CAS: 1145-93-3; Diethyl 4-Methoxybenzylphosphonate

相似化合物

108957-75-1 4546-04-7 3762-25-2

上下游产品

triethyl phosphate p-methoxybenzyl chloride 1-(4-Methoxy-benzyl)-2-methylsulfanyl-4,6-diphenyl-pyridinium; iodide triethyl phosphite2-amino-7,8-dihydro-6-(4-methoxystyryl)-7,7-dimethylpteridin-4(3H)-one benzofuran5-(benzyloxy)-2,3-dihydro-3,3-dimethyl-2-2-(4-methoxyphenyl)ethenylbenzofuran rel-(2R,3R,4R)-trans-5-(p-methoxyphenyl)-3-(methoxymethoxy)-4-methyl-1-hex-5-en-1-ol 1-(cyclohexylidenemethyl)-4-methoxy-benzene

📜对甲苯甲醚置于n-溴代丁二酰亚胺(Nbs),偶氮二异丁腈体系中,用 四氯化碳 用作溶剂,化学反应生成4-甲氧基苯基磷酸二乙酯
参考文献:Engineered Chimeric Enzymes As Tools For Drug Discovery: Generating Reliable Bacterial Screens For The Detection,Discovery,And Assessment Of Estrogen Receptor Modulators
标题:Engineered Chimeric Enzymes As Tools For Drug Discovery: Generating Reliable Bacterial Screens For The Detection,Discovery,And Assessment Of Estrogen Receptor Modulators
摘要:Engineered Protein-Based Sensors Of Ligand Binding Have Emerged As Attractive Tools For The Discovery Of Therapeutic Compounds Through Simple Screening Systems. We Have Previously Shown That Engineered Chimeric Enzymes,Which Combine The Ligand-Binding Domains Of Nuclear Hormone Receptors With A Highly Sensitive Thymidylate Synthase Reporter,Yield Simple Sensors That Report The Presence Of Hormone-Like Compounds Through Changes In Bacterial Growth. This Work Describes An Optimized Estrogen Sensor In Escherichia Coli With Extraordinary Reliability In Identifying Diverse Estrogenic Compounds And In Differentiating Between Their Agonistic/antagonistic Pharmacological Effects. The Ability Of This System To Assist The Discovery Of New Estrogen-Mimicking Compounds Was Validated By Screening A Small Compound Library,Which Led To The Identification Of Two Structurally Novel Estrogen Receptor Modulators And The Accurate Prediction Of Their Agonistic/antagonistic Biocharacter In Human Cells. Strong Evidence Is Presented Here That The Ability Of Our Sensor To Detect Ligand Binding And Recognize Pharmacologically Critical Properties Arises From Allosteric Communication Between The Artificially Combined Protein Domains,Where Different Ligand-Induced Conformational Changes In The Receptor Are Transmitted To The Catalytic Domain And Translated To Distinct Levels Of Enzymic Efficiency. To The Best Of Our Knowledge,This Is One Of The First Examples Of An Engineered Enzyme With The Ability To Sense Multiple Receptor Conformations And To Be Either Activated Or Inactivated Depending On The Nature Of The Bound Effector Molecule. Because The Proposed Mechanism Of Ligand Dependence Is Not Specific To Nuclear Hormone Receptors,We Anticipate That Our Protein Engineering Strategy Will Be Applicable To The Construction Of Simple Sensors For Different Classes Of (Therapeutic) Binding Proteins.
Doi:10.1021/ja067754J

专利信息

专利号:US-7501407-B2
优先权日:2001-12-20
标题 :Pyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO; COLLINGTON ERIC
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n nwherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms;n R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

专利号:MX-PA04005862-A
优先权日:2001-12-20
标 题 :SELECTED ANTAGONIST COMPOUNDS OF PYRIMIDINE A2B, ITS SYNTHESIS AND USE.