CAS: 1887014-12-1; (S)-5-((1-(6-Chloro-2-Oxo-1,2-Dihydroquinolin-3-yl)Ethyl)Amino)-1-Methyl-6-Oxo-1,6-Dihydropyridine-2-Carbonitrile

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    专利号:WO-2023144235-A1
    优先权日:2022-01-27
    标 题 :Methods for monitoring and treating warburg effect in patients with pi3k-related disorders
    发明人:CANAUD GUILLAUME; LADRAA SOPHIA
    权利人:INST NAT SANTE RECH MED; ASSIST PUBLIQUE HOPITAUX PARIS APHP; CENTRE NAT RECH SCIENT; UNIV PARIS CITE
    摘要:Using a unique tool of PROS, they demonstrate that PIK3CA mutation leads to GLUT4 membrane accumulation with a negative feedback loop on insulin secretion, a burst of liver IGFBP1 synthesis with IGF1 sequestration and low circulating levels. They further show that AKT2 drives a large part of the phenotype. In addition, they demonstrate for the first time that a single PIK3CA mutation induces metabolic reprogramming with the Warburg effect and protein and lipid synthesis—hallmarks of cancer cells—in vitro, in vivo and in patients. They finally show that alpelisib, an approved PIK3CA inhibitor in oncology, is efficient at preventing and improving PIK3CA-adipose tissue overgrowth and reversing metabolomic anomalies in both animal models and patients. Accordingly, the present invention relates to an in vitro method for monitoring the efficiency of a PI3K inhibitor treatment in a subject in need thereof comprising the step of determining the level of at least one metabolite selected in the group consisting of cis-aconitate, succinic acid, 5-methylcytosine, acetyl-carnitine, acetyl-lysine, argininosuccinate, betaine, butyric acid, carnitine, creatine, glucose, glycine, hexanoyl-carnitine, L-fucose, lactate, L-dihydroorotic acid, linolenic acid, nicotinamide N-oxide, palmitoyl-carnitine, panthotenate, pyruvate, quinolinic acid, tryptophan, urate, in a biological sample obtained from the subject.

    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.

    专利号:CN-115850240-B
    优先权日:2022-12-28
    标 题 :A kind of synthesis method of olutacinib, a drug for treating acute myeloid leukemia

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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Olutasidenib. 2023 Jan 15. 2012–. Olutasidenib. 2024 Feb 20. 83(4):341-346. doi: 10.1007/s40265-023-01844-1. 7(16):4358-4365. doi: 10.1182/bloodadvances.2023009854.
    5: de Botton S, Fenaux P, Yee K, Récher C, Wei AH, Montesinos P, Taussig DC, Pigneux A, Braun T, Curti A, Grove C, Jonas BA, Khwaja A, Legrand O, Peterlin P, Arnan M, Blum W, Cilloni D, Hiwase DK, Jurcic JG, Krauter J, Thomas X, Watts JM, Yang J, Polyanskaya O, Brevard J, Sweeney J, Barrett E, Cortes J. Olutasidenib (FT-2102) induces durable complete remissions in patients with relapsed or refractory IDH1-mutated AML. Blood Adv. 2023 Jul 11;7(13):3117-3127. doi: 10.1182/bloodadvances.2022009411.
    6: Olutasidenib. Am J Health Syst Pharm. 2023 Mar 21;80(7):398-400. doi: 10.1093/ajhp/zxad002. 75(1):46-67. doi: 10.3322/caac.21873. Epub 2024 Dec 10.

    合成参考文献


    摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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