📜烟酰氯置于溴体系中,化学反应 1.0H,反应生成 5-溴吡啶-3-羰酰氯 参考文献:A General Synthesis Of 5-Arylnicotinates 标题:A General Synthesis Of 5-Arylnicotinates 摘要: DOI:10.1021/jo00200A045
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-2021134398-A1 优先权日:2019-11-06 标题:Combinatorial Chemistry Computational System and Enhanced Selection Method 发明人:WISE JOHN G; VOGEL PIA D 权利人:UNIV SOUTHERN METHODIST 摘要:A method for identifying a potentially useful molecular combination includes applying a selection procedure to a compound to identify a first set of candidate molecules, the procedure including providing a chemical synthesis scheme, a virtual scaffold molecule of the compound, and a virtual reactant fragment to react with the scaffold molecule according to the scheme; preparing the reactant fragment and the scaffold molecule for analyzing combinations of them; designating a remaining scaffold subset and a remaining fragment subset if a product molecule can be formed from them; rotating the fragment subset about an axis connecting the scaffold subset and the fragment subset incrementally through 360 degrees; and identifying potentially useful combinations of the reactant fragment and the scaffold molecule; identifying a set of combinatorial fragments from the first set of candidates; and applying the selection procedure to the set of combinatorial fragments to identify a second set of candidate molecules.
专利号:CN-114716434-A 优先权日:2022-05-13 标题:A kind of nicergoline crude drug and its synthesis process