CAS: 149805-92-5; 6-(Dimethylamino)Nicotinaldehyde

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82846-28-4 666721-10-4 1355223-58-3

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5-bromo-2-dimethylaminopyridine N,N-dimethyl-formamide 2-(Dimethylamino)pyridine 2,3-dimethyl-2,3-diaminobutane tert-butyl (4-{(E)-2-[6-(dimethylamino)pyridin-3-yl]vinyl}phenyl)methylcarbamate 5-(((3-methoxyphenyl)imino)methyl)-N,N-dimethylpyridin-2-amine 2-(6-(dimethylamino)pyridin-3-yl)-1-(1H-indol-3-yl)-2-((3-methoxyphenyl)amino)ethanone (E)-5-(2,6-difluorostyryl)-2-(N,N-dimethylamino)pyridine

📜2-二甲氨基吡啶置于溴,Sodium Carbonate,Magnesium,1,2-二溴乙烷体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应生成6-(二甲基氨基)-3-吡啶羧醛
参考文献:Design Of 2,5-Dimethyl-3-(6-Dimethyl-4-Methylpyridin-3-yl)-7-Dipropylaminopyrazolo[1,5-A]Pyrimidine (Nbi 30775/r121919) And Structure−activity Relationships Of A Series Of Potent And Orally Active Corticotropin-Releasing Factor Receptor Antagonists
标题:Design Of 2,5-Dimethyl-3-(6-Dimethyl-4-Methylpyridin-3-yl)-7-Dipropylaminopyrazolo[1,5-A]Pyrimidine (Nbi 30775/r121919) And Structure−activity Relationships Of A Series Of Potent And Orally Active Corticotropin-Releasing Factor Receptor Antagonists
摘要:We Have Previously Shown That 3-Phenylpyrazolo[1,5-A]Pyrimidines Exemplified By 8 Were Potent Antagonists Of The Human Corticotropin-Releasing Factor-1 Receptor. A Series Of 3-Pyridylpyrazolo[1,5-A]Pyrimidines 15,25-30,34,And 35 Containing A Weakly Basic Pyridine Ring At The 3-Position Of The Bicyclic Nucleus Was Designed To Reduce Lipophilicity From The Initial Leads Such As 7. Here,We Showed That These 3-Pyridyl Compounds Exhibited Potent Antagonists At The Human Crf1,Receptor. Moreover,The Hydrophilic And Weakly Basic Pyridine Moiety Increased The Water Solubility Of Some Analogues. Compound 26H Exhibited Good Binding Affinity At The Human Crf1 Receptor With A K-I Value Of 3.5 Nm. As A Functional Antagonist,It Dose-Dependently Inhibited Crf-Stimulated Camp Production In Cells Expressing The Crf1 Receptor [ic50 = 50 Nm),And Crf-Stimulated Acth Release From Cultured Rat Pituitary Cells [ic50 = 20 Nm). 26H Had A Log P Value Of 4.9 And Water Solubility Of Greater Than 10 Mg/ml. Pharmacokinetic Studies In Rats Showed That 26H Was Orally Bioavailable And Able To Penetrate Into The Brain. 26H Has Been Demonstrated In Vivo Efficacy In Animal Behavioral Models That Measure Anxiolytic Activity. These Results Suggest That Analogues From This Series Were Potent Crf1,Receptor Antagonists With Proper Physicochemical Properties And Good Pharmacokinetic Profiles. 26H Was Developed Into A Clinical Compound And Exhibited Efficacy In Patients With Major Depression.
Doi:10.1021/jm040058E

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.