CAS: 937263-43-9; N4-(4-([1,2,4]Triazolo[1,5-A]Pyridin-7-Yloxy)-3-Methylphenyl)-N6-(4,4-Dimethyl-4,5-Dihydrooxazol-2-yl)Quinazoline-4,6-Diamine

上下游产品

N4-(4-([1,2,4]Triazolo[1,5-A]Pyridin-7-Yloxy)-3-Methylphenyl)Quinazoline-4,6-Diamine
图卡替尼n-1 1-(4-((4-([1,2,4]Triazolo[1,5-A]Pyridin-7-Yloxy)-3-Methylphenyl)Amino)Quinazolin-6-yl)-3-(1-Hydroxy-2-Methylpropan-2-yl)Thiourea 1429755-58-7
N-(4-([1,2,4]Triazolo[1,5-A]Pyridin-7-Yloxy)-3-Methylphenyl)-6-Nitroquinazolin-4-Amine

2-氰基-4-硝基苯胺置于palladium 10% On Activated Carbon,氢气,溶剂黄146,对甲苯磺酰氯,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,甲基叔丁基醚,醋酸异丙酯 作为反应溶剂,化学反应生成 妥卡替尼
参考文献:Preclinical Activity Of Her2-Selective Tyrosine Kinase Inhibitor Tucatinib As A Single Agent Or In Combination With Trastuzumab Or Docetaxel In Solid Tumor Models
标题:Preclinical Activity Of Her2-Selective Tyrosine Kinase Inhibitor Tucatinib As A Single Agent Or In Combination With Trastuzumab Or Docetaxel In Solid Tumor Models
摘要:摘要 Her2 是一种跨膜酪氨酸激酶受体,可介导细胞生长,分化和存活.大约 20% 的乳腺癌以及胃癌,结肠直肠癌和食管癌亚群中 Her2 过表达.靶向 Her2 并阻断其酪氨酸激酶活性的抗体药物和小分子药物都能有效治疗 Her2 驱动的癌症.在这篇文章中,我们描述了一种口服,可逆的 Her2 靶向小分子酪氨酸激酶抑制剂--图卡替尼的临床前特性.在生化和细胞信号实验中,图卡替尼以个位数纳摩尔的效力抑制her2激酶的活性,与相关受体酪氨酸激酶表皮生长因子受体相比,图卡替尼对her2具有优异的选择性,在细胞信号实验中对her2的效力提高了1000倍.图卡替尼通过 Mapk 和 Pi3K/akt 通路有效抑制 Her2 和 Her3 下游的信号转导,在体外对 Her2 扩增的乳腺癌细胞株具有选择性细胞毒性.在体内,作为单药,图卡替尼在多种 Her2+ 肿瘤模型中均有活性,与曲妥珠单抗或多西他赛联合用药可增强抗肿瘤活性,提高肿瘤部分和完全消退率.这些临床前数据与显示初步安全性和活性的图卡替尼一期临床试验结果相结合,确立了图卡替尼的独特药理特性,并强调了研究其在 Her2+ 癌症中应用的合理性.
DOI:10.1158/1535-7163.Mct-19-0873

专利信息

专利号:US-2023391824-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
发明人：JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
权利人:NARENDRAN ARUMUGAVADIVEL
摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.

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-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:US-2022396794-A1
优先权日:2019-06-04
标题:APTAMERS AGAINST TRANSFERRIN RECEPTOR (TfR)
发明人：HABIB NAGY; ROSSI JOHN; YOON SORAH; SWIDERSK PIOTR MAREK
权利人:APTERNA LTD; HOPE CITY
摘要:Methods of treating or preventing a disease or disorder are disclosed comprising administering to a subject in need thereof an effective amount of a nucleic acid compound comprising, or consisting of, a nucleic acid sequence capable of binding to a transferrin receptor (TfR) and an effective amount of an inhibitor of DNA synthesis. Also disclosed is a nucleic acid compound comprising, or consisting of, a nucleic acid sequence having at least 85% sequence identity to SEQ ID NO: 1, wherein said nucleic acid sequence is at least 30 nucleotides in length and at most 50 nucleotides in length, and wherein the nucleic acid sequence is capable of binding to a transferrin receptor (TfR).

专利号:US-11968895-B2
优先权日:2015-03-31
标 题 :N and P active materials for organic photoelectric conversion layers in organic photodiodes
发明人：ROSSELLI SILVIA; DANNER DAVID; MITEVA TZENKA; NELLES GABRIELE; DEICHMANN VITOR; FORD WILLIAM E; CHERCKA DENNIS; YAKUTKIN VLADIMIR; SCHELLER LARS PETER; KNORR NIKOLAUS
权利人:SONY CORP
摘要:The field of the DISCLOSURE lies in active materials for organic image sensors. The present disclosure relates to transparent N materials and/or to transparent P materials and their use in absorption layer(s), photoelectric conversion layer(s) and/or an organic image sensor and methods for their synthesis. The present disclosure also relates to photoelectric conversion layer(s) including an active material according to the present disclosure, to a device, including active material(s) according to the present disclosure or photoelectric conversion layer(s) according to the present disclosure. Moreover, the present disclosure relates to an organic image sensor including photoelectric conversion layer(s) according to the present disclosure.

专利号:WO-2025137620-A1
优先权日:2023-12-21
标题:Methods for high quality and high accuracy methylation sequencing
发明人：KENNEDY ANDREW
权利人:GUARDANT HEALTH INC
摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.