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(2,6-dimethylpyridin-3-yl)methanol ethyl 2,6-dimethylnicotinate (E)-3-(2,6-Dimethyl-pyridin-3-yl)-acrylic acid (E)-N-[4-(4-Benzhydryl-piperazin-1-yl)-butyl]-3-(2,6-dimethyl-pyridin-3-yl)-acrylamide methyl N-[(2,6-dimethyl-3-pyridinyl)methylidene]-D-alloisoleucine methyl N-[(2R)-2-(2,3-dihydro-1H-inden-2-yl)-2-({[(phenylmethyl)oxy]-carbonyl}amino)acetyl]-N-[1-(2,6-dimethyl-3-pyridinyl)-2-oxo-2-({2-[(phenylmethyl)oxy]phenyl}amino)ethyl]-D-alloisoleucinate 📜2,6-二甲基烟酸乙酯/2,6-二甲基-3-羧酸甲酯置于吡啶,Chromium(Vi) Oxide,Lithium Aluminium Tetrahydride体系中,用 乙醚 作为反应溶剂,化学反应生成 2,6-二甲基吡啶-3-醛
参考文献:Acrylamide Derivatives As Antiallergic Agents. 2. Synthesis And Structure Activity Relationships Of N-[4-[4-(Diphenylmethyl)-1-Piperazinyl]Butyl]-3-(3-Pyridyl)Acrylamides
标题:Acrylamide Derivatives As Antiallergic Agents. 2. Synthesis And Structure Activity Relationships Of N-[4-[4-(Diphenylmethyl)-1-Piperazinyl]Butyl]-3-(3-Pyridyl)Acrylamides
摘要:A New Series Of 3-(3-Pyridyl)Acrylamides 16,17,19,And 26,And 5-(3-Pyridyl)-2,4-Pentadienamides 20-25 Were Prepared And Evaluated For Their Antiallergic Activity. Several Of These Compounds Exhibited More Potent Inhibitory Activities Than The Parent Compound 1A [(E)-N-[4-[4-(Diphenylmethyl)-1-Piperazinyl]Butyl]-3-(3-Pyridyl)Acrylamide] Against The Rat Passive Cutaneous Anaphylaxis (Pca) Reaction And The Enzyme 5-Lipoxygenase. Particularly,(E)-N-[4-[4-(Diphenylmethyl)-1-Piperazinyl]Butyl]-3-(6-Methyl-3-Pyridyl)Acrylamide (17P) Showed An Ed50 Value Of 3.3 Mg/kg Po In The Rat Pca Test,Which Was One-Fifth Of Ketotifen And Oxatomide. As Compared With Ketotifen And Oxatomide,Compound 17P (Al-3264) Possessed A Better Balance Of Antiallergic Properties Due To Inhibition Of Chemical Mediator Release,Inhibition Of 5-Lipoxygenase,And Antagonism Of Histamine.
DOI:10.1021/jm00123A012
专利信息
专利号:US-9938258-B2
优先权日:2012-11-29
标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof
发明人:BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.