CAS: 202592-23-2; (S)-2-(4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-Thieno[3,2-F][1,2,4]Triazolo[4,3-A][1,4]Diazepin-6-yl)Acetic Acid

上下游产品

2-(4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-Thieno[3,2-F][1 ,2,4]Triazolo[4,3-A][1,4]Diazepin-6-yl)Acetic Acid 202592-28-7
Methyl 2-((6S,Z)-4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-Thieno[3,2-F][1,2,4]Triazolo[4,3-A][1,4]Diazepin-6-yl)Acetate 916489-36-6
(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)乙酸叔丁酯 (S)-Tert-Butyl 2-(4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-Thieno[3,2-F][1,2,4]Triazolo[4,3-A][1,4]Diazepin-6-yl)Acetate 1268524-70-4
[(R,S)-4-（4-氯苯基）-2,3,9-三甲基-6H-1-硫杂-5,7,8,9A-四氮杂-环戊环[e]氮杂-6-基]-乙酸叔丁酯 Jq1 1268524-69-1
4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-1-Thia-5,7,8,9A-Tetraazacyclopenta[e]Azulene 166880-01-9
(S)-3-([[(9H-芴-9-基)甲氧基]羰基]氨基)-4-[[3-(4-氯苯甲酰基)-4,5-二甲基噻吩-2-基]叔丁基酯氨基]-4-氧代丁酸甲酯 (S)-Tert-Butyl 3-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-4-((3-(4-Chlorobenzoyl)-4,5-Dimethylthiophen-2-yl)Amino)-4-Oxobutanoate 1268524-65-7

(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)乙酸叔丁酯置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 1.0H,以97%的收率获得(+)-Jq1羧酸
参考文献:抗体介导的嵌合brd4降解物的递送.第1部分:抗体接头,有效负载负载和有效负载分子特性的探索
标题:抗体介导的嵌合brd4降解物的递送.第1部分:抗体接头,有效负载负载和有效负载分子特性的探索
摘要:靶向蛋白水解的嵌合体(protac)和相关的嵌合分子通过泛素连接酶介导的泛素化影响靶蛋白胞内降解的生物学和医学影响继续增长.但是,这些嵌合实体是相对较大的化合物,通常具有分子特征,这可能会损害口服生物利用度,溶解度和/或体内药代动力学特性.因此,我们使用最初为细胞毒性有效载荷开发的技术,探索了此类分子与单克隆抗体的缀合,以便为这些新型药物提供替代的递送选择.在本报告中,我们描述了从含溴结构域蛋白4(brd4)靶向嵌合降解体实体衍生的抗体-药物偶联物(adc)系统开发的第一阶段.我们证明了降解物有效载荷对pc3-S1前列腺癌细胞的抗原依赖性传递以及对myc转录和细胞内brd4水平的相关影响.这些实验以鉴定一种降解物缀合物达到高潮,该缀合物在lncap前列腺癌细胞中表现出抗原依赖性的抗增殖作用.
Doi:10.1021/acs.Jmedchem.0C01845

专利信息

专利号:WO-2024151344-A9
优先权日:2022-11-18
标题:A device that enables the combinatorial synthesis of small molecule libraries
发明人：COPELAND Gregory; LIU JANE
权利人:BRT BIOTECHNOLOGIES INC
摘要:A device for the synthesis of small molecules on a substrate is provided. The device includes a synthesis plate with vias, and a microfluidic patterning plate with a series ot open-faced channels that can be aligned with the vias on the synthesis plate. The device may be used to synthesize combinatorial libraries of small molecules.

专利号:US-2024261416-A1
优先权日:2023-01-31
标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.

专利号:US-2022143183-A1
优先权日:2019-02-23
标题:Photoswitchable protacs and synthesis and uses thereof
发明人：TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE
权利人:UNIV NEW YORK
摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.

专利号:WO-2024151344-A2
优先权日:2022-11-18
标题 :A device that enables the combinatorial synthesis of small molecule libraries