专利号:US-11801232-B2 优先权日:2019-11-27 标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway 发明人:HUANG GLORIA 权利人:UNIV YALE 摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.
专利号:US-2025064840-A1 优先权日:2021-12-16 标 题 :Drug delivery systems based on endoperoxides useful in diagnosis and therapy, and methods thereof 发明人:SILVA MAGALHAES DIOGO; MOREIRA RUI; LOPES FRANCISCA; RODRIGUES CECILIA; MARQUES VANDA 权利人:FACULDADE DE FARMACIA DA UNIV DE LISBOA 摘要:The present invention relates to novel drug delivery systems based on endoperoxide moieties such as 1,2,4,5-tetraoxanes, namely compounds of formula I, appropriately modified to release active pharmaceutical ingredients (API) in the presence of higher levels of Fe (II), in a subject, whereinIron metabolism dysregulation occurs in diseases such as malaria and cancer. Therefore, the present invention also relates to biomarkers comprising said compounds of formula I.Another aspect, the present invention relates to a process of synthesis of compounds of formula I and respective intermediaries.Further, the present invention also relates to a process for labelling, detection, and identification of tumours in a tissue sample.The present invention is thus applicable to the medical and pharmacological areas, in related to particular the ones cancer detection and treatment, and malaria treatment.
专利号:US-2025162973-A1 优先权日:2022-02-22 标题:Methods of synthesis and uses of agrimol compounds 发明人:CHE CHI MING; FU ZHIWEN; LEUNG YIU CHUNG GULICE 权利人:VERSITECH LTD; LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:Synthetic agrimol B and derivatives thereof (“compoundsâ€?) that have anticancer properties are disclosed. Methods for synthesizing the compounds with an overall yield ≥7% are disclosed. Pharmaceutical formulations in forms suitable for the delivery of the compounds to a subject in need thereof are disclosed. Methods of using the compounds for treating a cancer, reducing a cancer, or treating or ameliorating one or more symptoms associated with a cancer, such as non-small-cell lung cancer, in a subject are also disclosed. The methods include (i) administering to the subject the pharmaceutical formulation containing one or more compounds, for one or more times. The compounds can selectively kill cancer cells and/or cancer stem cells over noncancerous cells by inducing mitochondria dysfunction and/or inhibiting ER to Golgi trafficking in the cancer cells and/or cancer stem cells.
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-2023160543-A1 优先权日:2022-02-22 标 题 :Methods of synthesis and uses of agrimol compounds
专利号:WO-2023160543-A9 优先权日:2022-02-22 标题 :Methods of synthesis and uses of agrimol compounds
1: Dittakavi S, Hallur G, Purra BR, Kiran V, Zakkula A, Mullangi R. Validated LC-MS/MS Method for Simultaneous Quantitation of Enasidenib and its Active Metabolite, AGI-16903 in Small Volume Mice Plasma: Application to a Pharmacokinetic Study. Drug Res (Stuttg). 2019 Oct 25. doi: 10.1055/a-1024-3623. [Epub ahead of print] Available from http://www.ncbi.nlm.nih.gov/books/NBK548492/ doi: 10.2147/CMAR.S162784. eCollection 2019. 4: Del Principe MI, Paterno G, Palmieri R, Maurillo L, Buccisano F, Venditti A. An evaluation of enasidenib for the treatment of acute myeloid leukemia. Expert Opin Pharmacother. 2019 Nov;20(16):1935-1942. doi: 10.1080/14656566.2019.1654456. Epub 2019 Aug 27. doi: 10.1002/bmc.4658. Epub 2019 Sep 2. doi: 10.2147/CE.S172912. eCollection 2019. 7: Pollyea DA, Tallman MS, de Botton S, Kantarjian HM, Collins R, Stein AS, Frattini MG, Xu Q, Tosolini A, See WL, MacBeth KJ, Agresta SV, Attar EC, DiNardo CD, Stein EM. Enasidenib, an inhibitor of mutant IDH2 proteins, induces durable remissions in older patients with newly diagnosed acute myeloid leukemia. Leukemia. 2019 Nov;33(11):2575-2584. doi: 10.1038/s41375-019-0472-2. Epub 2019 Apr 9. doi: 10.2147/CPAA.S192687. eCollection 2019.
合成参考文献
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