CAS: 883531-28-0; 2-Fluoro-4-Methoxyphenylacetic Acid

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CAS号1403674-64-5 2,2,2-trichloro... | CAS号74457-86-6 2-氟-4-甲氧基苯乙酮 | CAS号331-64-6 2-氟-4-甲氧基苯甲醛 | CAS号68886-07-7 2-氟-4-羟基苯乙酸

2,2,2-三氯-1-(2-氟-4-甲氧基苯基)乙醇置于sodium Tetrahydroborate,乙醇,二苯基二硒醚,Sodium Hydroxide体系中,用95%的收率获得产物2-氟-4-甲氧基苯乙酸
参考文献:Influence Of Chlorine Or Fluorine Substitution On The Estrogenic Properties Of 1-Alkyl-2,3,5-Tris(4-Hydroxyphenyl)-1H-Pyrroles
标题:Influence Of Chlorine Or Fluorine Substitution On The Estrogenic Properties Of 1-Alkyl-2,3,5-Tris(4-Hydroxyphenyl)-1H-Pyrroles
摘要:In Continuation Of Our Previous Work,Several 1-Alkyl-2,3,5-Tris(4-Hydroxyphenyl)Aryl-1H-Pyrroles With Chlor-Me Or Fluorine Substituents In The Aryl Residues Were Synthesized And Tested For Estrogen Receptor (Er) Binding At Isolated Er Alpha/er Beta. Receptors (Hap Assay),And. In Trans Activation Assays Using Er Alpha-Positive Mcf-7/2A As Well As U2-Os/er Alpha And U2-Os/er Beta Cells. In The Competition Experiment At Er Alpha The Compounds Displayed Very High Relative Binding-Affinities Of Up To 37% (Determined For 8M) But With Restricted Subtype Selectivity (E.G.,Er Alpha/er Beta (8Ma) = 9). The Highest Estrogenic Potency In Er Alpha-Positive Mcp-7/2A Cells Was Determined For 2,3,5-Tris(2-Fluoro-4-Hydroxyphenyl)-1-Prolayl-1H-Pyriole 8M (Ec50 = 23 Nm),While In U2-Os/er Alpha Cells 2-(2-Fluoro-4-Hydroxyphenyl)-3,5-Bis(4-Hydroxyphenyl)-1H Propyl-1H Pyrrole 8B (Ec50 = 0.12 Nm) Was The Most Potent Agonist,Only 30 Fold Less Active Than Estradiol (E2,Ec50 = 0.004 Nm). In U2-Os/er Beta Cells For All Pyrroles No Transactivation Could Be Observed,Which Indicates That They Are Selective Er Alpha Agonists In Cellular Systems.
DOI:10.1021/jm300860J

专利信息

专利号:US-9700543-B2
优先权日:2011-05-31
标题 :GLP-1 receptor stabilizers and modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; BRAHMACHARY ENUGURTHI; YEAGER ADAM RICHARD
权利人:CELGENE INT II SÀRL
摘要:Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.