CAS: 97322-87-7; 5-(4-((6-Hydroxy-2,5,7,8-Tetramethylchroman-2-yl)Methoxy)Benzyl)Thiazolidine-2,4-Dione

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CAS号109-86-4 乙二醇甲醚 | CAS号79907-49-6 3,4-二氢-2-羟基甲基-2... | CAS号107188-58-9 6-Hydroxy-2,5,7... | CAS号118070-84-1 6-(Methoxymetho... | CAS号107187-56-4 (+/-)-5-[4-(6-h...

📜5-[4-(6-Benzyloxy-2,5,7,8-Tetramethyl-Chroman-2-Ylmethoxy)-Benzyl]-Thiazolidine-2,4-Dione置于盐酸,溶剂黄146体系中,用70%的收率获得产物曲格列酮
参考文献:Novel Antidiabetic And Hypolipidemic Agents. 5. Hydroxyl Versus Benzyloxy Containing Chroman Derivatives
标题:Novel Antidiabetic And Hypolipidemic Agents. 5. Hydroxyl Versus Benzyloxy Containing Chroman Derivatives
摘要:Several Thiazolidinediones Having Chroman Moieties Were Synthesized And Evaluated For Their Euglycemic And Hypolipidemic Activities. Some Of The Analogues Having An Aminoalkyl Group As A Linker Between The Chroman Ring And 4-[5-(2,4-Dioxo-1,3-Thiazolidinyl)Methyl]Phenoxy Moiety Seem To Be Better Than Troglitazone. In Vitro Transactivation Assays Of Ppar Gamma Have Been Carried Out With These Glitazones To Understand Their Molecular Mechanism. For The First Time We Have Found That Some Of The Unsaturated Thiazolidinediones Are Superior To Their Saturated Counterpart In The In Vivo Assay. A More Potent Thiazolidinedione Analogue Than Troglitazone Is Reported. Pharmacokinetic Studies Have Shown That Protection Of The Oh Group In The Chroman Moiety Leads To A Decrease In Metabolism,Thereby Resulting In A Superior Pharmacological Profile.
DOI:10.1021/jm9805541

专利信息

专利号:WO-2009148195-A1
优先权日:2008-06-02
标题:5-(4-hydroxybenzyl)thiazolidine-2,4-dione as intermediate for synthesis of thiazolidinedione based compounds and process for preparing the same
发明人：PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI
权利人:DAEBONG LS LTD; PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI
摘要:The present invention relates to 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by the following Chemical Formula [1], which is useful as an intermediate for synthesis of thiazolidinedione based compounds, a method for preparing the compound, and a method for preparing pioglitazone or pioglitazone hydrochloride, which is a thiazolidinedione based drug and useful in treating and preventing diabetes, using the 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by Chemical Formula [1] as an intermediate:

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-7473541-B2
优先权日:2004-07-09
标 题:Identification, cloning, expression, and purification of three novel human calcium-independent phospholipase A2 family members possessing triacylglycerol lipase and acylglycerol transacylase activities
发明人：GROSS RICHARD W; JENKINS CHRISTOPHER
权利人:GROSS RICHARD W; JENKINS CHRISTOPHER
摘要:Isolated novel and purified and characterized phospholipase A 2 , referred to herein as calcium-independent phospholipase A 2 zeta (iPLA 2 zeta) having SEQ. ID. NO: 2 (See FIG. 1 ), and nucleic acid sequence (SEQ. ID. NO: 4), and calcium-independent phospholipase A 2 eta (iPLA 2 eta) having SEQ. ID. NO: 3 (See FIG. 1 ), and nucleic acid sequences (SEQ. ID. NO: 5). For the first time herein, these novel enzymes have been isolated and characterized and are involved in the catalysis, synthesis and hydrolysis of lipids in a living mammalian cell. Moreover, these enzymes iPLA 2 zeta and iPLA 2 eta through the process of transesterification can catalyze the net anabolic synthesis of triglycerides through a variety of metabolic precursors (e.g. monoacylglycerol, diacylglycerol and acyl CoA).

专利号:WO-2019016826-A1
优先权日:2017-07-17
标 题:NOVEL 5- [4- (2-BIPHENYL-4-YL-2-OXOETHOXY) BENZYLIDENE] THIAZOLIDINE-2,4-DIONES, THEIR SYNTHESIS AND USES THEREOF
发明人：THAREJA SURESH; VERMA SANT KUMAR; JAIN AKHLESH KUMAR; BHARDWAJ TILAK RAJ
权利人:GURU GHASIDAS VISHWAVIDYALAYA A CENTRAL UNIV; INDIAN COUNCIL OF MEDICAL RES ICMR
摘要:Disclosed are novel 5-[4-(2-biphenyl-4-yl-2-oxo-ethoxy)-benzylidene]-thiazolidine-2,4-dione compounds of general formula (I), their pharmaceutically acceptable salts, solvates their synthesis and uses thereof, to pharmaceutical compositions containing compounds and to the use of such compounds and composition in medicines either alone or in combination with other compounds.

专利号:US-8846916-B2
优先权日:2009-05-11
标题:Sitagliptin synthesis
发明人：GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH
权利人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH; GENERICS UK LTD
摘要:The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.

专利号:US-7807349-B2
优先权日:2002-11-29
标 题 :Protein synthesis monitoring (PSM)
发明人：SMILANSKY ZEEV
权利人:ANIMA CELL METROLOGY
摘要:A method and a device are disclosed for monitoring the synthesis of proteins by the ribosome in real time, in vivo as well as in in-vitro. The ribosome is engineered to carry a donor fluorophore, and tRNA and/or amino acids and/or some other part of the ribosome are either engineered to carry acceptor fluorophores or else their natural fluorescent properties are utilized as acceptors. As the ribosomes mechanism processed the mRNA and tRNA molecules and synthesizes a polypeptide chain, a light source illuminates the ribosome, exciting the donor fluorophores and thereby the acceptor fluorophores whenever these are in sufficient proximity to a donor. The resulting signals are detected and used as a key for real-time database searching and identification of the protein being synthesized. The resulting data can be tabulated and interpreted in different ways. FIG. ( 1 ) describes the properties of a FRET pair and the dependence of FRET on pair distance.