Abstract: Resveratrol has been reported to have hypolipidemic properties. We investigated whether resveratrol and its analogs: pterostilbene, piceatannol and resveratrol trimethyl ether, would activate the peroxisome proliferator-activated receptor alpha (PPAR?) isoform. This nuclear receptor is proposed to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPAR? in H4IIEC3 cells transfected with a luciferase gene reporter construct. Pterostilbene demonstrated the highest induction of PPAR?; the maximal response to pterostilbene was similar to that obtained with the hypolipidemic drug, ciprofibrate.

Abstract: Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. Resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) were evaluated for their effects on the activation of the peroxisome proliferator-activated receptor alpha (PPAR?) isoforms, a receptor shown to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPAR? in H4IIEC3 cells. Pterostilbene demonstrated the highest induction of PPAR? demonstrating increases of 7- and 9-14 fold relative to control. The maximal responses to pterostilbene are similar to those obtained with the hypolipidemic drug, ciprofibrate; that is, pterostilbene acts as a PPAR? agonist, like that of the fibrate class, and is a more effective hypolipidemic agent than resveratrol.

Abstract: Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. Resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) were evaluated for their effects on the activation of the peroxisome proliferator-activated receptor alpha (PPAR?) isoforms, a receptor shown to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPAR? in H4IIEC3 cells. Pterostilbene demonstrated the highest induction of PPAR? demonstrating increases of 7- and 9-14 fold relative to control. The maximal responses to pterostilbene are similar to those obtained with the hypolipidemic drug, ciprofibrate; that is, pterostilbene acts as a PPAR? agonist, like that of the fibrate class, and is a more effective hypolipidemic agent than resveratrol.

Abstract: Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of the present invention are preferably characterized by selective activity as ?2c-AR antagonists. Use of the compounds, or pharmaceutical composition containing them, for treating or preventing an ?2c adrenergic receptor mediated condition or disorder, and for antagonizing activity of an ?2c adrenergic receptor are also disclosed.

Abstract: The invention provides ?3-adrenoreceptor agonists, pharmaceutical compositions comprising ?3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.

Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.

Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.

Abstract: The invention provides compounds of formula: wherein R1 is —NHS(O)mR, wherein R is alkyl, substituted alkyl, alkoxy, substituted alkoxy, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; X is independently selected from the group consisting of halo, alkyl, substituted alkyl, alkoxy, substituted alkoxy, hydroxy, nitro, amino, and substituted amino; R2 is benzyl or benzyl substituted with one or more substituents selected from the group consisting of halo, CF3, hydroxy, nitro, alkoxy, substituted alkoxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, amino, and substituted amino of formula —NHR' or —NR′R′, wherein each R′ is alkyl, substituted alkyl, —C(O)Y, —C(O)NHY, or —C(O)SY, wherein Y is alkyl or substituted alkyl; R3 is H or alkyl; n

Abstract: The invention provides compounds useful as &bgr;3-adrenorecptor agonists and pharmaceutical compositions comprising such compounds. The invention further includes a method for stimulating, regulating, and modulating metabolism in fats of adipose tissue in mammals by administering an effective amount of a compound of the invention.

Abstract: Compounds which are highly potent and highly specific &bgr;3-Adrenoreceptor agonists are provided. The compounds are formulated into pharmaceutical preparations and administered for stimulating, regulating and modulating metabolism of fats in adipose tissues in animals, particularly humans and other mammals. The compounds of the invention have the structure (A). R1 and R2 arc each independently members selected from the group consisting of H, OH, Cl, NO2, CH3SO2NH, NH2, CH3O and weak e4 acids of the structure R7—NH, where R7 is an acyl group, wherein at least one of R1 and R2 is OH. It is generally preferred that R2 be OH; R3, R4, and R5 are variously and independently members selected from I, Br, Cl, F, OCH3, CH3, alkyl, alkylaryl, aminoalkyl, thioalkyl, and O-alkyl. Preferably, R4 and R5 are each a halogen, the same or different; R6 is an acid moiety which forms an acid salt with the NH group. R6 is desirably HCl or (COOH)2.

Abstract: The present invention relates to novel benzopyranone aci-reductone compounds of the formula I wherein X and Y are selected from the group comprising H (except that X and Y are not both H, unless otherwise indicated) Cl or other halogen, OH, a straight or branched C.sub.1 14 C.sub.6 alkyl or alkoxy group or phenyl or phenyloxy groups, such as, for example a phenyl or a tertiary butyl group. The invention also provides for compounds of the general formula I wherein X, Y.dbd.OCH.sub.2 O.

Abstract: The present invention relates to novel 5-fluoro- and 8-fluoro-trimetoquinol compounds of the general formula I wherein X.sub.1 =F, X.sub.2 =H or X.sub.1 =H, X.sub.2 =F ##STR1## The present invention also relates to a process for making the 5-fluoro- and 8-fluoro-trimetoquinol compounds by condensation of an appropriately substituted phenethylamine to afford an appropriately substituted phenlethylacetamide compound. The amides are cyclized to give appropriately substituted intermediate dihydroisoquinolines. Without isolation, the dihydroisoquinolines are reduced to give appropriately substituted tetrahydroisoquinolines. The hydrochloride salts of tetrahydroisoquinolines are prepared and subjected to hydrogenolysis, to give the fluorine substituted trimetoquinol compounds of the present invention.

Abstract: The present invention relates to novel benzopyranone aci-reductone compounds of the formula I wherein X and Y are selected from the group comprising H (except that X and Y are not both H, unless otherwise indicated) Cl or other halogen, OH, a straight or branched C.sub.1 -C.sub.6 alkyl or alkoxy group or phenyl or phenyloxy groups, such as, for example a phenyl or a tertiary butyl group. The invention also provides for compounds of the general formula I wherein X, Y=OCH.sub.2 O. ##STR1## The compounds of the invention are useful in the treatment or prevention of thromboembolic disorders.

Abstract: The present invention relates to novel 5-fluoro- and 8-fluoro-trimetoquinol compounds of the general formula I wherein X.sub.1 =F,X.sub.2 =H or X.sub.1 =H,X.sub.2 =F ##STR1## The present invention also relates to a process for making the 5-fluoro- and 8-fluoro-trimetoquinol compounds by condensation of an appropriately substituted phenethylamine to afford an appropriately substituted phenethylacetamide compound. The amides are cyclized to give appropriately substituted intermediate dihydroisoquinolines. Without isolation, the dihydroisoquinolines are reduced to give appropriately substituted tetrahydroisoqinolines. The hydrochloride salts of tetrahydroisoqinolines are prepared and subjected to hydrogenolysis, to give the fluorine substituted trimetoquinol compounds of the present invention.