CAS: 1817626-54-2; 1-(((2S,3S,4S)-3-Ethyl-4-Fluoro-5-Oxopyrrolidin-2-yl)Methoxy)-7-Methoxyisoquinoline-6-Carboxamide
该化合物是一种针对细胞扩散和生存的关键信号路径的选择性和强大的小型分子抑制剂,其分子目标具有高度特殊性,最大限度地减少非目标效应并增强治疗潜力;临床研究显示其有利的药用植物基因特征,包括良好的口服生物利用率和持续的目标接触;Zimlovisertib在抗性或耐性癌症模型中表现出有希望的活动,表明其在克服治疗抗药性方面的潜在效用;其精细化的行动机制和可管理的安全特征支持进一步临床调查;该化合物目前正在早期试验中评估其功效和耐性肿瘤迹象.
- 英文名称1-(((2S,3S,4S)-3-Ethyl-4-Fluoro-5-Oxopyrrolidin-2-yl)Methoxy)-7-Methoxyisoquinoline-6-Carboxamide
- 中文名称1-[[(2S,3S,4S)-3-乙基-4-氟-5-氧代-2-吡咯烷基]甲氧基]-7-甲氧基-6-异喹啉羧酰胺
- IUPAC名称1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide
- CAS编号1817626-54-2
- MFCD编号:MFCD30343869
- EINECS号:815-268-1
- FDA UNII编号:S3F315JJXI
- 分子式:C18H20FN3O4分子量:361.37
- 产品CID: 935588
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
MSDS等安全信息
欧盟法规
C&L通报合成工艺路线路线简述
📜3-羟基-4-碘苯甲酸置于甲醇,过氧乙酸,Manganese(Iv) Oxide,Sodium Tetrahydroborate,甲烷磺酸,三氟化硼乙醚,双(三甲基硅烷基)氨基钾,Potassium Carbonate,三氟乙酸酐,三氯氧磷体系中,用 四氢呋喃,二氯甲烷,氯仿,二甲基亚砜,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 99.25H,反应生成1-[[(2S,3S,4S)-3-乙基-4-氟-5-氧代-2-吡咯烷基]甲氧基]-7-甲氧基-6-异喹啉羧酰胺
参考文献:Bicyclic-Fused Heteroaryl Or Aryl Compounds
标题:Bicyclic-Fused Heteroaryl Or Aryl Compounds
摘要:所述化合物的异构体和药学上可接受的盐已被披露,其中所述化合物具有如规范中定义的ia式结构.相应的药物组合物,治疗方法,合成方法和中间体也已被披露.
海关参考信息
- 2905121000-正丙醇
2905130000-正丁醇
2912110000-甲醛
2912120000-乙醛 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-9879022-B2
优先权日:2014-04-04
标题:Bicyclic-fused heteroaryl or aryl compounds
发明人：TRZUPEK JOHN DAVID; LEE KATHERINE LIN; BUNNAGE MARK EDWARD; HAN SEUNGIL; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; PAPAIOANNOU NIKOLAOS; PIERCE BETSY SUSAN; STROHBACH JOSEPH WALTER; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG; GAVRIN LORI KRIM; LEE ARTHUR; ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; DEHNHARDT CHRISTOPH MARTIN; SAIAH EDDINE; GOLDBERG JOEL ADAM; WANG XIAOLUN; HUANG HORNG-CHIH; VARGAS RICHARD; LOWE MICHAEL DENNIS; PATNY AKSHAY
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Wright SW, Farley KA, Han S, Knafels JD, Lee KL. In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833). ACS Med Chem Lett. 2024 Mar 21;15(4):540-545. doi: 10.1021/acsmedchemlett.4c00036.
2: Kimball AB, Peeva E, Forman S, Moiin A, Khattri S, Porter ML, Mangold AR, Ghosh P, Banfield C, Oemar B. Brepocitinib, Zimlovisertib, and Ropsacitinib in Hidradenitis Suppurativa. NEJM Evid. 2024 Mar;3(3):EVIDoa2300155. doi: 10.1056/EVIDoa2300155. Epub 2024 Feb 9. 23(24):e202200455. doi: 10.1002/cphc.202200455. Epub 2022 Oct 18.
4: Singh RSP, Dowty ME, Salganik M, Brodfuehrer JI, Walker GS, Sharma R, Beebe JS, Danto SI. A Phase 1 Study to Assess Mass Balance and Absolute Bioavailability of Zimlovisertib in Healthy Male Participants Using a 14 C-Microtracer Approach. Clin Pharmacol Drug Dev. 2022 Jul;11(7):815-825. doi: 10.1002/cpdd.1109. Epub 2022 May 4.
合成参考文献
参考文献:10.1055/s-0039-1690089
摘要:Moloney MG, Khan MK, Wang D. Functionalised Nitrogen Heterocycles and the Search for New Antibacterials and Bioactives. Synthesis. 2020 Mar 30;52(11):1602–16. doi: 10.1055/s-0039-1690089.
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尽可能描述清楚需求与问题信息
