Abstract: Compounds of Formula (1) are disclosed. These compounds include selective activators of human PPAR delta.

Abstract: The present invention discloses novel PPAR gamma ligands of Formula (I) and pharmaceutically acceptable salts and solvates thereof. The present invention also discloses a method for treating osteoporosis by administration of a PPAR gamma antagonist.

Abstract: A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein; X1 represents O or S; R1 and R2 independently represent H, halogen, —CH3 and —OCH3; n represents 1 or 2; X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R3 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, NO2, NH2, CF3, OCF3, OC1-6 straight or branched alkyl, C1-6 straight or branched alkyl, alkenyl or alkynyl with the provision that when R3 is pyridyl, the N is unsubstituted; R4 represents CF3 or CH3

Abstract: A method is disclosed for rational design of a PPAR, FXR, LXR-alpha, or LXR-beta antagonist comprising chemical modification of a PPAR, FXR, LXR-alpha, or LXR-beta agonist to: a) prevent formation of a hydrogen bond between the agonist and tyrosine or histidine, or tryptophan involved in receptor activation; and/or b) displace the tyrosine or histidine, or tryptophan involved in receptor activation from its agonist bound position. Preferably, little or no additional changes are made in the structure of the agonist so that the resulting antagonist is a close structural analogue of the agonist.

Abstract: The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual activators of hPPAR&ggr; and hPPAR{acute over (&agr;)}.

Abstract: A thermoplastic composition comprises (a) a major amount of a semi-crystalline thermoplastic first polymer; (b) an amount of a fluoroaliphatic radical-containing surface-modifying additive sufficient to modify surface properties of articles made of the composition; and (c) a minor amount of a second thermoplastic polymer sufficient to enhance the effects of the surface-modifying additive.

Abstract: Novel compounds of Formula (1) and esters, salts, and physiologically functional derivatives thereof are disclosed. Methods for preparing and using the compounds are also disclosed. Many of these compounds are selective activators of PPAR alpha. The compounds are particularly useful for treating obesity.

Abstract: A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) H

Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,

Abstract: This invention relates to novel oxoazepine derivatives of Formula (I),R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I)to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.

Abstract: Oxazole compounds having formula (I) wherein R.sup.1 and R.sup.3 are selected from the group consisting of hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl, phenyl or phenyl mono- or disubstituted with C.sub.1-6 alkyl, halogen, hydroxy, C.sub.1-6 alkoxy, aminosulfonyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkylsulfonylaminoC.sub.1-6 alkyl or carbamylC.sub.1-6 alkylaminosulfonyl; R.sup.2 is selected from hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl or (fluorinated C.sub.1-6 alkyl)oxyC.sub.1-6 alkyl; W is a C.sub.1-6 alkylene chain or nitrogen; m is independently the integer 0 or 1; X is CH or nitrogen, provided that when W is nitrogen then X is CH; q is independently an integer selected from the group consisting of 1, 2, 3 or 4; or a pharmaceutically acceptable acid-addition or base-addition salt thereof, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention relates to phenethanolamine derivatives of formula (I) wherein R.sup.1 represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R.sup.2 represents hydrogen or C.sub.1-6 -alkyl; R.sup.3 represents a group (A) where the ring is substituted by one to four further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; or R.sup.3 represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; R.sup.4 represents hydrogen, or C.sub.1-6 -alkyl; R.sup.5 represents ZCH.sub.2 CO.sub.2 H wherein Z represents a bond, or O; Y represents (CH.sub.2).sub.

Abstract: The use of compound of formula (I) in which: R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group; R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.6 aliphatic acyl group, a (C.sub.5 -C.sub.7 cycloalkane) carbonyl group, an aromatic acyl group which is a benzoyl or naphthoyl group optionally with one or more nitro, amino, alkylamino, dialkylamino, alkoxy, halo, alkyl or hydroxy substituents, a heterocyclic acyl group having one or more oxygen, sulphur or nitrogen hetero atoms and with 4 to 7 ring atoms, an optionally halo-substituted phenylacetyl or phenylpropionyl group, a cinnamoyl group, a (C.sub.1 -C.sub.6 alkoxy) carbonyl group or a benzolyloxycarbonyl group; R.sup.4 and R.sup.5 are the same or different and each represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or a C.sub.1 -C.sub.5 alkoxy group, or R.sup.4 and R.sup.5 together represent a C.sub.1 -C.sub.4 alkylenedioxy group; n is 1, 2, or 3; W represents the --CH.sub.

Abstract: The use of agonists of the peroxisome proliferator activated receptor alpha (PPAR.alpha.) for the manufacture of a medicament for the treatment of obesity and methods of treating obesity comprising the administration of a therapeutic amount of a PPAR.alpha. agonist.

Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (B) wherein X, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

Abstract: The present invention provides radiolabeled 5-{4-[2-(Methyl-pyridine-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dion e. In another aspect, the present invention provides a method for determining whether a compound does or does not interact directly with PPAR-gamma, comprising the step of specifically binding a radiolabeled compound of this invention to the ligand binding domain of PPAR-gamma.

Abstract: The present invention relates to methods for preparing and using compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) wherein X, W, Z, R.sup.4, and R.sup.5, are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

Abstract: The present invention provides activator compounds, including agonists, to the peroxisome proliferator-activated receptor gamma. Particular PPAR.gamma. activators are set forth, as are a pharmaceutical composition for treating diabetes, non-insulin-dependent diabetes mellitus, cardiovascular disorders, and methods for such treatment.

Abstract: This invention relates to novel oxoazepine derivatives of Formula (I),R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I)to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.

Abstract: Group IV organometallic compounds, e.g. alkylsilane, or alkylsiloxane compounds, are used as chain transfer agent in the radical initiated polymerization of ethylenically unsaturated monomers, to give polymers comprising non-ionic end groups.