CAS: 728033-96-3; 3-((Quinolin-4-Ylmethyl)Amino)-N-(4-(Trifluoromethoxy)Phenyl)Thiophene-2-Carboxamide

该化合物是一个小分子,主要作为某些受体性强氧素直系细胞的选择性抑制器,特别是那些参与癌症信号路径的受体性强氧素流动体,研究其肿瘤学的潜在治疗应用,特别是针对通过这些离谱细胞显示异常信号的肿瘤;该化合物的特征是它能够干预细胞扩散和生存机制,使其成为癌症治疗的候选对象;OSI-930通常在临床环境中进行,其药用植物动力学,包括吸收,分布,代谢和排泄,对于确定其功效和安全特征至关重要;与许多调查药物一样,目前进行的研究旨在阐明其所有生物效应,最佳剂量疗法和潜在副作用;OSI-930的研制反映了癌症治疗的更广泛趋势,即以有针对性的治疗为目的,在有效防治恶性细胞的同时尽量减少对健康组织造成的伤害.

结构式图片

上下游产品

quinoline-4-carboxaldehyde 3-smino-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide Methyl 3-aminothiophene-2-carboxylate 4-(trifluoromethoxy)aniline

合成工艺路线路线简述

    📜对三氟甲氧基苯胺置于三乙基硅烷,三甲基铝,三氟乙酸体系中,用 二氯甲烷,甲苯 作为反应溶剂,化学反应 58.0H,反应生成 3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺
    参考文献:3-(Benzo[d][1,3]Dioxol-5-Ylamino)-N-(4-Fluorophenyl)Thiophene-2-Carboxamide Overcomes Cancer Chemoresistance Via Inhibition Of Angiogenesis And P-Glycoprotein Efflux Pump Activity
    标题:3-(Benzo[d][1,3]Dioxol-5-Ylamino)-N-(4-Fluorophenyl)Thiophene-2-Carboxamide Overcomes Cancer Chemoresistance Via Inhibition Of Angiogenesis And P-Glycoprotein Efflux Pump Activity
    摘要:噻吩-2-甲酰胺显示出对血管反应生成和p-Gp外流泵的双重抑制作用.
    DOI:10.1039/c5Ob00233H

    海关参考信息

    专利信息


    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    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.

    专利号:US-2025250280-A1
    优先权日:2021-09-03
    标 题 :Nitrogen-containing derivatives of narasin, synthesis and uses thereof
    发明人:RODRIGUEZ RAPHAËL; CAÑEQUE TATIANA; MÜLLER SEBASTIAN; ANTOSZCZAK MICHAL
    权利人:CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; INST CURIE
    摘要:The present invention relates to nitrogen-containing derivatives of narasin having the formula (I), as well as synthesis and uses thereof, in particular for the treatment and/or prevention of cancer. Also disclosed are medicaments including the nitrogen-containing derivatives of narasin, which include medicaments for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.

    专利号:US-12180228-B2
    优先权日:2019-06-05
    标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
    发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

    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

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    1. Dihel, Larry; Kittleson, Christine; Mulvihill, Kristen; Johnson, William W. Oxidative metabolism of the trifluoromethoxy moiety of OSI-930. Drug Metabolism and Drug Interactions (2009), 24(2-4), 95-121. CODEN: DMDIEQ ISSN:0792-5077. AN
    2010:437994 2. Gruber, Harry E.; Jolly, Douglas; Perez, Omar. Recombinant replication-competent retroviral vectors expressing therapeutic products for treatment of proliferative disorders. PCT Int. Appl. (2010), 194pp. CODEN: PIXXD2 WO 2010036986 A2 20100401 CAN
    152:423197 AN
    2010:402977 3. Patel, Jay; Korlipara, Vijaya L. Design, synthesis, and evaluation of OSI-930 analogs as dual c-Kit and KDR (VEGFR-2) tyrosine kinase inhibitors. Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), MEDI-144. CODEN: 69LVCL AN

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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