CAS: 1380087-89-7; (S)-2-(6-(4-Chlorophenyl)-1-Methyl-4H-Benzo[c]Isoxazolo[4,5-E]Azepin-4-yl)Acetamide

📜Tert-Butyl (S)-2-(1-Methyl-6-Oxo-5,6-Dihydro-4H-Benzo[c]Isoxazolo[4,5-E]Azepin-4-yl)Acetate置于4-二甲氨基吡啶,草酰氯,氨,三氟乙酸体系中,用 四氢呋喃,二氯甲烷,氯仿,N,N-二甲基甲酰胺 用作溶剂,化学反应 27.5H,反应生成Bet溴区抑制剂(Cpi-0610)
参考文献:溴结构域和末端(bet)家族的苯并异恶唑氮平抑制剂(cpi-0610)的鉴定可作为人类临床试验的候选药物
标题:溴结构域和末端(bet)家族的苯并异恶唑氮平抑制剂(cpi-0610)的鉴定可作为人类临床试验的候选药物
摘要:近年来,抑制溴结构域和染色质接头的末端外结构域(bet)家族以及染色质上的乙酰赖氨酸残基之间的相互作用已成为一种有前景的方法,可以调节重要的疾病相关基因(包括myc)的表达,Bcl-2和nf-κb.在这里,我们描述了一种强效和选择性的苯并异氮杂恶唑烷bet溴结构域抑制剂的鉴定和表征,该抑制剂可在体内减弱bet依赖的基因表达,在mv-4-11小鼠异种移植模型中显示出抗肿瘤功效,目前正在接受血液系统恶性肿瘤的人类临床试验. (cpi-0610).
Doi:10.1021/acs.Jmedchem.5B01882

专利信息

专利号:WO-2025137396-A1
优先权日:2023-12-20
标题 :Synthesis of bromodomain inhibitors
发明人：PLAMONDON LOUIS; PATEL JATIN; WANG YI; SUN CUIXIANG
权利人:CONSTELLATION PHARMACEUTICALS INC
摘要:Provided herein are processes which are useful for the preparation of small molecule bromodomain inhibitors.

专利号:US-12103929-B2
优先权日:2018-06-25
标题:Tricyclic compounds
发明人：FANG HAIQUAN; CHEN MINGMING; YANG GUIQUN; DU YUELEI; WANG YANPING; WU TONG; LI QINGLONG; ZHANG LEI; HU SHAOJING
权利人:JACOBIO PHARMACEUTICALS CO LTD
摘要:Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

专利号:CN-118754894-A
优先权日:2024-07-26
标题 :JQ1 derivative containing o-naphthoquinone structure, synthesis method thereof and application of JQ1 derivative in preparation of anti-triple-negative breast cancer drugs

专利号:CN-118812557-A
优先权日:2024-07-26
标 题:BRD4/GPX4 double-target inhibitor, synthesis method thereof and application of inhibitor in preparation of triple-negative breast cancer therapeutic drug