CAS: 901119-35-5; (6-((5-Fluoro-2-((3,4,5-Trimethoxyphenyl)Amino)Pyrimidin-4-yl)Amino)-2,2-Dimethyl-3-Oxo-2H-Pyrido[3,2-B][1,4]Oxazin-4(3H)-yl)Methyl Dihydrogen Phosphate

该化合物是一种口服药物,主要用于治疗某些自发性疾病,特别是慢性免疫性血清细胞障碍(ITP),它作为一种脾脏结膜结膜抑制剂,在免疫细胞的信号路径中起着关键作用.Fostamatinib通过抑制SYK,帮助调节免疫反应,减少IPT病人的切片破坏.该物质的特征是其分子配方,反映其复杂结构,通常看起来像白到白粉.Fostamatiminib以平板形式施用,在肝脏中代谢,其药性肿瘤受包括食物摄入在内的各种因素影响.常见副作用可能包括腹泻,高血压和肝酶升高,在治疗期间必须进行监测.与任何药物一样,病人在开始治疗前必须与其保健提供者讨论潜在风险和好处.

结构式图片

欧盟法规

C&L通报REACH预注册

上下游产品

ortho-methylbenzoic acid 1-amino-3-methylbenzene 4-(2,2-dimethyl-4-[(di-tert-butyl-phosphonoxy)methyl]-3-oxo-5-pyrido[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamineN4-(2,2-dimethyl-4-[(di-tert-butyl-phosphonoxy)methyl]-3-oxo-5-pyrido[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine ortho-toluoyl chloride

合成工艺路线路线简述

  • 合成目标产物 Fostamatinib 主要起始原料 Ditert-Butyl [6-[[5-Fluoro-2-(3,4,5-Trimethoxyanilino)Pyrimidin-4-Yl]Amino]-2,2-Dimethyl-3-Oxo-Pyrido[3,2-B][1,4]Oxazin-4-Yl]Methyl Phosphate
  • (文献来源)合成步骤主要原料 Ditert-Butyl [6-[[5-Fluoro-2-(3,4,5-Trimethoxyanilino)Pyrimidin-4-Yl]Amino]-2,2-Dimethyl-3-Oxo-Pyrido[3,2-B][1,4]Oxazin-4-Yl]Methyl Phosphate
6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-2H-吡啶并[3,2-B]-1,4-噁嗪-3(4H)-酮置于caesium Carbonate,溶剂黄146体系中,用 水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 33.0H,反应生成 福他替尼
参考文献:Wo2021030526A5
标题:Wo2021030526A5

海关参考信息

专利信息


专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2024360247-A1
优先权日:2021-08-10
标 题:Compositions and methods for treatment of cancer
发明人:CHATTERJEE SUBROTO
权利人:UNIV JOHNS HOPKINS
摘要:Compositions in the prevention and treatment of cancers, such as colorectal cancer or diseases associated with abnormal levels of β-1,4-galactosyltransferase-V (β-1,4-GalT-V), include at least one inhibitor of glycosphingolipid synthesis.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人:EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-2015217006-A1
优先权日:2014-02-06
标题:Al-f-18-labeled, al-f-19-labeled and ga-68-labeled gastrin-releasing peptide receptor (grpr)-antagonists for imaging of prostate cancer
发明人:MCBRIDE WILLIAM J; CHATALIC KRISTELL L S; HENDRIKS-DE JONG MARION; BOERMAN OTTO C; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F-, 19 F- or 68 Ga-labeled molecules of use in PET, SPECT and/or MRI imaging of prostate cancer. Preferably, the 18 F, 19 F or 68 Ga is attached to a chelator moiety on a prostate cancer targeting molecule, more preferably a bombesin analog, more preferably a GRPR antagonist, most preferably JMV5132 or JMV4168. The 18 F or 19 F may form a complex with a group IIIA metal to promote binding to the chelators. The labeled molecules may be used to detect, diagnose and/or image prostate cancer, including metastatic prostate cancer, in vivo.
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合成参考文献


摘要:Yazici Y, Steiger B. Kinase inhibitors for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2012;70(3):204–7.
参考文献:10.1159/000520438
摘要:Mehta AR, Kefela A, Toste C, Sweet D. Real-World Use of Fostamatinib in Patients with Immune Thrombocytopenia and Thrombotic Risk. Acta Haematol. 2022;145(2):221–8.
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