专利号:US-2025011272-A1 优先权日:2021-09-23 标 题:Long-chain compound that acts on acly, preparation method therefor and use thereof 发明人:NAN FAJUN; LI JINGYA; CHEN YI; Song Gaolei; XIE ZHIFU; FANG YANFEN; ZHANG MEI; SUN XINYU; CAO LEI; MA HUI; YANG YUROU 权利人:SHANGHAIINSTITUTE OF MATERIA MEDICA CHINESE ACAD OF SCIENCES 摘要:A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia.
专利号:WO-2025092475-A1 优先权日:2023-11-02 标题 :Synthesis method for bempedoic acid and bempedoic acid intermediate, and bempedoic acid intermediate 发明人:ZHAI NING; WANG GUOPING; ZHAO MIN; YU ZHENPENG; WANG SHIKANG 权利人:YANGZHOU AURISCO PHARMACEUTICAL CO LTD 摘要:The present invention provides a preparation method for bempedoic acid and a bempedoic acid intermediate, and a bempedoic acid intermediate. The preparation method comprises: taking a novel intermediate compound 6 as a raw material, and carrying out hydrolysis, removal of protecting groups on hydroxyl groups, and reduction to obtain bempedoic acid; and taking caprolactone as a starting material, carrying out self-condensation of caprolactone, and then carrying out ring opening, bromination, carbonyl protection, and α-alkylation to obtain the intermediate compound 6. The preparation method for bempedoic acid in the present invention is simple, convenient and safe to operate, high in yield, low in production cost, and easy for industrial production.
专利号:WO-2022058896-A1 优先权日:2020-09-15 标 题 :Inhibitors of low molecular weight protein tyrosine phosphatase for management of metabolic disorder 发明人:SHARMA RAJIV; KUMAR SANJAY; SRIVASTAVA BRIJESH KUMAR; GITE SANJAY; SHEDAGE SANDEEP; KADAM PRAVIN; DHOLAKIA PARIND 权利人:CADILA HEALTHCARE LTD 摘要:The present invention relates to novel modulators of low molecular weight protein tyrosine phosphatases and their use for the treatment of diseases or conditions mediated by LMPTP. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, their safe pre-mixtures with polymers such as HPMC, HPMC-AS, Copovidone and methods for using such compounds, and pharmaceutical compositions containing them.
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:CN-117551009-A 优先权日:2022-08-05 标题 :A kind of synthesis method of bepedic acid intermediate
专利号:CN-111285760-B 优先权日:2020-05-12 标 题:Synthesis method and intermediate of pipadiric acid