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Peroxisome proliferator activated receptor alpha agonistsPeroxisome proliferator activated receptor alpha agonists description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20090062358, Peroxisome proliferator activated receptor alpha agonists. Brief Patent Description - Full Patent Description - Patent Application Claims
BACKGROUND OF THE INVENTION
Peroxisome Proliferator Activated Receptors (PPARS) are members of the nuclear hormone receptor super family, which are ligand-activated transcription factors regulating gene expression. Various subtypes of PPARs have been discovered. These include PPARα, NUC1, PPARγ and PPARδ. The PPARα receptor subtypes are reported to be activated by medium and long-chain fatty acids. They are involved in stimulating beta-oxidation of fatty acids and with the activity of fibrates which reportedly produce a substantial reduction in plasma triglycerides and moderate reduction in low density lipoprotein (LDL) cholesterol. PPARα, PPARγ and PPARδ receptors have been implicated in diabetes mellitus, cardiovascular disease, obesity, Syndrome X and gastrointestinal disease, such as, inflammatory bowel disease. Syndrome X is the combination of symptoms which include hyperinsulemia combined with hypertension, elevated body weight, elevated triglycerides and elevated LDL. Current PPAR agonist treatment for Syndrome X relates to the use of thiazolidinediones (TZDs) or other insulin sensitivity enhancers (ISEs). TZDs are a class of PPAR gamma agonists which have been shown to increase the sensitivity of insulin sensitive cells. Increasing insulin sensitivity rather than the amount of insulin in the blood reduces the likelihood of hypoglycemic coma. However, TZDs and ISEs typically have little effect in preventing the cardiovascular part of Syndrome X in that their administration usually dose not result in the lowering of triglycerides and LDL-cholesterol while raising HDL-cholesterol. Furthermore, side effects commonly associated with treatment with TZDs include significant weight gain, and, for troglitazone, liver toxicity. Therefore, a need exists for new pharmaceutical agents which affect treat or prevent cardiovascular disease, particularly that associated with Syndrome X, while preventing or minimizing weight gain, and more preferably while improving insulin sensitivity. SUMMARY OF THE INVENTIONThe present invention is directed to compounds represented by the following structural Formula I:
and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein:
(a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl;
(b) W is O or S;
(c) R2 is H or a substituted or unsubstituted group selected from the group consisting of C1-C6 alkyl, C1-C6 allyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, sulfonamide, amide, OR10 and C3-C6 cycloalkyl;
(d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S;
(e) Y is C, O, S, NH or a single bond; and
(f) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, substituted or unsubstituted selected from the group consisting of (CH2)nCOOR19, C1-C6 alkyl, C1-C6 allyl, aryl-C0-4-alkyl, thio-C1-4-alkyl, thioaryl, C1-4alkoxyaryl, C1-4alkoxy C1-4alkyl, aminoaryl, and aminoC1-4alkyl, and wherein
(i) n is 0, 1, 2 or 3,
(ii) A is an functional group selected from the group consisting of carboxyl, C1-C3alkylnitrile, carboxamide, substituted or unsubstituted sulfonamide, substituted or unsubstituted acylsulfonamide and substituted or unsubstituted tetrazole;
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