专利号:EP-3686190-A1 优先权日:2013-07-11 标 题 :Synthesis of therapeutically active compounds
专利号:US-11117906-B2 优先权日:2018-12-21 标题:Methods for synthesizing zinc-lysine-chloride complex 发明人:HAO ZHIGANG; CHENG CHI-YUAN; BRINZARI TATIANA; PAN LONG; SUBRAMANYAM RAVI; EVANS LAUREN; LEITE SERGIO 权利人:COLGATE PALMOLIVE CO 摘要:Disclosed herein are improved methods for the synthesis of zinc-amino acid-halide complexes via reaction of zinc oxide and amino acid hydrochloride in a solvent comprising a polyol, as well as oral care compositions comprising said complexes made according to said method.
专利号:US-11091502-B2 优先权日:2018-12-21 标 题:Methods for synthesizing zinc-lysine-chloride complex 发明人:HAO ZHIGANG; CHENG CHI-YUAN; BRINZARI TATIANA; PAN LONG; SUBRAMANYAM RAVI 权利人:COLGATE PALMOLIVE CO 摘要:Disclosed herein are improved methods for the synthesis of zinc-amino acid-halide complexes via reaction of zinc halide and amino acid free base in a solvent comprising a polyol, as well as oral care compositions comprising said complexes made according to said method.
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:US-7427690-B2 优先权日:2004-06-05 标 题 :Multifunction “crown complexesâ€? from amino acids and peptides for skin and hair restoration 发明人:GUPTA SHYAM K 权利人:BIODERM RESEARCH 摘要:This invention relates to Schiff's bases derived from amino acids and hydroxyaryl alkyl ketones, or a plant extract containing the same, having general chemical structure in FIG. 1 for topical application. This invention also relates to certain metal complex of said Schiff's bases, which have a crown-like appearance in their three-dimensional chemical structure, as in FIG. 2 . The Schiff's bases and their metal complexes of the present invention are useful for the modulation of metal-activated enzymes and metalloenzymes, such as Phenylalanine Hydroxylase, Tyrosine Transaminase, Phenylalanine Transaminase, Tyrosinase, various MMP (Matrix metalloproteases), Superoxide dismutase, 5-Alpha Reductase, and citrate lyase. These are further suitable for multifunctional topical methods for skin whitening, skin wrinkles reduction, skin antiaging, collagen synthesis, acne control, hair loss prevention, hair graying control, and facial oil control.
1: Chen J, Yang J, Cao P. The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors. Mini Rev Med Chem. 2016;16(16):1344-1358. Review.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).