CAS: 1245537-68-1; 8-(6-Methoxypyridin-3-yl)-3-Methyl-1-(4-(Piperazin-1-yl)-3-(Trifluoromethyl)Phenyl)-1,3-Dihydro-2H-Imidazo[4,5-C]Quinolin-2-One Maleate

该化合物是化学医学领域引起注意的一种化学化合物,特别是其潜在的治疗用途,被归类为小分子抑制剂,具体针对细胞信号和扩散的某些途径.BGT226已知抑制了磷酸锡基三K(PI3K)和哺乳动物3K(mtor)的拉帕米辛(mtor)活动,这对控制细胞生长,存活和代谢至关重要.这种抑制可导致肿瘤生长的抑制,使其成为癌症治疗的候选.该化合物的典型特征是其特定的分子结构,其中包括有助于其生物活动的各种功能群体.此外,BGT226还对其药用皮肤特性进行了研究,包括吸收,分布,新陈代谢和排泄(ADME),这对于了解其在临床环境中的功效和安全状况至关重要.随着研究的继续,正在进一步探讨其行动机制及其潜在影响.

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    海关参考信息

    专利信息


    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-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-12187735-B2
    优先权日:2018-09-17
    标 题:Matter of composition, synthesis, formulation and application of FL118 platform positions 7 and 9-derived analogues for treatment of human disease
    发明人:LING XIANG; LI QINGYONG; LI FENGZHI
    权利人:CANGET BIOTEKPHARMA LLC
    摘要:Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.

    专利号:US-2025092058-A1
    优先权日:2018-09-17
    标 题 :Matter of composition, synthesis, formulation and application of fl 118 platform positions 7 and 9-derived analogues for treatment of human disease
    发明人:LING XIANG; LI QINGYONG; LI FENGZHI
    权利人:CANGET BIOTEKPHARMA LLC
    摘要:Described herein, are the chemical synthesis, compounds, methods and uses of the fluoroaryl-substituted derivatives at the FL118 position 7, which target multiple cellular human disease-relevant proteins and their signaling pathways.

    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.

    专利号:US-2022047711-A1
    优先权日:2018-12-10
    标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
    发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA
    权利人:GENENTECH INC
    摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.
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    主要参考文献


    1: Hassett MR, Sternberg AR, Roepe PD. Inhibition of Human Class I vs Class III Phosphatidylinositol 3'-Kinases. Biochemistry. 2017 Aug 22;56(33):4326-4334. doi: 10.1021/acs.biochem.7b00413. Epub 2017 Aug 8. doi: 10.18632/oncotarget.13035.
    3: Alameen AA, Simioni C, Martelli AM, Zauli G, Ultimo S, McCubrey JA, Gonelli A, Marisi G, Ulivi P, Capitani S, Neri LM. Healthy CD4+ T lymphocytes are not affected by targeted therapies against the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia. Oncotarget. 2016 Aug 23;7(34):55690-55703. doi: 10.18632/oncotarget.10984.
    4: Simioni C, Cani A, Martelli AM, Zauli G, Alameen AA, Ultimo S, Tabellini G, McCubrey JA, Capitani S, Neri LM. The novel dual PI3K/mTOR inhibitor NVP-BGT226 displays cytotoxic activity in both normoxic and hypoxic hepatocarcinoma cells. Oncotarget. 2015 Jul 10;6(19):17147-60.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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