CAS: 1045792-66-2; Tert-Butyl (4-(3-((7-(Hydroxyamino)-7-Oxoheptyl)Carbamoyl)Isoxazol-5-yl)Phenyl)Carbamate

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CAS号1045792-87-7 7-{[5-(4-tert-b...

📜Methyl 7-[5-(4-Tert-Butoxycarbonylaminophenyl)-3-Isoxazolecarboxamido]Heptanoate置于氢氧化钾,盐酸羟胺体系中,用 甲醇 用作溶剂,化学反应 0.5H,以30%的收率获得n-[4-[3-[[[7-(羟基氨基)-7-氧代庚基]氨基]羰基]-5-异恶唑基]苯基]氨基甲酸叔丁酯
参考文献:使用氧化腈环加成 (Noc) 反应生成分子探针:一类新的酶选择性组蛋白脱乙酰酶抑制剂 (Hdacis)置于hdac6 上显示出皮摩尔活性.
标题:使用氧化腈环加成 (Noc) 反应生成分子探针:一类新的酶选择性组蛋白脱乙酰酶抑制剂 (Hdacis)置于hdac6 上显示出皮摩尔活性.
摘要:已经使用腈氧化物环加成化学合成了一系列含有苯基异恶唑作为 Cap 基团的基于异羟肟酸酯的 Hdac 抑制剂.鉴定了效力约为2皮摩尔的hdac6选择性抑制剂.检查了一些化合物阻断胰腺癌细胞生长的能力,发现其效力比 Saha 强约 10 倍.这项研究为探索 Hdac 生物学提供了有价值的新分子探针.
Doi:10.1021/jm8002894

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-11059815-B2
优先权日:2018-07-23
标 题:Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; Yang Ka; WU HAO; ZHANG ZHONGRUI
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Histone deacetylase (“HDACâ€?)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.

专利号:US-11939363-B2
优先权日:2017-02-28
标题:Translatable molecules and synthesis thereof
发明人：LIMPHONG PATTRARANEE; TACHIKAWA KIYOSHI; CHIVUKULA PADMANABH; MATSUDA DAIKI; CALE ARISA
权利人:ARCTURUS THERAPEUTICS INC
摘要:A range of therapeutic mRNA molecules expressible to provide a target polypeptide or protein. The RNA molecules can contain one or more 5-methoxyuridines and 5-methylcytidines. Further provided are DNA templates, which can be transcribed to provide a target mRNA, and can have altered nucleotides, such as reduced deoxyadenosines. Also provided are processes for making the therapeutic mRNA molecules. The RNA molecules can be translated in vitro or in vivo to provide an active polypeptide or protein. The RNA molecules can be included in a composition used for preventing, treating, or ameliorating at least one symptom of a disease or condition in a subject in need thereof.

专利号:US-2020190079-A1
优先权日:2018-07-23
标题 :Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them

专利号:US-2020022966-A1
优先权日:2018-07-23
标题 :Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them

专利号:US-11801251-B2
优先权日:2015-11-03
标 题 :Selective HDAC8 inhibitors and their uses
发明人：MEYER-ALMES FRANZ-JOSEF; MEYNERS CHRISTIAN; KLEINSCHEK ALEXANDER; HAUS PATRICIA
权利人:HOCHSCHULE DARMSTADT
摘要:The present invention relates to small molecule compounds based on benzopyrimido- or benzoimidazo-thiazin-imine as well as their (synthesis) intermediates and their use as HDAC inhibitors, in particular HDAC8 inhibitors. The present invention also relates to the use of said compounds in the treatment of cancer and as therapeutic agents for eukaryotic parasites and respective methods of treatment.