RUBEN L; STERNBERG SAMUEL H; PULUKKUNAT DILEEP K; UNIV COLUMBIA 摘要:Provided are probes comprising a class 1 release factor conjugated to a fluorescent label and methods of making the probes. Also provided are methods for detecting conformational changes in ribosomes and associated molecules, such as class 1 release factors. In addition, methods of identifying a compound for reducing nonsense-mediated decay of mRNA and/or for inhibiting termination of protein synthesis at a premature stop codon, are described. Methods of assaying RF3 activity are also included.
专利号:WO-2024213057-A1 优先权日:2023-04-12 标题:Use of combination of lsd1 inhibitor and drug to treat cancer 发明人:LIU HONG; LI JIA; HUANG HE; WANG JIANG; ZHOU YUBO; REN XUELIAN; LI CHUNPU; KAN WEIJUAN; XU ZICHAO; HU XIAOBEI; WU HENGBO; WANG HANLIN; YE YUNFEI; QIU XIAOHUI; SU MINGBO 权利人:SHANGHAI INST MATERIA MEDICA CAS 摘要:A use of a combination of an LSD1 inhibitor and a drug to treat cancer. Specifically, provided is a composition comprising: a tranylcypromine compound and/or a derivative thereof; and a drug selected from a kinase inhibitor, an anti-cancer drug acting upon or affecting the DNA, an antiviral compound, an antihypertension compound, an antidiabetic compound, a JAK-STAT signaling pathway inhibitor, an NF-κB signaling pathway inhibitor, a protein synthesis inhibitor, a 5-hydroxytryptamine receptor agonist, a dystroglycan modulator, a GABA receptor modulator, or a combination thereof. The two active ingredients have a synergistic effect, and the synergistic treatment effect is significantly better than that of the two individually, thereby remarkably improving the cancer treatment effect.
专利号:US-8129540-B2 优先权日:2003-04-11 标题:Methods for the synthesis of 1,2,4-oxadiazole benzoic acid compounds
专利号:US-2010121070-A1 优先权日:2003-04-11 标 题 :Methods for the synthesis of 1,2,4-oxadiazole benzoic acid compounds
专利号:CN-106279057-B 优先权日:2016-08-15 标题:Synthesis of Ataluren
1: McDonald CM, Muntoni F, Penematsa V, Jiang J, Kristensen A, Bibbiani F, Goodwin E, Gordish-Dressman H, Morgenroth L, Werner C, Li J, Able R, Trifillis P, Tulinius M; Study 019 investigators. Ataluren delays loss of ambulation and respiratory decline in nonsense mutation Duchenne muscular dystrophy patients. J Comp Eff Res. 2022 Feb;11(3):139-155. doi: 10.2217/cer-2021-0196. Epub 2021 Nov 18. 2: Michorowska S. Ataluren-Promising Therapeutic Premature Termination Codon Readthrough Frontrunner. Pharmaceuticals (Basel). 2021 Aug 9;14(8):785. doi: 10.3390/ph14080785. 3: Fox H, Millington L, Mahabeer I, van Ruiten H. Duchenne muscular dystrophy. BMJ. 2020 Jan 23;368:l7012. doi: 10.1136/bmj.l7012. Clinical Evaluator Training Group; ACT DMD Study Group. Ataluren in patients with nonsense mutation Duchenne muscular dystrophy (ACT DMD): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial. Lancet. 2017 Sep 23;390(10101):1489-1498. doi: 10.1016/S0140-6736(17)31611-2. Epub 2017 Jul 17. 182(10):1262-72. doi: 10.1164/rccm.201001-0137OC. Epub 2010 Jul 9. 100(8):1223-1235. doi: 10.1007/s00109-022-02232-0. Epub 2022 Jul 20.
合成参考文献
参考文献:10.1007/s00109-011-0787-6 摘要:Rowe SM, Sloane P, Tang LP, Backer K, Mazur M, Buckley-Lanier J, Nudelman I, Belakhov V, Bebok Z, Schwiebert E, Baasov T, Bedwell DM. Suppression of CFTR premature termination codons and rescue of CFTR protein and function by the synthetic aminoglycoside NB54. Journal of Molecular Medicine. 2011 Jul 22;89(11):1149. doi: 10.1007/s00109-011-0787-6.