328919-32-0Relevant articles and documents
CONDENSED PYRAZOLE DERIVATIVES AS PPAR AGONISTS II
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Page/Page column 45, (2010/11/26)
The invention discloses compounds of formula (I) wherein: R is a carboxylic acid or a derivative thereof; R1 and R2 are independently H or alkyl, or together R1 and R2 form an alkylene group; L1 is a
Synthesis of a 5-((Aryloxy)methyl)-3-(4-(trifluoromethyl)phenyl)[1,2,4] thiadiazole derivative: A promising PPARα,δ agonist
Reuman, Michael,Hu, Zhiyong,Kuo, Gee-Hong,Li, Xun,Russell, Ronald K.,Shen, Lan,Youells, Scott,Zhang, Yongzheng
, p. 1010 - 1014 (2012/12/30)
The preparation of the PPARα,δ agonist 2-methyl-2-(2-methyl-4- (3-(4-(trifluoromethyl)phenyl)[1,2,4]thiadiazol-5-ylmethoxy)phenoxy)propionic acid sodium salt (17) is described and compared with earlier in-house preparations of this important target compound. Key concerns around a large-scale synthesis of this thiadiazole derivative were a large number of purification steps, the use of dichlorobenzene as a solvent, and a possible large-scale Baeyer-Villiger oxidation. This paper describes a straightforward preparation of the target agonist using methylhydroquinone (MHQ) as an inexpensive precursor that eliminates the need of an oxidation step.
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
TRIAZOLE, OXADIAZOLE AND THIADIAZOLE DERIVATIVE AS PPAR MODULATORS FOR THE TREATMENT OF DIABETES
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Page/Page column 100, (2008/06/13)
The present invention is directed to compounds represented by the following structural formula, Formula (I): wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) W is N, O or S; (e) E is C(R3)(R4)A or A and wherein; (f) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsufonamide. The other substituents are defined in the claims; the compounds are modulators of peroxisome proleferator activated receptors (PPARs) and are useful for the treatment of diabetes and other metabolic disorders.
BICYCLIC DERIVATIVES AS PPAR MODULATORS
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Page/Page column 43, (2008/06/13)
The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) R2 is selected from the group consisting of C0-C8 alkyl and C1-4- heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (c) U is an aliphatic linker wherein one carbon atom of the aliphatic linker is optionally replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with from one to four substituents each independently selected from R30; (d) Y is selected from the group consisting of C, O, S, NH and a single bond; and (e) E is C(R3)(R4)A or A.
Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists
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, (2008/06/13)
Compounds represented by the following (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubsituted or substituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is H, alkyl or haloalkyl. R4 is H, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.
FUSED HETEROCYCLIC DERIVATIVES AS PPAR MODULATORS
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Page 49, (2008/06/13)
The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S. S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3) (R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.
Modulators of peroxisome proliferator activated receptors
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, (2008/06/13)
The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented b