CAS: 1787294-07-8; N-(3-(6-Amino-5-(2-(N-Methylacrylamido)Ethoxy)Pyrimidin-4-yl)-5-Fluoro-2-Methylphenyl)-4-Cyclopropyl-2-Fluorobenzamide
该化合物是用于治疗自动免疫和炎症的高度选择性的,小分子Bruton(BTK)刺激剂,其共价约束机制确保长期目标接触,为B细胞信号路径提供强大和持续的抑制. 复合物展示出极好的生物利用率和药用动力特性,能够优化剂量疗程. 临床和临床研究凸显出其有利的安全性能,比以前的BTK抑制剂减少非目标效果. Remibrutynib的特性和功效使它成为慢性自发尿和多发性硬化症等条件的有希望的治疗对象,在这些条件下,受病理调节的B细胞活动发挥着关键病理作用.
- 英文名称N-(3-(6-Amino-5-(2-(N-Methylacrylamido)Ethoxy)Pyrimidin-4-yl)-5-Fluoro-2-Methylphenyl)-4-Cyclopropyl-2-Fluorobenzamide
- 中文名称瑞布替尼
- IUPAC名称N-(3-(6-amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide
- 其它别名N-(3-(6-Amino-5-(2-(N-Methylacrylamido)Ethoxy)Pyrimidin-4-yl)-5-Fluoro-2-Methylphenyl)-4-Cyclopropyl-2-Fluorobenzamide; N-[3-[6-Amino-5-[2-[methyl(1-Oxo-2-Propen-1-yl)Amino]Ethoxy]-4-Pyrimidinyl]-5-Fluoro-2-Methylpheny
- CAS编号1787294-07-8
- MFCD编号:MFCD32215329
- EINECS号:188-778-9
- FDA UNII编号:I7MVZ8HDNU
- 分子式:C27H27F2N5O3分子量:507.54
- 产品CID: 919052
- 产品分类Chemistry → Heterocyclic Building Blocks → Aromatic Heterocycles | Pyrimidines | Protein Tyrosine Kinase/RTK → BTK
物理性质
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专利信息
专利号:EP-4594306-A1
优先权日:2022-09-30
标 题 :Synthesis methods and intermediates for the production of remibrutinib
专利号:WO-2024069507-A1
优先权日:2022-09-30
标题 :Synthesis methods and intermediates for the production of remibrutinib
发明人：FIGUCCIA AUDE; Lovelle Lucie; PARMENTIER MICHAEL
权利人:NOVARTIS AG
摘要:This invention relates to novel processes for synthesizing N-(3-(6-Amino-5-(2-(N- methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide and to intermediates which are used in such processes.
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主要参考文献
1: Maurer M, Berger W, Giménez-Arnau A, Hayama K, Jain V, Reich A, Haemmerle S, Lheritier K, Walsh P, Xia S, Storim J. Remibrutinib, a novel BTK inhibitor, demonstrates promising efficacy and safety in chronic spontaneous urticaria. J Allergy Clin Immunol. 2022 Dec;150(6):1498-1506.e2. doi: 10.1016/j.jaci.2022.08.027. Epub 2022 Sep 9. Erratum in: J Allergy Clin Immunol. 2023 Feb;151(2):579. doi: 10.1016/j.jaci.2022.12.001. 153(2):479-486.e4. doi: 10.1016/j.jaci.2023.10.007. Epub 2023 Oct 20. 14(5):1756-1768. doi: 10.1111/cts.13005. Epub 2021 Apr 9.
4: Nuesslein-Hildesheim B, Ferrero E, Schmid C, Huck C, Smith P, Tisserand S, Rubert J, Bornancin F, Eichlisberger D, Cenni B. Remibrutinib (LOU064) inhibits neuroinflammation driven by B cells and myeloid cells in preclinical models of multiple sclerosis. J Neuroinflammation. 2023 Aug 26;20(1):194. doi: 10.1186/s12974-023-02877-9.
5: Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood- Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B. Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. J Med Chem. 2020 May 28;63(10):5102-5118. doi: 10.1021/acs.jmedchem.9b01916. Epub 2020 Mar 4. 83(3):360-371. doi: 10.1136/ard-2023-224691.
合成参考文献
参考文献:10.1055/s-0040-1707094
摘要:Synthesis of Remibrutinib. Synfacts. 2020 Jul 21;16(08):0888. doi: 10.1055/s-0040-1707094.
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