CAS: 364757-36-8; 4-Chloro-2-Hydrazinylpyridine

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4-chloro-2-fluoro-pyridine

📜2-氟-4-氯吡啶置于hydrazine Hydrate体系中,用 乙醇 作为反应溶剂,化学反应生成 4-氯-肼酮(9CI)-2(1H)-吡啶酮
参考文献:用于治疗脓毒性急性肾损伤的新型 P2X7 受体拮抗剂的设计,合成和生物学评价
标题:用于治疗脓毒性急性肾损伤的新型 P2X7 受体拮抗剂的设计,合成和生物学评价
摘要:脓毒症相关的急性肾损伤(aki)是一个严重的临床问题,目前尚无有效的药物.脓毒症肾脏中嘌呤能 P2X7 受体 (P2X7R) 的异常激活使其拮抗剂成为一种有前途的治疗方法.在此,设计,合成了一系列新型p2X7R拮抗剂,并进行了结构优化.基于使用 Hek293 细胞在人/小鼠 P2X7R 中的体外效力,肝微粒体稳定性以及药代动力学和初步体内评估,化合物14A通过分别为 64.7 和 10.1 Nm 的人和小鼠 P2X7R Ic 50值以及非常好的药代动力学特性进行鉴定.重要的是,14A剂量依赖性地减轻了脂多糖 (Lps) 和盲肠结扎/穿孔 (Clp) 诱导的脓毒症 Aki 小鼠的肾功能障碍和病理损伤,且具有非常好的安全性.从机制上讲,14A可以抑制 Nlrp3 炎症小体的激活,从而抑制脓毒症小鼠受损肾脏中 Cleaved Caspase-1,Gasdermin D,Il-1β 和 Il-18 的表达.总的来说,这些结果强调了
DOI:10.1021/acs.Jmedchem.3C00837

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:CN-114540846-B
优先权日:2022-02-10
标题:Synthesis method of 1,2, 4-triazolo six-membered nitrogen heterocycle-3-amine