CAS: 377727-87-2; 2-(Furan-2-yl)-7-(2-(4-(4-(2-Methoxyethoxy)Phenyl)Piperazin-1-yl)Ethyl)-7H-Pyrazolo[4,3-E][1,2,4]Triazolo[1,5-C]Pyrimidin-5-Amine

上下游产品

2-(5-Amino-2-(Furan-2-yl)-7H-Pyrazolo[4,3-E][1,2,4]Triazolo[1,5-C]Pyrimidin-7-yl)Ethyl 4-Methylbenzenesulfonate 377729-82-3
2-(Furan-2-yl)-7H-Pyrazolo[4,3-E][1,2,4]Triazolo[1,5-C]Pyrimidin-5-Amine 321661-12-5
Tert-Butyl 2-(6-Amino-1-(2-(4-(4-(2-Methoxyethoxy) Phenyl) Piperazin-1-yl)Ethyl)-1H-Pyrazolo[3,4-D]Pyrimidin-4-yl)Hydrazine Carboxylate 929884-33-3
4-Chloro-1-[2-[4-[4-(2-Methoxyethoxy)Phenyl]Piperazin-1-Yl]Ethyl]Pyrazolo[3,4-D]Pyrimidin-6-Amine 1401067-77-3
5-Amino-7-Chloro-2-(Furan-2-yl)-[1,2,4]Triazolo[1,5-C]Pyrimidine-8-Carbaldehyde 1401067-81-9
2-[6-氨基-1-(2-羟基乙基)-1H-吡唑并[3,4-D]嘧啶-4-基]-2-呋喃羧酸肼 N'-(6-Amino-1-(2-Hydroxyethyl)-1H-Pyrazolo[3,4-D]Pyrimidin-4-yl)Furan-2-Carbohydrazide 377729-86-7

📜1-乙酰基-4-(4-羟基苯基)哌嗪置于盐酸,Sodium Hydride,N,N-二异丙基乙胺体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应生成瑞德南特
参考文献:氟化物激发的氟化腺苷a2A受体拮抗剂作为潜在的癌症免疫治疗剂
标题:氟化物激发的氟化腺苷a2A受体拮抗剂作为潜在的癌症免疫治疗剂
摘要:T细胞上腺苷受体的拮抗作用可阻断缺氧腺苷能途径,从而促进肿瘤排斥.使用基于伴刀豆球蛋白a小鼠模型的体内免疫分析方法,研究了一系列拮抗剂,并确定了preladenant是有效的潜在先导化合物,可用于开发.采用分子建模来辅助药物设计和随后合成类似物和托扎定的化合物,包括氟化聚乙二醇peg化衍生物.使用两次体外功能性生物测定法评估了类似物的功效,并确认了化合物29(一种预合成的氟化三甘醇衍生物)被确认为潜在的免疫治疗剂.
Doi:10.1155/2017/4852537

专利信息

专利号:WO-2012127472-A1
优先权日:2011-03-22
标题:Process and intermediates for the preparation of preladenant and related compounds
发明人：MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI
权利人:MAPI PHARMA LTD; MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI
摘要:The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1 ), and solvates and salts thereof, especially salts with pharmaceutically acceptable acids. The process of the present invention is useful not only for Preladenant production, but also for the preparation of other biologically active compounds of general formula (17), such as A2a receptor antagonists used for the treatment of central nervous system diseases, among others. The present invention further relates to certain intermediates formed in such processes.

专利号:US-2023271983-A1
优先权日:2020-07-29
标题 :Functionalized isonitriles and products, preparation and uses thereof
发明人：SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
权利人:UNIV SANTIAGO COMPOSTELA
摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

专利号:US-2022259202-A1
优先权日:2019-06-17
标题:1-(4-(aminomethyl)benzyl)-2-butyl-2h-pyrazolo[3,4-c]quinolin-4-amine derivatives and related compounds as toll-like receptor (tlr) 7/8 agonists, as well as antibody drug conjugates thereof for use in cancer therapy and diagnosis
发明人：MEIMETIS LABROS
权利人:SUTRO BIOPHARMA INC
摘要:1-(4-(aminomethyl)benzyl)-2-butyl-2H-pyrazolo[3,4-c]quinolin-4-amine derivatives thereof and related compounds of formula (I) as toll-like receptor (TLR) 7/8 agonists for cancer therapy. Linker payload compounds thereof, and antibody conjugates thereof for cancer diagnosis. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 145 to 156; examples 1 to 3; biological examples 1 to 6; tables 1 and 2).