CAS: 206872-01-7; 2-Amino-6-Bromo-4-Methoxyphenol

上下游产品

CAS号115929-59-4 2-溴-4-甲氧基-6-硝基苯酚 | CAS号1568-70-3 4-甲氧基-2-硝基酚 | CAS号24036-52-0 6-溴-2H-1,4-苯并恶嗪... | CAS号524684-52-4 普林贝瑞

4-甲氧基-2-硝基酚置于氢气,溴,Sodium Acetate,溶剂黄146体系中,用 四氢呋喃 用作溶剂,20.0~70.0 °C,172.37 Kpa 条件下,反应 5.0H,反应生成2-氨基-6-溴-4-甲氧基苯酚
参考文献:Design And Synthesis Of Aryl Diphenolic Azoles As Potent And Selective Estrogen Receptor-β Ligands
标题:Design And Synthesis Of Aryl Diphenolic Azoles As Potent And Selective Estrogen Receptor-β Ligands
摘要:New Diphenolic Azoles As Highly Selective Estrogen Receptor-Beta Agonists Are Reported. The More Potent And Selective Analogues Of These Series Have Comparable Binding Affinities For Erbeta As The Natural Ligand 17Beta-Estradiol But Are > 100-Fold Selective Over Eralpha. Our Design Strategy Not Only Followed A Traditional Sar Approach But Also Was Supported By X-Ray Structures Of Erbeta Cocrystallized With Various Ligands As Well As Molecular Modeling Studies. These Strategies Enabled Us To Take Advantage Of A Single Conservative Residue Substitution In The Ligand-Binding Pocket,Eralpha Met(421)--> Erbeta Ile(373),To Optimize Erbeta Selectivity. The 7-Position-Substituted Benzoxazoles (Table 5) Were The Most Selective Ligands Of Both Azole Series,With Erb-041 (117) Being >200-Fold Selective For Erbeta. The Majority Of Erbeta Selective Agonists Tested That Were At Least Similar To50-Fold Selective Displayed A Consistent In Vivo Profile: They Were Inactive In Several Models Of Classic Estrogen Action (Uterotrophic,Osteopenia,And Vasomotor Instability Models) And Yet Were Active In The Hla-B27 Transgenic Rat Model Of Inflammatory Bowel Disease. These Data Suggest That Erbeta-Selective Agonists Are Devoid Of Classic Estrogenic Effects And May Offer A Novel Therapy To Treat Certain Inflammatory Conditions.
Doi:10.1021/jm049719Y

专利信息

专利号:US-2024335442-A1
优先权日:2021-08-02
标 题:N-acylhydrazone compounds capable of inhibiting nav1.7 and/or nav1.8, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits
发明人：BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; GAMBA LUIS EDUARDO REINA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA; LIMA LÃ?DIA MOREIRA
权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO UFRJ
摘要:N-acylhydrazone compounds that are Nav 1.7 and/or Nav 1.8 inhibitors, including N-acylhydrazone compounds of Formula (I), wherein the substituents R1 to R6 are independently selected from the groups defined in the specification, as well as to the processes for the preparation thereof, compositions comprising at least one of said compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits, and which are applicable in the fields of medicinal chemistry and organic synthesis, as well as in the treatment of pain-related disorders.