- (2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents
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A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
- Koyama, Hiroo,Boueres, Julia K.,Miller, Daniel J.,Berger, Joel P.,MacNaul, Karen L.,Wang, Pei-Ran,Ippolito, Marc C.,Wright, Samuel D.,Agrawal, Arun K.,Moller, David E.,Sahoo, Soumya P.
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p. 3347 - 3351
(2007/10/03)
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- Novel 2,3-dihydrobenzofuran-2-carboxylic acids: Highly potent and subtype-selective PPARα agonists with potent hypolipidemic activity
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The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2- carboxylic acids as highly potent and subtype-selective PPARα agonists are reported. Systematic study of structure-activity relationships has identified several key structural elements within this class for maintaining the potency and subtype selectivity. Select compounds were evaluated in animal models of dyslipidemia using Syrian hamsters and male Beagle dogs, and all these compounds displayed excellent cholesterol- and triglyceride-lowering activity at dose levels that were much lower than the marketed weak PPARα agonist fenofibrate.
- Shi, Guo Q.,Dropinski, James F.,Zhang, Yong,Santini, Conrad,Sahoo, Soumya P.,Berger, Joel P.,MacNaul, Karen L.,Zhou, Gaochao,Agrawal, Arun,Alvaro, Raul,Cai, Tian-Quan,Hernandez, Melba,Wright, Samuel D.,Moller, David E.,Heck, James V.,Meinke, Peter T.
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p. 5589 - 5599
(2007/10/03)
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- Biguanide and dihydrotriazine derivatives
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Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the
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- Carbamoylimidazole derivatives and fungicidal use thereof
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Novel carbamoylimidazole derivatives of the formula (I) STR1 in which R1 represents lower alkyl, lower alkoxy-lower alkyl or cycloalkyl having 3 to 8 carbon atoms, R2 represents fluoro-substituted lower alkyl, X represents oxygen or sulfur, Y represents halogen or lower alkyl, m represents the numbers 0, 1 or 2, and n represents the numbers 2, 3, 4, 5 or 6, and the use of the new compounds as agricultural and horticultural fungicides.
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- Herbicidal ethers
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Ethers, such as 2-[[4-[4-(trifluoromethoxy)phenoxy]phenoxy]]propanoic acid, methyl ester, useful for control of weeds.
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