- HETEROCYCLIC COMPOUNDS SUITABLE FOR THE TREATMENT OF DYSLIPIDEMIA
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The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds
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Paragraph 0185; 0186
(2013/11/05)
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- HETEROCYCLIC COMPOUNDS SUITABLE FOR THE TREATMENT OF DYSLIPIDEMIA
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The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds
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Paragraph 0055
(2013/11/19)
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- Ethacrynic acid as a lead structure for the development of potent urease inhibitors
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Ethacrynic acid and a series of its analogues were synthesized and subsequently evaluated for their inhibitory effect on jack bean urease. Ethacrynic acid showed, even at low concentrations, very potent inhibitory activity against the enzyme. For ethacrynic acid, the inhibition potential increased with increasing preincubation time of ethacrynic acid and enzyme, whereas for some other compounds a higher preincubation time lead to a significant reduction of their activity. We could demonstrate that the α,β-unsaturated carbonyl unit of our compounds is mandatory to inhibit the enzyme, possibly due to its ability to bind to cysteine residues in the active site of the jack bean urease.
- Janser, Ingo,Vortolomei, Caitlyn M.,Meka, Ranjith K.,Walsh, Courtney A.,Janser, Romy F.J.
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p. 660 - 664
(2013/08/15)
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- Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists
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A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARδ selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a, 12c, 17a and 18a showed PPAR-pan agonists activities and among these four compounds tested, 12a emerged as highly potent and efficacious compound, while 17a exhibited moderate and balanced PPAR-pan agonistic activity. In vivo, selected test compounds 12a and 17a exhibited significant anti-hyperglycemic and anti-hyperlipidemic activities in relevant animal models. These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists.
- Makadia, Pankaj,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Patel, Darshit,Pola, Suresh,Thube, Baban,Priyadarshini, Priyanka,Suthar, Dinesh,Shah, Maanan,Giri, Suresh,Trivedi, Chitrang,Jain, Mukul,Patel, Pankaj,Bahekar, Rajesh
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experimental part
p. 771 - 782
(2011/03/18)
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- CHEMICAL COMPOUNDS
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The present invention discloses novel compounds with a variety of therapeutic uses. More particularly, the invention discloses novel symmetrical triphenyl compounds that are particularly useful for selective estrogen receptor modulation.
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Page/Page column 40-41
(2008/06/13)
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