CAS: 1723-27-9; Thieno[3,2-B]Thiophene-2-Carboxylic Acid

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b]thiophen-2-yl-ethanone1-thieno[3,2-b]thiophen-2-yl-ethanone 3-(2-thienyl)-2-sulfanylpropenoic acid ethyl thieno[3,2,-b]thiophene-2-carboxylate thieno[3,2-b]thiophenetetrabromo-thieno[3,2-b]thiophene 2,3,5-tribromothieno[3,2-b]thiophene 2-(4-chlorophenyl)-4-(thiopheno[2,3-d]thiophen-2-ylcarbonylamino)thiophene-3-carboxylic acid 27H18ClNO5S3C27H18ClNO5S3

噻吩并[3,2-B]噻吩置于sodium Chlorite,Sodium Dihydrogenphosphate Dihydrate,2-甲基-2-丁烯,三氯氧磷体系中,用 四氢呋喃,水,1,2-二氯乙烷,叔丁醇 用作溶剂,化学反应 48.0H,反应生成噻吩并[3,2-B]噻吩-2-甲酸
参考文献:Discovery Of Potent And Orally Bioavailable Gpr40 Full Agonists Bearing Thiophen-2-Ylpropanoic Acid Scaffold
标题:Discovery Of Potent And Orally Bioavailable Gpr40 Full Agonists Bearing Thiophen-2-Ylpropanoic Acid Scaffold
摘要:The Free Fatty Acid Receptor Gpr40 Is Predominantly Expressed In Pancreatic Beta-Cells And Enhances Insulin Secretion In A Glucose Dependent Manner. Therefore,Gpr40 Agonists Are Possible Novel Insulin Secretagogues With Reduced Or No Risk Of Hypoglycemia For The Treatment Of Type 2 Diabetes Mellitus (T2Dm). Chemically And Structurally Diverse Gpr40 Agonists With High Safety Are Pursued For The Clinical Development Of Gpr40-Based Pharmacotherapeutics. Herein We Report Our Design And Discovery Of A New Chemotype Of Gpr40 Agonists Free Of The Typical Phenylpropanoic Acid Scaffold. The Thiophen-2-Ylpropanoic Acid Containing Gpr40 Modulators Functioned As Full Agonists With High-Efficacy Response (E-Max) And Reduced Lipophilicity. Significantly,The Lead Compound In This Series,(R)-7K,Exhibited More Potent In Vitro Glucose-Stimulated Insulin Secretion And In Vivo Glucose-Lowering Effects (10 Mg/kg,Po) Than The Gpr40 Partial Agonist Tak-875,Which Was Once In Phase Iii Clinical Trials,And High Selectivity Over The Relevant Receptors Gpr120 And Ppar Gamma.
Doi:10.1021/acs.Jmedchem.6B01357

专利信息

专利号:WO-03045909-A2
优先权日:2001-11-21
标 题 :Methods and intermediates for the synthesis of azepines

专利号:NO-318910-B1
优先权日:1998-12-23
标 题:Protease inhibitors, method of synthesis and use thereof, and pharmaceutical composition

专利号:RO-106402-B1
优先权日:1989-04-18
标 题:DERIVATIVES OF 2-OXINDOL-3-SUBSTITUTES, THE PROCESS OF OBTAINING AND INTERMEDIARIES IN THEIR SYNTHESIS