944401-56-3 + 73183-34-3 = 106447-97-6 + 944401-57-4 反应条件:1.1 Reagents: Potassium Acetate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,4-Dioxane; 8 H,115 °C 标题:Identification Of Nvp-Bkm120 As A Potent,Selective,Orally Bioavailable Class I Pi3 Kinase Inhibitor For Treating Cancer 作者:Burger,Matthew T.; Pecchi,Sabina; Wagman,Allan; Ni,Zhi-Jie; Knapp,Mark; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2011 卷标:2(10) 页码:774-779
4-(Trifluoromethyl)Pyridine N-Oxide置于盐酸体系中,用 二氯甲烷 用作溶剂,化学反应生成2-氨基-4-三氟甲基吡啶 参考文献:Substituted 2-Aminopyridines As Inhibitors Of Nitric Oxide Synthases 标题:Substituted 2-Aminopyridines As Inhibitors Of Nitric Oxide Synthases 摘要:A Series Of Substituted 2-Aminopyridines Was Prepared And Evaluated As Inhibitors Of Human Nitric Oxide Synthases (Nos). 4,6-Disubstitution Enhanced Both Potency And Specificity For The Inducible Nos With The Most Potent Compound Having An Ic50 Of 28 Nm. (C) 2000 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0960-894X(00)00389-9
专利信息
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-9815842-B2 优先权日:2014-05-28 标题 :Pyrazolo pyrimidine derivatives and their use as MALT1 inhibitors 发明人:SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS 权利人:SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS; NOVARTIS AG 摘要:The present invention describes new pyrazolo-pyrimidine derivatives which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
专利号:CN-115385852-A 优先权日:2022-09-05 标题:Efficient synthesis method of 2-amino-4-trifluoromethylpyridine
专利号:CN-117143026-A 优先权日:2023-08-31 标题:A kind of synthesis method of heteroaryl trifluoromethyl compound