CAS: 857064-38-1; (S,E)-3-(6-Bromopyridin-2-yl)-2-Cyano-N-(1-Phenylethyl)Acrylamide

上下游产品

6-bromo-2-pyridinecarbaldehyde

📜6-溴吡啶-2-甲醛,2-Cyano-N-[(1S)-1-Phenylethyl]Acetamide置于β-丙氨酸体系中,用 乙醇,水 作为反应溶剂,化学反应生成 Wp 1066;(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基乙基]-2-丙烯酰胺
参考文献:Preclinical Characterization Of Signal Transducer And Activator Of Transcription 3 Small Molecule Inhibitors For Primary And Metastatic Brain Cancer Therapy
标题:Preclinical Characterization Of Signal Transducer And Activator Of Transcription 3 Small Molecule Inhibitors For Primary And Metastatic Brain Cancer Therapy
摘要:信号转导子和转录激活子 3 (Stat3) 被认为是多种致癌途径的枢纽. Stat3 的组成型激活存在于多种癌症中,包括神经胶质瘤 (Gbm),并且与不良治疗反应相关. Stat3 的磷酸化会触发其二聚化和核运输,从而促进刺激肿瘤生长的基因转录.鉴于这一作用,Stat3 通路抑制剂是有吸引力的癌症治疗靶点.为此,我们评估了三种化合物(cpa-7 [三氯亚硝基二氨铂(iv)],Wp1066 [(S,E)-3-(6-Bromopyridin-2-yl)-2-Cyano-N培养的啮齿动物和人类神经胶质瘤细胞(包括 Gbm)中的-(1-苯乙基)丙烯酰胺,C17H14Brn3O] 和 Ml116 [4-Benzyl-1-{噻吩并[2,3-D]嘧啶-4-基}哌啶,C18H19N3S])癌症干细胞.我们的结果表明,药物治疗后可有效诱导 Gbm 细胞生长停滞,同时诱导细胞死亡.尽管这些化合物能有效抑制 Stat3 磷酸化,但它们也对活化 B 细胞的 Stat1,Stat5 和核因子 K 轻链增强子表现出不同的剂量依赖性抑制作用.这些化合物的治疗功效在外周和颅内小鼠肿瘤模型中得到了进一步评估.尽管 Cpa-7 能引起周围肿瘤(黑色素瘤和 Gbm)消退,但当肿瘤植入脑内时,其功效并不明显.我们的数据表明该化合物对中枢神经系统内肿瘤的渗透性较差. Wp1066和ml116表现出较差的体内功效.总之,Cpa-7 在外周实体癌模型中构成了强大的抗癌剂.我们的数据强烈支持进一步开发具有增加渗透性的 Cpa-7 衍生化合物,以增强其对原发性和转移性脑肿瘤的疗效.
DOI:10.1124/jpet.114.214619

专利信息

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-2024336679-A1
优先权日:2021-08-06
标题 :Methods for the treatment of cancer
发明人：LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.

专利号:CN-113166767-B
优先权日:2018-09-05
标 题 :Method for engineering synthesis of cis-regulatory DNA