CAS: 639089-54-6; N-(4-((4-((5-Methyl-1H-Pyrazol-3-yl)Amino)-6-(4-Methylpiperazin-1-yl)Pyrimidin-2-yl)Thio)Phenyl)Cyclopropanecarboxamide

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1-methyl-piperazine N-[4-({4-chloro-6-[(3-methyl-1H-pyrazol-5-yl)amino]pyrimidin-2-yl}sulfanyl)phenyl]cyclopropane carboxamide (N-(4-mercaptophenyl)cyclopropylcarboxamide)

📜4-氨基苯硫酚置于三乙胺,N,N-二异丙基乙胺,Sodium Iodide体系中,用 四氢呋喃,N,N-二甲基甲酰胺,乙腈 作为反应溶剂,化学反应 24.0H,反应生成 陶扎色替
参考文献:Tozasertib 类似物作为坏死性细胞死亡的抑制剂
标题:Tozasertib 类似物作为坏死性细胞死亡的抑制剂
摘要:受体相互作用蛋白激酶 1 (Ripk1) 在肿瘤坏死因子 (Tnf) 诱导的坏死性凋亡中起着至关重要的作用,这表明该途径可能是可药用的.大多数 Ripk1 抑制剂被归类为 Ii 型或 Iii 型激酶抑制剂.这为发现靶向 Ripk1 活性位点的新型抑制剂开辟了一些有趣的前景.tozasertib 是一种 I 型泛极光激酶 (Aurk) 抑制剂,被发现对 Ripk1 显示出非常高的亲和力.由于 Tozasertib 具有 I 型激酶抑制剂的典型结构元素,因此开发 Tozasertib 的结构类似物是识别新型 I 型 Ripk1 抑制剂的非常好起点.在本文中,我们确定了有趣的 Mtnf 诱导的坏死性凋亡抑制剂,对 Aurk A 和 B 没有显着影响,导致没有像 Tozasertib 那样的核异常.化合物在体内 Tnf 诱导的全身炎症反应综合征 (Sirs) 小鼠模型中,71和72的表现优于 Tozasertib.
DOI:10.1021/acs.Jmedchem.7B01449

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

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-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

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-2024400576-A1
优先权日:2021-09-03
标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof
发明人：RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM
权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV
摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.