CAS: 1421373-65-0; N-(2-((2-(Dimethylamino)Ethyl)(Methyl)Amino)-4-Methoxy-5-((4-(1-Methyl-1H-Indol-3-yl)Pyrimidin-2-yl)Amino)Phenyl)Acrylamide

上下游产品

4-fluoro-2-methoxy-5-nitro-phenylamine N2[[2(dimethylamino)ethyl]methylamino]4methoxy5[[4(1methyl1Hindole-3-yl)-2-pyrimidinyl]amino]aniline acryloyl chloride 2-chloropropionyl chlorideN-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

N-(2-{[2-(Dimethylamino)Ethyl](Methyl)Amino}-4-Methoxy-5-{[4-(1-Methyl-1H-Indol-3-yl)Pyrimidin-2-Yl]Amino}Phenyl)-2-Hydroxypropanamide置于硫酸体系中,用24.08 G的收率获得n-[2-[[2-(二甲基氨基)乙基]甲基氨基]-4-甲氧基-5-[[4-(1-甲基-1H-吲哚-3-基)-2-嘧啶基]氨基]苯基]-2-丙烯酰胺
参考文献:高效选择性egfr突变体抑制剂azd9291的制备方法
标题:高效选择性egfr突变体抑制剂azd9291的制备方法
摘要:本发明公开了高效选择性egfr突变体抑制剂azd9291的制备方法,所述高效选择性egfr突变体抑制剂azd9291化学名称为n‑{2‑[[2‑(二甲基氨基)乙基]甲基氨基]‑4‑甲氧基‑5‑[[4‑(1‑甲基‑1H‑吲哚‑3‑基)‑2‑嘧啶基]氨基]苯基}‑2‑丙烯酰胺,其化学式为c28H33N7O2,其结构式为:;本发明制备工艺过程简洁,原料易得,经济环保,有利于实现工业化,可促azd9291原料药的经济技术发展,降低了生成成本,适于大批量生产.

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-11414415-B2
优先权日:2020-04-23
标题 :6H-imidazo[4,5,1-ij]quinolone, synthesis method and use thereof
发明人：ZHANG PENGFEI; HUANG WEI; SHEN CHAO; XU JUN; SHEN JIABIN; XU WEIMING
权利人:UNIV HANGZHOU NORMAL
摘要:The present invention relates to the technical field of chemical synthesis of pharmaceutical chemicals, and provides a 6H-imidazo[4,5,1-ij]quinolone, a synthesis method and use thereof. 6H-imidazo[4,5,1-ij]quinolone derivatives provided by the present invention are a novel group of active quinolone derivatives, which have tumor cell inhibition activity and exhibit IC50 values equivalent to anti-lung cancer drug osimertinib; these quinolone derivatives have a broad application prospect in the preparation of antitumor drugs. The 6H-imidazo[4,5,1-ij]quinolone provided by the present invention is of high research and application value and has potential application prospects in fields of pharmaceutical chemicals, materials, dyes, etc. The present invention uses thioquinolinamide as a raw material to synthesize 6H-imidazo[4,5,1-ij]quinolones, featuring simple operation, excellent selectivity, high yield, mild reaction conditions, and easy product separation.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.