(S)-N-((R)-1-(2-Chlorophenyl)-2-((3,3-Difluorocyclobutyl)Amino)-2-Oxoethyl)-1-(4-Cyanopyridin-2-yl)-N-(5-Fluoropyridin-3-yl)-5-Oxopyrrolidine-2-Carboxamide置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 四氢呋喃 用作溶剂,化学反应 14.0H,以52 G的收率获得艾伏尼布 参考文献: An Improved Process Of Preparation Of Ivosidenib[fr] Procédé Amélioré De Préparation D'Ivosidenib 标题: An Improved Process Of Preparation Of Ivosidenib[fr] Procédé Amélioré De Préparation D'Ivosidenib 摘要:本发明涉及一种改进的伊伏西替尼(ivosidenib)制备过程,该化合物的化学式为(i).更具体地,本发明提供了中间体的制备过程.同时提供了伊伏西替尼的非晶形态的制备过程.此外,本发明提供了手性纯度的伊伏西替尼的制备过程,该化合物的化学式为(i).
专利号:US-2023391824-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent 发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL 权利人:NARENDRAN ARUMUGAVADIVEL 摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
专利号:US-12390420-B1 优先权日:2024-10-22 标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof 发明人:EGUCHI MASAKATSU 权利人:BRYET US INC 摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
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:EP-4288444-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
专利号:CN-116986986-A 优先权日:2023-07-19 标 题 :A kind of synthesis method of 3-oxo-1-cyclobutanecarboxylic acid intermediate