71659-82-0Relevant academic research and scientific papers
Process development for sodelglitazar: A ppar panagonist
Brown, Andrew D.,Davis, Roman D.,Fitzgerald, Russ N.,Glover, Bobby N.,Harvey, Kim A.,Jones, Lynda A.,Liu, Bing,Patterson, Daniel E.,Sharp, Matthew J.
experimental part, p. 297 - 302 (2010/04/22)
Three efficient syntheses of sodelglitazar (1) have been developed. In particular, the third synthesis avoids the use of zinc and eliminates the resulting heavy metal waste stream as well as the potential genotoxic methanesulfonate in the two earlier syntheses. This process produces sodelglitazar in 74% overall yield from readily available thiophenol (8) and thiazole alcohol (3).
Increasing selectivity of CC chemokine receptor 8 antagonists by engineering nondesolvation related interactions with the intended and off-target binding sites
Shamovsky, Igor,De Graaf, Chris,Alderin, Lisa,Bengtsson, Malena,Bladh, H?kan,B?rjesson, Lena,Connolly, Stephen,Dyke, Hazel J.,Van Den Heuvel, Marco,Johansson, Henrik,Josefsson, Bo-G?ran,Kristoffersson, Anna,Linnanen, Tero,Lisius, Annea,M?nnikk?, Roope,Nordén, Bo,Price, Steve,Ripa, Lena,Rognan, Didier,Rosendahl, Alexander,Skrinjar, Marco,Urbahns, Klaus
supporting information; experimental part, p. 7706 - 7723 (2010/07/04)
The metabolic stability and selectivity of a series of CCR8 antagonists against binding to the hERGion channel and cytochrome Cyp2D6 are studied by principal component analysis. It is demonstrated that an efficient way of increasing metabolic stability an
Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors α and δ
Shen, Lan,Zhang, Yan,Wang, Aihua,Sieber-McMaster, Ellen,Chen, Xiaoli,Pelton, Patricia,Xu, Jun Z.,Yang, Maria,Zhu, Peifang,Zhou, Lubing,Reuman, Michael,Hu, Zhiyong,Russell, Ronald,Gibbs, Alan C.,Ross, Hamish,Demarest, Keith,Murray, William V.,Kuo, Gee-Hong
, p. 3954 - 3963 (2008/02/11)
Cardiovascular disease is the most common cause of morbidity and mortality in developed nations. To effectively target dyslipidemia to reduce the risk of cardiovascular disease, it may be beneficial to activate the peroxisome proliferator-activated recept
Development of a scalable synthesis of GSK183390A, a PPAR α/γ agonist
Oh, Lynette M.,Wang, Huan,Shilcrat, Susan C.,Hermann, Robert E.,Patience, Daniel B.,Spoors, P. Grant,Sisko, Joseph
, p. 1032 - 1042 (2012/12/30)
A scalable synthesis of GSK183390A, a PPAR α/γ agonist, is described. This synthesis is highlighted by (1) a regioselective formal 1,3-dipolar cycloaddition reaction between an enamine and a nitrile inline dipole to form a 1,3,5-trisubstmited pyrazole and (2) a regioselective amidomethylation of an o-cresol derivative using 2-chloro-JV- hydroxymethylacetamide.
4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs
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Page/Page column 18, (2010/10/20)
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.
4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs
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Page/Page column 24; 25, (2010/10/20)
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.
4-((Phenoxyalkyl)thio)-phenoxyacetic acids and analogs
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Page/Page column 18-19, (2008/06/13)
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.
PARA-SULFONYL SUBSTITUTED PHENYL COMPOUNDS AS MODULATORS OF PPARS
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Page 55, (2008/06/13)
Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Beta(3)-adrenoceptor agonists for the treatment of frequent urination and urinary incontinence: 2-[4-(2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl)phenoxy]-2-methylpropionic acid.
Tanaka,Tamai,Mukaiyama,Hirabayashi,Muranaka,Ishikawa,Akahane,Akahane
, p. 3265 - 3271 (2007/10/03)
In a search for novel analogues of beta(3)-adrenoceptor (AR) agonists relaxing the bladder for treatment of urinary dysfunction, 2-[4-(2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl)phenoxy]-2-methylpropionic acids (1a-e), into which a fibrate-like structure had been incorporated, were synthesised. Compound 1a was found to be a selective beta(3)-AR agonist in functional assays using the ferret detrusor (beta(3)-AR), rat uterus (beta(2)-AR), and rat atrium (beta(1)-AR); beta(3): EC(50)=7.8 nM, beta(2): IC(50)=7,300 nM, beta(1): EC(20)=23,000 nM. The introduction of a chlorine atom or methyl substituent at the ortho-position on the phenyl ring of 1a further improved beta(3)-AR selectivity. In an in vivo study, 1a lowered intrabladder pressure (ED(50)=31 microg/kg) in rats, without increasing heart rate, in keeping with the in vitro results. Consequently, it is proposed that 1a and its analogues (1b-e), possess beta(3)-AR agonistic activity in the absence of undesirable beta(1)- or beta(2)-AR mediated actions, and may be useful for clinical treatment and pharmacological studies.
