CAS: 1268524-70-4; (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

上下游产品

CAS号1268524-67-9 (S)-2-(5-(4-氯苯基... | CAS号1068-57-1 乙酰肼 | CAS号50508-66-2 2-氨基-3-(4-氯苯甲酰基... | CAS号4640-66-8 4-氯苯甲酰乙腈

(S)-Tert-Butyl-3-Amino-4-((3-(4-Chlorobenzoyl)-4,5-Dimethylthiophen-2-yl)Amino)-4-Oxobutanoate置于potassium Tert-Butylate,溶剂黄146体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 3.0H,反应生成(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
参考文献:靶向实体瘤的双 Ezh2/brd4 抑制剂的设计和合成
标题:靶向实体瘤的双 Ezh2/brd4 抑制剂的设计和合成
摘要:防止组蛋白赖氨酸 27 (H3K27) 三甲基化的 Ezh2 抑制剂通常仅限于治疗一部分血液恶性肿瘤.在大多数实体瘤中,Ezh2 抑制剂诱导相互的 H3K27 乙酰化,随后导致获得性耐药性.Ezh2 和 Brd4 抑制剂的组合使实体癌细胞对 Ezh2 抑制剂重新敏感已被证明是有效的,这表明开发双重抑制剂的重要性.在此,我们介绍了一流的双 Ezh2/brd4 抑制剂的设计,合成和生物学评估.我们最有前途的化合物 Ym458 显示出对 Ezh2 和 Brd4 的有效抑制活性以及对 11 种实体癌细胞系的显着抗增殖能力.
Doi:10.1021/acs.Jmedchem.1C01876

专利信息

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-2025222120-A1
优先权日:2024-01-09
标题 :Synthesis of novel small molecule carm1 degraders, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; XU WEI; XIE HAIBO; BACABAC MEGAN
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Provided herein are CARM1 PROTACs comprising a binding molecule of CARM1 with an optimized linker attached to an E3 ubiquitin ligase ligand that recruits the E3 ubiquitin ligase to CARM1. The PROTACs find use, e.g., for selectively targeted degradation of CARM1 protein in cancer cells. Also provided herein are compositions comprising the PROTACs, as well as methods of using the PROTACs.

专利号:EP-4580642-A2
优先权日:2022-09-01
标 题 :Genetically engineered cd4 t-cells for in situ synthesis of proteins

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-2024050325-A2
优先权日:2022-09-01
标 题:Genetically engineered cd4 t-cells for in situ synthesis of proteins

专利号:CN-108379591-B
优先权日:2018-04-03
标 题 :Synthesis of Immune Agonist Targeting Compounds and Their Applications